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L002

🥰Excellent
Catalog No. T11807Cas No. 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.

L002

L002

🥰Excellent
Purity: 98.59%
Catalog No. T11807Cas No. 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.
Pack SizePriceAvailabilityQuantity
2 mg$34In Stock
5 mg$54In Stock
10 mg$81In Stock
25 mg$179In Stock
50 mg$343In Stock
100 mg$567In Stock
1 mL x 10 mM (in DMSO)$60In Stock
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Purity:98.59%
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Product Introduction

Bioactivity
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
GCN5:34 µM , KAT3B:1.98 uM , PCAF:35 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.
Chemical Properties
Molecular Weight321.35
FormulaC15H15NO5S
Cas No.321695-57-2
SmilesCOc1ccc(cc1)S(=O)(=O)ON=C1C=C(C)C(=O)C(C)=C1
Relative Density.1.28 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (186.71 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.1119 mL15.5594 mL31.1187 mL155.5936 mL
5 mM0.6224 mL3.1119 mL6.2237 mL31.1187 mL
10 mM0.3112 mL1.5559 mL3.1119 mL15.5594 mL
20 mM0.1556 mL0.7780 mL1.5559 mL7.7797 mL
50 mM0.0622 mL0.3112 mL0.6224 mL3.1119 mL
100 mM0.0311 mL0.1556 mL0.3112 mL1.5559 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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