LSD1-IN-6

发表于2024年9月14日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

LSD1-IN-6

LSD1-in-2 (Compound 4m) 是一种有效、可逆的赖氨酸特异性去甲基化酶 (LSD1) 抑制剂，IC₅₀ 值为 123 nM。LSD1-in-2 (4m) 能增加组蛋白 H3 Lys4 的二甲基化，但对 LSD1 的表达无作用。

LSD1-IN-6 Chemical Structure

CAS No. : 2035912-43-5

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性	LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC₅₀ of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1^[1].
IC₅₀ & Target	IC50: 123 nM (LSD1)^[1]
分子量	349.18
Formula	C₁₅H₁₃BrN₂O₃
CAS 号	2035912-43-5
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Duan YC, et al. Discovery of resveratrol derivatives as novel LSD1 inhibitors: Design, synthesis and their biological evaluation. Eur J Med Chem. 2017 Jan 27;126:246-258.

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LSD1-IN-5

发表于2024年9月13日由上海金畔生物科技有限公司

LSD1-IN-5

LSD1-in-1 (Compound 4e) 是一种有效、可逆的赖氨酸特异性去甲基化酶 (LSD1) 抑制剂，IC₅₀ 值为 121 nM。LSD1-in-1 能增加组蛋白 H3 Lys4 的二甲基化，但对 LSD1 的表达无作用。

LSD1-IN-5 Chemical Structure

CAS No. : 2035912-55-9

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性	LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC₅₀ of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1^[1].
IC₅₀ & Target	IC50: 121 nM (LSD1)^[1]
分子量	349.18
Formula	C₁₅H₁₃BrN₂O₃
CAS 号	2035912-55-9
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Duan YC, et al. Discovery of resveratrol derivatives as novel LSD1 inhibitors: Design, synthesis and their biological evaluation. Eur J Med Chem. 2017 Jan 27;126:246-258.

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GSK-LSD1 dihydrochloride

发表于2024年8月5日由上海金畔生物科技有限公司

GSK-LSD1 dihydrochloride 纯度: ≥98.0%

GSK-LSD1 dihydrochloride 是有效，选择性，不可逆的赖氨酸特异性脱甲基酶 (LSD1) 抑制剂，IC₅₀ 值为 16 nM。

GSK-LSD1 dihydrochloride Chemical Structure

CAS No. : 2102933-95-7

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥880	In-stock
5 mg	￥800	In-stock
10 mg	￥1200	In-stock
25 mg	￥2400	In-stock
50 mg	￥4200	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

GSK-LSD1 dihydrochloride 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Epigenetics Compound Library
Neuronal Signaling Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Covalent Screening Library
Reprogramming Compound Library
Anti-Parkinson’s Disease Compound Library
Neurodegenerative Disease-related Compound Library
Mitochondria-Targeted Compound Library
Targeted Diversity Library

生物活性

GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.

IC₅₀ & Target

IC50: 16 nM (LSD1)^[1]

体外研究
(In Vitro)

GSK-LSD1 shows more than 1000 fold selectivity over other closely related FAD utilizing enzymes including LSD2, and monoamine oxidases MAO-A, MAO-B^[1]. GSK-LSD1 can inhibit KDM1A/LSD1 enzyme activity. GSK-LSD1 induces the formation of LC3-II in U2OS cells. The electronic microscopy shows the formation of autophagosome with GSK-LSD1 treatment. GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

289.24

Formula

C₁₄H₂₂Cl₂N₂

CAS 号

2102933-95-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 62.5 mg/mL (216.08 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4573 mL	17.2867 mL	34.5734 mL
5 mM	0.6915 mL	3.4573 mL	6.9147 mL
10 mM	0.3457 mL	1.7287 mL	3.4573 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (7.19 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.19 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (7.19 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.19 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (7.19 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.19 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Purich D. The Inhibitor Index A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. ISBN 9781138739215

[2]. Wang Z, et al. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.

