Molibresib (I-BET-762)

Name: Molibresib (I-BET-762)
Brand: Selleck Chemicals
SKU: S7189
Rating: 5 (17 reviews)

For research use only.

Catalog No.S7189 Synonyms: GSK525762, GSK525762A

17 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 17 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 )

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 )

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 )

2 Customer Reviews

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.

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	NULLOWJQTnWwY4Tpc44h[XO\|YYm=		M2CwRVE5KGi{cx?=	NVLOWXlbUW6mdXP0bY9vKG:oIHj1cYFvKEGyb1GxJIdmdmViZYjwdoV{e2mxbjDpckB{fGGkbImgeJJidnOoZXP0[YQhcHWvYX6gTIVxTzJiY3XscJMh[2:neIDy[ZN{cW6pIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjZoTldkAyQCCqcoOgZpkhdHWvaX7ld4NmdmOnIHHzd4F6NCCHQ{WwJF0hOC55IN88UU4>	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV4OEOyNkc,OjF3NkizNlI9N2F-
HepG2	MkTMSpVv[3Srb36gZZN{[Xl?		MkHiOkBpenN?	M2nQR2lv\HWldHnvckBw\iCqdX3hckBCeG:DMTDwdo91\WmwIIP5cpRp\XOrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCwZX;zfY51cGW\|aYPl[EBz[WSrb3zhZoVt\WRicILveIVqdiC\|ZXPy[ZRqd25iYX\0[ZIhPiCqcoOgZpkhW0SVIGDBS2Uh[W6jbInzbZMhcW5icILld4Vv[2Vib3[gX\|M2W12vZYTobY9vcW6n	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV4OEOyNkc,OjF3NkizNlI9N2F-
HepG2	NHfy[\|ZHfW6ldHnvckBie3OjeR?=		MXixPEBpenN?	MVzVdJJm\3WuYYTpc44hd2ZiQYDvRVEh\XiycnXzd4lwdiCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bkd26lZX70doF1cW:wIILldZVqemWmIITvJIlv[3KnYYPlJFcxLSCxZjDseYNq\mW{YYPlJIFkfGm4aYT5JIFnfGW{IEG4JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFMUewJF0hOC5{IN88UU4>	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN6NkWyPUc,OjJ\|OE[1Nlk9N2F-
HepG2	NGrFU\|FHfW6ldHnvckBie3OjeR?=		MUWxPEBpenN?	NG\GOYlKdmS3Y4Tpc44hd2ZiaIXtZY4hSXCxQUGg[4Vv\SCneIDy[ZN{cW:wIHnuJJN1[WKueTD0doFve2[nY4Tl[EBpfW2jbjDI[ZBIOiClZXzsd{Bkd2W6cILld5NqdmdibIXjbYZmemG\|ZTDy[ZBwenSncjDn[Y5mKGGodHXyJFE5KGi{czDifUBtfW2rbnXzZ4Vv[2ViYYPzZZktKEWFNUCgQUAxNjdizszNMi=>	NYnpcnJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5NlQ1OzRpPkKyPVI1PDN2PD;hQi=>
PBMC	NXn1S5R3SW62aXnu[oxidW2jdH;yfUBie3OjeR?=			NHXYPYNCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFLNR{Bk\WyuczDhd5Nme3OnZDDhd{BNWFNvaX7keYNm\CCLTD22JJBzd2S3Y4Tpc44h[nliY3jlcYltfW2rbnXzZ4Vv[2ViYYPzZZktKEmFNUCgQUAxNjNzNkKzJO69VS5?	MlHoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMUW5OlcoRjJ2MEG1PVY4RC:jPh?=
Raji	MWDGeY5kfGmxbjDhd5NigQ>?		NVzISXl[PCCqcoO=	NHL4Rm1KdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hWmGsaTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhVVmFIHX4dJJme3Orb36gZYZ1\XJiNDDodpMtKEmFNUCgQUAxNjF7IN88UU4>	M{\oSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwO\|U5Lz5{NEmwNFc2QDxxYU6=
Rosetta2 DE3	NELiNm5HfW6ldHnvckBie3OjeR?=		Mo\lN\|AhdWmwcx?=	NX\zbVYzTGm\|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFMhSkR{IDizNFYhfG9iNEG3JIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB\|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEurIE2gNE4xOzB\|IN88UU4>	MmqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	M1nYfGZ2dmO2aX;uJIF{e2G7		NV;wUldyOzBibXnudy=>	MoPiSIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKURESgRmQzKCh\|M{OgeI8hPDZyIHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wN\|I{KM7:TT6=	MnLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	NFy0fXlHfW6ldHnvckBie3OjeR?=		NH3WSJI{OCCvaX7z	NFjCepFFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEOEBDTDFiKES0JJRwKDF4ODDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFM5QCEQvF2u	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	M1fCfGZ2dmO2aX;uJIF{e2G7			MlXFRolv\GmwZzDh[oZqdmm2eTD0c{BjcW:2aX75cIF1\WRiQmLEN{BDTDJiKEOwOkB1dyB2MUegZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHL5JIJqdy2uYYnldkBqdnSncn\ldo9u\XS{eTDt[ZRpd2RuIFvkJF0hOC5yNEC3JO69VS5?	