C646 - CAS 328968-36-1
Catalog number: B0084-370250
Category: Inhibitor
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Molecular Formula:
C24H19N3O6
Molecular Weight:
445.42
COA:
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Targets:
Histone Acetyltransferases (HATs)
Description:
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. Preferentially selective for p300 versus other acetyltransferases.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-370250 25 mg $198 In stock
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Purity:
>98%
Synonyms:
C646; C-646; C 646.
MSDS:
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InChIKey:
HEKJYZZSCQBJGB-UNOMPAQXSA-N
InChI:
InChI=1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30)/b19-12-
Canonical SMILES:
CC1=C(C=C(C(=C1)C2=CC=C(O2)C=C3C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C)[N+](=O)[O-])C
1.C646, a Novel p300/CREB-Binding Protein-Specific Inhibitor of Histone Acetyltransferase, Attenuates Influenza A Virus Infection.
Zhao D1, Fukuyama S1, Sakai-Tagawa Y2, Takashita E3, Shoemaker JE1, Kawaoka Y4. Antimicrob Agents Chemother. 2015 Dec 28;60(3):1902-6. doi: 10.1128/AAC.02055-15.
New strategies to develop novel broad-spectrum antiviral drugs against influenza virus infections are needed due to the emergence of antigenic variants and drug-resistant viruses. Here, we evaluated C646, a novel p300/CREB-binding protein-specific inhibitor of histone acetyltransferase (HAT), as an anti-influenza virus agent in vitro and in vivo and explored how C646 affects the viral life cycle and host response. Our studies highlight the value of targeting HAT activity for anti-influenza drug development.
2.The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases.
van den Bosch T1, Boichenko A2, Leus NG1, Ourailidou ME1, Wapenaar H1, Rotili D3, Mai A4, Imhof A5, Bischoff R2, Haisma HJ1, Dekker FJ6. Biochem Pharmacol. 2016 Feb 15;102:130-40. doi: 10.1016/j.bcp.2015.12.010. Epub 2015 Dec 21.
Lysine acetylations are reversible posttranslational modifications of histone and non-histone proteins that play important regulatory roles in signal transduction cascades and gene expression. Lysine acetylations are regulated by histone acetyltransferases as writers and histone deacetylases as erasers. Because of their role in signal transduction cascades, these enzymes are important players in inflammation. Therefore, histone acetyltransferase inhibitors could reduce inflammatory responses. Among the few histone acetyltransferase inhibitors described, C646 is one of the most potent (Ki of 0.4μM for histone acetyltransferase p300). C646 was described to affect the NF-κB pathway; an important pathway in inflammatory responses, which is regulated by acetylation. This pathway has been implicated in asthma and COPD. Therefore, we hypothesized that via regulation of the NF-κB signaling pathway, C646 can inhibit pro-inflammatory gene expression, and have potential for the treatment of inflammatory lung diseases.
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