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LSD1/HDAC6-IN-1

发表于2024年5月26日由上海金畔生物科技有限公司

LSD1/HDAC6-IN-1

LSD1/HDAC6-IN-1 是一种具有口服活性的组蛋白去甲基化酶 LSD1 和组蛋白去乙酰酶 HDAC6 (LSD1/HDAC6) 双重抑制剂，具有抗肿瘤活性。LSD1/HDAC6-IN-1 可用于多发性骨髓瘤 (MM) 的研究。

LSD1/HDAC6-IN-1 Chemical Structure

规格	价格	是否有货
5 mg	￥3900	询问价格 & 货期
10 mg	￥6250	询问价格 & 货期
25 mg	￥12500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性	LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM)^[1].
体外研究 (In Vitro)	LSD1/HDAC6-IN-1 shows superior potency in multiple MM lines^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)	LSD1/HDAC6-IN-1 is efficacy in the MM.1S xenograft model^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	407.55
Formula	C₅₀H₆₆N₆O₄
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. M Naveen Sadhu, et al. Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. Bioorg Med Chem Lett. 2020 Dec 24;34:127763.

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Precisa普利赛斯精密天平LS10200D

发表于2024年1月4日由上海金畔生物科技有限公司

Precisa普利赛斯精密天平LS10200D

品牌普利赛斯|Precisa

型号 LS10200D

可选配件及服务

Precisa普利赛斯精密天平LS10200D

Precisa普利赛斯专用打印机

¥2000.00

请询价

商品详情

产品介绍：
321系列电子天平， Precisa中高端电子天平，精度高，反应快，稳定性好，性价比高，满足您预算的同时，提供高质量的称量结果。

主要特点：
全铝合金外壳铸造，防震、防尘、防辐射性能良好
内置时钟，支持3Q认证
全自动内校功能，可以根据温度时间的变化进行校准（部分型号选配）
可选配密封性良好的圆柱形风罩
实验室称重分析、物质称重分析等。

型号	产品描述	价格
LS120ASCS	LS120A分析天平（称量范围120g,读数精度0.1mg）SCS智能内校功能	13000
LS220ASCS	LS220A分析天平（称量范围220g,读数精度0.1mg）SCS智能内校功能	14200
LS320MSCS	LS320M精密天平（称量范围320g,读数精度1mg）SCS智能内校功能	12800
LS620MSCS	LS620M精密天平（称量范围620g,读数精度1mg）SCS智能内校功能	14000
LS1220MSCS	LS1220M精密天平（称量范围1220g,读数精度1mg）SCS智能内校功能	15000
LS1200CSCS	LS1220C精密天平（称量范围1220g,读数精度0.01g）SCS智能内校功能	12500
LS3200CSCS	LS3200C精密天平（称量范围3200g,读数精度0.01g）SCS智能内校功能	13500
LS4200CSCS	LS4200C精密天平（称量范围4200g,读数精度0.01g）SCS智能内校功能	18850
LS6200CSCS	LS6200C精密天平（称量范围6200g,读数精度0.01g）SCS智能内校功能	14500
LS3200DSCS	LS3200D精密天平（称量范围3200g,读数精度0.1g）SCS智能内校功能	12200
LS6200DSCS	LS6200D精密天平（称量范围6200g,读数精度0.1g）SCS智能内校功能	13300
LS10200DSCS	LS10200D精密天平（称量范围10200g,读数精度0.1g）SCS智能内校功能	14800
LS120A	LS120A分析天平（称量范围120g,读数精度0.1mg）	11600
LS220A	LS220A分析天平（称量范围220g,读数精度0.1mg）	12600
LS320M	LS320M精密天平（称量范围320g,读数精度1mg）	10800
LS620M	LS620M精密天平（称量范围620g,读数精度1mg）	11800
LS1220M	LS1220M精密天平（称量范围1220g,读数精度1mg）	12800
LS1200C	LS1220C精密天平（称量范围1220g,读数精度0.01g）	10800
LS3200C	LS3200C精密天平（称量范围3200g,读数精度0.01g）	11000
LS6200C	LS6200C精密天平（称量范围6200g,读数精度0.01g）	12500
LS3200D	LS3200D精密天平（称量范围3200g,读数精度0.1g）	10800
LS6200D	LS6200D精密天平（称量范围6200g,读数精度0.1g）	11200
LS10200D	LS10200D精密天平（称量范围10200g,读数精度0.1g）	12000

