92831-11-3
92831-11-3 structure
- Name: 2-(4-Isopropylpheny)-4H-chroMen-4-one
- Chemical Name: 4H-1-Benzopyran-4-one, 2-[4-(1-methylethyl)phenyl]
- CAS Number: 92831-11-3
- Molecular Formula: C18H16O2
- Molecular Weight: 264.31800
- Catalog: Research Areas Cancer
- Create Date: 2017-05-04 04:24:45
- Modify Date: 2024-01-02 08:34:29
-
MN-64 is a potent tankyrase 1 inhibitor, with IC50s of 6 nM, 72 nM, 19.1 μM, and 39.4 μM for TNKS1, TNKS2, ARTD1 and ARTD2, respectively.
| Name | 4H-1-Benzopyran-4-one, 2-[4-(1-methylethyl)phenyl] |
|---|---|
| Synonyms |
2-[4-(1-Methylethyl)phenyl4H-1-benzopyran-4-one
2-(4-Isopropylpheny)-4H-chroMen-4-one MN-64 |
| Description | MN-64 is a potent tankyrase 1 inhibitor, with IC50s of 6 nM, 72 nM, 19.1 μM, and 39.4 μM for TNKS1, TNKS2, ARTD1 and ARTD2, respectively. |
|---|---|
| Related Catalog | |
| Target |
TNKS1:6 nM (IC50) TNKS2:72 nM (IC50) ARTD1:19.1 μM (IC50) ARTD2:39.4 μM (IC50) |
| In Vitro | MN-64 is a potent tankyrase 1 inhibitor, with IC50s of 6 nM, 72 nM, 19.1 μM, 39.4 μM for TNKS1, TNKS2, ARTD1 and ARTD2, respectively. MN-64 effectively inhibits Wnt/β-catenin at 1 μM, and blocks STF luciferase activity at 200 nM[1]. |
| Kinase Assay | Inhibitory potency of compounds on Tankyrase-1 enzymatic activity is evaluated using a Scintillation Proximity Assay (SPA). The assay is designed to measure compound inhibition of Tankyrase-1 autoPARsylation (Tankyrase-1 is both enzyme and substrate in this assay). Truncated recombinant human Tankyrase-1 protein (amino acids E1023-T1327) is purified from SF9 cells. The assay is conducted using 0.11 μM of Tankyrase-1 protein and 3 μM nicotinamide adenine dinucleotide (NAD+, 2.12 μM 3H-NAD+ with a specific radioactivity of 1690 Ci/mol, 0.88 μM biotin- NAD+), in pH 7.5 Tris buffer (60 mM Tris, 1 mM DTT, 0.01% (v/v) Tween-20®, 2.5 mM MgCl2, 0.3 mg/mL BSA). For IC50 determination, 10 mM DMSO stock solution of a compound (MN-64) is sequentially diluted by two-fold in DMSO, and aliquots of the diluted solutions are transferred to 384-well assay plates and mixed with Tankyrase-1 solution[1]. |
| References |
| Density | 1.152±0.06 g/cm3 (20 °C, 760 mmHg) |
|---|---|
| Boiling Point | 389.8±42.0 °C (760 mmHg) |
| Melting Point | 63-64 °C (ethanol) |
| Molecular Formula | C18H16O2 |
| Molecular Weight | 264.31800 |
| Exact Mass | 264.11500 |
| PSA | 30.21000 |
| LogP | 4.58340 |
| Appearance | white solid |
| Storage condition | -20℃ |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 |
| RIDADR | UN 2811 6.1 / PGIII |