Name: C646
Price: 268.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    C646, a pyrazolone-containing small molecule, is a cell-permeable histone acetyltransferase (HAT) inhibitor that competitively and selectively inhibits the HAT activity of p300, a transcriptional co-activator involved in a variety of gene regulatory pathways and protein acetylation events, with the inhibition constant Ki value of 400 nM and the half maximal inhibition concentration IC50 value of 1.6 μM [1].
    C646 binds to p300 as the Z-isomer forming hydrogen bonds between Thr1411, tYR1467, Trp1466 and Arg1410 on the side chains of p300 and oxygen atoms of C646 [1].
    C646 is also capable of inhibiting a variety of p300 HAT mutants, including T1411A, Y1467F, W1466F and R1410A with IC50 values of 3.4 μM, 7 μM, 5 μM and 2.5 μM respectively [1].
    
    [1] Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA, Liszczak G, Yuan H, Larocca C, Saldanha SA, Abagyan R, Sun Y, Meyers DJ, Marmorstein R, Mahadevan LC, Alani RM, Cole PA. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol. 2010 May 28;17(5):471-82. doi: 10.1016/j.chembiol.2010.03.006.
- Properties
  - Alternative Name
    
    4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid
    
    CAS Number
    
    328968-36-1
    
    Molecular Formula
    
    C24H19N3O6
    
    Molecular Weight
    
    445.42
    
    Appearance
    
    A solid
    
    Purity
    
    93.65%
    
    Solubility
    
    insoluble in H2O; ≥11.14 mg/mL in DMSO; ≥3.29 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Jiang W, Yuan X, et al. "Inhibition of Histone H3K27 Acetylation Orchestrates Interleukin-9-Mediated and Plays an Anti-Inflammatory Role in Cisplatin-Induced Acute Kidney Injury." Front Immunol. 2020;11:231. PMID:32194547
    2. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031

C646

C646

Background

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