SST0287CL1 is a potent, small molecule Heat Shock Protein 90 (HSP90) inhibitor. SST0287CL1 is more active than NVP-AUY922. SST0287CL1 was selected for further investigation as the most promising compound candidate.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.
Taddei M, et al. J Med Chem. 2014 Mar 27;57(6):2258-74. PMID: 24588105.
|Related HSP90 Products|
Teprenone(Geranylgeranylacetone; GGA)is commonly utilized to protect the gastric mucosa in peptic ulcer disease; has been shown to protect the myocardium from ischemia/reperfusion by activating heat shock proteins.
Celastrol is a potent antioxidant and anti-inflammatory agent and a novel HSP90 inhibitor.
CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
Retaspimycin is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90).
KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM.
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