Molibresib (I-BET-762)

For research use only. Not for use in humans.

目录号：S7189 别名： GSK525762, GSK525762A

Molibresib (I-BET-762) Chemical Structure

CAS No. 1260907-17-2

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。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 2923.83	现货
2mg	RMB 1859.99	现货
10mg	RMB 3838.64	现货
50mg	RMB 9582.91	现货
大包装	有超大折扣

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今日订购，明日送达，全国免运费！

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18篇：

Cancer Discov, 2018, 8(4):458-477

PubMed: 29386193 ( click the link to review the publication )

Cancer Cell, 2017, 31(5):635-652

PubMed: 28434841 ( click the link to review the publication )

Nat Commun, 2020, 14;11(1):1833

PubMed: 32286255 ( click the link to review the publication )

Signal Transduct Target Ther, 2020, 4;5(1):20

PubMed: 32296021 ( click the link to review the publication )

Aging (Albany NY), 2020, 12(10):9240-9259

PubMed: 32392533 ( click the link to review the publication )

Cancer Sci, 2020, 112(1):133-143

PubMed: 33067904 ( click the link to review the publication )

J Hematol Oncol, 2019, 12(1):73

PubMed: 31288832 ( click the link to review the publication )

EBioMedicine, 2019, 43:201-210

PubMed: 30975544 ( click the link to review the publication )

Am J Transl Res, 2019, 11(2):1030-1039

PubMed: 30899402 ( click the link to review the publication )

Leuk Res, 2019, 77:42-50

PubMed: 30642575 ( click the link to review the publication )

Mol Cell, 2018, 71(4):592-605

PubMed: 30057199 ( click the link to review the publication )

Cancer Res, 2018, 78(15):4331-4343

PubMed: 29792310 ( click the link to review the publication )

Cancer Res, 2018, 78(20):5731-5740

PubMed: 30135193 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(12):2796-2810

PubMed: 30242092 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(2):285-299

PubMed: 27980108 ( click the link to review the publication )

Cancer Discov, 2016, 6(6):612-29

PubMed: 27099234 ( click the link to review the publication )

Nature, 2016, 534(7607):407-411

PubMed: 27281208 ( click the link to review the publication )

Oncotarget, 2016, 7(24):35753-35767

PubMed: 26840085 ( click the link to review the publication )

客户使用该产品的2个实验数据：

PECAPJ49 parental and cetuximab-resistant clones were treated with 100 nmol/L cetuximab ± 800 nmol/L I-BET-762(IBET) for 72 hours. Cells were stained with crystal violet and quantified as described in Materials and Methods (n = 3; *, P < 0.02). Figures are representative of three independent experiments.

Cancer Res, 2018, 78(15):4331-4343. Molibresib (I-BET-762) purchased from Selleck.
A., B. and C. Dose response curves of MPNST-derived cell lines treated with three bromodomain inhibitors: JQ1, OTX015 and I-BET-762.

Oncotarget, 2016, 7(24):35753-35767. Molibresib (I-BET-762) purchased from Selleck.

