Molibresib (I-BET-762)

Name: Molibresib (I-BET-762)
Brand: Selleck Chemicals
SKU: S7189
Rating: 5 (21 reviews)

For research use only.

Catalog No.S7189 Synonyms: GSK525762, GSK525762A

21 publications

Molibresib (I-BET-762) Chemical Structure

CAS No. 1260907-17-2

Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.

Selleck's Molibresib (I-BET-762) has been cited by 21 publications

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 )

Acta Neuropathol, 2021, 10.1007/s00401-021-02341-z

PubMed: 34283254 ( click the link to review the publication )

Cell Chem Biol, 2021, S2451-9456(21)00400-1

PubMed: 34525344 ( click the link to review the publication )

Commun Biol, 2021, 4(1):878

PubMed: 34267311 ( 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 )

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description

Targets

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

35 nM

In vitro

I-BET-762 is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with K_d of 50.5–61.3 nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of BET proteins and inhibits binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes. ^[1] I-BET-762 treatment during the first 2 d of differentiation alters CD4⁺ T-cell cytokine production, up-regulated expression of several antiinflammatory gene products and down-regulated expression of several proinflammatory cytokines. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
HepG2	MmnUSpVv[3Srb36gZZN{[Xl?		MlzJNVghcHK\|	NXnjWocyUW6mdXP0bY9vKG:oIHj1cYFvKEGyb1GxJIdmdmViZYjwdoV{e2mxbjDpckB{fGGkbImgeJJidnOoZXP0[YQhcHWvYX6gTIVxTzJiY3XscJMh[2:neIDy[ZN{cW6pIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjZoTldkAyQCCqcoOgZpkhdHWvaX7ld4NmdmOnIHHzd4F6NCCHQ{WwJF0hOC55IN88UU4>	MlHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3NkizNlIoRjJzNU[4N\|IzRC:jPh?=
HepG2	MUTGeY5kfGmxbjDhd5NigQ>?		Mn;YOkBpenN?	M3P4TGlv\HWldHnvckBw\iCqdX3hckBCeG:DMTDwdo91\WmwIIP5cpRp\XOrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCwZX;zfY51cGW\|aYPl[EBz[WSrb3zhZoVt\WRicILveIVqdiC\|ZXPy[ZRqd25iYX\0[ZIhPiCqcoOgZpkhW0SVIGDBS2Uh[W6jbInzbZMhcW5icILld4Vv[2Vib3[gX\|M2W12vZYTobY9vcW6n	NIHzNWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW2PFMzOid-MkG1Olg{OjJ:L3G+
HepG2	M13i[2Z2dmO2aX;uJIF{e2G7		NXHrXlhwOThiaILz	M2nHeXVxemWpdXzheIlwdiCxZjDBdI9COSCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W\|c3XkJIF{KGOxbnPlcpRz[XSrb36gdoVyfWm{ZXSgeI8hcW6lcnXhd4UhPzBnIH;mJIx2[2moZYLhd4Uh[WO2aY\peJkh[W[2ZYKgNVghcHK\|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVOxO\|AhRSByLkKg{txONg>?	NUeyNIZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzPFY2OjlpPkKyN\|g3PTJ7PD;hQi=>
HepG2	NUnsTFB4TnWwY4Tpc44h[XO\|YYm=		MWGxPEBpenN?	NY\he3JUUW6mdXP0bY9vKG:oIHj1cYFvKEGyb1GxJIdmdmViZYjwdoV{e2mxbjDpckB{fGGkbImgeJJidnOoZXP0[YQhcHWvYX6gTIVxTzJiY3XscJMh[2:neIDy[ZN{cW6pIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjZoTldkAyQCCqcoOgZpkhdHWvaX7ld4NmdmOnIHHzd4F6NCCHQ{WwJF0hOC55IN88UU4>	M3vuWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUK0OFM1Lz5{MkmyOFQ{PDxxYU6=
PBMC	MkKzRY51cWmwZnzhcY1ifG:{eTDhd5NigQ>?			NYjP[WpvSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDCUWMh[2WubIOgZZN{\XO\|ZXSgZZMhVFCVLXnu[JVk\WRiSVytOkBxem:mdXP0bY9vKGK7IHPo[Y1qdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwJF0hOC5\|MU[yN{DPxE1w	NYG1W3dDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVU6PjdpPkK0NFE2QTZ5PD;hQi=>
Raji	NVnjR3NYTnWwY4Tpc44h[XO\|YYm=		MlvqOEBpenN?	M4GxPWlvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBT[WqrIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDv[kBOYUNiZYjwdoV{e2mxbjDh[pRmeiB2IHjyd{whUUN3MDC9JFAvOTlizszNMi=>	MkXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC3OVgoRjJ2OUCwO\|U5RC:jPh?=