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	M2DOXGZ2dmO2aX;uJIF{e2G7			NXjzeYhFSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFOiCEREKgLFM1QSC2bzC0OlAh[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6wOFU1KM7:TT6=	MnPhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3	MUPGeY5kfGmxbjDhd5NigQ>?			NXrvTWNySmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFPCCEREKgLFM{OyC2bzC0OlAh[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6wOFc3KM7:TT6=	NUTDcJVpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	M{nVNWZ2dmO2aX;uJIF{e2G7		M362RlMxKG2rboO=	NHywcmxFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLENkBDTDJiKEO0PUB1dyB2NkCgZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlA1QTJizszNMi=>	NVvhUFRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	NXfXTmRkTnWwY4Tpc44h[XO\|YYm=		MkXGN\|AhdWmwcx?=	NHX3RpdFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEN{BDTDFiKEK0JJRwKDF2NDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBMcSB;IECuNFU{QSEQvF2u	NVvnOmk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	MWLGeY5kfGmxbjDhd5NigQ>?		NYPaSJJQOzBibXnudy=>	M1T2WGRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSyJGJFOSBqN{KgeI8hOjB3IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO\|YYmsJGtqKD1iMD6wOVY5KM7:TT6=	NHnMUYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3	NFf1VXhHfW6ldHnvckBie3OjeR?=			MWfCbY5lcW6pIHHm[olvcXS7IITvJIJqd3SrbonsZZRm\CCEUlSzJGJFOSBqMkSgeI8hOTR2IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCkeTDibY8udGG7ZYKgbY51\XKoZYLvcYV1enlibXX0bI9lNCCNZDC9JFAvODZyNzFOwG0v	NWT2WXNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
MV4-11	NFLJfmJEgXSxdH;4bYNqfHliYYPzZZk>		M3LxeVQh\GG7cx?=	NUnZbnFIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVZ2LUGxJINmdGy\|IHjhdoJwemmwZzDNUGwyKG[3c3nvckBo\W6nIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IESg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHHzd4F6NCCLQ{WwJF0hOC5yOUOg{txONg>?	NVnZVIhWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	MXvGeY5kfGmxbjDhd5NigQ>?		NITY[mc{OCCvaX7z	NX3Gd5lrTGm\|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFQhSkR{IDizN\|MhfG9iNE[wJIFucW6xIHHjbYQhemW\|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB\|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEmFNUCgQUAxNjB7OESg{txONg>?	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3	MonBSpVv[3Srb36gZZN{[Xl?			NXKwd5JTSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFPCCEREGgLFQ1KHSxIEG2PEBidWmwbzDhZ4llKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDSc5NmfHSjMjDESVMh[2WubIOgZpkh[mmxLXzhfYVzKGmwdHXy[oVzd22ndIL5JI1mfGixZDygT4QhRSByLkC5PVQh\|ryPLh?=	M2XXSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3	M125dmZ2dmO2aX;uJIF{e2G7		MknDN\|AhdWmwcx?=	NXS4XYNXTGm\|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFQhSkRzIDi0OEB1dyBzNkigZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3MDC9JFAvOTV4IN88UU4>	NYLEVYFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3	NULpe\|BzTnWwY4Tpc44h[XO\|YYm=			M{[5[2JqdmSrbnegZYZncW6rdImgeI8h[mmxdHnufYxifGWmIFLSSFIhSkRzIDi3NkB1dyB{MEWgZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHL5JIJqdy2uYYnldkBqdnSncn\ldo9u\XS{eTDt[ZRpd2RuIFvkJF0hOC5zNUmg{txONg>?	NI\PRXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