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	Activity Description	PMID
HepG2	M4XqPWZ2dmO2aX;uJIF{e2G7		M4TBUVE5KGi{cx?=	MV7JcoR2[3Srb36gc4YhcHWvYX6gRZBwSTFiZ3Xu[UBmgHC{ZYPzbY9vKGmwIIP0ZYJtgSC2cnHud4Zm[3SnZDDoeY1idiCKZYDHNkBk\WyuczDjc4V5eHKnc4PpcochdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIFnfGW{IEG4JIhzeyCkeTDseY1qdmW\|Y3XuZ4Uh[XO\|YYmsJGVEPTBiPTCwMlch\|ryPLh?=	NFLkc4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW2PFMzOid-MkG1Olg{OjJ:L3G+
HepG2	MYnGeY5kfGmxbjDhd5NigQ>?		NY\5VlZkPiCqcoO=	M{Hlb2lv\HWldHnvckBw\iCqdX3hckBCeG:DMTDwdo91\WmwIIP5cpRp\XOrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCwZX;zfY51cGW\|aYPl[EBz[WSrb3zhZoVt\WRicILveIVqdiC\|ZXPy[ZRqd25iYX\0[ZIhPiCqcoOgZpkhW0SVIGDBS2Uh[W6jbInzbZMhcW5icILld4Vv[2Vib3[gX\|M2W12vZYTobY9vcW6n	NWOxeYE1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1Olg{OjJpPkKxOVY5OzJ{PD;hQi=>
HepG2	NVqyR4hWTnWwY4Tpc44h[XO\|YYm=		NGHGZ4oyQCCqcoO=	NUK2THlpXXC{ZXf1cIF1cW:wIH;mJGFxd0FzIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO\|ZYPz[YQh[XNiY3;uZ4VvfHKjdHnvckBz\XG3aYLl[EB1dyCrbnPy[YF{\SB5MDWgc4YhdHWlaX\ldoF{\SCjY4Tpeol1gSCjZoTldkAyQCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR\|E4OCB;IECuNkDPxE1w	NH\WSVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkO4OlUzQSd-MkKzPFY2Ojl:L3G+
HepG2	MYjGeY5kfGmxbjDhd5NigQ>?		M3XkbVE5KGi{cx?=	NH\k[ItKdmS3Y4Tpc44hd2ZiaIXtZY4hSXCxQUGg[4Vv\SCneIDy[ZN{cW:wIHnuJJN1[WKueTD0doFve2[nY4Tl[EBpfW2jbjDI[ZBIOiClZXzsd{Bkd2W6cILld5NqdmdibIXjbYZmemG\|ZTDy[ZBwenSncjDn[Y5mKGGodHXyJFE5KGi{czDifUBtfW2rbnXzZ4Vv[2ViYYPzZZktKEWFNUCgQUAxNjdizszNMi=>	NVjGTW9VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5NlQ1OzRpPkKyPVI1PDN2PD;hQi=>
PBMC	M1PJd2FvfGmrbn\sZY1u[XSxcomgZZN{[Xl?			M3Phc2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCSQl3DJINmdGy\|IHHzd4V{e2WmIHHzJGxRWy2rbnT1Z4VlKEmOLU[gdJJw\HWldHnvckBjgSClaHXtbYx2dWmwZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFAvOzF4MkOg{txONg>?	NX;R[YFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVU6PjdpPkK0NFE2QTZ5PD;hQi=>
Raji	M1Tx[WZ2dmO2aX;uJIF{e2G7		M{\0eFQhcHK\|	NIjaOXJKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hWmGsaTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhVVmFIHX4dJJme3Orb36gZYZ1\XJiNDDodpMtKEmFNUCgQUAxNjF7IN88UU4>	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEe1PEc,OjR7MEC3OVg9N2F-
Rosetta2 DE3	NWLPW\|RCTnWwY4Tpc44h[XO\|YYm=		MnfJN\|AhdWmwcx?=	NHLNSXFFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEN{BDTDJiKEOwOkB1dyB2MUegZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlA{ODNizszNMi=>	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	M17oVWZ2dmO2aX;uJIF{e2G7		M{Xlc\|MxKG2rboO=	NF\JOGNFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEOEBDTDJiKEOzN{B1dyB2NkCgZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlA{OjNizszNMi=>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	NY\yTYd[TnWwY4Tpc44h[XO\|YYm=		NGe1RYI{OCCvaX7z	M1\rOGRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlS0JGJFOSBqNESgeI8hOTZ6IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wN\|g5KM7:TT6=	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	M{m0RmZ2dmO2aX;uJIF{e2G7			M2LyXWJqdmSrbnegZYZncW6rdImgeI8h[mmxdHnufYxifGWmIFLSSFMhSkR{IDizNFYhfG9iNEG3JIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDifUBjcW9vbHH5[ZIhcW62ZYLm[ZJwdWW2comgcYV1cG:mLDDL[EA:KDBwMESwO{DPxE1w	NGS5XFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	NYe0OZJ{TnWwY4Tpc44h[XO\|YYm=			NV7OSVJoSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFOiCEREKgLFM1QSC2bzC0OlAh[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6wOFU1KM7:TT6=	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	MXvGeY5kfGmxbjDhd5NigQ>?			M{K2cGJqdmSrbnegZYZncW6rdImgeI8h[mmxdHnufYxifGWmIFLSSFQhSkR{IDizN\|MhfG9iNE[wJIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDifUBjcW9vbHH5[ZIhcW62ZYLm[ZJwdWW2comgcYV1cG:mLDDL[EA:KDBwMES3OkDPxE1w	NXvINFJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	NEn4T3FHfW6ldHnvckBie3OjeR?