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Molibresib (I-BET-762)

目录号：S7189 别名: GSK525762, GSK525762A

仅限科研使用

Molibresib (I-BET-762, GSK525762, GSK525762A) 是一种BET蛋白抑制剂，无细胞试验中IC50约为35 nM，抑制巨噬细胞产生促炎性蛋白质，并抑制急性炎症，对其他溴区结合域包含的蛋白具有高度选择性。

Molibresib (I-BET-762) Chemical Structure

CAS: 1260907-17-2

规格	价格	库存
10mM (1mL in DMSO)	RMB 2923.83	现货
2mg	RMB 1859.99	现货
10mg	RMB 3838.64	现货
大包装	有超大折扣

今日订购，明日送达全国免运费分装免费分装成小规格产品（单支最小为1mg）如1支10mg产品可分装为10支1mg产品全国免费电话：400-668-6834 \| Email：info@selleck.cn

客户使用Selleck生产的Molibresib (I-BET-762)发表文献26篇：

产品安全说明书

Epigenetic Reader Domain抑制剂选择性比较

生物活性

产品描述

靶点

BET proteins ^[1]
(Cell-free assay)

35 nM

体外研究

I-BET-762抑制BET(溴区和额外的末端结构域) 蛋白, BRD2, BRD3 和 BRD4, 结合到BET的串联溴区，K_d为50.5-61.3 nM, 在FRET分析中，置换BET串联溴区的一种四乙酰化的H4肽，IC50为32.5-42.5 nM。I-BET-762占据BET蛋白的乙酰基-赖氨酸结合口袋，并抑制BET蛋白结合到乙酰化的组蛋白，从而破坏了炎性基因表达必不可少的染色质复合物的形成。^[1]分化过程中的第2天使用I-BET-762处理，改变CD4⁺T细胞的细胞因子产生，上调一些抗炎基因产物的表达，并下调一些促炎细胞因子的表达。^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

