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C 646 - 98%, high purity , CAS No.328968-36-1, Inhibitor of E1A binding protein p300

Moligand™
≥98%

CAS#: 328968-36-1
Formula: C₂₄H₁₉N₃O₆
Molecular Weight: 445.42
PubChem CID: 1285941

Item Number

C274682

Grouped product items
SKU	Size	Availability	Price
C274682-1mg	1mg	In stock	$9.90
C274682-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$13.90
C274682-25mg	25mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$27.90
C274682-100mg	100mg	In stock	$91.90
C274682-250mg	250mg	In stock	$154.90
C274682-1g	1g	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$400.90

Cell-permeable, competitive, selective, potent p300/CBP HAT inhibitor

View related series

E1A binding protein p300 Inhibitor

Basic Description

Synonyms	328968-36-1\|C646\|4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid\|C 646\|4-(4-((5-(4,5-Dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid\|4-[(4E)-4-[
Specifications & Purity	98%
Storage Temp	Store at -20°C,Argon charged,Desiccated
Shipped In	Dry ice
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of E1A binding protein p300
Product Description	C646 was used to study the role of p300 in chronic neuropathic pain in rats with chronic constriction injury.

Names and Identifiers

IUPAC Name	4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid
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-
InChi Key	HEKJYZZSCQBJGB-UNOMPAQXSA-N
Canonical SMILES	CC1=CC(=C(C=C1C)[N+](=O)[O-])C2=CC=C(O2)C=C3C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C
Isomeric SMILES	CC1=CC(=C(C=C1C)[N+](=O)[O-])C2=CC=C(O2)/C=C\3/C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C
PubChem CID	1285941
Molecular Weight	445.42

PubChem CID

1285941

CAS Registry No.

328968-36-1

ChEMBL Ligand

CHEMBL1797936

Certificates

Certificate of Analysis(COA)

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6 results found

Lot Number	Certificate Type	Date	Item
L2123473	Certificate of Analysis	Oct 20, 2022	C274682
L2123474	Certificate of Analysis	Oct 20, 2022	C274682
L2123475	Certificate of Analysis	Oct 20, 2022	C274682
L2123476	Certificate of Analysis	Oct 20, 2022	C274682
L2123071	Certificate of Analysis	Oct 20, 2022	C274682
L2123072	Certificate of Analysis	Oct 20, 2022	C274682

References

1. Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA, Liszczak G, Yuan H et al.. (2010) Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.. Chem Biol, 17 (5): (471-82). [PMID:20534345]
2. Dekker FJ, van den Bosch T, Martin NI. (2014) Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases.. Drug Discov Today, 19 (5): (654-660). [PMID:24269836]
3. van den Bosch T, Boichenko A, Leus NGJ, Ourailidou ME, Wapenaar H, Rotili D, Mai A, Imhof A, Bischoff R, Haisma HJ et al.. (2016) The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases.. Biochem Pharmacol, 102 (3): (130-140). [PMID:26718586]
4. Dahlin JL, Nelson KM, Strasser JM, Barsyte-Lovejoy D, Szewczyk MM, Organ S, Cuellar M, Singh G, Shrimp JH, Nguyen N et al.. (2017) Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors.. Nat Commun, 8 (1): (1527). [PMID:29142305]
5. Sacta MA et al.. (2018) Gene-specific mechanisms direct glucocorticoid-receptor-driven repression of inflammatory response genes in macrophages.. Elife, 7 [PMID:29424686]
6. Butcher NJ et al.. (2020) Modulation of Human Arylamine N-Acetyltransferase 1 Activity by Lysine Acetylation: Role of p300/CREB-Binding Protein and Sirtuins 1 and 2.. Mol Pharmacol, 98 (2): (88-95). [PMID:32487734]
7. Fischer A et al.. (2017) Membrane localization of acetylated CNK1 mediates a positive feedback on RAF/ERK signaling.. Sci Adv, 3 (8): (e1700475). [PMID:28819643]
8. Bandyopadhaya A et al.. (2017) NF-?Bp50 and HDAC1 Interaction Is Implicated in the Host Tolerance to Infection Mediated by the Bacterial Quorum Sensing Signal 2-Aminoacetophenone.. Front Microbiol, 8 (1211). [PMID:28713342]
9. Hao Y et al.. (2022) p300 arrests intervertebral disc degeneration by regulating the FOXO3/Sirt1/Wnt/β-catenin axis.. Aging Cell, 21 (8): (e13677). [PMID:35907249]
10. Wei L et al.. (2019) Silencing of lncRNA MALAT1 Prevents Inflammatory Injury after Lung Transplant Ischemia-Reperfusion by Downregulation of IL-8 via p300.. Mol Ther Nucleic Acids, 18 (285-297). [PMID:31604167]
11. Smith ER et al.. (2019) TGF-ß1 modifies histone acetylation and acetyl-coenzyme A metabolism in renal myofibroblasts.. Am J Physiol Renal Physiol, [PMID:30623724]
12. Peghaire C et al.. (2019) The transcription factor ERG regulates a low shear stress-induced anti-thrombotic pathway in the microvasculature.. Nat Commun, 10 (5014). [PMID:31676784]

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C 646 - 98%, high purity , CAS No.328968-36-1, Inhibitor of E1A binding protein p300

Basic Description

Associated Targets

EP300 Tchem Histone acetyltransferase p300 7 Activities

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

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References

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