C646

Catalog No.S7152

For research use only.

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. C646 induces cell cycle arrest, apoptosis and autophagy.

C646 Chemical Structure

CAS No. 328968-36-1

Selleck's C646 has been cited by 66 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. C646 induces cell cycle arrest, apoptosis and autophagy.
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 NYC5dJhZTnWwY4Tpc44h[XO|YYm= NFfzZngxNTVizszN MX3obYdpKGeudXPvd4UhcW6mdXPl[EBqdmO{ZXHz[ZMhd2ZiSETLOYFkKGGwZDDIOGs2NzhxMUKvNVZi[yCuZY\lcJMhcW5iTlWtOGMh[2WubIOgZZJmKGmwaHnibZRm\CCkeTDh[IRqfGmxbjDv[kBiKHOnbHXjeIl3\SCFQmCvdFMxOCCrbnjpZol1d3JiQ{[0OkBqdiCjIHTvd4Uu\GWyZX7k[Y51KHejeTCo[pJwdSByIITvJFUh|ryPKR?= M37vbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUG0N|Q3Lz5|MEGxOFM1PjxxYU6=
SH-SY5Y NWK5TFZ4TnWwY4Tpc44h[XO|YYm= NVHiXWY5OjEEoN88US=> M2Lqb|I1KGh? M3nHN2NwNXS{ZXH0cYVvfCC5aYToJFIxKML3TTDDOlQ3KHO3cIDy[ZN{\WRidHjlJIVn\mWldDDv[kBVW0FidILlZZRu\W62IH;uJGFtd3hzNTDtVm5CKGW6cILld5Nqd25iYomgOlUvPyV? M{DLUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MkO1NFM3Lz5{OUKzOVA{PjxxYU6=
GES-1 MVnGeY5kfGmxbjDhd5NigQ>? MW[xNEDPxE1? NVTDclh2PiCq M{e2T2M3PDZidILlZZRu\W62IIPp[45q\mmlYX70cJkhemWmdXPl[EB1cGVibHX2[Yx{KG:oIHjpd5RwdmViSEOgZYNmfHmuYYTpc44hcW5iYn;0bEBISyClZXzsd{BidmRibn;ycYFtKGejc4TybYMh\XCrdHjlcIlidCClZXzsd{ApWDxyLkC1LS=> NXnRZpFURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwO|U4QTVpPkK5NFc2Pzl3PD;hQi=>
SGC-7901 MVvGeY5kfGmxbjDhd5NigQ>? M4H3XVExKM7:TR?= M3zBXFYhcA>? NV\IZ2hiSzZ2NjD0doVifG2nboSgd4lodmmoaXPhcpRtgSC{ZXT1Z4VlKHSqZTDs[ZZmdHNib3[gbIl{fG:wZTDIN{Bi[2W2eXzheIlwdiCrbjDic5RpKEeFIHPlcIx{KGGwZDDuc5Ju[WxiZ3HzeJJq[yCncHn0bIVtcWGuIHPlcIx{KCiSPECuNFUq NV3hXWlKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwO|U4QTVpPkK5NFc2Pzl3PD;hQi=>
MKN45 Ml7rSpVv[3Srb36gZZN{[Xl? M2\4dVExKM7:TR?= MXu2JIg> M1zPXmM3PDZidILlZZRu\W62IIPp[45q\mmlYX70cJkhemWmdXPl[EB1cGVibHX2[Yx{KG:oIHjpd5RwdmViSEOgZYNmfHmuYYTpc44hcW5iYn;0bEBISyClZXzsd{BidmRibn;ycYFtKGejc4TybYMh\XCrdHjlcIlidCClZXzsd{ApWDxyLkC1LS=> NWHZd5lURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwO|U4QTVpPkK5NFc2Pzl3PD;hQi=>
MGC-803 NILxdmlHfW6ldHnvckBie3OjeR?= NHTVTJcyOCEQvF2= MWi2JIg> MlS1R|Y1PiC2cnXheI1mdnRic3nncolncWOjboTsfUBz\WS3Y3XkJJRp\SCuZY\lcJMhd2ZiaHnzeI9v\SCKMzDhZ4V1gWyjdHnvckBqdiCkb4ToJGdEKGOnbHzzJIFv\CCwb4LtZYwh\2G|dILpZ{BmeGm2aHXsbYFtKGOnbHzzJEhRRDBwMEWp MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTB5NUe5OUc,OjlyN{W3PVU9N2F-
