C646 is a potent, cell permeable and selective inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases. Inhibition of p300/CBP by C646 affects the activity of a variety of transcriptional factors such as NF-κB, p53 and MyoD that are associated wit
Storage Temp
Store at -20°C,Argon charged,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of E1A binding protein p300
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
C646 was used to study the role of p300 in chronic neuropathic pain in rats with chronic constriction injury.
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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