HepG2	NH;ze3NHfW6ldHnvckBie3OjeR?=		M4\1V\|E5KGi{cx?=	MYTJcoR2[3Srb36gc4YhcHWvYX6gRZBwSTFiZ3Xu[UBmgHC{ZYPzbY9vKGmwIIP0ZYJtgSC2cnHud4Zm[3SnZDDoeY1idiCKZYDHNkBk\WyuczDjc4V5eHKnc4PpcochdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIFnfGW{IEG4JIhzeyCkeTDseY1qdmW\|Y3XuZ4Uh[XO\|YYmsJGVEPTBiPTCwMlch\|ryPLh?=	Mm\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3NkizNlIoRjJzNU[4N\|IzRC:jPh?=
HepG2	NFrGXHhHfW6ldHnvckBie3OjeR?=		MlfhOkBpenN?	M1;Eemlv\HWldHnvckBw\iCqdX3hckBCeG:DMTDwdo91\WmwIIP5cpRp\XOrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCwZX;zfY51cGW\|aYPl[EBz[WSrb3zhZoVt\WRicILveIVqdiC\|ZXPy[ZRqd25iYX\0[ZIhPiCqcoOgZpkhW0SVIGDBS2Uh[W6jbInzbZMhcW5icILld4Vv[2Vib3[gX\|M2W12vZYTobY9vcW6n	NG\sfHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW2PFMzOid-MkG1Olg{OjJ:L3G+
HepG2	MXLGeY5kfGmxbjDhd5NigQ>?		NEPBZocyQCCqcoO=	MknUWZBz\We3bHH0bY9vKG:oIFHwc2EyKGW6cILld5Nqd25iaX6gbJVu[W5iSHXwS\|Ih[2WubIOgZZN{\XO\|ZXSgZZMh[2:wY3XueJJifGmxbjDy[ZF2cXKnZDD0c{BqdmO{ZXHz[UA4OCVib3[gcJVkcW[ncnHz[UBi[3Srdnn0fUBi\nSncjCxPEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{G3NEA:KDBwMjFOwG0v	NVWxPYR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzPFY2OjlpPkKyN\|g3PTJ7PD;hQi=>
HepG2	MlzzSpVv[3Srb36gZZN{[Xl?		MnfyNVghcHK\|	NGf0fW1KdmS3Y4Tpc44hd2ZiaIXtZY4hSXCxQUGg[4Vv\SCneIDy[ZN{cW:wIHnuJJN1[WKueTD0doFve2[nY4Tl[EBpfW2jbjDI[ZBIOiClZXzsd{Bkd2W6cILld5NqdmdibIXjbYZmemG\|ZTDy[ZBwenSncjDn[Y5mKGGodHXyJFE5KGi{czDifUBtfW2rbnXzZ4Vv[2ViYYPzZZktKEWFNUCgQUAxNjdizszNMi=>	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl{NESzOEc,OjJ7MkS0N\|Q9N2F-
PBMC	MX3BcpRqcW6obHHtcYF1d3K7IHHzd4F6			NGewTZFCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFLNR{Bk\WyuczDhd5Nme3OnZDDhd{BNWFNvaX7keYNm\CCLTD22JJBzd2S3Y4Tpc44h[nliY3jlcYltfW2rbnXzZ4Vv[2ViYYPzZZktKEmFNUCgQUAxNjNzNkKzJO69VS5?	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDBzNUm2O{c,OjRyMUW5Olc9N2F-
Raji	MnTISpVv[3Srb36gZZN{[Xl?		MmTkOEBpenN?	M1jnbmlvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBT[WqrIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDv[kBOYUNiZYjwdoV{e2mxbjDh[pRmeiB2IHjyd{whUUN3MDC9JFAvOTlizszNMi=>	MkP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC3OVgoRjJ2OUCwO\|U5RC:jPh?=
Rosetta2 DE3	MVLGeY5kfGmxbjDhd5NigQ>?		MV:zNEBucW6\|	M4C2UWRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSzJGJFOiBqM{C2JJRwKDRzNzDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFMxOyEQvF2u	MnLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MWjGeY5kfGmxbjDhd5NigQ>?		MoHUN\|AhdWmwcx?=	MlHSSIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKURESgRmQzKCh\|M{OgeI8hPDZyIHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wN\|I{KM7:TT6=	NHXUeY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	NX30NmM4TnWwY4Tpc44h[XO\|YYm=		NH;zb28{OCCvaX7z	M3[2O2Rqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlS0JGJFOSBqNESgeI8hOTZ6IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wN\|g5KM7:TT6=	Ml7OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MVfGeY5kfGmxbjDhd5NigQ>?			M4jCRWJqdmSrbnegZYZncW6rdImgeI8h[mmxdHnufYxifGWmIFLSSFMhSkR{IDizNFYhfG9iNEG3JIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDifUBjcW9vbHH5[ZIhcW62ZYLm[ZJwdWW2comgcYV1cG:mLDDL[EA:KDBwMESwO{DPxE1w	M3nTeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	M3;zdmZ2dmO2aX;uJIF{e2G7			NGTwUW9DcW6maX7nJIFn\mmwaYT5JJRwKGKrb4Tpcplt[XSnZDDCVmQzKEKGMjCoN\|Q6KHSxIES2NEBidWmwbzDhZ4llKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDSc5NmfHSjMjDESVMh[2WubIOgZpkh[mmxLXzhfYVzKGmwdHXy[oVzd22ndIL5JI1mfGixZDygT4QhRSByLkC0OVQh\|ryPLh?=	M2DqbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	M{LHOGZ2dmO2aX;uJIF{e2G7			NV\iSnRGSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFPCCEREKgLFM{OyC2bzC0OlAh[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6wOFc3KM7:TT6=	NXLP[2xlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	NFXwXZBHfW6ldHnvckBie3OjeR?