BGC-823 M3LhN2Z2dmO2aX;uJIF{e2G7 NIHBbHAyOCEQvF2= NE\xblU3KGh? NF\uTZhEPjR4IITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHKnZIXj[YQhfGinIHzleoVteyCxZjDobZN1d26nIFizJIFk\XS7bHH0bY9vKGmwIHLveIghT0NiY3XscJMh[W6mIH7vdo1idCCpYYP0dolkKGWyaYTo[Yxq[WxiY3XscJMhMFB:MD6wOUk> NYTO[HVbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwO|U4QTVpPkK5NFc2Pzl3PD;hQi=>
KATO III M2[ybmZ2dmO2aX;uJIF{e2G7 MnPQNVAh|ryP M4rMT|YhcA>? NHGzOIFEPjR4IITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHKnZIXj[YQhfGinIHzleoVteyCxZjDobZN1d26nIFizJIFk\XS7bHH0bY9vKGmwIHLveIghT0NiY3XscJMh[W6mIH7vdo1idCCpYYP0dolkKGWyaYTo[Yxq[WxiY3XscJMhMFB:MD6wOUk> M4ezO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MEe1O|k2Lz5{OUC3OVc6PTxxYU6=
Raw246.7 NYDvNXF4TnWwY4Tpc44h[XO|YYm= M1WyR|EtKDVuIEGwMEAyPSxiMkCsJFI2NCCxcjCzNEDPxE1? MY[xOkBp NUT1TlV2emW|dXz0d{BqdiC|aXfubYZq[2GwdDDpcohq[mm2aX;uJI9nKEySUzDhcoQhUU[QzsOgbY5lfWOnZDDOSk3PwkJicILvcY91\XJiYXP0bZZqfHliYYSgNVUh|ryPIH;yJIhq\2incjDjc45k\W62cnH0bY9vew>? MoDqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5MUi1PFYoRjJ4N{G4OVg3RC:jPh?=
WM35 NXfKTXFITnWwY4Tpc44h[XO|YYm= NWOwbIhDOTBizszNJIFv\CB{MDFOwG0> NEjVUoIzPCCq NInVOIJiKGSxc3Wt[IVx\W6mZX70JIRm[3KnYYPlJIlvKHSqZTDwdo91\WmwIHzleoVteyCxZjDjfYNtcW6|IFGgZY5lKEVuIHHjZ49ueGGwaXXkJIJ6KGGwIHnuZ5Jm[XOnZDDlfJBz\XO|aX;uJI9nKHB3MzDhcoQhcXS|IHTve45{fHKnYX2g[YZn\WO2b4KgdFIy M1LOcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nkm4NFcyLz5{M{[5PFA4OTxxYU6=
1205Lu MnXKSpVv[3Srb36gZZN{[Xl? NI\KU2kyOCEQvF2gZY5lKDJyIN88US=> NFq2N2YzPCCq MUXhJIRwe2VvZHXw[Y5l\W62IHTlZ5Jm[XOnIHnuJJRp\SCycn;0[YlvKGyndnXsd{Bw\iCleXPsbY5{KEFiYX7kJGUtKGGlY3;tdIFvcWWmIHL5JIFvKGmwY4LlZZNm\CCneIDy[ZN{cW:wIH;mJJA2OyCjbnSgbZR{KGSxd37zeJJm[W1iZX\m[YN1d3JicEKx MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ7OEC3NUc,OjN4OUiwO|E9N2F-
WM983B M{WzWmZ2dmO2aX;uJIF{e2G7 Mn3rNVAh|ryPIHHu[EAzOCEQvF2= M4fiN|I1KGh? NYjuO5k{[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiC2aHWgdJJwfGWrbjDs[ZZmdHNib3[gZ5lkdGmwczDBJIFv\CCHLDDhZ4NwdXCjbnnl[EBjgSCjbjDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKGm2czDkc5dve3S{ZXHtJIVn\mWldH;yJJAzOQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ7OEC3NUc,OjN4OUiwO|E9N2F-
Kasumi-1 NVjrUnJ[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnfCNVAtKDJ3IHHu[EA2OCEQvF2= NULnSpJqOCxiMkSsJFQ5NCB5MjDo MnfQZ4VtdHWuYYKg[5Jwf3SqIHHu[EBkd2yxbomg[o9zdWG2aX;uJJdmemViZILhcYF1cWOjbHz5JJN2eHC{ZYPz[YQhfXCxbjDDOlQ3KHS{ZXH0cYVvfC5? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7MEWzOkc,OjN|OUC1N|Y9N2F-
