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L002

Cat No.:V30923 Purity: ≥98%
L002 is a potent, cell-penetrating/penetrable, reversible and specific inhibitor of acetyltransferase p300 (KAT3B) with IC50 of 1.98 μM.
L002
L002 Chemical Structure CAS No.: 321695-57-2
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
100mg
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Product Description
L002 is a potent, cell-penetrating/penetrable, reversible and specific inhibitor of acetyltransferase p300 (KAT3B) with IC50 of 1.98 μM. L002 binds to the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocking histone acetylation and p53 acetylation, and inhibiting STAT3 activation. L002 may be used to be utilized in study/research of hypertension-induced cardiac hypertrophy and fibrosis.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
L002 also exhibits a weak inhibitory effect on a group of p300s with Manhattan on additional cardiac transferases, decyclases, and methyltransferases, as well as PCAF and GCN5 (IC50=35 and 34 μM) [1].
ln Vivo
L002, an intraperitoneal injection administered every three days for two weeks at a dose of 20 μg/gm body weight, is used to treat hypertensive cardiac hypertrophy and fibrosis. It also has the ability to significantly reverse these conditions. In comparison to treatment, it also lowers the amounts of interstitial and perivascular collagen in the heart [3].
Animal Protocol
Animal/Disease Models: Wild-type C57BL/6 male mice were implanted with a mini-osmotic pump (angiotensin II 1500 ng/kg/min) for 4 weeks [3]
Doses: 20 μg/g body weight; once every three days; given every 2 weeks Drug: intraperitoneal (ip) injection
Experimental Results: reversed cardiac fibrosis in mice caused by hypertension.
References

[1]. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013.

[2]. The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis. Front Oncol. 2015 May 26;5:108.

[3]. Acetyltransferase p300 inhibitor reverses hypertension-induced cardiac fibrosis.J Cell Mol Med. 2019 Apr;23(4):3026-3031.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H15NO5S
Molecular Weight
321.348303079605
Exact Mass
321.067
CAS #
321695-57-2
PubChem CID
2221149
Appearance
Light yellow to yellow solid powder
Density
1.3±0.1 g/cm3
Boiling Point
459.8±55.0 °C at 760 mmHg
Flash Point
231.9±31.5 °C
Vapour Pressure
0.0±1.1 mmHg at 25°C
Index of Refraction
1.574
LogP
4.06
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
4
Heavy Atom Count
22
Complexity
607
Defined Atom Stereocenter Count
0
InChi Key
VEWFTYOFWIXCIO-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H15NO5S/c1-10-8-12(9-11(2)15(10)17)16-21-22(18,19)14-6-4-13(20-3)5-7-14/h4-9H,1-3H3
Chemical Name
[(3,5-dimethyl-4-oxocyclohexa-2,5-dien-1-ylidene)amino] 4-methoxybenzenesulfonate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~311.19 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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