Bisindolylmaleimide I HCl

Names

[ Name ]:
Bisindolylmaleimide I HCl

[Synonym ]:
Bisindolylmaleimide I,HCl
Bisindolylmaleimide I
3-[1-(Dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride
Go-6850
BIM I
Bisindolylmaleimide I hydrochloride
Bisindolylmaleimide
2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide,HCl

Biological Activity

[Description]:

Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor[1][2][3].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Signaling Pathways >> Stem Cell/Wnt >> GSK-3

Research Areas >> Cancer

Research Areas >> Metabolic Disease

Signaling Pathways >> TGF-beta/Smad >> PKC

Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

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)

[In Vitro]

Bisindolylmaleimide I hydrochloride (5 μM) 抑制 α-凝血酶诱导的 P47 磷酸化[1]。 Bisindolylmaleimide I hydrochloride (0-1 μM) 抑制静息态 swiss 3T3 细胞中的 DNA 合成[1]。 Bisindolylmaleimide I hydrochloride (5 μM) 可将脂肪细胞裂解物中的 GSK-3 活性降低至 25.1±4.3%[3]。 Bisindolylmaleimide I hydrochloride (10 μM，24 小时) 抑制 PC3 细胞释放外泌体和微泡 (EMV)[4]。 Bisindolylmaleimide I hydrochloride (10 μM，24 小时) 增强 5-fluorouracil (HY-90006) 的细胞毒性[4]。

[In Vivo]

Bisindolylmaleimide I hydrochloride (0.02 mg/kg，腹腔注射.) 降低小鼠机械通气 (MV) 组中升高的 NLRP3、P-PKCɑ 和 PKCɑ 水平[5]。 Bisindolylmaleimide I hydrochloride (0-20 mg/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]。 Animal Model: Quinpirole-treated shrews[2] Dosage: 0-20 mg/kg Administration: i.p. Result: Reduced the mean frequency of Quinpirole-induced vomiting. Blocked Quinpirole-mediated ERK1/2 phosphorylation in shrew brainstems.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₅ClN₄O₂

[ Molecular Weight ]:
448.94500

[ Exact Mass ]:
448.16700

[ PSA ]:
73.62000

[ LogP ]:
4.71940

[ Storage condition ]:
-20℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

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...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.