Precisa普利赛斯精密天平LS6200D

发表于2024年1月4日由上海金畔生物科技有限公司

Precisa普利赛斯精密天平LS6200D

品牌普利赛斯|Precisa

型号 LS6200D

可选配件及服务

Precisa普利赛斯精密天平LS6200D

Precisa普利赛斯专用打印机

¥2000.00

请询价

商品详情

产品介绍：
321系列电子天平， Precisa中高端电子天平，精度高，反应快，稳定性好，性价比高，满足您预算的同时，提供高质量的称量结果。

型号	产品描述	价格
LS120ASCS	LS120A分析天平（称量范围120g,读数精度0.1mg）SCS智能内校功能	13000
LS220ASCS	LS220A分析天平（称量范围220g,读数精度0.1mg）SCS智能内校功能	14200
LS320MSCS	LS320M精密天平（称量范围320g,读数精度1mg）SCS智能内校功能	12800
LS620MSCS	LS620M精密天平（称量范围620g,读数精度1mg）SCS智能内校功能	14000
LS1220MSCS	LS1220M精密天平（称量范围1220g,读数精度1mg）SCS智能内校功能	15000
LS1200CSCS	LS1220C精密天平（称量范围1220g,读数精度0.01g）SCS智能内校功能	12500
LS3200CSCS	LS3200C精密天平（称量范围3200g,读数精度0.01g）SCS智能内校功能	13500
LS4200CSCS	LS4200C精密天平（称量范围4200g,读数精度0.01g）SCS智能内校功能	18850
LS6200CSCS	LS6200C精密天平（称量范围6200g,读数精度0.01g）SCS智能内校功能	14500
LS3200DSCS	LS3200D精密天平（称量范围3200g,读数精度0.1g）SCS智能内校功能	12200
LS6200DSCS	LS6200D精密天平（称量范围6200g,读数精度0.1g）SCS智能内校功能	13300
LS10200DSCS	LS10200D精密天平（称量范围10200g,读数精度0.1g）SCS智能内校功能	14800
LS120A	LS120A分析天平（称量范围120g,读数精度0.1mg）	11600
LS220A	LS220A分析天平（称量范围220g,读数精度0.1mg）	12600
LS320M	LS320M精密天平（称量范围320g,读数精度1mg）	10800
LS620M	LS620M精密天平（称量范围620g,读数精度1mg）	11800
LS1220M	LS1220M精密天平（称量范围1220g,读数精度1mg）	12800
LS1200C	LS1220C精密天平（称量范围1220g,读数精度0.01g）	10800
LS3200C	LS3200C精密天平（称量范围3200g,读数精度0.01g）	11000
LS6200C	LS6200C精密天平（称量范围6200g,读数精度0.01g）	12500
LS3200D	LS3200D精密天平（称量范围3200g,读数精度0.1g）	10800
LS6200D	LS6200D精密天平（称量范围6200g,读数精度0.1g）	11200
LS10200D	LS10200D精密天平（称量范围10200g,读数精度0.1g）	12000

