PeptideDB

Histone Acetyltransferase Inhibitor II 932749-62-7

Histone Acetyltransferase Inhibitor II 932749-62-7

CAS No.: 932749-62-7

Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective, cell-penetrable p300 inhibitor (antagonist)
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective, cell-penetrable p300 inhibitor (antagonist) with IC50 of 5 µM for use in cancer-related research.

Physicochemical Properties


Molecular Formula C20H16BR2O3
Molecular Weight 464.1472
Exact Mass 461.947
CAS # 932749-62-7
PubChem CID 16203606
Appearance Light yellow to yellow solid powder
LogP 5.842
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 3
Rotatable Bond Count 2
Heavy Atom Count 25
Complexity 511
Defined Atom Stereocenter Count 0
SMILES

C1C/C(=C\C2=CC(=C(C=C2)O)Br)/C(=O)/C(=C/C3=CC(=C(C=C3)O)Br)/C1

InChi Key YOLKEKNTCBWPSD-VOMDNODZSA-N
InChi Code

InChI=1S/C20H16Br2O3/c21-16-10-12(4-6-18(16)23)8-14-2-1-3-15(20(14)25)9-13-5-7-19(24)17(22)11-13/h4-11,23-24H,1-3H2/b14-8+,15-9+
Chemical Name

(2E,6E)-2,6-bis[(3-bromo-4-hydroxyphenyl)methylidene]cyclohexan-1-one
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)

Biological Activity


ln Vitro In HeLa-H2B-EYFP cells, Histone Acetyltransferase Inhibitor II (20–40 μM) lowers H3 acetylation levels [1].
References

[1]. Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase. J Med Chem. 2007 Apr 19;50(8):1973-7. Epub 2007 Mar 10.


Solubility Data


Solubility (In Vitro) DMSO : ≥ 30 mg/mL (~64.63 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (5.39 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 25.0 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 2.1545 mL 10.7724 mL 21.5448 mL
5 mM 0.4309 mL 2.1545 mL 4.3090 mL
10 mM 0.2154 mL 1.0772 mL 2.1545 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.