二吲哚基顺丁烯二酰亚胺 I盐酸

二吲哚基顺丁烯二酰亚胺 I盐酸用途

双吲哚甲酰胺I(GF109203X)盐酸盐是一种细胞可渗透和可逆的PKC抑制剂(PKCα、PKCβI、PKCαII和PKCγ的IC50分别为20nM、17nM、16nM和20nM。双吲吲哚甲酰胺I盐酸盐也是一种GSK-3抑制剂[1][2][3]。

二吲哚基顺丁烯二酰亚胺 I盐酸名称

[ CAS 号 ]:
176504-36-2

[ 中文名 ]:
二吲哚基顺丁烯二酰亚胺 I盐酸

[ 英文名 ]:
Bisindolylmaleimide I HCl

[英文别名 ]:

Bisindolylmaleimide I,HCl
Bisindolylmaleimide I
Go-6850
BIM I
Bisindolylmaleimide I hydrochloride
Bisindolylmaleimide

二吲哚基顺丁烯二酰亚胺 I盐酸生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

信号通路 >> 干细胞及 Wnt 通路 >> GSK-3

研究领域 >> 癌症

研究领域 >> 代谢疾病

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

信号通路 >> PI3K/Akt/mTOR 信号通路 >> GSK-3

[ 靶点 ]

Bovine brain PKC:10 nM (IC50)

PKC-βII:16 nM (IC50)

PKC-βI:17 nM (IC50)

PKCα:20 nM (IC50)

PKCγ:20 nM (IC50)

FDGFG:65 μM (IC50)

[体外研究]

盐酸双吲哚美胺I(5μM)抑制 α-凝血酶诱导的第47页磷酸化[1]。盐酸双吲哚美胺I(0-1μM)抑制静息态瑞士3T3细胞中的脱氧核糖核酸合成[1]。盐酸双吲哚美胺I(5μM)可将脂肪细胞裂解物中的 GSK-3型活性降低至 25.1±4.3%[3]。盐酸双吲哚美胺I(10μM,24小时) 抑制第3页细胞释放外泌体和微泡 (EMV)[4]盐酸双吲哚美胺I(10μM,24小时) 增强 5-氟尿嘧啶(HY-90006)的细胞毒性[4]。

[体内研究]

盐酸双吲哚美胺I(0.02mg/kg腹腔注射.) 降低小鼠机械通气 (MV)组中升高的 NLRP3、P-PKC和 PKCå水平[5]。盐酸双吲哚美胺I(0-20mg/kg腹腔注射) 降低了鼩鼱中喹吡罗诱导的呕吐的平均频率[6]。动物模型：喹吡罗治疗的泼妇[2]剂量：0-20 mg/kg给药：腹腔注射结果：降低了喹吡罗诱发呕吐的平均频率。阻断喹吡唑介导的泼妇脑干ERK1/2磷酸化。

[参考文献]

[1]. Toullec D, 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.

[2]. Vetri F, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54.

[3]. Hers I, et al. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6.

[4]. Kosgodage US, et al. Chloramidine/Bisindolylmaleimide-I-Mediated Inhibition of Exosome and Microvesicle Release and Enhanced Efficacy of Cancer Chemotherapy. Int J Mol Sci. 2017 May 9;18(5):1007.

[5]. Liu M, et al. Aerobic exercise alleviates ventilator-induced lung injury by inhibiting NLRP3 inflammasome activation. BMC Anesthesiol. 2022 Dec 1;22(1):369.

[6]. Belkacemi L, et al. Signal transduction pathways involved in dopamine D2 receptor-evoked emesis in the least shrew (Cryptotis parva). Auton Neurosci. 2021 Jul;233:102807.

二吲哚基顺丁烯二酰亚胺 I盐酸物理化学性质

[ 分子式 ]:
C₂₅H₂₅ClN₄O₂

[ 分子量 ]:
448.94500

[ 精确质量 ]:
448.16700

[ PSA ]:
73.62000

[ LogP ]:
4.71940

[ 储存条件 ]:
-20℃

二吲哚基顺丁烯二酰亚胺 I盐酸MSDS

详细MSDS(安全技术说明书)

二吲哚基顺丁烯二酰亚胺 I盐酸安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

二吲哚基顺丁烯二酰亚胺 I盐酸文献

Protein kinase C-mediated phosphorylation of a single serine residue on the rat glial glutamine transporter SN1 governs its membrane trafficking.

J. Neurosci. 31 , 6565-75, (2011)

Molecular mechanisms involved in the replenishment of the fast neurotransmitters glutamate and GABA are poorly understood. Glutamine sustains their generation. However, glutamine formation from the re...

The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.

J. Biol. Chem. 266 , 15771, (1991)

Staurosporine is the most potent inhibitor of protein kinase C (PKC) described in the literature with a half-maximal inhibitory concentration (IC50) of 10 nM. Nevertheless, this natural product is poo...

PDGF receptor activation induces p120-catenin phosphorylation at serine 879 via a PKCalpha-dependent pathway.

Exp. Cell Res. 315 , 39-49, (2009)

p120-catenin (p120) is required for cadherin stability and is thought to have a central role in modulating cell-cell adhesion. Several lines of evidence suggest that S/T phosphorylation may regulate p...

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