SB-747651A dihydrochloride 是一种 ATP 竞争性的丝裂原和应激激活激酶 1 (MSK1) 抑制剂，IC50为 11 nM。SB-747651A dihydrochloride 还抑制 PRK2，RSK1，p70S6K 和 ROCK-II。SB-747651A dihydrochloride 具有炎症研究潜力。

SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC 50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride has potential for inflammation research [1].

SB-747651A dihydrochloride (5 μM; neutrophils) affects CXCL2-induced intraluminal crawling of neutrophils in a Mac-1-dependent manner. SB-747651A dihydrochloride prevents the intraluminal crawling of adherent neutrophils to optimal sites of emigration. SB-747651A dihydrochloride (5 μM; neutrophils) significantly increases transmigration time and detachment time. SB-747651A dihydrochloride affects mechanisms that regulate transendothelial migration of neutrophils in response to CXCL2 chemotactic gradient. SB-747651A dihydrochloride inhibits the migration speed of extravascular chemotaxing neutrophils but does not affect their directionality in response to CXCL2 chemotactic gradient [2].

SB747651A (3 mg/kg; intrascrotal injection) dihydrochloride causes increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2 [3]. SB-747651A (3 mg/kg; i.p.) dihydrochloride affects neutrophil extravasation by increasing neutrophil emigration only at 3 and 4 hours in mouse peritonitis model of acute inflammation [3]. Animal Model: Male C57BL/6N mice (8~16 weeks) [3] Dosage: 3 mg/kg Administration: Intrascrotal injection Result: Resulted in increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2.

1781882-72-1

C16H24Cl2N8O

415.32

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years