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Grp94 Inhibitor-1

Cat. No. M13681
Grp94 Inhibitor-1 Structure
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Biological Activity

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.

Chemical Information
Molecular Weight 352.47
CAS Number 2234897-35-7
Solubility (25°C) DMSO 150 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] Mengmeng Niu, et al. Nat Commun. FBXL2 counteracts Grp94 to destabilize EGFR and inhibit EGFR-driven NSCLC growth

[2] Jeong Hwan Oh, et al. Mar Drugs. Hydrophilic Glycoproteins of an Edible Green Alga Capsosiphon fulvescens Prevent Aging-Induced Spatial Memory Impairment by Suppressing GSK-3β-Mediated ER Stress in Dorsal Hippocampus

[3] Alexandra C Schrimpe-Rutledge, et al. J Proteome Res. Discovery of novel glucose-regulated proteins in isolated human pancreatic islets using LC-MS/MS-based proteomics

[4] J G Kiang, et al. Chin J Physiol. 17 beta-estradiol-induced increases in glucose-regulated protein 78kD and 94kD protect human breast cancer T47-D cells from thermal injury

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Keywords: Grp94 Inhibitor-1 supplier, HSP, inhibitors, activators


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