MOLM13	NE\ib21EgXSxdH;4bYNqfHliYYPzZZk>		MV60JIRigXN?	NFf3TmFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOV0yPMUOgZ4VtdHNiaHHyZo9zcW6pIF3MUFEh\nW\|aX;uJIdmdmViYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNDDkZZl{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiYYPzZZktKEmFNUCgQUAxNjJ2MTFOwG0v	MmflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
BL21(DE3)	NVnubnVmTnWwY4Tpc44h[XO\|YYm=			NFTMNZZDcW6maX7nJIFn\mmwaYT5JJRwKE5vdHXycYlv[WxiSHnzOk11[WepZXStRnJFPCCkcn;tc4RwdWGrbjCyJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKGOxbYDleIVvfCCHc3Po[ZJq[2irYTDjc4xqKEKOMkGoSGU{MSClZXzsd{BjgSCrc3;0bIVzdWGuIITpeJJifGmxbjDjZYxwemmvZYTyfUwhU2RiPTCwMlA3PSEQvF2u	NHnLVWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO2O\|U{QSd-Mk[zOlc2Ozl:L3G+
BL21(DE3)	NVzrSnF[TnWwY4Tpc44h[XO\|YYm=			M4rVeGJqdmSrbnegZYZncW6rdImgeI8hVi22ZYLtbY5idCCKaYO2MZRi\2enZD3CVmQ1KGK{b33v[I9u[WmwIEGgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4h[2:vcHX0[Y51KEW\|Y3jldolkcGmjIHPvcIkhSkx{MTjESVMqKGOnbHzzJIJ6KGm\|b4To[ZJu[WxidHn0doF1cW:wIHPhcI9zcW2ndIL5MEBM\CB;IECuNFk2KM7:TT6=	MlnNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|Nke1N\|koRjJ4M{[3OVM6RC:jPh?=
BL21(DE3)	NE\oOYpHfW6ldHnvckBie3OjeR?=			M3KxT2JqdmSrbnegZYZncW6rdImgeI8h\nWubDDs[Y5ofGhiTj30[ZJucW6jbDDIbZM3NXSjZ3fl[E1DWkR{IHLyc41w\G:vYXnuJFIhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iY3;tdIV1\W62IFXzZ4hmemmlaHnhJINwdGliQlyyNUhFTTNrIHPlcIx{KGK7IHnzc5Rp\XKvYXygeIl1emG2aX;uJINidG:{aX3leJJ6NCCNZDC9JFAvOSEQvF2u	MnPRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|Nke1N\|koRjJ4M{[3OVM6RC:jPh?=
BL21(DE3)	NVrVTG9FTnWwY4Tpc44h[XO\|YYm=			NEj0TXJDcW6maX7nJIFn\mmwaYT5JJRwKG[3bHygcIVv\3SqIF6teIVzdWmwYXygTIl{Pi22YXfn[YQuSlKGMjDido9ud2SxbXHpckAyKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIHPvcZBmfGWwdDDFd4Np\XKrY3jpZUBkd2yrIFLMNlEpTEV\|KTDj[YxteyCkeTDpd491cGW{bXHsJJRqfHKjdHnvckBk[Wyxcnnt[ZRzgSxiS3SgQUAxNjJ\|IN88UU4>	NH;YRmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO2O\|U{QSd-Mk[zOlc2Ozl:L3G+
BL21(DE3)-R3-pRARE2	NIDZPVRHfW6ldHnvckBie3OjeR?=			NVjmT3g4UW6qaXLpeIlwdiCxZjDoeY1idiCKaYOteIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMjDlfJBz\XO\|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBDVDJzKFTFN{kuWjNvcGLBVmUzKGOnbHzzJIJ6KE[URWSgZZN{[XluIFnDOVAhRSByLkCzOkDPxE1w	NVO3boRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3N\|E1QTBpPkK2O\|MyPDlyPD;hQi=>
BL21(DE3)-R3-pRARE2	MnnLSpVv[3Srb36gZZN{[Xl?			NIHzeWdKdmirYnn0bY9vKG:oIHj1cYFvKEircz30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiBzIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJGJNOjFqRFWzLU1TOy2yUlHSSVIh[2WubIOgZpkhTlKHVDDhd5NigSxiSVO1NEA:KDBwMEO2JO69VS5?	NVPtXmJXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3N\|E1QTBpPkK2O\|MyPDlyPD;hQi=>
Rosetta2 DE3	NWDJdZdkTnWwY4Tpc44h[XO\|YYm=		MkfLN\|AhdWmwcx?=	NFLqS45KdmirYnn0bY9vKG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDibY5lcW6pIITvJJJm[2:vYnnuZY51KGi3bXHuJG4ufGW{bXnuZYwhUGm\|Nj30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiB{IDizN\|MhfG9iNE[wJJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlAzOyEQvF2u	M{XacFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N\|Q5PzxxYU6=
Rosetta2 DE3	NYjKWXVPTnWwY4Tpc44h[XO\|YYm=		MlvKN\|AhdWmwcx?=	NXXEVmlqUW6qaXLpeIlwdiCxZjDGRW0udGGkZXzl[EBbSkF{NEigZolv\GmwZzD0c{Bz\WOxbXLpcoFvfCCqdX3hckBPNXSncn3pcoFtKEirc{[teIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMTCoOFQhfG9iMU[4JJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlA1PjRizszNMi=>	NGfRUmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES2N\|Q5Pyd-Mki0OlM1QDd:L3G+
