17-AAG (Tanespimycin) is a less toxic analogue of the geldanamycin which binds to Hsp90 and alters its function. HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, and oncogenesis. 17-AAG (Tanespimycin) binds into the ATP binding pocket in Hsp90 and induces the degradation of proteins that require this chaperone for conformational maturation. 17-AAG (Tanespimycin) inhibits Akt activation and expression in tumors and synergizes with a number of antitumor agents such as taxol, cisplatin, and UCN-014.
|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.
|Solubility||DMSO 80 mg/mL|
|Related HSP90 Products|
Apoptozole is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
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).
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