Precisa普利赛斯精密天平LS3200D

发表于2024年1月4日由上海金畔生物科技有限公司

Precisa普利赛斯精密天平LS3200D

品牌普利赛斯|Precisa

型号 LS3200D

可选配件及服务

Precisa普利赛斯精密天平LS3200D

Precisa普利赛斯专用打印机

¥2000.00

请询价

商品详情

产品介绍：
321系列电子天平， Precisa中高端电子天平，精度高，反应快，稳定性好，性价比高，满足您预算的同时，提供高质量的称量结果。

型号	产品描述	价格
LS120ASCS	LS120A分析天平（称量范围120g,读数精度0.1mg）SCS智能内校功能	13000
LS220ASCS	LS220A分析天平（称量范围220g,读数精度0.1mg）SCS智能内校功能	14200
LS320MSCS	LS320M精密天平（称量范围320g,读数精度1mg）SCS智能内校功能	12800
LS620MSCS	LS620M精密天平（称量范围620g,读数精度1mg）SCS智能内校功能	14000
LS1220MSCS	LS1220M精密天平（称量范围1220g,读数精度1mg）SCS智能内校功能	15000
LS1200CSCS	LS1220C精密天平（称量范围1220g,读数精度0.01g）SCS智能内校功能	12500
LS3200CSCS	LS3200C精密天平（称量范围3200g,读数精度0.01g）SCS智能内校功能	13500
LS4200CSCS	LS4200C精密天平（称量范围4200g,读数精度0.01g）SCS智能内校功能	18850
LS6200CSCS	LS6200C精密天平（称量范围6200g,读数精度0.01g）SCS智能内校功能	14500
LS3200DSCS	LS3200D精密天平（称量范围3200g,读数精度0.1g）SCS智能内校功能	12200
LS6200DSCS	LS6200D精密天平（称量范围6200g,读数精度0.1g）SCS智能内校功能	13300
LS10200DSCS	LS10200D精密天平（称量范围10200g,读数精度0.1g）SCS智能内校功能	14800
LS120A	LS120A分析天平（称量范围120g,读数精度0.1mg）	11600
LS220A	LS220A分析天平（称量范围220g,读数精度0.1mg）	12600
LS320M	LS320M精密天平（称量范围320g,读数精度1mg）	10800
LS620M	LS620M精密天平（称量范围620g,读数精度1mg）	11800
LS1220M	LS1220M精密天平（称量范围1220g,读数精度1mg）	12800
LS1200C	LS1220C精密天平（称量范围1220g,读数精度0.01g）	10800
LS3200C	LS3200C精密天平（称量范围3200g,读数精度0.01g）	11000
LS6200C	LS6200C精密天平（称量范围6200g,读数精度0.01g）	12500
LS3200D	LS3200D精密天平（称量范围3200g,读数精度0.1g）	10800
LS6200D	LS6200D精密天平（称量范围6200g,读数精度0.1g）	11200
LS10200D	LS10200D精密天平（称量范围10200g,读数精度0.1g）	12000

LSD1-IN-21

发表于2023年12月22日由上海金畔生物科技有限公司

LSD1-IN-21

LSD1-IN-21 (化合物 5a) 是一种有效的可透过血脑屏障的 LSD1 (赖氨酸特异性去甲基化酶 -1) 抑制剂，其 IC₅₀ 为 0.956 µM。LSD1-IN-21 显著降低促炎细胞因子 TNF-α。LSD1-IN-21 具有良好的抗癌和抗炎活性。

LSD1-IN-21 Chemical Structure

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生物活性

LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC₅₀ of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity^[1].

IC₅₀ & Target

TNF-α

体外研究
(In Vitro)

LSD1-IN-21 (compound 5a) shows potent anti-cancer activity with GI₅₀ values of 0.414 and 0.417 µM against HOP-62 and OVCAR-4 cell lines, respectively^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

447.55

Formula

C₂₄H₂₅N₅O₂S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Tasneem S, et al. Synthesis, biological evaluation and docking studies of methylene bearing cyanopyrimidine derivatives possessing a hydrazone moiety as potent Lysine specific demethylase-1 (LSD1) inhibitors: A promising anticancer agents. Bioorg Chem. 2022 May 21;126:105885.

