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L002

Catalog No. T11807 CAS 321695-57-2

L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.

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L002, CAS 321695-57-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 54.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 179.00
50 mg	In stock	$ 343.00
100 mg	In stock	$ 567.00
1 mL * 10 mM (in DMSO)	In stock	$ 60.00

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Purity: 98.59%

Biological Description

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Storage & Solubility Information

Description	L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.
Targets&IC50	PCAF:35 µM , KAT3B:1.98 uM , GCN5:34 µM
In vitro	L002 also has weak inhibitory effects against PCAF and GCN5 (IC50s =35 and 34 μM, respectively) and is specific for p300 over a panel of deacetylases, additional acetyltransferases, and methyltransferases.
In vivo	L002 reverses hypertension‐induced cardiac hypertrophy and fibrosis by treatment of mice after inducing hypertension for two weeks significantly.It also reduces the levels of perivascular and interstitial collagen in the myocardium compared to non-treated hypertensive mice.

Molecular Weight	321.35
Formula	C15H15NO5S
CAS No.	321695-57-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (186.71 mM), Sonication is recommended.

References and Literature

1. Rai R, et al. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013. 2. Sun XJ, et al. The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis. Front Oncol. 2015 May 26;5:108. 3. Rai R, et al. Acetyltransferase p300 inhibitor reverses hypertension-induced cardiac fibrosis.J Cell Mol Med. 2019 Apr;23(4):3026-3031.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Epigenetics Compound Library JAK-STAT Compound Library Anti-Pancreatic Cancer Compound Library Stem Cell Differentiation Compound Library Bioactive Compound Library Histone Modification Compound Library Reprogramming Compound Library Immunology/Inflammation Compound Library Anti-Prostate Cancer Compound Library

Related Products

Related compounds with same targets

MC4171 CPTH2 KAT modulator-1 CTX-0124143 NSC 228155 C646 EML 425 NEO2734

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

L002 321695-57-2 Chromatin/Epigenetic JAK/STAT signaling Others Stem Cells STAT Histone Acetyltransferase p300 acetylation L 002 Inhibitor HATs HAT inhibit fibrosis cardiac L-002 histone inhibitor

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