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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).
| 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 |
| 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.
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CPI-1612 is a tool compound that appears to be a fairly efficient EP300/CBP histone acetyltransferase (HAT) inhibitor, exhibiting activity in xenograft models with good PK of higher species. |
| CTPB
CTPB is a good activator of p300 histone acetyl transferase (HAT) enzyme. |
| Butyrolactone 3
Butyrolactone 3 (MB-3) is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. |
| WM-3835
WM-3835 is a potent, highly specific HBO1 (KAT7 or MYST2) inhibitor that binds directly to the acetyl-Coenzyme A binding site of HBO1 33 and WM-3835 activates apoptosis while inhibiting proliferation, migration, and invasion of osteosarcoma (OS) cells. WM-3835 has anti-tumor activity and effectively inhibits the growth of osteosarcoma xenografts in mice. |
| TH1834
TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. |
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