C646

Catalog No.S7152

C646 Chemical Structure

Molecular Weight(MW): 445.42

C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases.

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Cited by 21 Publications

Purity & Quality Control

Choose Selective Histone Acetyltransferase Inhibitors

Biological Activity

Description C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases.
Features Extensively used as a pharmacologic probe in cancer cells. Potential use for prostate and lung cancers.
Targets
p300/CBP [1]
(Cell-free assay)
400 nM(Ki)
In vitro

C646 is an inhibitor for histone acetyltransferase, inhibits p300 with a Ki of 400 nM and is selective versus other acetyltransferases. C646 produces 86% inhibition of p300 in vitro at 10 μM. C646 is a classical reversible p300 inhibitor. C646 treatment (25μM) reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. [1] C646 (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways. [2] C646 blocks dynamic acetylation of H3K4me3 globally in mouse and fly cells, and locally across the promoter and start-site of inducible genes in the mouse, thereby disrupting RNA polymerase II association and the activation of these genes. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NE-4C cells M1LFVGZ2dmO2aX;uJIF{e2G7 MVOwMVUh|ryP MnvFbIlocCCpbIXjc5NmKGmwZIXj[YQhcW6lcnXhd4V{KG:oIFi0T|Vi[yCjbnSgTFRMPS96L{GyM|E3[WNibHX2[Yx{KGmwIF7FMVREKGOnbHzzJIFz\SCrbnjpZol1\WRiYomgZYRlcXSrb36gc4Yh[SC|ZXzlZ5RqfmViQ1LQM5A{ODBiaX7obYJqfG:{IFO2OFYhcW5iYTDkc5NmNWSncHXu[IVvfCC5YYmgLIZzd21iMDD0c{A2KM7:TTm= M{PCOVMxOTF2M{S2
SH-SY5Y M2TuOGZ2dmO2aX;uJIF{e2G7 NXvBeGhJOjEEoN88US=> MmHyNlQhcA>? NUDHOmh5S29vdILlZZRu\W62IIfpeIghOjBiwsXNJGM3PDZic4XwdJJme3OnZDD0bIUh\W[oZXP0JI9nKFSVQTD0doVifG2nboSgc44hSWyxeEG1JI1TVkFiZYjwdoV{e2mxbjDifUA3PS55JR?= M2fQe|I6OjN3MEO2
GES-1 MX3GeY5kfGmxbjDhd5NigQ>? NUHYPVl3OTBizszN M4jCd|YhcA>? NHrsXGlEPjR4IITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHKnZIXj[YQhfGinIHzleoVteyCxZjDobZN1d26nIFizJIFk\XS7bHH0bY9vKGmwIHLveIghT0NiY3XscJMh[W6mIH7vdo1idCCpYYP0dolkKGWyaYTo[Yxq[WxiY3XscJMhMFB:MD6wOUk> MV2yPVA4PTd7NR?=
SGC-7901 NXHubWhiTnWwY4Tpc44h[XO|YYm= Moj4NVAh|ryP MXu2JIg> M1jGTmM3PDZidILlZZRu\W62IIPp[45q\mmlYX70cJkhemWmdXPl[EB1cGVibHX2[Yx{KG:oIHjpd5RwdmViSEOgZYNmfHmuYYTpc44hcW5iYn;0bEBISyClZXzsd{BidmRibn;ycYFtKGejc4TybYMh\XCrdHjlcIlidCClZXzsd{ApWDxyLkC1LS=> NV6zSWZFOjlyN{W3PVU>
MKN45 M2ew[2Z2dmO2aX;uJIF{e2G7 MUexNEDPxE1? MVK2JIg> NVfETmM2SzZ2NjD0doVifG2nboSgd4lodmmoaXPhcpRtgSC{ZXT1Z4VlKHSqZTDs[ZZmdHNib3[gbIl{fG:wZTDIN{Bi[2W2eXzheIlwdiCrbjDic5RpKEeFIHPlcIx{KGGwZDDuc5Ju[WxiZ3HzeJJq[yCncHn0bIVtcWGuIHPlcIx{KCiSPECuNFUq MmnGNlkxPzV5OUW=