=		NV;NbGFVOzBibXnudy=>	M1;1OWRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSyJGJFOiBqM{S5JJRwKDR4MDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFQ6OiEQvF2u	NFGxRWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	M4jzPGZ2dmO2aX;uJIF{e2G7		NEHSOIw{OCCvaX7z	NICzfWFFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEN{BDTDFiKEK0JJRwKDF2NDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFU{QSEQvF2u	M3XTZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	NW\HboRjTnWwY4Tpc44h[XO\|YYm=		NYjJR5A2OzBibXnudy=>	MXvEbZNxdGGlZX3lcpQhd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IH\yc40hSlKGMjDCSFEhMDd{IITvJFIxPSCjbXnuc{Bi[2mmIILld4llfWW\|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBTd3OndIThNkBFTTNiY3XscJMh[W[2ZYKgN\|AhdWmwczDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDLbUA:KDBwMEW2PEDPxE1w	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	M3O2SmZ2dmO2aX;uJIF{e2G7			MYjCbY5lcW6pIHHm[olvcXS7IITvJIJqd3SrbonsZZRm\CCEUlSzJGJFOSBqMkSgeI8hOTR2IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCkeTDibY8udGG7ZYKgbY51\XKoZYLvcYV1enlibXX0bI9lNCCNZDC9JFAvODZyNzFOwG0v	MkHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
MV4-11	M1riSWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MXG0JIRigXN?	MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMhcGG{Yn;ybY5oKE2OTEGg[pV{cW:wIHflcoUh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPCCmYYnzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO\|YYmsJGlEPTBiPTCwMlA6OyEQvF2u	Mo\6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MUTGeY5kfGmxbjDhd5NigQ>?		NH[0TpI{OCCvaX7z	NYLMOXZXTGm\|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFQhSkR{IDizN\|MhfG9iNE[wJIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB\|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEmFNUCgQUAxNjB7OESg{txONg>?	NF\UZZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	NF[xZYxHfW6ldHnvckBie3OjeR?=			Mom4Rolv\GmwZzDh[oZqdmm2eTD0c{BjcW:2aX75cIF1\WRiQmLEOEBDTDFiKES0JJRwKDF4ODDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYomgZolwNWyjeXXyJIlvfGW{ZnXyc41mfHK7IH3leIhw\CxiS3SgQUAxNjB7OUSg{txONg>?	NXL0ZY92RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	MXvGeY5kfGmxbjDhd5NigQ>?		M3nRNVMxKG2rboO=	Mny2SIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKURESgRmQyKCh2NDD0c{AyPjhiYX3pco8h[WOrZDDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hWm:\|ZYT0ZVIhTEV\|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygTWM2OCB;IECuNVU3KM7:TT6=	Mmn0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MnnqSpVv[3Srb36gZZN{[Xl?			NEDkPJdDcW6maX7nJIFn\mmwaYT5JJRwKGKrb4Tpcplt[XSnZDDCVmQzKEKGMTCoO\|IhfG9iMkC1JIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDifUBjcW9vbHH5[ZIhcW62ZYLm[ZJwdWW2comgcYV1cG:mLDDL[EA:KDBwMUW5JO69VS5?	NULnOVdoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
MOLM13	MU\DfZRwfG:6aXPpeJkh[XO\|YYm=		MWS0JIRigXN?	MknTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUW9NVTF\|IHPlcIx{KGijcnLvdolv\yCPTFyxJIZ2e2mxbjDn[Y5mKGG\|c3Xzd4VlKGG\|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDRiZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGG\|c3H5MEBKSzVyIE2gNE4zPDFizszNMi=>	NXXJUFFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
BL21(DE3)	MWjGeY5kfGmxbjDhd5NigQ>?			NIPCWXhDcW6maX7nJIFn\mmwaYT5JJRwKE5vdHXycYlv[WxiSHnzOk11[WepZXStRnJFPCCkcn;tc4RwdWGrbjCyJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKGOxbYDleIVvfCCHc3Po[ZJq[2irYTDjc4xqKEKOMkGoSGU{MSClZXzsd{BjgSCrc3;0bIVzdWGuIITpeJJifGmxbjDjZYxwemmvZYTyfUwhU2RiPTCwMlA3PSEQvF2u	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN4N{WzPUc,OjZ\|Nke1N\|k9N2F-
BL21(DE3)	Mo\CSpVv[3Srb36gZZN{[Xl?			NYfqPGdmSmmwZHnu[{Bi\m[rbnn0fUB1dyCQLYTldo1qdmGuIFjpd\|YufGGpZ3XkMWJTTDRiYoLvcY9ld22jaX6gNUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiClb33w[ZRmdnRiRYPjbIVzcWOqaXGgZ49tcSCETEKxLGRGOyliY3XscJMh[nliaYPveIhmem2jbDD0bZRz[XSrb36gZ4Ftd3KrbXX0dpktKEumIE2gNE4xQTVizszNMi=>	MmHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|Nke1N\|koRjJ4M{[3OVM6RC:jPh?=
BL21(DE3)	MU\GeY5kfGmxbjDhd5NigQ>?			MYjCbY5lcW6pIHHm[olvcXS7IITvJIZ2dGxibHXu[5RpKE5vdHXycYlv[WxiSHnzOk11[WepZXStRnJFOiCkcn;tc4RwdWGrbjCyJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKGOxbYDleIVvfCCHc3Po[ZJq[2irYTDjc4xqKEKOMkGoSGU{MSClZXzsd{BjgSCrc3;0bIVzdWGuIITpeJJifGmxbjDjZYxwemmvZYTyfUwhU2RiPTCwMlEh\|ryPLh?=	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN4N{WzPUc,OjZ\|Nke1N\|k9N2F-
BL21(DE3)	MlXrSpVv[3Srb36gZZN{[Xl?			MmHZRolv\GmwZzDh[oZqdmm2eTD0c{BnfWyuIHzlcod1cCCQLYTldo1qdmGuIFjpd\|YufGGpZ3XkMWJTTDJiYoLvcY9ld22jaX6gNUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiClb33w[ZRmdnRiRYPjbIVzcWOqaXGgZ49tcSCETEKxLGRGOyliY3XscJMh[nliaYPveIhmem2jbDD0bZRz[XSrb36gZ4Ftd3KrbXX0dpktKEumIE2gNE4zOyEQvF2u	NYXRXWJnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOlc2OzlpPkK2N\|Y4PTN7PD;hQi=>
BL21(DE3)-R3-pRARE2	MWjGeY5kfGmxbjDhd5NigQ>?			NXz1d5Z2UW6qaXLpeIlwdiCxZjDoeY1idiCKaYOteIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMjDlfJBz\XO\|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kuWjNvcGLBVmUzKGOnbHzzJIJ6KE[URWSgZZN{[XluIFnDOVAhRSByLkCzOkDPxE1w	M4\BTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{OxOFkxLz5{NkezNVQ6ODxxYU6=
BL21(DE3)-R3-pRARE2	M3v2fGZ2dmO2aX;uJIF{e2G7			NES2NJVKdmirYnn0bY9vKG:oIHj1cYFvKEircz30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiBzIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJGJNOjFqRFWzLU1TOy2yUlHSSVIh[2WubIOgZpkhTlKHVDDhd5NigSxiSVO1NEA:KDBwMEO2JO69VS5?	NIDW[IQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkezNVQ6OCd-Mk[3N\|E1QTB:L3G+
Rosetta2 DE3	M3;ZRWZ2dmO2aX;uJIF{e2G7		MnX2N\|AhdWmwcx?=	NHW1XGtKdmirYnn0bY9vKG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDibY5lcW6pIITvJJJm[2:vYnnuZY51KGi3bXHuJG4ufGW{bXnuZYwhUGm\|Nj30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiB{IDizN\|MhfG9iNE[wJJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlAzOyEQvF2u	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
Rosetta2 DE3	MkTnSpVv[3Srb36gZZN{[Xl?		NFrFUIE{OCCvaX7z	M3\IZWlvcGmkaYTpc44hd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JIJzd22xZH;tZYlvKDFiKES0JJRwKDF4ODDy[ZNq\HWnczmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KE[ub4Xy[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wOFY1KM7:TT6=	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
Rosetta2 DE3	MnTSSpVv[3Srb36gZZN{[Xl?		NY\we2lUOzBibXnudy=>	MofFTY5pcWKrdHnvckBw\iCIQV2tcIFj\WynZDDaRmEzPDhiYnnu[Ilv\yC2bzDy[YNwdWKrbnHueEBpfW2jbjDOMZRmem2rbnHsJGhqezZvdHHn[4VlKEKURESgZpJwdW:mb33hbY4hOiBqM{OzJJRwKDR4MDDy[ZNq\HWnczmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KE[ub4Xy[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGlEPTBiPTCwMlA4PzVizszNMi=>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
MV4-11	NWTp[3luT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MVG0JIRigXN?	NW[ydHB6T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVZ2LUGxJINmdGy\|IHHmeIVzKDRiZHH5d{BjgSCZU2StPEBie3OjeTygTWM2OCB;IECuNFk{KM7:TT6=	NX;pPWx{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
Rosetta2 DE3	NWSwc406TnWwY4Tpc44h[XO\|YYm=		MWSzNEBucW6\|	NIr2OGNKdmirYnn0bY9vKG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDibY5lcW6pIITvJJJm[2:vYnnuZY51KGi3bXHuJG4ufGW{bXnuZYwhUGm\|Nj30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiBzIDi0OEB1dyBzNkigdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCIbH;1doV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBKSzVyIE2gNE4yPDVizszNMi=>	NVjkT4J5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
MOLM13	M4XnTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M2PScFQh\GG7cx?=	MofuS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUW9NVTF\|IHPlcIx{KGGodHXyJFQh\GG7czDifUBYW1RvODDhd5NigSxiSVO1NEA:KDBwMkSxJO69VS5?	NEXzTZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES2N\|Q5Pyd-Mki0OlM1QDd:L3G+
TY82	NGHmfpBCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MoHuO\|IhcHK\|	NF\4WJVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTZPFIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT\|gh[XO\|YYmsJGlEPTBiPTCwMlIh\|ryPLh?=	MnXUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3OE[3NVgoRjJ6NUi2O\|E5RC:jPh?=
MM1S	MV;BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MYO3NkBpenN?	M2nVTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV2xV{Bk\WyuczDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IECuNlMh\|ryPLh?=	NGrORlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW4OlcyQCd-Mki1PFY4OTh:L3G+
BL21 (DE3)-codon plus-RIL	NYDFU\|hGTnWwY4Tpc44h[XO\|YYm=		NGTKR4E1KGi{cx?=	M4TxRWlvcGmkaYTpc44hd2ZiSmGxMWZKXENiYnnu[Ilv\yC2bzDIbZM3NXSjZ3fl[EBDWkR2LVLENUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKEKOMkGgLGRGOylvY3;kc44heGy3cz3STWwh[2WubIOgbY5kfWKjdHXkJIlvKGSjcnug[o9zKDRiaILzJIJ6KG[udX;y[ZNk\W6lZTDhcol{d3S{b4D5JIF{e2G7LDDJR\|UxKD1iMD6yOkDPxE1w	M4jmOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUi2O\|E5Lz5{OEW4OlcyQDxxYU6=
THP1	NEjwN\|JCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=			NX7Gdnc6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUTHAyKGOnbHzzMEBKSzVyIE2gNE4zQSEQvF2u	NXHMO2M{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5N\|kyOjFpPkK4PVM6OTJzPD;hQi=>
TY82	MkPYRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?			M3y3SGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVGm4NkBk\WyuczygTWM2OCB;IECuN\|kh\|ryPLh?=	NYDD[4xmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5N\|kyOjFpPkK4PVM6OTJzPD;hQi=>
NALM16	NILC[mREgXSxdH;4bYNqfHliYYPzZZk>		NFjtRpo2KGSjeYO=	NYKzc4tIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkGOTUG2JINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC1JIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhTUN3MDC9JFAvOjdizszNMi=>	NX3pVVFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxO\|AxOjRpPkK5NVcxODJ2PD;hQi=>
NALM6	NYrt[lJlS3m2b4TvfIlkcXS7IHHzd4F6		NWjmTnJ6PSCmYYnz	MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDORWxOPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPSCmYYnzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFXDOVAhRSByLkO5JO69VS5?	M3nMRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUewNFI1Lz5{OUG3NFAzPDxxYU6=
697	NHz2eI5EgXSxdH;4bYNqfHliYYPzZZk>		MXi1JIRigXN?	NV7MbGw5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hPjl5IHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB3IHThfZMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygSWM2OCB;IEGuNVch\|ryPLh?=	M3exOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUewNFI1Lz5{OUG3NFAzPDxxYU6=
HD-MB03	Mm\LR5l1d3SxeHnjbZR6KGG\|c3H5		MljCOUBl[Xm\|	NGr2ToFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJTC2PQkCzJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC1JIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhTUN3MDC9JFMvPSEQvF2u	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF5MECyOEc,OjlzN{CwNlQ9N2F-
A673	NWXNU4RHeUiWUzDhd5NigQ>?			NH;kR2FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?=	MonPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
DAOY	NVzHZ3NveUiWUzDhd5NigQ>?			Ml;GdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN?	MnnQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Saos-2	MkPhdWhVWyCjc4PhfS=>			MXvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy\|	NE\EXHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-37	M1m1ZZFJXFNiYYPzZZk>			M3\0ZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?=	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	MY\xTHRUKGG\|c3H5			NV;leph6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLEJINmdGy\|	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
MG 63 (6-TG R)	M4nuOZFJXFNiYYPzZZk>			M17hbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?=	MkDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB1643	NF;XNYFyUFSVIHHzd4F6			M4DBbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	M3LVUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50	MX;xTHRUKGG\|c3H5			NWD2fVNueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=>	M3XKclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41	NG\2VYxyUFSVIHHzd4F6			Mn;qdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN?	MoLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2	NX;BWIJJeUiWUzDhd5NigQ>?			M{fTR5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz	MoruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	NGnFfYxyUFSVIHHzd4F6			NIrvb5dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=>	M4Hzd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1	MYnxTHRUKGG\|c3H5			MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?=	MnPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	NHi5VmNyUFSVIHHzd4F6			NULSPZZWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz	M4HleVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TY82	NF7BS4FCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MnWxO\|IhcHK\|	NHT1[ZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTZPFIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT\|gh[XO\|YYmsJGlEPTBiPTCwMlMxPDNizszNMi=>	NVnzc245RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
MM1S	NF3XbJRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M3TRV\|czKGi{cx?=	NYXURo9USW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVFUKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG\|c3H5MEBKSzVyIE2gNE4{PDl{IN88UU4>	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV{NUSzOUc,Ojl3MkW0N\|U9N2F-
