L-002

Research use only, not for human use.

L-002 (NSC 764414, L002) is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with IC50 of 1.98 uM.

L-002 (NSC 764414, L002) is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with IC50 of 1.98 uM; also shows weak inhibitory activity against PCAF (KAT2B) and GCN5 (KAT2A) with IC50 of 34.7 and 33.9 uM, displays no inhibition against Tip60, MYST2 and MYST4 (IC50>100 uM), as well as a panel of HDACs and HMTs; inhibits acetylation of histones and p53, and suppresses STAT3 activation in cell-based assays; exhibits extreme sensitivity against leukemia, breas and lymphoma cell lines; potently suppresses tumor growth and histone acetylation of MDA-MB-468 xenografts.

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Animal Model:Wild‐type C57BL/6 male mice planted with osmotic minipumps ( Angiotensin II 1500?ng/kg/min) for 4 weeks Dosage:20?μg/gm body weight; every 3rd day; 2 weeks Administration:Intraperitoneal injection Result:Reversed hypertension-induced cardiac fibrosis in mice.

NSC 764414 | L002

Chromatin/Epigenetic

HAT

HAT

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321695-57-2

321.35

C15H15NO5S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (311.19 mM)

CC1=CC(=NOS(=O)(=O)C2=CC=C(C=C2)OC)C=C(C1=O)C

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

(-20℃)

With Ice Pack

≥ 2 years