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GSK-LSD1-d4 dihydrochloride

发表于2023年12月20日由上海金畔生物科技有限公司

GSK-LSD1-d4 dihydrochloride

GSK-LSD1-d4 dihydrochloride 是 GSK-LSD1 dihydrochloride 的氘代物。GSK-LSD1 dihydrochloride 是有效，选择性，不可逆的赖氨酸特异性脱甲基酶 (LSD1) 抑制剂，IC₅₀ 值为 16 nM。

GSK-LSD1-d4 dihydrochloride Chemical Structure

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生物活性	GSK-LSD1-d4 dihydrochloride is the deuterium labeled GSK-LSD1 dihydrochloride. GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	293.27
Formula	C₁₄H₁₇D₄ClN₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Purich D. The Inhibitor Index A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. ISBN 9781138739215 [3]. Wang Z, et al. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.

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GSK-LSD1-d4 dihydrochloride

发表于2023年12月20日由上海金畔生物科技有限公司

GSK-LSD1-d4 dihydrochloride

GSK-LSD1-d4 dihydrochloride Chemical Structure

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生物活性	GSK-LSD1-d4 dihydrochloride is the deuterium labeled GSK-LSD1 dihydrochloride. GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	293.27
Formula	C₁₄H₁₇D₄ClN₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Purich D. The Inhibitor Index A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. ISBN 9781138739215 [3]. Wang Z, et al. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.

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GSK-LSD1-d4 dihydrochloride

发表于2023年12月20日由上海金畔生物科技有限公司

GSK-LSD1-d4 dihydrochloride

GSK-LSD1-d4 dihydrochloride Chemical Structure

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生物活性	GSK-LSD1-d4 dihydrochloride is the deuterium labeled GSK-LSD1 dihydrochloride. GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	293.27
Formula	C₁₄H₁₇D₄ClN₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Purich D. The Inhibitor Index A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. ISBN 9781138739215 [3]. Wang Z, et al. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.

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LSD1/ER-IN-1

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1/ER-IN-1

LSD1/ER-IN-1 (compound 11g) 是一种有效的 ER 和 LSD1 抑制剂，其IC₅₀ 为 1.55 μM (LSD1)。LSD1/ER-IN-1 对 ERα 蛋白有高亲和力选择性，α/β 比为7.11。LSD1/ER-IN-1 对 MCF-7 乳腺癌细胞具有良好的抗增殖活性，其 IC₅₀ 为8.79 μM。

LSD1/ER-IN-1 Chemical Structure

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生物活性

LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC₅₀ of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC₅₀ of 8.79 μM^[1].

IC₅₀ & Target

ERα

ERβ

体外研究
(In Vitro)

LSD1/ER-IN-1 (compound 11g) (0-30 μM, 24 h) induces apoptosis in MCF-7 cells in a dose-dependent manner^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

455.46

Formula

C₂₃H₁₈FNO₆S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. He M, et al. Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor α (ERα) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer. Eur J Med Chem. 2020 Jun 1;195:112281.

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LSD1-IN-12

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-12

LSD1-IN-12 (compound 2) 是一种有效的 LSD1 抑制剂，其 K_i 值分别为 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), 和 3.5 μM (MAO-B)。

LSD1-IN-12 Chemical Structure

CAS No. : 1228143-76-7

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生物活性

LSD1-IN-12 (compound 2) is a potent LSD1 inhibitor, with K_i values of 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), and 3.5 μM (MAO-B), respectively^[1].

IC₅₀ & Target

MAO-A

2.3 μM (Ki)

MAO-B

3.5 μM (Ki)

分子量

252.31

Formula

C₁₆H₁₆N₂O

CAS 号

1228143-76-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Li C, et al. Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors. J Med Chem. 2022 Mar 10;65(5):4335-4349.

