Description
PU139 is a novel histone acetyltransferase (HAT) inhibitor. PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively.
Product information
CAS Number: 158093-65-3
Molecular Weight: 246.26
Formula: C12H7FN2OS
Chemical Name: 2-(4-fluorophenyl)-2H, 3H-[1, 2]thiazolo[5, 4-b]pyridin-3-one
Smiles: O=C1C2=CC=CN=C2SN1C1C=CC(F)=CC=1
InChiKey: QMCIVCACYJRAAY-UHFFFAOYSA-N
InChi: InChI=1S/C12H7FN2OS/c13-8-3-5-9(6-4-8)15-12(16)10-2-1-7-14-11(10)17-15/h1-7H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
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:
PU139 inhibits cell growth with GI50s of <60 μM (A431, A549, A2780, HepG2, SW480, U-87 MG, HCT116 and SK-N-SH and MCF7 cells). PU139 (0-100 μM; 24-72 hours) triggers caspase-independent cell death in the neuroblastoma cell line SK-N-SH.
References:
- Carneiro VC, de Abreu da Silva IC, Torres EJ, Caby S, Lancelot J, Vanderstraete M, Furdas SD, Jung M, Pierce RJ, Fantappié MR. Epigenetic changes modulate schistosome egg formation and are a novel target for reducing transmission of schistosomiasis. PLoS Pathog. 2014 May 8;10(5):e1004116. doi: 10.1371/journal.ppat.1004116. eCollection 2014 May. PubMed PMID: 24809504; PubMed Central PMCID: PMC4014452.
- Gajer JM, Furdas SD, Gründer A, Gothwal M, Heinicke U, Keller K, Colland F, Fulda S, Pahl HL, Fichtner I, Sippl W, Jung M. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis. 2015 Feb 9;4:e137. doi: 10.1038/oncsis.2014.51. PubMed PMID: 25664930; PubMed Central PMCID: PMC4338425.
Products are for research use only. Not for human use.
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