SB-747651A二盐酸盐 T9652
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Product IntroductionBioactivity英文名: SB-747651A Dihydrochloride描述: SB-747651A dihydrochloride是一种与ATP竞争性相互作用的抑制剂，特别针对丝裂原和应激
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Product Introduction
Bioactivity
英文名: SB-747651A Dihydrochloride
描述: SB-747651A dihydrochloride是一种与ATP竞争性相互作用的抑制剂，特别针对丝裂原和应激激活激酶1 (MSK1)，IC50值为11 nM。此化合物还能抑制PRK2、RSK1、p70S6K和ROCK-II等酶的活性。因其对上述激酶的抑制作用，SB-747651A dihydrochloride在炎症研究中显示出潜力。
体外活性: 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].
体内活性: 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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (120.39 mM)
关键字: SB747651A Dihydrochloride | SB 747651A Dihydrochloride | SB-747651A | SB-747651A Dihydrochloride
相关产品: Fasudil hydrochloride | Y-9738 | Hydroxyfasudil | RKI-1447 | SB-772077B dihydrochloride | Cotosudil | Ripasudil | CCG-222740 | WAY-656935 | URMC-099
相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | TGF-beta/Smad Compound Library | Bioactive Compound Library
Bioactivity
英文名: SB-747651A Dihydrochloride
描述: SB-747651A dihydrochloride是一种与ATP竞争性相互作用的抑制剂，特别针对丝裂原和应激激活激酶1 (MSK1)，IC50值为11 nM。此化合物还能抑制PRK2、RSK1、p70S6K和ROCK-II等酶的活性。因其对上述激酶的抑制作用，SB-747651A dihydrochloride在炎症研究中显示出潜力。
体外活性: 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].
体内活性: 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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (120.39 mM)
关键字: SB747651A Dihydrochloride | SB 747651A Dihydrochloride | SB-747651A | SB-747651A Dihydrochloride
相关产品: Fasudil hydrochloride | Y-9738 | Hydroxyfasudil | RKI-1447 | SB-772077B dihydrochloride | Cotosudil | Ripasudil | CCG-222740 | WAY-656935 | URMC-099
相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | TGF-beta/Smad Compound Library | Bioactive Compound Library
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