1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. Histone Acetyltransferase
    STAT
  3. L002

L002 

Cat. No.: HY-100671 Purity: 98.80%
Handling Instructions

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

For research use only. We do not sell to patients.

L002 Chemical Structure

L002 Chemical Structure

CAS No. : 321695-57-2

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10 mM * 1  mL in DMSO USD 69 In-stock
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10 mg USD 95 In-stock
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25 mg USD 220 In-stock
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50 mg USD 420 In-stock
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100 mg USD 695 In-stock
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Description

L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM[1]. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation[2]. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment[3].

IC50 & Target

IC50: 1.98 uM (KAT3B); 35 µM (PCAF); 34 µM (GCN5)[1] ;STAT3; p53[2]

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 additional acetyltransferases, deacetylases, and methyltransferases[1].

In Vivo

L002 (intraperitoneal injection; 20 μg/gm body weight; every 3rd day; 2 weeks) 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[3].

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

321.35

Formula

C₁₅H₁₅NO₅S

CAS No.

321695-57-2

SMILES

O=C1C(C)=C/C(C=C1C)=N\OS(=O)(C2=CC=C(OC)C=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (194.49 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1119 mL 15.5594 mL 31.1187 mL
5 mM 0.6224 mL 3.1119 mL 6.2237 mL
10 mM 0.3112 mL 1.5559 mL 3.1119 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.47 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

L002L 002L-002Histone AcetyltransferaseSTATHATsHATcardiacfibrosisp300histoneacetylationInhibitorinhibitorinhibit

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L002
Cat. No.:
HY-100671
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