TY82	MVTGeY5kfGmxbjDhd5NigQ>?	NFHlUJMxNjJidH:gNUB2VQ>?	NHLteHEzPCCqcoO=	M3HCV2lvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBVYTh{IHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBkNU27YzDwdo91\WmwIHX4dJJme3Orb36gZZQhOC5{IITvJFEhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	MmL3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MkW0N\|UoRjJ7NUK1OFM2RC:jPh?=
TY82	NF6zNoJHfW6ldHnvckBie3OjeR?=	MVKwMlIhfG9iMTD1US=>	MkL6NlQhcHK\|	NXK1OmxLUW6qaXLpeIlwdiCxZjDCVmQ1KGmwIHj1cYFvKFS\OEKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGNvTYnjJI1TVkFiZYjwdoV{e2mxbjDheEAxNjJidH:gNUB2VSCjZoTldkAzPCCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz	Mln1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MkW0N\|UoRjJ7NUK1OFM2RC:jPh?=
TY82 or NCI-H1299	NUTqOZplTnWwY4Tpc44h[XO\|YYm=	M2flWFAvOiC2bzCxJJVO	MWWyOEBpenN?	NELXWYdKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hXFl6MjDvdkBPS0lvSEGyPVkh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIGDEMWwyKHC{b4TlbY4h\XiycnXzd4lwdiCjdDCwMlIhfG9iMTD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	NXWwWnB7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
TY82 or NCI-H1299	NEHM[3hHfW6ldHnvckBie3OjeR?=	NXX3WWF2OC5{IITvJFEhfU1?	NGHyWZMzPCCqcoO=	M3G3T2lvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBVYTh{IH;yJG5EUS2KMUK5PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iUFStUFEhdVKQQTDlfJBz\XO\|aX;uJIF1KDBwMjD0c{AyKHWPIHHmeIVzKDJ2IHjyd{BjgSCUVD3QR3Ih[W6jbInzbZM>	NXXzeoxzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
C4-2B	MUXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M4n4blk3KGi{cx?=	NIXaUFdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFO0MVJDKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDD[YxtNVSrdHXyJIdtdyC{ZXHn[Y51KGKjc3XkJIx2dWmwZYPj[Y5k\SCjc4PhfS=>	NIjvRms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0NVM4OSd-Mkm1OFE{PzF:L3G+
22Rv1	MUjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NXXUWJlCQTZiaILz	MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDJ{Uo[xJINmdGy\|IHHmeIVzKDl4IHjyd{BjgSCFZXzsMXRqfGW{IHfsc{Bz\WGpZX70JIJie2WmIHz1cYlv\XOlZX7j[UBie3OjeR?=	MkLBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NEGzO\|EoRjJ7NUSxN\|cyRC:jPh?=
LNCAP	NXfuOppuSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M{DlbFk3KGi{cx?=	M1L1UmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFPlcIwuXGm2ZYKg[4xwKHKnYXflcpQh[mG\|ZXSgcJVucW6nc3PlcoNmKGG\|c3H5	NES1dIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0NVM4OSd-Mkm1OFE{PzF:L3G+
HL60	MY\DfZRwfG:6aXPpeJkh[XO\|YYm=			NIHjcHlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNVIh\|ryPLh?=	NFrXRoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[1O\|A6QSd-Mkm2OVcxQTl:L3G+
Raji	MWXGeY5kfGmxbjDhd5NigQ>?			NVTGNIpwUW6qaXLpeIlwdiCxZjDCVmQ1NUKGMTDpckBpfW2jbjDSZYpqKGOnbHzzJIF{e2W\|c3XkJIF{KGSxd37y[Yd2dGG2aX;uJI9nKE2\QzDn[Y5mKGW6cILld5Nqd25iYomgVGNTKG2ndHjv[EwhUUN3MDC9JFAvOTN{IN88UU4>	NE\wUI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[1O\|A6QSd-Mkm2OVcxQTl:L3G+
LNCAP	NX25bXVJSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=			MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy\|LDDJR\|UxKD1iMD6zOVY2KM7:TT6=	NYe5XmkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O\|U5PTF6PD;hQi=>
MV411	NEXG[3lEgXSxdH;4bYNqfHliYYPzZZk>		MkD3O\|IhcHK\|	NInaXY9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOXjRzMTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDhd5NigSxiSVO1NEA:KDBwODFOwG0v	MmPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{Nki3NFIoRjNyMk[4O\|AzRC:jPh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Growth inhibition assay	Cell viability ; PubMed: 26840085 Oncotarget A., B. and C. Dose response curves of MPNST-derived cell lines treated with three bromodomain inhibitors: JQ1, OTX015 and I-BET-762.	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]	- 合并荧光共振能量转移（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]	- 合并 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。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 小鼠 Dosages: 30 mg/kg Administration: 静脉注射 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	84 mg/mL (198.15 mM)
	Ethanol	42 mg/mL warmed (99.07 mM)
	Water	Insoluble

