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MG149 is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM). MG 149, at 200 μM, inhibites about 90% of Tip60 activity but has no inhibitory impact on p300 and PCAF. MG 149 is essentially competitive with Ac-CoA and noncompetitive with the histone substrate. MG149 inhibits acetyltransferase activity of nuclear extract from tissue samples from different brain regions in mice. MG149 inhibits the p53 and the NF-κB pathways.
| 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.
| Molecular Weight | 340.46 |
| Formula | C22H28O3 |
| CAS Number | 1243583-85-8 |
| Purity | >98% |
| Solubility | DMSO 10 mM |
| Storage | at -20°C |
| Related Histone Acetyltransferase Products |
|---|
| CPI-1612
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. |
| WM-1119
WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM, Kd of 2 nM, WM-1119 is a reversible competitor of acetyl coenzyme A and inhibits MYST-catalysed histone acetylation. |
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