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LSD1-IN-13

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-13

LSD1-IN-13 (compound 7e) 是一种口服有效的 LSD1 抑制剂，其 IC₅₀ 值为 24.43 nM。LSD1-IN-13 可激活 CD86 表达，其 EC₅₀ 值为 470 nM。LSD1-IN-13 诱导 AML (急性髓系白血病)细胞系分化。

LSD1-IN-13 Chemical Structure

CAS No. : 2170212-33-4

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生物活性	LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC₅₀ of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC₅₀ of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines^[1].
IC₅₀ & Target	IC₅₀: 24.43 ± 1.08 nM (LSD1), 5.00 ± 0.28 μM (LSD2), >100 μM (MAO-A), >100 μM (MAO-B)^[1]
体外研究 (In Vitro)	LSD1-IN-13 (compound 7e) shows good selectivity over LSD2 (205-fold) and MAOs (>4000-fold)^[1]. LSD1-IN-13 shows potent and selective antiproliferative activity in MV-4-11, with an IC₅₀ of 1.36 μM^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)	LSD1-IN-13 (compound 7e) (MV-4-11 xenograft mice, 0-20 mg/kg, Orally, daily for 15 days) suppresses tumor growth significantly in a dose-dependent manner^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	411.56
Formula	C₂₃H₂₉N₃O₂S
CAS 号	2170212-33-4
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Li C, et al. Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors. J Med Chem. 2022 Mar 10;65(5):4335-4349.

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LSD1-IN-13 hydrochloride

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-13 hydrochloride

LSD1-IN-13 hydrochloride (compound 7e) 是一种口服有效的 LSD1 抑制剂，其 IC₅₀ 值为 24.43 nM。LSD1-IN-13 hydrochloride 可激活 CD86 表达，其 EC₅₀ 值为 470 nM。LSD1-IN-13 hydrochloride 诱导 AML (急性髓系白血病)细胞系分化。

LSD1-IN-13 hydrochloride Chemical Structure

CAS No. : 2170347-90-5

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生物活性	LSD1-IN-13 hydrochloride (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC₅₀ of 24.43 nM. LSD1-IN-13 hydrochloride can activate CD86 expression, with an EC₅₀ of 470 nM. LSD1-IN-13 hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines^[1].
IC₅₀ & Target	IC₅₀: 24.43 ± 1.08 nM (LSD1), 5.00 ± 0.28 μM (LSD2), >100 μM (MAO-A), >100 μM (MAO-B)^[1]
体外研究 (In Vitro)	LSD1-IN-13 hydrochloride (compound 7e) shows good selectivity over LSD2 (205-fold) and MAOs (>4000-fold)^[1]. LSD1-IN-13 hydrochloride shows potent and selective antiproliferative activity in MV-4-11, with an IC₅₀ of 1.36 μM^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)	LSD1-IN-13 hydrochloride (compound 7e) (MV-4-11 xenograft mice, 0-20 mg/kg, Orally, daily for 15 days) suppresses tumor growth significantly in a dose-dependent manner^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	448.02
Formula	C₂₃H₃₀ClN₃O₂S
CAS 号	2170347-90-5
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Li C, et al. Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors. J Med Chem. 2022 Mar 10;65(5):4335-4349.

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LSD1-IN-15

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-15

LSD1-IN-15 (compound 1b) 是一种有效的 LSD1 抑制剂。LSD1-IN-15 对LSD1-CoREST、MAO-A 和 MAO-B 具有抑制作用，IC₅₀ 值分别为 0.149、0.028 和 0.324 μM。LSD1-IN-15 在前列腺癌 LNCaP 细胞中显示细胞生长阻滞，IC₅₀ 为 9.9 μM。

LSD1-IN-15 Chemical Structure

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生物活性

LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor. LSD1-IN-15 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC₅₀ values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 displays cell growth arrest in prostate cancer LNCaP cells, with an IC₅₀ of 9.9 μM^[1].

IC₅₀ & Target

MAO-A

0.028 ± 0. μM (IC₅₀)

MAO-B

0.327 ± 0. μM (IC₅₀)

分子量

328.41

Formula

C₂₂H₂₀N₂O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Fioravanti R, et al. Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity. J Enzyme Inhib Med Chem. 2022 Dec;37(1):973-985.

