Home>>Signaling Pathways>> Microbiology & Virology>> CMV>>Bisindolylmaleimide IV

Bisindolylmaleimide IV Sale

(Synonyms: 双吲哚马来酰亚胺IV,Arcyriarubin A,BIM IV) 目录号 : GC14716

Bisindolylmaleimide IV 是一种强效的细胞膜透过性蛋白激酶C(PKC)抑制剂,其IC50值为0.1-0.55μM。

Bisindolylmaleimide IV Chemical Structure

Cas No.:119139-23-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥353.00
现货
1mg
¥200.00
现货
5mg
¥490.00
现货
10mg
¥784.00
现货
25mg
¥1,582.00
现货
50mg
¥2,205.00
现货
100mg
¥3,080.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

Description

Bisindolylmaleimide IV is a potent cell-permeable inhibitor of protein kinase C (PKC) with IC50 values are 0.1- 0.55μM[1]. Bisindolylmaleimide IV inhibits the cAMP-dependent protein kinase (PKA) with IC50 ranging from 3.1-11.8μM[2]. Bisindolylmaleimide IV is primarily used in research related to cancer biology[3], cardiovascular diseases[4], and diabetes, particularly in studies investigating PKC-mediated signaling pathways and their impact on cellular functions[5].

Bisindolylmaleimide IV (20μM) down-regulates cellular caspase 8 (FLICE)-like inhibitory protein (c-FLIPL) expression and facilitates CD95-mediated apoptosis in monocyte-derived dendritic cells[6]. Bisindolylmaleimide IV (0.1-100μM) inhibits the release of reactive oxygen species (ROS) from human neutrophils stimulated by agents such as IL-3, phorbol-12-myristate-13-acetate (PMA), and sodium fluoride in a dose-dependent manner[7].

References:
[1]. Toullec D, Pianetti P, Coste H, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81. PMID: 1874734.
[2]. Fabre S, Prudhomme M, Rapp M. Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg Med Chem. 1993 Sep;1(3):193-6. doi: 10.1016/s0968-0896(00)82121-5. PMID: 8081852.
[3]. Pajak B, Orzechowska S, Gajkowska B, Orzechowski A. Bisindolylmaleimides in anti-cancer therapy - more than PKC inhibitors. Adv Med Sci. 2008;53(1):21-31. doi: 10.2478/v10039-008-0028-6. PMID: 18635421.
[4]. Silnitsky S, Rubin SJS, Zerihun M, Qvit N. An Update on Protein Kinases as Therapeutic Targets-Part I: Protein Kinase C Activation and Its Role in Cancer and Cardiovascular Diseases. Int J Mol Sci. 2023 Dec 18;24(24):17600. doi: 10.3390/ijms242417600. PMID: 38139428; PMCID: PMC10743896.
[5].Anderson PW, McGill JB, Tuttle KR. Protein kinase C beta inhibition: the promise for treatment of diabetic nephropathy. Curr Opin Nephrol Hypertens. 2007 Sep;16(5):397-402. doi: 10.1097/MNH.0b013e3281ead025. PMID: 17693752.
[6]. Willems F, Amraoui Z, Vanderheyde N, et al. Expression of c-FLIP(L) and resistance to CD95-mediated apoptosis of monocyte-derived dendritic cells: inhibition by bisindolylmaleimide. Blood. 2000 Jun 1;95(11):3478-82. PMID: 10828032.
[7]. Krämer HJ, Kessler D, Hipler UC, et al. Pityriarubins, novel highly selective inhibitors of respiratory burst from cultures of the yeast Malassezia furfur: comparison with the bisindolylmaleimide arcyriarubin A. Chembiochem. 2005 Dec;6(12):2290-7. doi: 10.1002/cbic.200500163. PMID: 16252297.

Bisindolylmaleimide IV是一种强效的细胞膜透过性蛋白激酶C(PKC)抑制剂,其IC50值为0.1-0.55μM[1]。Bisindolylmaleimide IV还能抑制cAMP依赖性蛋白激酶(PKA),其IC50值为3.1-11.8μM[2]。Bisindolylmaleimide IV主要用于癌症生物学[3]、心血管疾病[4]和糖尿病的研究,特别是在研究PKC介导的信号通路及其对细胞功能的影响方面[5]

Bisindolylmaleimide IV(20μM)可下调细胞型 caspase 8(FLICE)样抑制蛋白(c-FLIPL)的表达,并促进CD95介导的单核细胞来源的树突状细胞凋亡[6]。Bisindolylmaleimide IV(0.1-100μM)能够以剂量依赖的方式抑制由IL-3、佛波醇-12-肉豆蔻酸-13-乙酸酯(PMA)和氟化钠等刺激剂诱导的中性粒细胞活性氧(ROS)释放[7]

实验参考方法


References:

[1]. Willems F, Amraoui Z, Vanderheyde N, et al. Expression of c-FLIP(L) and resistance to CD95-mediated apoptosis of monocyte-derived dendritic cells: inhibition by bisindolylmaleimide. Blood. 2000 Jun 1;95(11):3478-82. PMID: 10828032.

化学性质

Cas No. 119139-23-0 SDF
别名 双吲哚马来酰亚胺IV,Arcyriarubin A,BIM IV
化学名 3,4-di-1H-indol-3-yl-1H-pyrrole-2,5-dione
Canonical SMILES O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1c[nH]c2ccccc12
分子式 C20H13N3O2 分子量 327.3
溶解度 ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 3.0553 mL 15.2765 mL 30.553 mL
5 mM 0.6111 mL 3.0553 mL 6.1106 mL
10 mM 0.3055 mL 1.5277 mL 3.0553 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

产品文档

Quality Control & SDS

View current batch: