NSC764414

Product Name: NSC764414
CAS No.: 321695-57-2
Chemical Name: NSC764414
Synonyms: L002;NSC764414;L002(NSC764414);p300/CBP Inhibitor VI, L002;L 002;NSC 764414;L-002;NSC-764414;p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem;4-[O-[(4-Methoxyphenyl)sulfonyl]oxime]-2,6-dimethyl-2,5-cyclohexadiene-1,4-dione;[(3,5-dimethyl-4-oxo-cyclohexa-2,5-dien-1-ylidene)amino] 4-methoxybenzenesulfonate;2,5-Cyclohexadiene-1,4-dione, 2,6-dimethyl-, 4-[O-[(4-methoxyphenyl)sulfonyl]oxime];p300,acetylation,L 002,Inhibitor,HATs,L-002,HAT,inhibit,fibrosis,L002,Histone Acetyltransferase,STAT,cardiac,histone
CBNumber: CB42750596
Molecular Formula: C15H15NO5S
Formula Weight: 321.35
MOL File: 321695-57-2.mol

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NSC764414 Property

Boiling point:: 459.8±55.0 °C(Predicted)
Density: 1.28±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: soluble20mg/mL, clear
form: powder
color: white to beige

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Safety

WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0759
Product name: L002
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $105
Updated: 2024/03/01

Sigma-Aldrich

Product number: 5.05298
Product name: p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem
Packaging: 10MG
Price: $138
Updated: 2023/01/07

Sigma-Aldrich

Product number: SML0759
Product name: L002
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $377
Updated: 2022/05/15

Cayman Chemical

Product number: 17778
Product name: L002
Purity: ≥98%
Packaging: 5mg
Price: $81
Updated: 2024/03/01

Cayman Chemical

Product number: 17778
Product name: L002
Purity: ≥98%
Packaging: 10mg
Price: $120
Updated: 2024/03/01

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NSC764414 Chemical Properties,Usage,Production

Description

L002 is an inhibitor of p300 histone acetyltransferase (KAT3B; IC₅₀ = 1.98 μM in vitro). It has weaker inhibitory effects against PCAF and GCN5 (IC₅₀s = 35 and 34 μM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases. L002 blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide, respectively, and reduces STAT3 phosphorylation, which requires p300-mediated acetylation of STAT3. It induces growth arrest and apoptosis in certain cancer cell lines and, when administered intraperitoneally in mice, suppresses the growth of triple-negative breast cancer xenografts.

Uses

L002 is an inhibitor of p300 histone acetyl transferase, which maintains weaker inhibitory effects against PCAF and GCN5. and is specific for p3000.

Biochem/physiol Actions

L002 (NSC764414) is an inhibitor of acetyltransferase p300, a lysine acetyltransferase that catalyzes acetyl group attachment to lysine residues of a variety of proteins including histones and p53, and acts as a critical coactivator of several oncogenic transcription factors involved in cancer cell survival and proliferation including STAT3, NF-kB, and hypoxia-inducible factor-1α (HIF-1α). L002 (NSC764414) was discovered from compounds assayed for cytotoxicity to the triple-negative breast cancer (TNBC) cell line MDA-MB-231 but not to the human mammary epithelial cells, then further screened for inhibition of p300. L002 has an in vitro IC50 of 1.98 μM for p300 with lesser inhibition of the GNAT (GCN5-related N-acetyltransferase) family, and no inhibition against the MYST family of histone acetyltransferases (HATs), histone deacetylases (HDACs), or histone methyltransferases (HMTs). L002 potently suppressed tumor growth and histone acetylation of MDA-MB-468 xenografts and leukemia and lymphoma cell lines.

NSC764414 Preparation Products And Raw materials

Raw materials

Preparation Products

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NSC764414 Suppliers

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321695-57-2, NSC764414Related Search:

4-[O-[(4-Methoxyphenyl)sulfonyl]oxime]-2,6-dimethyl-2,5-cyclohexadiene-1,4-dione

L002

NSC764414

p300/CBP Inhibitor VI, L002

[(3,5-dimethyl-4-oxo-cyclohexa-2,5-dien-1-ylidene)amino] 4-methoxybenzenesulfonate

L002(NSC764414)

L 002;NSC 764414;L-002;NSC-764414

p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem

p300,acetylation,L 002,Inhibitor,HATs,L-002,HAT,inhibit,fibrosis,L002,Histone Acetyltransferase,STAT,cardiac,histone

2,5-Cyclohexadiene-1,4-dione, 2,6-dimethyl-, 4-[O-[(4-methoxyphenyl)sulfonyl]oxime]

321695-57-2