SKNO-1 M4TiVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3izS|ExNCB{NTDhcoQhPTBizszN NXPyNGVtOCxiMkSsJFQ5NCB5MjDo NGPzfoRk\WyudXzhdkBoem:5dHigZY5lKGOxbH;ufUBnd3KvYYTpc44hf2W{ZTDkdoFu[XSrY3HscJkhe3WycILld5Nm\CC3cH;uJGM3PDZidILlZZRu\W62Lh?= Mly5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|OUC1N|YoRjJ|M{mwOVM3RC:jPh?=
BL21(RIL)-DE3 M3Ho[mZ2dmO2aX;uJIF{e2G7 NX3xUWVMOTBibXnudy=> MVHJcohq[mm2aX;uJI9nKHO7boTo[ZRq[yCYTVGteIFo\2WmIICzNFAhMDF{OEegeI8hOTZ3MjDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKGLJUEkuTEV|IHPlcIx{KHW|aX7nJGg1NTF3IIDldJRq\GVic4Xid5Rz[XSnIHnuZ5Vj[XSnZDDmc5IhOTBibXnud{BjgSC{YXTpc41mfHKrYzDmbYx1\XJiYnnu[Ilv\yCjc4PhfUBqdiCycnXz[Y5k\SCxZjDbNVREZWGlZYT5cE1Ed0FuIFvpJF0hOC52IN88UU4> Mn7SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5MEGxPFYoRjJ4N{CxNVg3RC:jPh?=
BL21(RIL)-DE3 NXXwZVVwTnWwY4Tpc44h[XO|YYm= NIDvVYEyOCCvaX7z M2nzd2lvcGmkaYTpc44hd2Zic4nueIhmfGmlIG\NRU11[WepZXSgdFMxOCBqMUK4O{B1dyBzNkWyJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKEKOMkGoVmlNMS2GRUOgZ4VtdHNidYPpcochUDRvMUWgdIVxfGmmZTDzeYJ{fHKjdHWgbY5kfWKjdHXkJIZweiBzMDDtbY5{KGK7IILh[IlwdWW2cnnjJIZqdHSncjDibY5lcW6pIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJHsyPEOfYXPleJltNUOxQTygTWM2OCB;IEGuOkDPxE1w NUnCXXpORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3NFEyQDZpPkK2O|AyOTh4PD;hQi=>
BL21-CodonPlus(DE3)-RIL NVf1bndGTnWwY4Tpc44h[XO|YYm= M4fMXFExKG2rboO= M3HOc2lvcGmkaYTpc44hd2ZiRlzBS{11[WepZXSgdFMxOCBqMUG5OUB1dyBzNkezJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiClb33w[ZRmdnRiRYPjbIVzcWOqaXGgZ49tcSCETEKxMWNw\G:wUHz1d{hFTTNrLWLJUEBk\WyuczD1d4lv\yCqaYP0c45mKEh2IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDFyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{Bu\XSqb3SgbY4heHKnc3XuZ4Uhd2ZiW{G0R31i[2W2eXytR49CNCCLQ{WwJF0hQSEQvF2u MmLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5MEGxPFYoRjJ4N{CxNVg3RC:jPh?=
Assay
Methods Test Index PMID
Western blot H3K27Ac ; Cyclin A1/2 / Cyclin E2 / p53 / p21 ; α-c-Myc 27322077 23698071 28630312
Immunofluorescence BRD4 / p300 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • Animal Models: mouse
  • 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 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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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.

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