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GSK467

Cat. No. M13832
GSK467 Structure
Size Price Availability Quantity
10mg USD 300  USD300 In stock
25mg USD 525  USD525 In stock
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Quality Control & Documentation
Biological Activity

GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.

Chemical Information
Molecular Weight 319.32
CAS Number 1628332-52-4
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] Sarder Arifuzzaman, et al. Pharmacol Res. Research update and opportunity of non-hormonal male contraception: Histone demethylase KDM5B-based targeting

[2] Catrine Johansson, et al. Nat Chem Biol. Structural analysis of human KDM5B guides histone demethylase inhibitor development

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  Catalog
Abmole Inhibitor Catalog




Keywords: GSK467 supplier, Histone demethylase, inhibitors, activators


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