DC Chemicals Limited
China
Product Name: Bisindolylmaleimide I HCl
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Purity: 98.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: BISINDOLYLMALEIMIDE I( HYDROCHLORIDE SALT)
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
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176504-36-2

176504-36-2 structure

Name: Bisindolylmaleimide I HCl
Chemical Name: 3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione,hydrochloride
CAS Number: 176504-36-2
Molecular Formula: C₂₅H₂₅ClN₄O₂
Molecular Weight: 448.94500
Catalog: Signaling Pathways Epigenetics PKC
Create Date: 2018-07-30 15:30:16
Modify Date: 2024-01-06 19:53:47
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].

Name	3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione,hydrochloride
Synonyms	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

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.

Molecular Formula	C₂₅H₂₅ClN₄O₂
Molecular Weight	448.94500
Exact Mass	448.16700
PSA	73.62000
LogP	4.71940
Storage condition	-20℃

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR	NONH for all modes of transport

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