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HSP27 inhibitor J2

Cat. No. M13682
HSP27 inhibitor J2 Structure
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Biological Activity

HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.

Chemical Information
Molecular Weight 264.3
CAS Number 2133499-85-9
Solubility (25°C) DMSO 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Cara C Rada, et al. Sci Signal. Heat shock protein 27 activity is linked to endothelial barrier recovery after proinflammatory GPCR-induced disruption

[2] Hawon Yoo, et al. Pharmaceutics. Drug-Like Small Molecule HSP27 Functional Inhibitor Sensitizes Lung Cancer Cells to Gefitinib or Cisplatin by Inducing Altered Cross-Linked Hsp27 Dimers

[3] Jee-Youn Kim, et al. Clin Cancer Res. The Hsp27-Mediated IkBα-NFκB Signaling Axis Promotes Radiation-Induced Lung Fibrosis

[4] Jee-Youn Kim, et al. Sci Rep. HSP27 inhibitor attenuates radiation-induced pulmonary inflammation

[5] Byeol Choi, et al. Oncotarget. Sensitization of lung cancer cells by altered dimerization of HSP27

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