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Bisindolylmaleimide I

Bisindolylmaleimide I GF109203X; Go 6850

Bisindolylmaleimide I (GF109203X) 是一种高度选择，可渗透细胞，可逆的 PKC抑制剂，Ki 值为14 nM。

货号：
TK0494
规格：

1mg

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	133052-90-1
生物活性	Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
分子式	C25H24N4O2
分子量	412.48
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	4°C, protect from light
溶解性数据	DMSO : ≥ 32 mg/mL (77.58 mM)
体内研究	Pial arteriole diameter changes are monitored using a closed cranial window in vivo microscopy technique. The pial arteriole dilatory response associated with SNS is decreased by 45%, when comparing DM vs either ND or TR rats. Also, pial arteriolar dilations to topical KCl and NS1619 are largely attenuated in DM rats, but not in ND or TR animals. These responses are completely restored by the acute application of Bisindolylmaleimide I to the brain surface. The PKC inhibitor has no effect on vascular responses in normoglycemic and TR animals. In conclusion, DM-associated chronic impairment of neurovascular coupling may be readily reversed by a PKC-α/β/γ inhibitor or prevented via pancreatic islet transplantation. Specific PCK isoforms (α/β/γ) are believed to be mechanistically linked to the neurovascular uncoupling seen with hyperglycemia.
体外研究	Bisindolylmaleimide I is a competitive inhibitor with respect to ATP (Ki=14 nM) and displays high selectivity for PKC as compared to five different protein kinases. GF 109203X efficiently prevents PKC-mediated phosphorylations of an Mr=47,000 protein in platelets and of an Mr=80,000 protein in Swiss 3T3 cells. GF 109203X inhibits collagen- and a-thrombin-induced platelet aggregation as well as collagen-triggered ATP secretion. However, ADP-dependent reversible aggregation is not modified. In Swiss 3T3 fibroblasts, GF 109203X reverses the inhibition of epidermal growth factor binding induced by phorbol 12,13-dibutyrate and prevents [H] thymidine incorporation into DNA, only when this is elicited by growth promoting agents which activate PKC.
纯度及产品资料	98%

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