1. Epigenetics TGF-beta/Smad Stem Cell/Wnt PI3K/Akt/mTOR
  2. PKC GSK-3
  3. Bisindolylmaleimide I hydrochloride

Bisindolylmaleimide I hydrochloride  (Synonyms: GF109203X hydrochloride; Go 6850 hydrochloride)

Cat. No.: HY-13867A Purity: 99.18%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Bisindolylmaleimide I hydrochloride Chemical Structure

Bisindolylmaleimide I hydrochloride Chemical Structure

CAS No. : 176504-36-2

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5 mg USD 156 In-stock
10 mg USD 250 In-stock
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Based on 28 publication(s) in Google Scholar

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  • Purity & Documentation

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  • Customer Review

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].

IC50 & Target[1]

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) inhibits α-thrombin-induced P47 phosphorylation[1].
Bisindolylmaleimide I hydrochloride (0-1 μM) inhibits DNA synthesis in quiescent swiss 3T3 cells[1].
Bisindolylmaleimide I hydrochloride (5 μM) reduces GSK-3 activity to 25.1±4.3% in adipocytes lysates[3].
Bisindolylmaleimide I hydrochloride (10 μM, 24 h) inhibits exosome and microvesicle (EMV) release from PC3 cells[4].
Bisindolylmaleimide I hydrochloride (10 μM, 24 h) enhances cytotoxicity of 5-fluorouracil (HY-90006)[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bisindolylmaleimide I hydrochloride (0.02 mg/kg, i.p.) reduced the inceased NLRP3, P-PKCɑ, and PKCɑ levels in mechanical ventilation (MV) group[5].
Bisindolylmaleimide I hydrochloride (0-20 mg/kg, i.p.) reduces the mean frequency of Quinpirole-induced vomiting in shrews[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

448.94

Appearance

Solid

Formula

C25H25ClN4O2

CAS No.
SMILES

[H]Cl.O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (139.22 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2275 mL 11.1373 mL 22.2747 mL
5 mM 0.4455 mL 2.2275 mL 4.4549 mL
10 mM 0.2227 mL 1.1137 mL 2.2275 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.63 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Bisindolylmaleimide I hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bisindolylmaleimide I hydrochloride
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