MGC-803 NH7nOnlHfW6ldHnvckBie3OjeR?= M3q4PVExKM7:TR?= MonsOkBp M2m2bGM3PDZidILlZZRu\W62IIPp[45q\mmlYX70cJkhemWmdXPl[EB1cGVibHX2[Yx{KG:oIHjpd5RwdmViSEOgZYNmfHmuYYTpc44hcW5iYn;0bEBISyClZXzsd{BidmRibn;ycYFtKGejc4TybYMh\XCrdHjlcIlidCClZXzsd{ApWDxyLkC1LS=> M3zWd|I6ODd3N{m1
BGC-823 MlnqSpVv[3Srb36gZZN{[Xl? MXyxNEDPxE1? Mm\ROkBp NEnKeHJEPjR4IITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHKnZIXj[YQhfGinIHzleoVteyCxZjDobZN1d26nIFizJIFk\XS7bHH0bY9vKGmwIHLveIghT0NiY3XscJMh[W6mIH7vdo1idCCpYYP0dolkKGWyaYTo[Yxq[WxiY3XscJMhMFB:MD6wOUk> NEHXVZgzQTB5NUe5OS=>
KATO III MXjGeY5kfGmxbjDhd5NigQ>? NIjH[GsyOCEQvF2= NWHkRnA4PiCq M37idWM3PDZidILlZZRu\W62IIPp[45q\mmlYX70cJkhemWmdXPl[EB1cGVibHX2[Yx{KG:oIHjpd5RwdmViSEOgZYNmfHmuYYTpc44hcW5iYn;0bEBISyClZXzsd{BidmRibn;ycYFtKGejc4TybYMh\XCrdHjlcIlidCClZXzsd{ApWDxyLkC1LS=> MYKyPVA4PTd7NR?=
Raw246.7 NWHqVnQ3TnWwY4Tpc44h[XO|YYm= M3TUdFEtKDVuIEGwMEAyPSxiMkCsJFI2NCCxcjCzNEDPxE1? NYDKUW5VOTZiaB?= NFHReHhz\XO3bITzJIlvKHOrZ37p[olk[W62IHnubIljcXSrb36gc4YhVFCVIHHu[EBKTk8QszDpcoR2[2WmIF7GMe67SiCycn;tc5RmeiCjY4Tpeol1gSCjdDCxOUDPxE1ib4KgbIlocGW{IHPvcoNmdnS{YYTpc45{ NF31NJkzPjdzOEW4Oi=>
WM35 NEL1TWtHfW6ldHnvckBie3OjeR?= M{jaUVExKM7:TTDhcoQhOjBizszN M3nZPVI1KGh? NEn2[WxiKGSxc3Wt[IVx\W6mZX70JIRm[3KnYYPlJIlvKHSqZTDwdo91\WmwIHzleoVteyCxZjDjfYNtcW6|IFGgZY5lKEVuIHHjZ49ueGGwaXXkJIJ6KGGwIHnuZ5Jm[XOnZDDlfJBz\XO|aX;uJI9nKHB3MzDhcoQhcXS|IHTve45{fHKnYX2g[YZn\WO2b4KgdFIy MojuNlM3QThyN{G=
1205Lu M4S3W2Z2dmO2aX;uJIF{e2G7 M1rsSFExKM7:TTDhcoQhOjBizszN NGHmeZUzPCCq M4PzTIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hfGinIIDyc5RmcW5ibHX2[Yx{KG:oIHP5Z4xqdnNiQTDhcoQhTSxiYXPjc41x[W6rZXSgZpkh[W5iaX7jdoVie2WmIHX4dJJme3Orb36gc4YheDV|IHHu[EBqfHNiZH;3cpN1emWjbTDl[oZm[3SxcjDwNlE> MVSyN|Y6QDB5MR?=
WM983B M3rBPWZ2dmO2aX;uJIF{e2G7 NYD6NpRnOTBizszNJIFv\CB{MDFOwG0> NILGOoMzPCCq M3vCVIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hfGinIIDyc5RmcW5ibHX2[Yx{KG:oIHP5Z4xqdnNiQTDhcoQhTSxiYXPjc41x[W6rZXSgZpkh[W5iaX7jdoVie2WmIHX4dJJme3Orb36gc4YheDV|IHHu[EBqfHNiZH;3cpN1emWjbTDl[oZm[3SxcjDwNlE> NGDHbXczOzZ7OEC3NS=>
Kasumi-1 MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXOxNEwhOjViYX7kJFUxKM7:TR?= MYqwMEAzPCxiNEisJFczKGh? NITydpVk\WyudXzhdkBoem:5dHigZY5lKGOxbH;ufUBnd3KvYYTpc44hf2W{ZTDkdoFu[XSrY3HscJkhe3WycILld5Nm\CC3cH;uJGM3PDZidILlZZRu\W62Lh?= M4XFOVI{OzlyNUO2
SKNO-1 MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2m2b|ExNCB{NTDhcoQhPTBizszN NXWyUWFoOCxiMkSsJFQ5NCB5MjDo NYXuR3RO[2WubIXsZZIh\3Kxd4ToJIFv\CClb3zvcpkh\m:{bXH0bY9vKHencnWg[JJidWG2aXPhcIx6KHO3cIDy[ZN{\WRidYDvckBEPjR4IITy[YF1dWWwdD6= MXiyN|M6ODV|Nh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
H3K27Ac; 

