Bisindolylmaleimide I


CAS No. : 133052-90-1

(Synonyms: GF109203X; Go 6850)

133052-90-1
Price and Availability of CAS No. : 133052-90-1
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Cat. No. : HY-13867
M.Wt: 412.48
Formula: C25H24N4O2
Purity: >98 %
Solubility: DMSO : ≥ 32 mg/mL
Introduction of 133052-90-1 :

Bisindolylmaleimide I (GF109203X) 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 is also a GSK-3 inhibitor[1][2][3]. IC50 & Target:IC50: 20±7 nM (PKC α); 17±5 nM (PKC βI); 16±5 nM (PKC βII); 20±5 nM (PKC γ)[1] In Vitro:Bisindolylmaleimide I (5 μM) inhibits α-thrombin-induced P47 phosphorylation[1].
Bisindolylmaleimide I (0-1 μM) inhibits DNA synthesis in quiescent swiss 3T3 cells[1].
Bisindolylmaleimide I (5 μM) reduces GSK-3 activity to 25.1±4.3% in adipocytes lysates[3].
Bisindolylmaleimide I (10 μM, 24 h) inhibits exosome and microvesicle (EMV) release from PC3 cells[4].
Bisindolylmaleimide I (10 μM, 24 h) enhances cytotoxicity of 5-fluorouracil (HY-90006)[4].
In Vivo:Bisindolylmaleimide I (0.02 mg/kg, i.p.) reduced the inceased NLRP3, P-PKCɑ, and PKCɑ levels in mechanical ventilation (MV) group in mice[5].
Bisindolylmaleimide I (0-20 mg/kg, i.p.) reduces the mean frequency of Quinpirole-induced vomiting in shrews[6].

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