Rosetta2 DE3	NXXsPXp5TnWwY4Tpc44h[XO\|YYm=		NWrjTFJyOzBibXnudy=>	M13FPWRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSzJGJFOiBqM{C2JJRwKDRzNzDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFMxOyEQvF2u	M2X1flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	M123ZWZ2dmO2aX;uJIF{e2G7		NFXJOm4{OCCvaX7z	M1LDT2Rqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlS0JGJFOiBqM{OzJJRwKDR4MDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFMzOyEQvF2u	Ml3zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MnrXSpVv[3Srb36gZZN{[Xl?		M4DLcVMxKG2rboO=	NEjpXGFFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEOEBDTDFiKES0JJRwKDF4ODDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFM5QCEQvF2u	M4DWZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	NUn4bZZ7TnWwY4Tpc44h[XO\|YYm=			NWjUZYhXSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFOyCEREKgLFMxPiC2bzC0NVch[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6wOFA4KM7:TT6=	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	MljISpVv[3Srb36gZZN{[Xl?			NUfXbXFNSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFOiCEREKgLFM1QSC2bzC0OlAh[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6wOFU1KM7:TT6=	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	MlmySpVv[3Srb36gZZN{[Xl?			NYHzfW1sSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFPCCEREKgLFM{OyC2bzC0OlAh[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6wOFc3KM7:TT6=	Mkf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	NHnlOFdHfW6ldHnvckBie3OjeR?=		MnH5N\|AhdWmwcx?=	M{jJeWRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSyJGJFOiBqM{S5JJRwKDR4MDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFQ6OiEQvF2u	NFzze5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	NECzdIxHfW6ldHnvckBie3OjeR?=		NIjPSYQ{OCCvaX7z	NG\6T2JFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEN{BDTDFiKEK0JJRwKDF2NDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFU{QSEQvF2u	NFvFWpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	MYTGeY5kfGmxbjDhd5NigQ>?		NGTLW4M{OCCvaX7z	MWHEbZNxdGGlZX3lcpQhd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IH\yc40hSlKGMjDCSFEhMDd{IITvJFIxPSCjbXnuc{Bi[2mmIILld4llfWW\|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBTd3OndIThNkBFTTNiY3XscJMh[W[2ZYKgN\|AhdWmwczDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDLbUA:KDBwMEW2PEDPxE1w	NFXrTo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	MVLGeY5kfGmxbjDhd5NigQ>?			MWLCbY5lcW6pIHHm[olvcXS7IITvJIJqd3SrbonsZZRm\CCEUlSzJGJFOSBqMkSgeI8hOTR2IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCkeTDibY8udGG7ZYKgbY51\XKoZYLvcYV1enlibXX0bI9lNCCNZDC9JFAvODZyNzFOwG0v	NEfYepA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
MV4-11	NYLaTWZ7S3m2b4TvfIlkcXS7IHHzd4F6		MUm0JIRigXN?	MmLaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXY1NTFzIHPlcIx{KGijcnLvdolv\yCPTFyxJIZ2e2mxbjDn[Y5mKGG\|c3Xzd4VlKGG\|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDRiZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGG\|c3H5MEBKSzVyIE2gNE4xQTNizszNMi=>	NUPZc4JmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	M3:xb2Z2dmO2aX;uJIF{e2G7		NYq1N\|B3OzBibXnudy=>	NXfnPYFlTGm\|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFQhSkR{IDizN\|MhfG9iNE[wJIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB\|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEmFNUCgQUAxNjB7OESg{txONg>?	NFnNUlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	MYHGeY5kfGmxbjDhd5NigQ>?			NWXJXVl2SmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFPCCEREGgLFQ1KHSxIEG2PEBidWmwbzDhZ4llKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDSc5NmfHSjMjDESVMh[2WubIOgZpkh[mmxLXzhfYVzKGmwdHXy[oVzd22ndIL5JI1mfGixZDygT4QhRSByLkC5PVQh\|ryPLh?=	NGfLd\|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	M1PrXGZ2dmO2aX;uJIF{e2G7		NWHqO5F{OzBibXnudy=>	MVvEbZNxdGGlZX3lcpQhd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IH\yc40hSlKGNDDCSFEhMDR2IITvJFE3QCCjbXnuc{Bi[2mmIILld4llfWW\|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBTd3OndIThNkBFTTNiY3XscJMh[W[2ZYKgN\|AhdWmwczDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDJR\|UxKD1iMD6xOVYh\|ryPLh?=	M2TmVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	MV\GeY5kfGmxbjDhd5NigQ>?			NHP3XlNDcW6maX7nJIFn\mmwaYT5JJRwKGKrb4Tpcplt[XSnZDDCVmQzKEKGMTCoO\|IhfG9iMkC1JIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDifUBjcW9vbHH5[ZIhcW62ZYLm[ZJwdWW2comgcYV1cG:mLDDL[EA:KDBwMUW5JO69VS5?	M{ezPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
MOLM13	NHf0eIpEgXSxdH;4bYNqfHliYYPzZZk>		NFvWWG41KGSjeYO=	NU[yWJVFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVU:OTUGzJINmdGy\|IHjhdoJwemmwZzDNUGwyKG[3c3nvckBo\W6nIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IESg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHHzd4F6NCCLQ{WwJF0hOC5{NEGg{txONg>?	NVvCNlc3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
BL21(DE3)	MUnGeY5kfGmxbjDhd5NigQ>?			Mo\JRolv\GmwZzDh[oZqdmm2eTD0c{BPNXSncn3pcoFtKEirc{[teIFo\2WmLVLSSFQh[nKxbX;kc41icW5iMjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBkd22yZYTlcpQhTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kh[2WubIOgZpkhcXOxdHjldo1idCC2aYTyZZRqd25iY3Hsc5JqdWW2comsJGtlKD1iMD6wOlUh\|ryPLh?=	M4T0U\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{[3OVM6Lz5{NkO2O\|U{QTxxYU6=
BL21(DE3)	NW\XUoFYTnWwY4Tpc44h[XO\|YYm=			NU\rbHBqSmmwZHnu[{Bi\m[rbnn0fUB1dyCQLYTldo1qdmGuIFjpd\|YufGGpZ3XkMWJTTDRiYoLvcY9ld22jaX6gNUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiClb33w[ZRmdnRiRYPjbIVzcWOqaXGgZ49tcSCETEKxLGRGOyliY3XscJMh[nliaYPveIhmem2jbDD0bZRz[XSrb36gZ4Ftd3KrbXX0dpktKEumIE2gNE4xQTVizszNMi=>	NEW5XpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO2O\|U{QSd-Mk[zOlc2Ozl:L3G+
BL21(DE3)	NFvFTGtHfW6ldHnvckBie3OjeR?=			NXvkVFB2SmmwZHnu[{Bi\m[rbnn0fUB1dyCodXzsJIxmdme2aDDOMZRmem2rbnHsJGhqezZvdHHn[4VlNUKUREKgZpJwdW:mb33hbY4hOiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDjc41x\XSnboSgSZNkcGW{aXPobYEh[2:uaTDCUFIyMESHMzmgZ4VtdHNiYomgbZNwfGincn3hcEB1cXS{YYTpc44h[2Gub4LpcYV1enluIFvkJF0hOC5zIN88UU4>	NXHHeodIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOlc2OzlpPkK2N\|Y4PTN7PD;hQi=>
BL21(DE3)	MYLGeY5kfGmxbjDhd5NigQ>?			M4XJZmJqdmSrbnegZYZncW6rdImgeI8h\nWubDDs[Y5ofGhiTj30[ZJucW6jbDDIbZM3NXSjZ3fl[E1DWkR{IHLyc41w\G:vYXnuJFEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iY3;tdIV1\W62IFXzZ4hmemmlaHnhJINwdGliQlyyNUhFTTNrIHPlcIx{KGK7IHnzc5Rp\XKvYXygeIl1emG2aX;uJINidG:{aX3leJJ6NCCNZDC9JFAvOjNizszNMi=>	MlrDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|Nke1N\|koRjJ4M{[3OVM6RC:jPh?=
BL21(DE3)-R3-pRARE2	MlL2SpVv[3Srb36gZZN{[Xl?			NV:3WWo5UW6qaXLpeIlwdiCxZjDoeY1idiCKaYOteIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMjDlfJBz\XO\|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kuWjNvcGLBVmUzKGOnbHzzJIJ6KE[URWSgZZN{[XluIFnDOVAhRSByLkCzOkDPxE1w	NV\nfXFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3N\|E1QTBpPkK2O\|MyPDlyPD;hQi=>
BL21(DE3)-R3-pRARE2	MVXGeY5kfGmxbjDhd5NigQ>?			MlLZTY5pcWKrdHnvckBw\iCqdX3hckBJcXNvdHHn[4VlKEKURESgZpJwdW:mb33hbY4hOSCneIDy[ZN{\WRiaX6gSZNkcGW{aXPobYEh[2:uaTDCUFIyMESHMzmtVlMueFKDUlWyJINmdGy\|IHL5JGZTTVRiYYPzZZktKEmFNUCgQUAxNjB\|NjFOwG0v	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd\|MUS5NEc,OjZ5M{G0PVA9N2F-