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LSD1-IN-16

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-16

LSD1-IN-16 (compound 4b) 是一种有效的 LSD1 抑制剂。LSD1-IN-16 对LSD1-CoREST、MAO-A 和 MAO-B 具有抑制作用，IC₅₀ 值分别为 0.015、0.024 和 0.366 μM。LSD1-IN-16 在前列腺癌 LNCaP 细胞中显示细胞生长阻滞，IC₅₀ 为 15.2 μM。

LSD1-IN-16 Chemical Structure

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生物活性

LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC₅₀ values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC₅₀ of 15.2 μM^[1].

IC₅₀ & Target

MAO-A

0.024 ± μM (IC₅₀)

MAO-B

0.366 ± μM (IC₅₀)

分子量

334.43

Formula

C₂₀H₁₈N₂OS

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Fioravanti R, et al. Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity. J Enzyme Inhib Med Chem. 2022 Dec;37(1):973-985.

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LSD1-IN-17

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-17

LSD1-IN-17 (compound 5b) 是一种有效的 LSD1 抑制剂。LSD1-IN-17 对LSD1-CoREST、MAO-A 和 MAO-B 具有抑制作用，IC₅₀ 值分别为 0.005、0.028 和 0.820 μM。LSD1-IN-17 在前列腺癌 LNCaP 细胞中显示细胞生长阻滞，IC₅₀ 为 17.2 μM。

LSD1-IN-17 Chemical Structure

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生物活性

LSD1-IN-17 (compound 5b) is a potent LSD1 inhibitor. LSD1-IN-17 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC₅₀ values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 displays cell growth arrest in prostate cancer LNCaP cells, with an IC₅₀ of 17.2 μM^[1].

IC₅₀ & Target

MAO-A

0.028 ± 0. μM (IC₅₀)

MAO-B

0.820 ± 0. μM (IC₅₀)

分子量

334.43

Formula

C₂₀H₁₈N₂OS

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Fioravanti R, et al. Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity. J Enzyme Inhib Med Chem. 2022 Dec;37(1):973-985.

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LSD1-IN-18

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-18

LSD1-IN-18 (compound 7) 是一种有效的，非共价的和选择性的 LSD1 抑制剂，其 K_i 值为 0.156 μM，K_D 为 0.075 μM。LSD1-IN-18 在 THP-1 白血病细胞和 MDA-MB-231 乳腺癌细胞中显示出抗增殖活性，其 IC₅₀ (72 h) 分别为 0.16 和 0.21 μM。

LSD1-IN-18 Chemical Structure

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生物活性	LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with K_i of 0.156 μM and K_D of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC₅₀ (72 h) of 0.16 and 0.21 μM, respectively^[1].
IC₅₀ & Target	K_i of 0.156 μM (LSD1, Lysine-specific demethylase 1)^[1]
分子量	528.69
Formula	C₃₁H₄₀N₆O₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Menna M, et al. Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models. Eur J Med Chem. 2022 Jul 5;237:114410.

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LSD1-IN-19

发表于2023年12月8日由上海金畔生物科技有限公司

LSD1-IN-19

LSD1-IN-19 (compound 29) 是一种有效的，非共价的和选择性的 LSD1 抑制剂，其 K_i 值为 0.108 μM，K_D 为 0.068 μM。LSD1-IN-19 在 THP-1 白血病细胞和 MDA-MB-231 乳腺癌细胞中显示出抗增殖活性，其 IC₅₀ (72 h) 分别为 0.17 和 0.40 μM。

LSD1-IN-19 Chemical Structure

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生物活性	LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with K_i of 0.108 μM and K_D of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC₅₀ (72 h) of 0.17 and 0.40 μM, respectively^[1].
IC₅₀ & Target	K_i of 0.108 μM (LSD1, Lysine-specific demethylase 1)^[1]
分子量	554.73
Formula	C₃₃H₄₂N₆O₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Menna M, et al. Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models. Eur J Med Chem. 2022 Jul 5;237:114410.

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标签归档：lsd

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