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GSK 343

GSK 343 structure

CAS No:
1346704-33-3
Formula:
C31H39N7O2
Chemical Name:
GSK 343
Synonyms:
1H-Indazole-4-carboxamide,N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-;N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide;1-(1-Methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide;GSK 343
Categories:
Biochemical Engineering > Inhibitors

Description

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

GSK343 is a member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM). It has a role as an EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor, an apoptosis inducer and an antineoplastic agent. It is a N-alkylpiperazine, a secondary carboxamide, an aminopyridine, a pyridone, a N-arylpiperazine and a member of indazoles.

GSK 343 Basic Attributes

Molecular Weight：

541.68706

Exact Mass：

541.69

Characteristics

PSA：

95.4

XLogP3：

Appearance：

white to beige to brown

Density：

1.26±0.1 g/cm3(Predicted)

Boiling Point：

797.4±60.0 °C(Predicted)

Flash Point：

436.0±32.9 °C

Refractive Index：

1.654

Water Solubility：

DMSO: soluble15mg/mL, clear

Storage Conditions：

2-8°C

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

Marks：

Precautionary statement(s)：

P301 + P312 + P330

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 39 companies from 2 notifications to the ECHA C&L Inventory.

Drug Information

MeSH Entry Terms：

GSK343

Computed Properties

Molecular Weight:541.7
XLogP3:4
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:8
Exact Mass:541.31652351
Monoisotopic Mass:541.31652351
Topological Polar Surface Area:95.4
Heavy Atom Count:40
Complexity:986
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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GSK343

CAS No.: 1346704-33-3

Content: 95%

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