生物活性

GF 109203X是一种有效且选择性的蛋白激酶C抑制剂，对α和β1亚型具有选择性（对于α，β1，δ，δ，ε和ζ亚型，IC50分别为0.0084、0.0180、0.210、0.132和5.8μM）。对MLCK，PKG和PKA具有选择性（IC50值分别为0.6、4.6和33μM）。5-HT3受体的强效拮抗剂（Ki = 29.5 nM）。= 29.5 nm)。

Targets

Target	Value
PKCβ2	IC50: 16nM
PKCβ1	IC50: 17nM
PKCα	IC50: 20nM
PKCγ	IC50: 20nM
PDGFR	IC50: 65μM
EGFR	IC50: >100μM
Insulin Receptor	IC50: >100μM

化学数据

目录号	A13197
作用机制	Inhibitor (抑制剂)
M. Wt	412.49
Formula	C25H24N4O2
Purity	>99%
Storage	Store lyophilized at -20?C, keep desiccated. In lyophilized form, the chemical is stable for36 months. In solution, store at -20?C and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
CAS No.	133052-90-1
Synonyms	GF-109203X, GF109203X, GO6850, GO-6850, Bisindolylmaleimide I
SMILES	CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

溶解度

In vitro	DMSO	70 mg/mL (169.7 mM)
	Water	Insoluble
	Ethanol	Insoluble
*<1 mg/ml means slightly soluble or insoluble. *Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

储备液配制

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	24.24 mL	121.22 mL	242.43 mL
0.5 mM	4.85 mL	24.24 mL	48.49 mL
1 mM	2.42 mL	12.12 mL	24.24 mL
5 mM	0.48 mL	2.42 mL	4.85 mL

*The above data is based on the productmolecular weight 412.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.