L002 (NSC764414) --- p300 Inhibitor


Catalog No. size PriceQuantity
M60198-2S 2mg solid $99
M60198-10S 10mg solid $391

Description

L002 (NSC764414) is a novel selective, cell permeable and reversible inhibitor of p300 histone acetyl transferase (IC50 ~1.98 µM). It has no activity in histone methyltransferases tested, including DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2 etc. L002 was shown to occupy Ac-CoA binding pocket of p300, and is less potent to CBP, PCAF, GCN5 and GNAT. It suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. L002 can suppress tumor growth and histone acetylation in a mouse MDA-MB-468 xenograft model.

Product information

CAS Number: 321695-57-2

Molecular Weight: 321.35

Formula: C15H15NO5S

Synonym:

NSC764414

Chemical Name: 4-((((4-methoxyphenyl)sulfonyl)oxy)imino)-2,6-dimethylcyclohexa-2,5-dienone

Smiles: COC1C=CC(=CC=1)S(=O)(=O)ON=C1C=C(C)C(=O)C(C)=C1

InChiKey: VEWFTYOFWIXCIO-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

L002 was used at 5-30 µM final concentration in various in vitro assays.

In Vivo:

L002 was administered through IP injection at 500 µg/100 µl twice a week for 3 weeks in xenografts models.

References:

  1. Yang H, et al. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. (2013) Mol Cancer Ther. 12(5):610-20.

Products are for research use only. Not for human use.


Documents

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed