SKLB325

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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。

SKLB325  纯度: 99.79%

SKLB325 是一种 JMJD6 抑制剂，其结合亲和力 (KD) 值为 0.755 μM，IC50 值为 0.7797 μM。SKLB325 在体内外对卵巢癌具有抗肿瘤作用。SKLB325 诱导细胞凋亡 (apoptosis)。SKLB325 在肾细胞癌 (RCC) 中表现出显着的抗肿瘤功效。

SKLB325

SKLB325 Chemical Structure

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg ￥5200 In-stock
25 mg ￥9800 In-stock
50 mg ￥14200 In-stock
100 mg   询价  
200 mg   询价  

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SKLB325 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library

生物活性

SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis[1]. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) [2].

体外研究
(In Vitro)

SKLB325 suppresses ovarian cancer growth through inhibition of proliferation and induction of apoptosis and cell death, and inhibiting angiogenesis may play a significant role in inhibiting tumor growth[1].
SKLB325 (0.25-16 μM; for 24-72 h) has significant inhibitory effects on the in vitro proliferation of ovarian cancer cells. Furthermore, the most effective concentration at which JMJD6 inhibited SKOV3 cell growth is 4 μM, and the optimal duration of action is 72 h[1].
SKLB325 upregulates the expression of p53 and its downstream effectors at both the mRNA and protein levels in vitro[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: SKOV3, ES2, A2780s and CP70 cells
Concentration: 0, 0.25, 0.5, 1, 2, 4, 8, and 16 μM
Incubation Time: 24 h, 48 h, and 72 h
Result: With increasing SKLB325 concentration, the inhibitory effect also increased, exhibiting a significant dose-response relationship. There was a significant difference between the drug group across different doses and the control group.

Western Blot Analysis[1]

Cell Line: SKOV3, ES2 and A2780s cells
Concentration: 4 μM
Incubation Time: 72 hours
Result: p53, p21, and PUMA protein levels were significantly upregulated in SKOV3, ES2 and A2780s cells.

体内研究
(In Vivo)

SKLB325 (10 mg/kg) has antitumor activities in an intraperitoneal xenograft model. SKLB325 significantly prolongs the survival of tumor-bearing mice without obvious side effects. SKLB325 treatment protocols were effective in suppressing SKOV3, ES2, CP70, and A2780s tumor growth in nude mice[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: Female athymic BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: I.p. injections every three days for eight doses total
Result: The average weight of intraperitoneal tumor nodules was 1.56 ± 0.70, 1.04 ± 0.62, and 0.14 ± 0.11 g in the control, vehicle and SKLB325 groups, respectively. Tumor weight was significantly reduced by 91 and 86% in the SKLB325 groups compared to the control and vehicle groups, respectively.

分子量

244.25

Formula

C12H12N4O2
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 : 20.83 mg/mL (85.28 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0942 mL 20.4708 mL 40.9417 mL
5 mM 0.8188 mL 4.0942 mL 8.1883 mL
10 mM 0.4094 mL 2.0471 mL 4.0942 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: ≥ 2.08 mg/mL (8.52 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.52 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% corn oil

    Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.52 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]. Heng Zheng, et al. Jumonji domain-containing 6 (JMJD6) identified as a potential therapeutic target in ovarian cancer. Signal Transduct Target Ther.2019 Jul 26;4:24.

    [2]. Chuanjie Zhang, et al. Epigenome screening highlights that JMJD6 confers an epigenetic vulnerability and mediates sunitinib sensitivity in renal cell carcinoma. Clin Transl Med. 2021 Feb;11(2):e328.

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