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

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
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Based on 1 publication(s) in Google Scholar

L002 Related Antibodies

Top Publications Citing Use of Products

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View All Isoforms
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

CBP/p300

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 CC50
1.03 μM
Compound: 70
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by [3H]-thymidine incorporation assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by [3H]-thymidine incorporation assay
[PMID: 33045661]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

L002 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Light yellow to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (194.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1119 mL 15.5594 mL 31.1187 mL 77.7968 mL
5 mM 0.6224 mL 3.1119 mL 6.2237 mL 15.5594 mL
10 mM 0.3112 mL 1.5559 mL 3.1119 mL 7.7797 mL
15 mM 0.2075 mL 1.0373 mL 2.0746 mL 5.1865 mL
20 mM 0.1556 mL 0.7780 mL 1.5559 mL 3.8898 mL
25 mM 0.1245 mL 0.6224 mL 1.2447 mL 3.1119 mL
30 mM 0.1037 mL 0.5186 mL 1.0373 mL 2.5932 mL
40 mM 0.0778 mL 0.3890 mL 0.7780 mL 1.9449 mL
50 mM 0.0622 mL 0.3112 mL 0.6224 mL 1.5559 mL
60 mM 0.0519 mL 0.2593 mL 0.5186 mL 1.2966 mL
80 mM 0.0389 mL 0.1945 mL 0.3890 mL 0.9725 mL
100 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7780 mL
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L002 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L002321695-57-2L 002L-002Histone AcetyltransferaseSTATHATsHATcardiacfibrosisp300histoneacetylationInhibitorinhibitorinhibit

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