Rosetta2 DE3	Mm\mSpVv[3Srb36gZZN{[Xl?		NXrCfHJbOzBibXnudy=>	M1XoWGlvcGmkaYTpc44hd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JIJzd22xZH;tZYlvKDJiKEOzN{B1dyB2NkCgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCIbH;1doV{[2WwY3WgdI9t[XKrenH0bY9vKGG\|c3H5MEBKSzVyIE2gNE4xPzd3IN88UU4>	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
MV4-11	NH;DRXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NV:4[4lwPCCmYYnz	MnnHS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUXY1NTFzIHPlcIx{KGGodHXyJFQh\GG7czDifUBYW1RvODDhd5NigSxiSVO1NEA:KDBwMEmzJO69VS5?	NWLz[FJsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
Rosetta2 DE3	MWDGeY5kfGmxbjDhd5NigQ>?		MlfLN\|AhdWmwcx?=	NUHXOVdJUW6qaXLpeIlwdiCxZjDGRW0udGGkZXzl[EBbSkF{NEigZolv\GmwZzD0c{Bz\WOxbXLpcoFvfCCqdX3hckBPNXSncn3pcoFtKEirc{[teIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMTCoOFQhfG9iMU[4JJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy\|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3MDC9JFAvOTR3IN88UU4>	NXzITYFzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
MOLM13	NXLzTmplT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NWPFUmZSPCCmYYnz	NH3SSoJIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOV0yPMUOgZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KFeVVD24JIF{e2G7LDDJR\|UxKD1iMD6yOFEh\|ryPLh?=	NGXpTm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES2N\|Q5Pyd-Mki0OlM1QDd:L3G+
TY82	NXrCc3V{SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3zQUFczKGi{cx?=	NXrIN\|ZtSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUXVgzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG\|c3H5MEBKSzVyIE2gNE4zKM7:TT6=	M1vzNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUi2O\|E5Lz5{OEW4OlcyQDxxYU6=
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BL21 (DE3)-codon plus-RIL	NGXUSnNHfW6ldHnvckBie3OjeR?=		MoKyOEBpenN?	M3;OcGlvcGmkaYTpc44hd2ZiSmGxMWZKXENiYnnu[Ilv\yC2bzDIbZM3NXSjZ3fl[EBDWkR2LVLENUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKEKOMkGgLGRGOylvY3;kc44heGy3cz3STWwh[2WubIOgbY5kfWKjdHXkJIlvKGSjcnug[o9zKDRiaILzJIJ6KG[udX;y[ZNk\W6lZTDhcol{d3S{b4D5JIF{e2G7LDDJR\|UxKD1iMD6yOkDPxE1w	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV6NkexPEc,Ojh3OE[3NVg9N2F-
THP1	MVTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?			MknERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCWSGCxJINmdGy\|LDDJR\|UxKD1iMD6yPUDPxE1w	NU[zRXNuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5N\|kyOjFpPkK4PVM6OTJzPD;hQi=>
TY82	NYjCV\|BkSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=			NETmdJdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTZPFIh[2WubIOsJGlEPTBiPTCwMlM6KM7:TT6=	MmKzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7M{mxNlEoRjJ6OUO5NVIyRC:jPh?=
NALM16	MVrDfZRwfG:6aXPpeJkh[XO\|YYm=		NU\mT4VnPSCmYYnz	MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDORWxOOTZiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDViZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDFR\|UxKD1iMD6yO{DPxE1w	M{W5NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUewNFI1Lz5{OUG3NFAzPDxxYU6=
NALM6	NIf6TGNEgXSxdH;4bYNqfHliYYPzZZk>		MUC1JIRigXN?	NHewdGpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPSUyPNjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiNTDkZZl{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGVEPTBiPTCwMlM6KM7:TT6=	M1rPSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUewNFI1Lz5{OUG3NFAzPDxxYU6=
697	NGe0WIREgXSxdH;4bYNqfHliYYPzZZk>		MWi1JIRigXN?	NE\CblJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckA3QTdiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDViZHH5d{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDFR\|UxKD1iMT6xO{DPxE1w	NE\XZYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG3NFAzPCd-MkmxO\|AxOjR:L3G+
HD-MB03	MV\DfZRwfG:6aXPpeJkh[XO\|YYm=		M13yTFUh\GG7cx?=	NVriW4dKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUERvTVKwN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOUBl[Xm\|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEWFNUCgQUA{NjVizszNMi=>	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF5MECyOEc,OjlzN{CwNlQ9N2F-
A673	MlnadWhVWyCjc4PhfS=>			MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	M4fZTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY	MXvxTHRUKGG\|c3H5			Mo\ydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN?	NHTYZW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	NV;vUXZ{eUiWUzDhd5NigQ>?			NGP5OolyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz	MmjHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
BT-37	MmP6dWhVWyCjc4PhfS=>			NHWy[nRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN\|ch[2WubIO=	M4Tie\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD	MmXVdWhVWyCjc4PhfS=>			MoK0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
MG 63 (6-TG R)	M2SzVpFJXFNiYYPzZZk>			NEjNbIhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO=	MlzTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB1643	MWjxTHRUKGG\|c3H5			MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	M3XXUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50	NIjqdGdyUFSVIHHzd4F6			MlewdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?=	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh41	Mk\ZdWhVWyCjc4PhfS=>			NWHJR\|hTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO=	MkjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2	NELJeoNyUFSVIHHzd4F6			NX7nPVBreUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	M1u0[pFJXFNiYYPzZZk>			MUHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	M{XaXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1	MkC3dWhVWyCjc4PhfS=>			NYXoNmZHeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM>	NX3OXnZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5	MYLxTHRUKGG\|c3H5			Mo\1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy\|	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
TY82	MV7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		Mke2O\|IhcHK\|	NXz6OI46SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUXVgzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG\|c3H5MEBKSzVyIE2gNE4{ODR\|IN88UU4>	NUDLSmxYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
MM1S	MkjmRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NVO1ToJDPzJiaILz	MlrPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPTUHTJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR\|UxKD1iMD6zOFkzKM7:TT6=	NX3sbmJlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
TY82	NWfkOHZITnWwY4Tpc44h[XO\|YYm=	NF3XbFkxNjJidH:gNUB2VQ>?	MUeyOEBpenN?	NYLQTIxXUW6qaXLpeIlwdiCxZjDCVmQ1KGmwIHj1cYFvKFS\OEKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGNvTYnjJJBzd3SnaX6g[ZhxemW\|c3nvckBifCByLkKgeI8hOSC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	NHfKRYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWyOVQ{PSd-Mkm1NlU1OzV:L3G+
TY82	NXe4eW55TnWwY4Tpc44h[XO\|YYm=	NWfXUVZWOC5{IITvJFEhfU1?	MlH5NlQhcHK\|	NE\SVGtKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hXFl6MjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[y2PeXOgcXJPSSCneIDy[ZN{cW:wIHH0JFAvOiC2bzCxJJVOKGGodHXyJFI1KGi{czDifUBTXC2SQ2KgZY5idHm\|aYO=	NWrnZXU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
TY82 or NCI-H1299	Mn;CSpVv[3Srb36gZZN{[Xl?	NHfhOXQxNjJidH:gNUB2VQ>?	M4P3clI1KGi{cx?=	Mmq2TY5pcWKrdHnvckBw\iCEUlS0JIlvKGi3bXHuJHR[QDJib4KgUmNKNUhzMkm5JINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCSRD3MNUBxem:2ZXnuJIV5eHKnc4Ppc44h[XRiMD6yJJRwKDFidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	NFPifm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWyOVQ{PSd-Mkm1NlU1OzV:L3G+
TY82 or NCI-H1299	NFTDPXZHfW6ldHnvckBie3OjeR?=	Ml36NE4zKHSxIEGgeW0>	MmfyNlQhcHK\|	MWrJcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gWHk5OiCxcjDOR2kuUDF{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFCGLVyxJI1TVkFiZYjwdoV{e2mxbjDheEAxNjJidH:gNUB2VSCjZoTldkAzPCCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz	M4joe\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUK1OFM2Lz5{OUWyOVQ{PTxxYU6=
C4-2B	M{LacmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NGrMOlA6PiCqcoO=	M3S4fWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ{StNmIh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IFPlcIwuXGm2ZYKg[4xwKHKnYXflcpQh[mG\|ZXSgcJVucW6nc3PlcoNmKGG\|c3H5	M3rMXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUSxN\|cyLz5{OUW0NVM4OTxxYU6=
22Rv1	MnWzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M2PTbFk3KGi{cx?=	MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDJ{Uo[xJINmdGy\|IHHmeIVzKDl4IHjyd{BjgSCFZXzsMXRqfGW{IHfsc{Bz\WGpZX70JIJie2WmIHz1cYlv\XOlZX7j[UBie3OjeR?=	NYi3NZhSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OFE{PzFpPkK5OVQyOzdzPD;hQi=>
LNCAP	M1rXTGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MmCxPVYhcHK\|	NH61O4NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzOR2FRKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDD[YxtNVSrdHXyJIdtdyC{ZXHn[Y51KGKjc3XkJIx2dWmwZYPj[Y5k\SCjc4PhfS=>	MnTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NEGzO\|EoRjJ7NUSxN\|cyRC:jPh?=
HL60	NIrxRYtEgXSxdH;4bYNqfHliYYPzZZk>			M1uyRWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[nliTWTTJIF{e2G7LDDJR\|UxKD1iMD6xNkDPxE1w	M3rncFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkW3NFk6Lz5{OU[1O\|A6QTxxYU6=
Raji	M4DKUmZ2dmO2aX;uJIF{e2G7			MU\Jcohq[mm2aX;uJI9nKEKUREStRmQyKGmwIHj1cYFvKFKjanmgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94dnKnZ4XsZZRqd25ib3[gUXlEKGenbnWg[ZhxemW\|c3nvckBjgSCSQ2KgcYV1cG:mLDDJR\|UxKD1iMD6xN\|Ih\|ryPLh?=	M1\LO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkW3NFk6Lz5{OU[1O\|A6QTxxYU6=
LNCAP	MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?			NWfT[mF4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{whUUN3MDC9JFAvOzV4NTFOwG0v	M17odFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{W4OVE5Lz5{OUe1PFUyQDxxYU6=
MV411	MnX0R5l1d3SxeHnjbZR6KGG\|c3H5		MUG3NkBpenN?	NUL0T2VpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVZ2MUGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFnDOVAhRSByLkig{txONg>?	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ4OEewNkc,OzB{Nki3NFI9N2F-

... 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

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% 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 MSDS / 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 MSDS / 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 2020-01-06)

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

Tech Support

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

Handling Instructions

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

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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.
Newest BET Inhibitor

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.
Classic BET Inhibitor

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.

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Molibresib (I-BET-762)