Rosetta2 DE3	NYT6UohjTnWwY4Tpc44h[XO\|YYm=		Ml;lN\|AhdWmwcx?=	MlHnTY5pcWKrdHnvckBw\iCIQV2tcIFj\WynZDDaRmEzPDhiYnnu[Ilv\yC2bzDy[YNwdWKrbnHueEBpfW2jbjDOMZRmem2rbnHsJGhqezZvdHHn[4VlKEKURESgZpJwdW:mb33hbY4hOiBqM{OzJJRwKDR4MDDy[ZNq\HWnczmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KE[ub4Xy[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wNlMh\|ryPLh?=	M2TNWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N\|Q5PzxxYU6=
Rosetta2 DE3	MkLPSpVv[3Srb36gZZN{[Xl?		M{XUdlMxKG2rboO=	M3myeWlvcGmkaYTpc44hd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JIJzd22xZH;tZYlvKDFiKES0JJRwKDF4ODDy[ZNq\HWnczmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KE[ub4Xy[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wOFY1KM7:TT6=	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
Rosetta2 DE3	NYnjXohrTnWwY4Tpc44h[XO\|YYm=		MV2zNEBucW6\|	NVToS2NJUW6qaXLpeIlwdiCxZjDGRW0udGGkZXzl[EBbSkF{NEigZolv\GmwZzD0c{Bz\WOxbXLpcoFvfCCqdX3hckBPNXSncn3pcoFtKEirc{[teIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMjCoN\|M{KHSxIES2NEBz\XOrZIXld{kh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB\|MDDtbY5{KGK7IF\sc5Vz\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEmFNUCgQUAxNjB5N{Wg{txONg>?	NGTVT2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES2N\|Q5Pyd-Mki0OlM1QDd:L3G+
MV4-11	M4jiWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MWS0JIRigXN?	M1[wWWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1XPC1zMTDj[YxteyCjZoTldkA1KGSjeYOgZpkhX1OWLUigZZN{[XluIFnDOVAhRSByLkC5N{DPxE1w	NHnPR5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES2N\|Q5Pyd-Mki0OlM1QDd:L3G+
Rosetta2 DE3	M2X1Z2Z2dmO2aX;uJIF{e2G7		MmXBN\|AhdWmwcx?=	NE\5eldKdmirYnn0bY9vKG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDibY5lcW6pIITvJJJm[2:vYnnuZY51KGi3bXHuJG4ufGW{bXnuZYwhUGm\|Nj30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiBzIDi0OEB1dyBzNkigdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCIbH;1doV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBKSzVyIE2gNE4yPDVizszNMi=>	NXzofJBvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
MOLM13	MmPLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M2njflQh\GG7cx?=	NYmxd\|hXT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OTUGzJINmdGy\|IHHmeIVzKDRiZHH5d{BjgSCZU2StPEBie3OjeTygTWM2OCB;IECuNlQyKM7:TT6=	MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2NkO0PFcoRjJ6NE[zOFg4RC:jPh?=
TY82	Mk[1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MXi3NkBpenN?	M4foTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVGm4NkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IECuNkDPxE1w	NVrSO\|B7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1PFY4OThpPkK4OVg3PzF6PD;hQi=>
MM1S	M2jXS2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		NGS3[Xo4OiCqcoO=	MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2PMWOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSByLkKzJO69VS5?	NYXmW\|QzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1PFY4OThpPkK4OVg3PzF6PD;hQi=>
BL21 (DE3)-codon plus-RIL	MoL5SpVv[3Srb36gZZN{[Xl?		NEfScXU1KGi{cx?=	NUPDTmQ4UW6qaXLpeIlwdiCxZjDKVVEuTkmWQzDibY5lcW6pIITvJGhqezZvdHHn[4VlKEKUREStRmQyKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFXzZ4hmemmlaHnhJINwdGliQlyyNUApTEV\|KT3jc4RwdiCybIXzMXJKVCClZXzsd{BqdmO3YnH0[YQhcW5iZHHyb{Bnd3JiNDDodpMh[nliZnz1c5Jme2OnbnPlJIFvcXOxdILvdJkh[XO\|YYmsJGlEPTBiPTCwMlI3KM7:TT6=	M{npe\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUi2O\|E5Lz5{OEW4OlcyQDxxYU6=
THP1	MVfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?			MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSKUEGgZ4VtdHNuIFnDOVAhRSByLkK5JO69VS5?	M1rITFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUO5NVIyLz5{OEmzPVEzOTxxYU6=
TY82	MWLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?			MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFS\OEKgZ4VtdHNuIFnDOVAhRSByLkO5JO69VS5?	MorHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7M{mxNlEoRjJ6OUO5NVIyRC:jPh?=
NALM16	MYnDfZRwfG:6aXPpeJkh[XO\|YYm=		M1vGUFUh\GG7cx?=	NEHmU4JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPSUyPMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEWg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGG\|c3H5MEBGSzVyIE2gNE4zPyEQvF2u	MoWyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzN{CwNlQoRjJ7MUewNFI1RC:jPh?=
NALM6	NFnEcFVEgXSxdH;4bYNqfHliYYPzZZk>		NVLafmxiPSCmYYnz	NEHoWJlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPSUyPNjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiNTDkZZl{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGVEPTBiPTCwMlM6KM7:TT6=	M{WxPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUewNFI1Lz5{OUG3NFAzPDxxYU6=
697	NGfqT\|ZEgXSxdH;4bYNqfHliYYPzZZk>		NXrm[Wc3PSCmYYnz	Mk\zR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gOlk4KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA2KGSjeYOgZpkhS2WubGTpeIVzNUeubzDhd5NigSxiRVO1NEA:KDFwMUeg{txONg>?	M3TPT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUewNFI1Lz5{OUG3NFAzPDxxYU6=
HD-MB03	MVHDfZRwfG:6aXPpeJkh[XO\|YYm=		MVi1JIRigXN?	NUXNXI5jS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUERvTVKwN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOUBl[Xm\|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEWFNUCgQUA{NjVizszNMi=>	M3vpUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUewNFI1Lz5{OUG3NFAzPDxxYU6=
A673	M1HGd5FJXFNiYYPzZZk>			MnmydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	NXnKd29uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
DAOY	NEHjOWZyUFSVIHHzd4F6			MnXYdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN?	NGixUYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	MXTxTHRUKGG\|c3H5			M1jTb5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-37	NI\RelRyUFSVIHHzd4F6			NF:4Wm1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN\|ch[2WubIO=	MnzWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
RD	NWe0NJhLeUiWUzDhd5NigQ>?			NXTMcJZ1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLEJINmdGy\|	NVT6XlZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R)	NHrqTGNyUFSVIHHzd4F6			MnW0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy\|	NYfQSGhSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643	NHWyZZlyUFSVIHHzd4F6			MkDkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?=	NEnSVVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	MUfxTHRUKGG\|c3H5			MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy\|	NG\Re\|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	NVLoc3VneUiWUzDhd5NigQ>?			MnLSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN?	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SJ-GBM2	NVuyWVgzeUiWUzDhd5NigQ>?			NXnBOWhHeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM>	M{DiNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	MlXldWhVWyCjc4PhfS=>			NXzLZppweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	NVTCfJFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1	MoC1dWhVWyCjc4PhfS=>			M3nkbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	NV7tNlhpeUiWUzDhd5NigQ>?			NF;n[WxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO=	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
TY82	NXvrdGx6SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M1XvSlczKGi{cx?=	MoXGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCWWUiyJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR\|UxKD1iMD6zNFQ{KM7:TT6=	NILTT409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWyOVQ{PSd-Mkm1NlU1OzV:L3G+
MM1S	Ml3lRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NVXpVVc3PzJiaILz	MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2PMWOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSByLkO0PVIh\|ryPLh?=	MmL4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MkW0N\|UoRjJ7NUK1OFM2RC:jPh?=
TY82	MlXaSpVv[3Srb36gZZN{[Xl?	MYCwMlIhfG9iMTD1US=>	NUnze2k6OjRiaILz	NHjLTJRKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hXFl6MjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[y2PeXOgdJJwfGWrbjDlfJBz\XO\|aX;uJIF1KDBwMjD0c{AyKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV{NUSzOUc,Ojl3MkW0N\|U9N2F-
TY82	NGHTfWhHfW6ldHnvckBie3OjeR?=	NHv6TIoxNjJidH:gNUB2VQ>?	NIPrUIozPCCqcoO=	MnnkTY5pcWKrdHnvckBw\iCEUlS0JIlvKGi3bXHuJHR[QDJiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIMuVXmlIH3SUmEh\XiycnXzd4lwdiCjdDCwMlIhfG9iMTD1UUBi\nSncjCyOEBpenNiYomgVnQuWEOUIHHuZYx6e2m\|	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV{NUSzOUc,Ojl3MkW0N\|U9N2F-
TY82 or NCI-H1299	NWLJWVdoTnWwY4Tpc44h[XO\|YYm=	NXfvVlFwOC5{IITvJFEhfU1?	NXLMclVuOjRiaILz	MX3Jcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gWHk5OiCxcjDOR2kuUDF{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFCGLVyxJJBzd3SnaX6g[ZhxemW\|c3nvckBifCByLkKgeI8hOSC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV{NUSzOUc,Ojl3MkW0N\|U9N2F-
TY82 or NCI-H1299	NV[5[\|VPTnWwY4Tpc44h[XO\|YYm=	NV;iWFhWOC5{IITvJFEhfU1?	MmfwNlQhcHK\|	M{fOdGlvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBVYTh{IH;yJG5EUS2KMUK5PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iUFStUFEhdVKQQTDlfJBz\XO\|aX;uJIF1KDBwMjD0c{AyKHWPIHHmeIVzKDJ2IHjyd{BjgSCUVD3QR3Ih[W6jbInzbZM>	MnjyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MkW0N\|UoRjJ7NUK1OFM2RC:jPh?=
C4-2B	MkDqRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NXuxd2dIQTZiaILz	MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEN2LULCJINmdGy\|IHHmeIVzKDl4IHjyd{BjgSCFZXzsMXRqfGW{IHfsc{Bz\WGpZX70JIJie2WmIHz1cYlv\XOlZX7j[UBie3OjeR?=	M{HEOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUSxN\|cyLz5{OUW0NVM4OTxxYU6=
22Rv1	MYrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MUK5OkBpenN?	M2nrbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iMkLSelEh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFPlcIwuXGm2ZYKg[4xwKHKnYXflcpQh[mG\|ZXSgcJVucW6nc3PlcoNmKGG\|c3H5	NVHiR4F[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OFE{PzFpPkK5OVQyOzdzPD;hQi=>
LNCAP	MkPnRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M{fDT\|k3KGi{cx?=	NYG4b21USW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjC5OkBpenNiYomgR4VtdC2WaYTldkBodG9icnXh[4VvfCCkYYPl[EBtfW2rbnXzZ4Vv[2ViYYPzZZk>	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV2MUO3NUc,Ojl3NEGzO\|E9N2F-
HL60	NGTubppEgXSxdH;4bYNqfHliYYPzZZk>			M2f2[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[nliTWTTJIF{e2G7LDDJR\|UxKD1iMD6xNkDPxE1w	MmG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NUewPVkoRjJ7NkW3NFk6RC:jPh?=
Raji	NEC5boVHfW6ldHnvckBie3OjeR?=			NYLiSmY5UW6qaXLpeIlwdiCxZjDCVmQ1NUKGMTDpckBpfW2jbjDSZYpqKGOnbHzzJIF{e2W\|c3XkJIF{KGSxd37y[Yd2dGG2aX;uJI9nKE2\QzDn[Y5mKGW6cILld5Nqd25iYomgVGNTKG2ndHjv[EwhUUN3MDC9JFAvOTN{IN88UU4>	NGPkeGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[1O\|A6QSd-Mkm2OVcxQTl:L3G+
LNCAP	NVTqb3ZJSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=			NHrvNJFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzMEBKSzVyIE2gNE4{PTZ3IN88UU4>	NV;MW3ZqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O\|U5PTF6PD;hQi=>
MV411	MVXDfZRwfG:6aXPpeJkh[XO\|YYm=		NUDoZVl7PzJiaILz	M{POfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1XPDFzIHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCLQ{WwJF0hOC56IN88UU4>	NFnKTZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEK2PFcxOid-M{CyOlg4ODJ:L3G+