=		MmL5N\|AhdWmwcx?=	NUXVSFBTTGm\|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFIhSkR{IDizOFkhfG9iNE[wJIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB\|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEurIE2gNE4xPDl{IN88UU4>	MnnOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MUHGeY5kfGmxbjDhd5NigQ>?		M3\HRlMxKG2rboO=	MofZSIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKUREOgRmQyKCh{NDD0c{AyPDRiYX3pco8h[WOrZDDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hWm:\|ZYT0ZVIhTEV\|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygT4khRSByLkC1N\|kh\|ryPLh?=	Ml7IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MkLPSpVv[3Srb36gZZN{[Xl?		MnTHN\|AhdWmwcx?=	NFm0dmZFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLENkBDTDFiKEeyJJRwKDJyNTDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFU3QCEQvF2u	MnW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	NF[yW21HfW6ldHnvckBie3OjeR?=			MXLCbY5lcW6pIHHm[olvcXS7IITvJIJqd3SrbonsZZRm\CCEUlSzJGJFOSBqMkSgeI8hOTR2IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCkeTDibY8udGG7ZYKgbY51\XKoZYLvcYV1enlibXX0bI9lNCCNZDC9JFAvODZyNzFOwG0v	MofJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
MV4-11	NYnKOlV7S3m2b4TvfIlkcXS7IHHzd4F6		NEfsUnU1KGSjeYO=	Mn\PR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGijcnLvdolv\yCPTFyxJIZ2e2mxbjDn[Y5mKGG\|c3Xzd4VlKGG\|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDRiZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGG\|c3H5MEBKSzVyIE2gNE4xQTNizszNMi=>	M4rtWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	M{DRVGZ2dmO2aX;uJIF{e2G7		MmLQN\|AhdWmwcx?=	Mke1SIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKURESgRmQzKCh\|M{OgeI8hPDZyIHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGlEPTBiPTCwMlA6QDRizszNMi=>	M3rIPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	MXvGeY5kfGmxbjDhd5NigQ>?			NH\MN2hDcW6maX7nJIFn\mmwaYT5JJRwKGKrb4Tpcplt[XSnZDDCVmQ1KEKGMTCoOFQhfG9iMU[4JIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDifUBjcW9vbHH5[ZIhcW62ZYLm[ZJwdWW2comgcYV1cG:mLDDL[EA:KDBwMEm5OEDPxE1w	NEnY[Ig9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	M2D0NGZ2dmO2aX;uJIF{e2G7		MWCzNEBucW6\|	MUDEbZNxdGGlZX3lcpQhd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IH\yc40hSlKGNDDCSFEhMDR2IITvJFE3QCCjbXnuc{Bi[2mmIILld4llfWW\|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBTd3OndIThNkBFTTNiY3XscJMh[W[2ZYKgN\|AhdWmwczDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDJR\|UxKD1iMD6xOVYh\|ryPLh?=	NXnibWVvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	MX\GeY5kfGmxbjDhd5NigQ>?			NHy1b2ZDcW6maX7nJIFn\mmwaYT5JJRwKGKrb4Tpcplt[XSnZDDCVmQzKEKGMTCoO\|IhfG9iMkC1JIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDifUBjcW9vbHH5[ZIhcW62ZYLm[ZJwdWW2comgcYV1cG:mLDDL[EA:KDBwMUW5JO69VS5?	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
MOLM13	NGThUXJEgXSxdH;4bYNqfHliYYPzZZk>		NXS3T3A1PCCmYYnz	NXj5Zo1US3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVU:OTUGzJINmdGy\|IHjhdoJwemmwZzDNUGwyKG[3c3nvckBo\W6nIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IESg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHHzd4F6NCCLQ{WwJF0hOC5{NEGg{txONg>?	NY\JfnJ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
BL21(DE3)	MV3GeY5kfGmxbjDhd5NigQ>?			Mnv2Rolv\GmwZzDh[oZqdmm2eTD0c{BPNXSncn3pcoFtKEirc{[teIFo\2WmLVLSSFQh[nKxbX;kc41icW5iMjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBkd22yZYTlcpQhTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kh[2WubIOgZpkhcXOxdHjldo1idCC2aYTyZZRqd25iY3Hsc5JqdWW2comsJGtlKD1iMD6wOlUh\|ryPLh?=	MorRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|Nke1N\|koRjJ4M{[3OVM6RC:jPh?=
