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WM-1119

Cat. No. M10585
WM-1119 Structure
Synonym:

WM1119

Size Price Availability Quantity
5mg USD 130  USD130 In stock
10mg USD 220  USD220 In stock
25mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding KD values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively. WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. Treatment of MEFs with WM-1119 results in cell cycle arrest in G1 and a senescence phenotype. WM-1119 arrests the progression of lymphoma in mice. WM-1119 is well-tolerated; mice show no generalized ill effects and weight loss is not observed. The proportion and overall number of tumour cells is substantially reduced by WM-1119 treatment (four times per day).

Chemical Information
Molecular Weight 389.38
Formula C18H13F2N3O3S
CAS Number 2055397-28-7
Solubility (25°C) DMSO 80 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] Jonathan B Baell, et al. Nature. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth

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  Catalog
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Keywords: WM-1119, WM1119 supplier, Histone Acetyltransferase, inhibitors, activators


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