... 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

In vivo

I-BET-762 confers protection against lipopolysaccharide-induced endotoxic shock and bacteria induced sepsisa. Single dose of I-BET applied at 1.5 h after LPS injection cures the mice. Twice-daily injections of I-BET for 2 days protects mice against death caused by sepsis. ^[1] Limited treatment with I-BET-762 exclusively during early priming inhibited the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in a mouse model of experimental autoimmune encephalomyelitis (EAE). ^[2]

Protocol

Kinase Assay:^[1]	- Collapse Fluorescence resonance energy transfer (FRET) titrations: Fluorescence resonance energy transfer (FRET) titrations. I-BET is titrated against BRD2 (200 nM), BRD3 (100 nM) and BRD4 (50 nM) in 50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS in the presence of tetra-acetylated Histone H4 peptide (200 nM). After equilibrating for 1 hour, the bromodomain protein : peptide interaction is detected using FRET following the addition of 2nM Europium cryptate labelled streptavidin and 10 nM XL-665-labelled anti-6His antibody in assay buffer containing 0.05% (v/v) BSA and 400 mM KF. Plates are read using an Envision Plate reader (excitation 320 nm, emission 615 nm and 665 nm).
Cell Research:^[2]	- Collapse Cell lines: CD4⁺ T cells Concentrations: ~500 nM Incubation Time: 60–72 h Method: CD4⁺ T cells are isolated from lymph nodes and spleens of 10- to 12-wk old mice and activated with plate bound anti-CD3 and anti-CD28 antibodies in the presence of indicated cytokines. I-BET-762 compounds is included during the 60–72 h of initial activation. Over the course of 5 d of T-cell culture and expansion, the compounds is diluted 12-fold relative to the starting concentrations. (Only for Reference)
Animal Research:^[1]	- Collapse Animal Models: Mouse Dosages: 30 mg/kg Administration: i.v. (Only for Reference)

References

Solubility (25°C)

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

* 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 Download Molibresib (I-BET-762) SDF

Molecular Weight	423.9
Formula	C₂₂H₂₂ClN₅O₂
CAS No.	1260907-17-2
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	GSK525762, GSK525762A
Smiles	CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C

In vivo Formulation Calculator (Clear solution)

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

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

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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

Calculate Reset

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.

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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

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):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-09-06)

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 1
NCT01943851	Completed	Drug: GSK525762	Neoplasms	GlaxoSmithKline	May 14 2014	Phase 2
NCT01587703	Completed	Drug: GSK525762	Carcinoma Midline	GlaxoSmithKline	March 28 2012	Phase 1

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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Epigenetic Reader Domain Signaling Pathway Map

Epigenetic Reader Domain Inhibitors with Unique Features

Selective BET Inhibitor

PFI-1 (PF-6405761) : BRD4-selective, IC50=0.22 μM.
BET Inhibitor in Clinical Trial

RVX-208 ^New : Phase II for Dyslipidemia.

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Molibresib (I-BET-762)