2-(4-Isopropylpheny)-4H-chroMen-4-one

Modify Date: 2024-01-02 08:34:29

2-(4-Isopropylpheny)-4H-chroMen-4-one Structure
2-(4-Isopropylpheny)-4H-chroMen-4-one structure
Common Name 2-(4-Isopropylpheny)-4H-chroMen-4-one
CAS Number 92831-11-3 Molecular Weight 264.31800
Density 1.152±0.06 g/cm3 (20 °C, 760 mmHg) Boiling Point 389.8±42.0 °C (760 mmHg)
Molecular Formula C18H16O2 Melting Point 63-64 °C (ethanol)
MSDS Chinese USA Flash Point N/A
Symbol GHS06
GHS06
Signal Word Danger

 Use of 2-(4-Isopropylpheny)-4H-chroMen-4-one


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.

 Names

Name 4H-1-Benzopyran-4-one, 2-[4-(1-methylethyl)phenyl]
Synonym More Synonyms

 2-(4-Isopropylpheny)-4H-chroMen-4-one Biological Activity

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

[1]. Narwal M, et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9.

 Chemical & Physical Properties

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 of Characters white solid
Storage condition -20℃

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
RIDADR UN 2811 6.1 / PGIII

 Synonyms

2-[4-(1-Methylethyl)phenyl4H-1-benzopyran-4-one
2-(4-Isopropylpheny)-4H-chroMen-4-one
MN-64
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Price: $92/10mM*1mLinDMSO

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