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BL21(DE3)	M4XKNmZ2dmO2aX;uJIF{e2G7			NGXDZZRDcW6maX7nJIFn\mmwaYT5JJRwKG[3bHygcIVv\3SqIF6teIVzdWmwYXygTIl{Pi22YXfn[YQuSlKGMjDido9ud2SxbXHpckAzKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIHPvcZBmfGWwdDDFd4Np\XKrY3jpZUBkd2yrIFLMNlEpTEV\|KTDj[YxteyCkeTDpd491cGW{bXHsJJRqfHKjdHnvckBk[Wyxcnnt[ZRzgSxiS3SgQUAxNjFizszNMi=>	Mk\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|Nke1N\|koRjJ4M{[3OVM6RC:jPh?=
BL21(DE3)	MnjxSpVv[3Srb36gZZN{[Xl?			MWPCbY5lcW6pIHHm[olvcXS7IITvJIZ2dGxibHXu[5RpKE5vdHXycYlv[WxiSHnzOk11[WepZXStRnJFOiCkcn;tc4RwdWGrbjCxJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKGOxbYDleIVvfCCHc3Po[ZJq[2irYTDjc4xqKEKOMkGoSGU{MSClZXzsd{BjgSCrc3;0bIVzdWGuIITpeJJifGmxbjDjZYxwemmvZYTyfUwhU2RiPTCwMlI{KM7:TT6=	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN4N{WzPUc,OjZ\|Nke1N\|k9N2F-
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Rosetta2 DE3	NWS0cIZ1TnWwY4Tpc44h[XO\|YYm=		MVuzNEBucW6\|	Mo\RTY5pcWKrdHnvckBw\iCIQV2tcIFj\WynZDDaRmEzPDhiYnnu[Ilv\yC2bzDy[YNwdWKrbnHueEBpfW2jbjDOMZRmem2rbnHsJGhqezZvdHHn[4VlKEKURESgZpJwdW:mb33hbY4hOiBqM{OzJJRwKDR4MDDy[ZNq\HWnczmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KE[ub4Xy[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGlEPTBiPTCwMlA4PzVizszNMi=>	NX7RbVZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
MV4-11	MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NWfHOWpjPCCmYYnz	NVrTeW0{T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVZ2LUGxJINmdGy\|IHHmeIVzKDRiZHH5d{BjgSCZU2StPEBie3OjeTygTWM2OCB;IECuNFk{KM7:TT6=	M1\R[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N\|Q5PzxxYU6=
Rosetta2 DE3	NEH3PYtHfW6ldHnvckBie3OjeR?=		NIr1eXY{OCCvaX7z	MofDTY5pcWKrdHnvckBw\iCIQV2tcIFj\WynZDDaRmEzPDhiYnnu[Ilv\yC2bzDy[YNwdWKrbnHueEBpfW2jbjDOMZRmem2rbnHsJGhqezZvdHHn[4VlKEKURESgZpJwdW:mb33hbY4hOSBqNESgeI8hOTZ6IILld4llfWW\|KTDlfJBz\XO\|ZXSgbY4hWm:\|ZYT0ZVIhTEV\|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkhTmyxdYLld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygTWM2OCB;IECuNVQ2KM7:TT6=	M{[zSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N\|Q5PzxxYU6=
MOLM13	M{LiRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NH7hW281KGSjeYO=	NIn2bXVIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOV0yPMUOgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KFeVVD24JIF{e2G7LDDJR\|UxKD1iMD6yOFEh\|ryPLh?=	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
TY82	NHjESYlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NHy4VXI4OiCqcoO=	MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFS\OEKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSByLkKg{txONg>?	M2DBNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUi2O\|E5Lz5{OEW4OlcyQDxxYU6=
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BL21 (DE3)-codon plus-RIL	NYnKXIFNTnWwY4Tpc44h[XO\|YYm=		MXG0JIhzew>?	NIXIRXhKdmirYnn0bY9vKG:oIFrRNU1HUVSFIHLpcoRqdmdidH:gTIl{Pi22YXfn[YQhSlKGND3CSFEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iRYPjbIVzcWOqaXGgZ49tcSCETEKxJEhFTTNrLXPv[I9vKHCudYOtVmlNKGOnbHzzJIlv[3WkYYTl[EBqdiCmYYLrJIZweiB2IHjyd{BjgSCobIXvdoV{[2WwY3WgZY5qe2:2cn;wfUBie3OjeTygTWM2OCB;IECuNlYh\|ryPLh?=	NEn0Onc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW4OlcyQCd-Mki1PFY4OTh:L3G+
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HD-MB03	NV6wVXRjS3m2b4TvfIlkcXS7IHHzd4F6		M3\XWFUh\GG7cx?=	NIjZVlhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJTC2PQkCzJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC1JIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhTUN3MDC9JFMvPSEQvF2u	NE\MfZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG3NFAzPCd-MkmxO\|AxOjR:L3G+
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Saos-2	Mo\ndWhVWyCjc4PhfS=>			MoDudWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?=	M3PwNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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TY82	Mm\GSpVv[3Srb36gZZN{[Xl?	MUWwMlIhfG9iMTD1US=>	M1P2O\|I1KGi{cx?=	MYfJcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gWHk5OiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ{1OgWNicILveIVqdiCneIDy[ZN{cW:wIHH0JFAvOiC2bzCxJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	MkTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MkW0N\|UoRjJ7NUK1OFM2RC:jPh?=
TY82	NW[xdotWTnWwY4Tpc44h[XO\|YYm=	Mn\GNE4zKHSxIEGgeW0>	MX6yOEBpenN?	MXnJcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gWHk5OiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ{1OgWNibWLORUBmgHC{ZYPzbY9vKGG2IECuNkB1dyBzIIXNJIFnfGW{IEK0JIhzeyCkeTDSWE1RS1JiYX7hcJl{cXN?	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV{NUSzOUc,Ojl3MkW0N\|U9N2F-
TY82 or NCI-H1299	M2XVdWZ2dmO2aX;uJIF{e2G7	MoXHNE4zKHSxIEGgeW0>	NFnjcoIzPCCqcoO=	M{nkW2lvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBVYTh{IH;yJG5EUS2KMUK5PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iUFStUFEheHKxdHXpckBmgHC{ZYPzbY9vKGG2IECuNkB1dyBzIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	M320TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUK1OFM2Lz5{OUWyOVQ{PTxxYU6=
TY82 or NCI-H1299	MVXGeY5kfGmxbjDhd5NigQ>?	NWXFWm1GOC5{IITvJFEhfU1?	MlHRNlQhcHK\|	NHjCWXZKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hXFl6MjDvdkBPS0lvSEGyPVkh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIGDEMWwyKG2UTlGg[ZhxemW\|c3nvckBifCByLkKgeI8hOSC3TTDh[pRmeiB{NDDodpMh[nliUmStVGNTKGGwYXz5d4l{	M37Od\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUK1OFM2Lz5{OUWyOVQ{PTxxYU6=
C4-2B	MXjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M3;N[Vk3KGi{cx?=	MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEN2LULCJINmdGy\|IHHmeIVzKDl4IHjyd{BjgSCFZXzsMXRqfGW{IHfsc{Bz\WGpZX70JIJie2WmIHz1cYlv\XOlZX7j[UBie3OjeR?=	NUm3fFR5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OFE{PzFpPkK5OVQyOzdzPD;hQi=>
22Rv1	NVfsVoFjSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MWW5OkBpenN?	NUP6dZV2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjCyNnJ3OSClZXzsd{Bi\nSncjC5OkBpenNiYomgR4VtdC2WaYTldkBodG9icnXh[4VvfCCkYYPl[EBtfW2rbnXzZ4Vv[2ViYYPzZZk>	NH61b2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0NVM4OSd-Mkm1OFE{PzF:L3G+
LNCAP	MW\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NUDUR5NVQTZiaILz	MoKyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCOTlPBVEBk\WyuczDh[pRmeiB7NjDodpMh[nliQ3XscE1VcXSncjDncI8hemWjZ3XueEBj[XOnZDDseY1qdmW\|Y3XuZ4Uh[XO\|YYm=	NHPqe2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0NVM4OSd-Mkm1OFE{PzF:L3G+
HL60	NV;sWJdxS3m2b4TvfIlkcXS7IHHzd4F6			MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMUKg{txONg>?	NUHZeph3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2OVcxQTlpPkK5OlU4ODl7PD;hQi=>
Raji	NVyyPGlsTnWwY4Tpc44h[XO\|YYm=			M2rEXGlvcGmkaYTpc44hd2ZiQmLEOE1DTDFiaX6gbJVu[W5iUnHqbUBk\WyuczDhd5Nme3OnZDDhd{Bld3ewcnXneYxifGmxbjDv[kBOYUNiZ3Xu[UBmgHC{ZYPzbY9vKGK7IGDDVkBu\XSqb3SsJGlEPTBiPTCwMlE{OiEQvF2u	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ3N{C5PUc,Ojl4NUewPVk9N2F-
LNCAP	NU\MbpJvSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=			MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy\|LDDJR\|UxKD1iMD6zOVY2KM7:TT6=	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd3OEWxPEc,Ojl5NUi1NVg9N2F-
MV411	MX;DfZRwfG:6aXPpeJkh[XO\|YYm=		MVO3NkBpenN?	MknxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1OTFiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUCgQUAxNjhizszNMi=>	M4q0VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMk[4O\|AzLz5\|MEK2PFcxOjxxYU6=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Growth inhibition assay

Cell viability

26840085

体内研究

I-BET-762保护防止脂多糖诱导的内毒素休克和细菌诱导的脓毒病。LPS注射后1.5小时，单剂量I-BET处理，可治愈小鼠。I-BET每日两次注射，持续2天，保护小鼠免于脓毒症引起的死亡。^[1]早期I-BET-762处理实验性自身免疫性脑脊髓炎（EAE）小鼠模型，抑制Th1分化的2D2 T细胞诱发神经性炎症的能力。^[2]

激酶实验：^[1]	荧光共振能量转移（FRET）滴定: 在有四乙酰化的组蛋白H4肽（200 nM）存在时，在50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS中进行对BRD2 (200 nM), BRD3 (100 nM) 和 BRD4 (50 nM)的I-BET滴定。平衡1小时后，在含0.05% (v/v) BSA 和 400 mM KF的实验缓冲液中加入2nM 铕穴状化合物标记的链霉亲和素和10 nM XL-665标记的anti-6His 抗体，使用FRET检测溴区蛋白：肽相互作用。使用Envision酶标仪（激发菠菜320 nm，发射波长615 nm和665 nm）对实验板进行读数。
细胞实验：^[2]	Cell lines: CD4⁺ T 细胞 Concentrations: ~500 nM Incubation Time: 60-72 小时 Method: 从10到12周的小鼠淋巴结和脾中分离CD4⁺ T细胞，在指定细胞因子存在时，使用与板结合的anti-CD3和anti-CD28抗体活化。在最初激活的60-72小时，包含I-BET-762化合物。在T细胞培养和扩张的5天过程中，化合物稀释到初始浓度的12倍。
动物实验：^[1]	Animal Models: 小鼠 Dosages: 30 mg/kg Administration: 静脉注射

参考文献	[1] Nicodeme E, et al. Nature, 2010, 468(7327), 1119-1123. [2] Bandukwala HS, et al. PNAS, 2012, 109(36), 14532-14537.

溶解度（25°C）

体外

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量	423.9
化学式	C₂₂H₂₂ClN₅O₂
CAS号	1260907-17-2
储存条件	3年	-20°C	粉状
储存条件	2年	-80°C	溶于溶剂

Download Molibresib (I-BET-762) SDF

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

临床试验信息

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03266159	Withdrawn	Drug: GSK525762 Besylate tablets\|Drug: Trametinib tablets	Solid Tumours	GlaxoSmithKline	November 27 2017	Phase 2
NCT02964507	Completed	Drug: GSK525762\|Drug: Placebo\|Drug: Fulvestrant	Neoplasms	GlaxoSmithKline	February 2 2017	Phase 1
NCT01943851	Completed	Drug: GSK525762	Neoplasms	GlaxoSmithKline	May 14 2014	Phase 2
NCT01587703	Completed	Drug: GSK525762	Carcinoma Midline	GlaxoSmithKline	March 28 2012	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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