* 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 Download Molibresib (I-BET-762) SDF

分子量	423.9
化学式	C₂₂H₂₂ClN₅O₂
CAS号	1260907-17-2
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	GSK525762, GSK525762A

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

每只动物给药体积

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

计算重置

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。

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。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

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	Active not recruiting	Drug: GSK525762\|Drug: Placebo\|Drug: Fulvestrant	Neoplasms	GlaxoSmithKline	February 2 2017	Phase 2
NCT01943851	Completed	Drug: GSK525762	Neoplasms	GlaxoSmithKline	May 14 2014	Phase 2
NCT01587703	Completed	Drug: GSK525762	Carcinoma Midline	GlaxoSmithKline	March 28 2012	Phase 1

技术支持

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操作手册

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Epigenetic Reader Domain Signaling Pathway Map

Epigenetic Reader Domain Inhibitors with Unique Features

选择性强的BET抑制剂

PFI-1 (PF-6405761) : BRD4-selective, IC50=0.22 μM.
用于临床的BET抑制剂

RVX-208 ^New : Phase II for Dyslipidemia.
最新的BET抑制剂

Bromosporine : Broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.
经典的BET抑制剂

I-BET151 (GSK1210151A) : Novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM, respectively.

研究领域

产品类型

定制您的化合物库

Molibresib (I-BET-762)

客户使用Selleck生产的Molibresib (I-BET-762)发表文献18篇：

客户使用该产品的2个实验数据：

产品安全说明书

Epigenetic Reader Domain抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Molibresib (I-BET-762) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

技术支持

Epigenetic Reader Domain Signaling Pathway Map

Epigenetic Reader Domain Inhibitors with Unique Features