MALT1 inhibitor MI-2

发表于由

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。

MALT1 inhibitor MI-2  纯度: 99.88%

MALT1 inhibitor MI-2 是一种 MALT1 抑制剂 (IC50=5.84 μM)，MALT1 inhibitor MI-2 直接与 MALT1 结合，不可逆地抑制蛋白酶功能，并伴有 NF-κB 报告子活性抑制、c-REL 核定位抑制和 NF-κB 靶基因下调。MALT1 inhibitor MI-2 对动物无毒。

MALT1 inhibitor MI-2

MALT1 inhibitor MI-2 Chemical Structure

CAS No. : 1047953-91-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥1450 In-stock
50 mg ￥4800 In-stock
100 mg ￥8600 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MALT1 inhibitor MI-2 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • NF-κB Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Targeted Diversity Library

生物活性

MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals[1].

IC50 & Target

IC50: 5.84 μM (MALT1)[1]
体外研究
(In Vitro)

MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 µM, respectively[1].
MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage[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.

Cell Proliferation Assay[1]

Cell Line: HBL-1, TMD8, OCI-Ly3, OCI-Ly10 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 48 hours
Result: The GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells was 0.2, 0.5, 0.4, and 0.4 µM, respectively.

Western Blot Analysis[1]

Cell Line: HBL-1 cells
Concentration: 62, 125, 250, 500, 1000 nM
Incubation Time: 24 hours
Result: Inhibits MALT1 cleavage of CYLD in HBL-1 cells.

体内研究
(In Vivo)

MALT1 inhibitor MI-2 (25 mg/kg; i.p.; daily for 14 days) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts[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.

Animal Model: Eight-week-old male SCID NOD (bearing HBL-1 and TMD8 cells)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; daily for 14 days
Result: Profoundly suppressed the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts versus vehicle.

分子量

455.72

Formula

C19H17Cl3N4O3
CAS 号

1047953-91-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 46 mg/mL (100.94 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 2.1943 mL 10.9716 mL 21.9433 mL
5 mM 0.4389 mL 2.1943 mL 4.3887 mL
10 mM 0.2194 mL 1.0972 mL 2.1943 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。-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: ≥ 2.5 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.49 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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% corn oil

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.49 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 25.0 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]. Fontan L, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012 Dec 11;22(6):812-24.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务