PubMed: 27322077     


The effect of C646 on p300 HAT activity. Cells were treated with C646 at 30 uM for MIAPaCa2 and 40 uM for Panc1 for 48 hours and then cell lysates were applied for western blotting to evaluate acetylated H3K27 as a surrogate of p300 HAT activity. C646 inhibited p300 HAT activity.

Cyclin A1/2 / Cyclin E2 / p53 / p21 ; 

PubMed: 23698071     


Western blot analyses on WM35, 1205Lu and WM983B cells. Lanes 1-4 represent 24 h of treatment with 0.2% DMSO, 10 μM C646, 20 μM C646 and 20 μM C37, respectively. 

α-c-Myc; 

PubMed: 28630312     


HCC2429 cells were treated with DMSO or with 20, 30, or 40 μM C646 for 6 h. Whole-cell lysates were analyzed on SDS/PAGE and immunoblotted with indicated antibodies.

27322077 23698071 28630312
Immunofluorescence
BRD4 / p300 ; 

PubMed: 28630312     


HCC2429 cells were treated with 20 μM C646 for 1 h, 1 μM (+)-JQ1 for 1 h, or 5 mM HMBA for 12 h. Untreated control cells and treated cells were fixed and immunostained with BRD4 C and p300 antibodies and were counterstained with DAPI. (Scale bars: 10 μm) 

28630312
In vivo C646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory. [4] C646 attenuates mechanical allodynia and thermal hyperalgesia, accompanied by a suppressed COX-2 expression, in the spinal cord. [5]

Protocol

Kinase Assay:[1]
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Radioactive assay:

IC50 values for the putative p300 HAT inhibitors are determined using the direct radioactive assay described above. Reactions are performed in 20 mM HEPES (pH 7.9), and contained 5 mM DTT, 80μM EDTA, 40μg/ml BSA, 100μM H4-15, and 5 nM p300. Putative inhibitors are added over a range of concentrations, with DMSO concentration kept constant (<5%). Reactions are incubated at 30°C for 10 min, then initiated with addition of a 1:1 mixture of 12C-acetyl-CoA and 14C-acetyl-CoA to 20 mM. After 10 min at 30°C, reactions are quenched with 14% SDS (w/v). All concentrations are screened in duplicate. Gels are run, washed, dried, and exposed to a PhosphorImager plate, and production of Ac-H4-15 quantified to obtain IC50s.
Cell Research:[1]
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  • Cell lines: C3H10T1/2
  • Concentrations: ~25 μM
  • Incubation Time: 1 to 3 hr
  • Method: Histone acetylation assays in mouse cells. C3H10T1/2 mouse fibroblasts are grown in DMEM with 10% FCS at 37°C with 6% CO2. Confluent cultures are rendered quiescent in DMEM with 0.5% FCS for 18-20 hr prior to treatment. Cells are treated with the following compounds: TSA (10 ng/ml [33 nM]), C646 (25 μM), C37 (25 μM). Antibodies are used at the following concentrations: total H3 (1:10000; ab7834; Abcam); H4K12ac (1:2500; 06-761; Upstate). Rabbit anti-H3K9ac (1:10000) antibodies are generated in-house. Histones are isolated from cells by acid extraction, separated by SDS and acid-urea polyacrylamide gel electrophoresis and analyzed by western blotting.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: mouse
  • Formulation: 10% DMSO
  • Dosages: 2×0.75 μl injection volume in each case, 1.5 μg, administered over 2 min
  • Administration: infusion into ILPFC
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (29.18 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5%Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 445.42
Formula

C24H19N3O6

CAS No. 328968-36-1
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I am planning to conduct IP studies in mice, any specific vehicle that you can recommend to me?

  • Answer:

    We found it can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 1 mg/ml as a clear solution. It should be ok for i.p. injection.

Histone Acetyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID