BX-795

For research use only.

Catalog No.S1274

53 publications

CAS No. 702675-74-9

BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1.

Selleck's BX-795 has been cited by 53 publications

Immunity, 2021, S1074-7613(21)00069-8

PubMed: 33667382 ( click the link to review the publication )

Nature, 2019, 567(7747):262-266

PubMed: 30842662 ( click the link to review the publication )

Cell, 2019, 176(6):1447-1460

PubMed: 30799039 ( click the link to review the publication )

Science, 2015, 13;347(6227):aaa2630.

PubMed: 25636800 ( click the link to review the publication )

Nat Commun, 2021, 12(1):5401

PubMed: 34518549 ( click the link to review the publication )

J Immunother Cancer, 2021, 9(10)e003050

PubMed: 34663641 ( click the link to review the publication )

Autophagy, 2021, 1-17

PubMed: 34382907 ( click the link to review the publication )

J Virol, 2021, JVI.00127-21

PubMed: 34011542 ( click the link to review the publication )

Antiviral Res, 2021, 194:105145

PubMed: 34303747 ( click the link to review the publication )

iScience, 2021, 24(9):103080

PubMed: 34585118 ( click the link to review the publication )

J Thromb Haemost, 2020, 10.1111/jth.14748

PubMed: 31997536 ( click the link to review the publication )

Biochim Biophys Acta Mol Cell Res, 2020, S0167-4889(20)30287-1

PubMed: 33310066 ( click the link to review the publication )

Antimicrob Agents Chemother, 2020, AAC.00245-20

PubMed: 32601167 ( click the link to review the publication )

Oral Dis, 2020, 10.1111/odi.13583

PubMed: 32730654 ( click the link to review the publication )

Cell Death Differ, 2020, 10.1038/s41418-020-0588-y

PubMed: 32678307 ( click the link to review the publication )

iScience, 2020, 23(7):101257

PubMed: 32599557 ( click the link to review the publication )

Cell Rep, 2020, 32(5):107983

PubMed: 32755577 ( click the link to review the publication )

Ocul Surf, 2019, 10.1016/j.jtos.2019.11.011

PubMed: 31770600 ( click the link to review the publication )

Cell Rep, 2019, 27(2):631-647

PubMed: 30970263 ( click the link to review the publication )

Cancer Lett, 2019, 466:23-34

PubMed: 31521695 ( click the link to review the publication )

J Leukoc Biol, 2019, 106(6):1325-1335

PubMed: 31509298 ( click the link to review the publication )

Int J Mol Sci, 2019, 20(3)

PubMed: 30717477 ( click the link to review the publication )

Cancer Med, 2019, 8(5):2380-2391

PubMed: 30993888 ( click the link to review the publication )

Int Immunopharmacol, 2019, 77:105914

PubMed: 31634789 ( click the link to review the publication )
Nat Immunol, 2019, 20(1):18-28

PubMed: 30510222 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2018, 115(26):6798-6803

PubMed: 29891701 ( click the link to review the publication )

Cell Death Dis, 2018, 9(7):747

PubMed: 29970878 ( click the link to review the publication )

Oncoimmunology, 2018, 7(5):e1426434

PubMed: 29721392 ( click the link to review the publication )

J Thromb Haemost, 2018, 16(6):1211-1225

PubMed: 29575487 ( click the link to review the publication )

Endocrinology, 2018, 159(1):285-296

PubMed: 29029116 ( click the link to review the publication )

BMC Cancer, 2018, 18(1):595

PubMed: 29801480 ( click the link to review the publication )

Vet Microbiol, 2018, 227:61-68

PubMed: 30473353 ( click the link to review the publication )

Cell Death Dis, 2018, 9(3):269

PubMed: 29449645 ( click the link to review the publication )

Blood Adv, 2018, 2(23):3428-3442

PubMed: 30504235 ( click the link to review the publication )

Nucleic Acids Res, 2017, 45(20):11622-11642

PubMed: 28977426 ( click the link to review the publication )

Nucleic Acids Res, 2017, 45(16):9654-9678

PubMed: 28934469 ( click the link to review the publication )

Cell Death Dis, 2017, 8(4):e2752

PubMed: 28425986 ( click the link to review the publication )

Sci Rep, 2017, 7(1):982

PubMed: 28428627 ( click the link to review the publication )

Front Cell Infect Microbiol, 2017, 7:169

PubMed: 28529930 ( click the link to review the publication )

Nat Commun, 2016, 7:11363

PubMed: 27193833 ( click the link to review the publication )

Cancer Discov, 2016, 6(10):1134-1147

PubMed: 27604488 ( click the link to review the publication )

J Immunol, 2016, 196(5):2272-82

PubMed: 26826240 ( click the link to review the publication )

J Biol Chem, 2016, 291(20):10904-15

PubMed: 27002159 ( click the link to review the publication )

Tissue Eng Part A, 2016, 22(17-18):1075-85

PubMed: 27477105 ( click the link to review the publication )

Front Cell Infect Microbiol, 2016, 6:182

PubMed: 28018864 ( click the link to review the publication )

PLoS One, 2016, 11(5):e0155052

PubMed: 27148873 ( click the link to review the publication )

Am J Reprod Immunol, 2016, 75(4):451-60

PubMed: 26892235 ( click the link to review the publication )

Am J Reprod Immunol, 2016, 76(5):348-357

PubMed: 27613665 ( click the link to review the publication )
J Biomol Screen, 2016, 10.1177/1087057116656314

PubMed: 27358388 ( click the link to review the publication )

Proc Natl Acad Sci USA, 2014, 111(49):17438-43

PubMed: 25326420 ( click the link to review the publication )

FEBS J, 2014, 281(17):3816-27

PubMed: 25040165 ( click the link to review the publication )

Virology, 2014, 450-451:182-95

PubMed: 24503081 ( click the link to review the publication )

PLoS One, 2014, 9(11):e112014

PubMed: 25390891 ( click the link to review the publication )

Purity & Quality Control

Choose Selective PDK Inhibitors

Biological Activity

Description

Targets

PDK-1 ^[1] (Cell-free assay)	c-Kit ^[1] (Cell-free assay)	CDK2/CyclinE ^[1] (Cell-free assay)	Chk1 ^[1] (Cell-free assay)
6 nM	320 nM	430 nM	510 nM

In vitro

BX-795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX-795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX-795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively. ^[1] In addition, BX-795, as an inhibitor of the TBK1/IKKɛ, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. ^[2] In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation. ^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
THP1	Ml3KSpVv[3Srb36gZZN{[Xl?		NFzUR5UyKGi{	NXe3OY1uUW6qaXLpeIlwdiCxZjDjS2FUKGmwIHj1cYFvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHOjbH3vckB{eGW{bTDkd2RPSS2rbnT1Z4VlKEmITj3i[ZRiKGW6cILld5Nqd25icILlbY5kfWKjdHXkJIZweiBzIHjyJIZwdGyxd3XkJIJ6KGS\|RF7BJJN1cW23bHH0bY9vKG[xcjCxNkBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yNjFOwG0v	Mnz6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7M{SyOFYoRjJ6OUO0NlQ3RC:jPh?=
KRX	M1zGSmZ2dmO2aX;uJIF{e2G7		MYi3JI1qdnN?	NEHGXHNKdmirYnn0bY9vKG:oIGPVUW8ufGGpZ3XkJHVNUzFiKIXub45wf25ib4Lp[4lvMSCtaX7hd4Uh\G:vYXnuJIV5eHKnc4Pl[EBqdiCNUmigZ4VtdHNidYPpcochYzN{UG2t[4FudWFvQWTQJIFv\CCveXXsbY4h[mG\|aXOgdJJwfGWrbjDzeYJ{fHKjdHWgbY5kfWKjdHXkJIZweiB5IH3pcpMtKEmFNUCgQUAxNjB6NzFOwG0v	MkHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{N{W2PFEoRjJ4Mke1OlgyRC:jPh?=
KRX	NH:yPZdHfW6ldHnvckBie3OjeR?=		MYi3JI1qdnN?	M3m2c2lvcGmkaYTpc44hd2ZiU2XNU{11[WepZXSgWWxMOiBqdX7rco94diCxcnnnbY4qKGurbnHz[UBld22jaX6g[ZhxemW\|c3XkJIlvKEuUWDDj[YxteyC3c3nu[{BcOzKSXT3nZY1u[S2DVGCgZY5lKG27ZXzpckBj[XOrYzDwdo91\WmwIIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDdibXnud{whUUN3MDC9JFAvOzFizszNMi=>	MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ5NU[4NUc,OjZ{N{W2PFE9N2F-
HeLa	NH\YW5pHfW6ldHnvckBie3OjeR?=	NYThcINmPCC3TR?=	NInYPFQzPCCqcoO=	M4jvbWlvcGmkaYTpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIFjlUIEh[2WubIOgZZN{\XO\|ZXSgZZMhcW6mdXP0bY9vKG:oIFzDN{1KKHC{b4TlbY4h[WOldX31cIF1cW:wIHH0JFQhfU1iaX7jeYJifGWmIH\vdkAzPCCqcoOgZpkhcW2vdX7vZoxwfHSrbnegcYV1cG:m	NXzKZXlpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yO\|U3QDFpPkK2Nlc2PjhzPD;hQi=>
TC32	MVvxTHRUKGG\|c3H5			NFHjb4NyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?=	NY\1UJBmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673	MoLqdWhVWyCjc4PhfS=>			NITFVmpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?=	M{LiSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY	NYLSWlNpeUiWUzDhd5NigQ>?			M{LQ[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy\|	M{jWcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2	M13xZZFJXFNiYYPzZZk>			M1Xj[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	MluyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
BT-37	NH;XVnRyUFSVIHHzd4F6			NV3DV44zeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz	NI\oWII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
RD	NIjUNJhyUFSVIHHzd4F6			NYfjUFcxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLEJINmdGy\|	M4LZZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH	MlPsdWhVWyCjc4PhfS=>			NHf3fFNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=>	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-12	NGjPVoZyUFSVIHHzd4F6			Ml3VdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy\|	NGHvUYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
MG 63 (6-TG R)	MYHxTHRUKGG\|c3H5			M1TCTpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
NB1643	NXvyfYl{eUiWUzDhd5NigQ>?			MV3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	MmPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
OHS-50	MUnxTHRUKGG\|c3H5			MkS0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?=	Ml3FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	NEO5WnZyUFSVIHHzd4F6			M3HVN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy\|	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SJ-GBM2	NV;1PVRleUiWUzDhd5NigQ>?			MVfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	M2rtXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	NVi1W\|E3eUiWUzDhd5NigQ>?			M3mxVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz	NWn5ZXExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1	M1jmeJFJXFNiYYPzZZk>			NYHuSWwyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM>	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	MV;xTHRUKGG\|c3H5			M{TmNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?=	MmnHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh18	NFHVV3VyUFSVIHHzd4F6			NEjmWllyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?=	M3n3flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MV-4-11	MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?			MUTJcohq[mm2aX;uJI9nKGi3bXHuJG1XNTRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvODN4ODFOwG0v	MnG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc4Pzh2Lze+V2FPT0WUPD;hQi=>
NKM-1	Mnj2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?			M1zkXmlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOzZzOUSg{txONg>?	NHH0d\|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2Pzd5OESvK\|5USU6JRWK8M4E,
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CAL-72	MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?			M1fHSGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1NjJ{M{[2JO69VS5?	MmTKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc4Pzh2Lze+V2FPT0WUPD;hQi=>
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DBTRG-05MG	NH;EXnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=			MUfJcohq[mm2aX;uJI9nKGi3bXHuJGRDXFKJLUC1UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDRzLkS1OVYh\|ryPLh?=	Ml:yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc4Pzh2Lze+V2FPT0WUPD;hQi=>
MKN28	NF3DW3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?=			MX\Jcohq[mm2aX;uJI9nKGi3bXHuJG1MVjJ6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTC0NU42PTl6IN88UU4>	NVzReFJmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd5N{i0M{c,W0GQR1XSQE9iRg>?
U031	NYXidZVMT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=			NH36WJNKdmirYnn0bY9vKG:oIHj1cYFvKFVyM{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ{NjB5OUOg{txONg>?	NF\DPWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2Pzd5OESvK\|5USU6JRWK8M4E,
HT	NEnKb2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?=			MUPJcohq[mm2aX;uJI9nKGi3bXHuJGhVKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB2Mz6xOFIh\|ryPLh?=	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O\|c4QDRxJ{7TRW5ITVJ:L3G+
HCC1419	M4LrPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7			NV7ESFdUUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxOFE6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB2Mz60NFA4KM7:TT6=	NHG1T4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2Pzd5OESvK\|5USU6JRWK8M4E,
NCI-H1650	NGXjbHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=			NFXFfm1KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxKD1iNESuPFUzPSEQvF2u	MlPzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc4Pzh2Lze+V2FPT0WUPD;hQi=>
ESS-1	MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?			MVXJcohq[mm2aX;uJI9nKGi3bXHuJGVUWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTC0OU4xOzZ3IN88UU4>	Ml64QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc4Pzh2Lze+V2FPT0WUPD;hQi=>
NCI-H661	MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?			NGLWZY9KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOlYyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB2NT6zOVch\|ryPLh?=	NVrMXJNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd5N{i0M{c,W0GQR1XSQE9iRg>?
NCI-H2052	M1L4[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7			NGGwNWVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA2OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxKD1iNE[uOFYzQSEQvF2u	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O\|c4QDRxJ{7TRW5ITVJ:L3G+
SK-MEL-24	M4nuNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7			NGDsPZNKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxKD1iNEeuOVUyPyEQvF2u	NVLpfJl6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd5N{i0M{c,W0GQR1XSQE9iRg>?
KYSE-520	M1P0VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7			MXjJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvNUKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1QS5zM{WzJO69VS5?	MnjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc4Pzh2Lze+V2FPT0WUPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-p38 / p38 / p-JNK / JNK / gD-2 ; PubMed: 28112176 Acta Pharmacol Sin BX-795 inhibition on HSV replication attenuated by overexpression of p38/JNK. HeLa cells with or without JNK1 or p38 overexpression were infected with HSV-2 and total cellular protein was prepared for WB analysis. gD-2, the phosphorylation level of p38 MA䲧疝Ỵ疞㧀疜膉痘瘿뙠ෆᾰƌෆĀ㺣痖帉痖Ѐ瑖堘 pTBK1 / TBK1 / pPLK1 / PLK1; PubMed: 26772203 Mol Cancer Ther TBK1 mediated activation of the mitotic kinase PLK1. SW210.5 cells were treated with indicated TBK1 inhibitors for 1 hour and then exposed to 50 ng/mL of nocodazole for 18 hours. Western blot detected the signaling change using indicated antibodies, and β䲧疝Ỵ疞㧀疜膉痘瘿⟸෕ᾰƌ෕Ð㺣痖帉痖Ѐ	28112176 26772203
Growth inhibition assay	Cell viability ; PubMed: 26772203 Mol Cancer Ther Four SCLC cell lines with no MYC amplification were treated with TBK1 inhibitor BX-795 at the titration concentration. Cell viability was performed by CellTiter Glo 4 days after treatment. The growth curve was constructed by GraphPad Prism 6.	26772203

Protocol

Kinase Assay:^[1]	- Collapse Kinase assays: PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μl of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager.
Cell Research:^[1]	- Collapse Cell lines: MDA-468, PC-3, HCT-116 and MiaPaca cells Concentrations: ~10 μM Incubation Time: 72 hours Method: Cells seeded at a low density (1,500–3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average ± S.E. of two or more replicates. (Only for Reference)

Kinase Assay:^[1]

- Collapse

Kinase assays:

PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μl of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager.

Cell Research:^[1]

- Collapse

Cell lines: MDA-468, PC-3, HCT-116 and MiaPaca cells
Concentrations: ~10 μM
Incubation Time: 72 hours
Method: Cells seeded at a low density (1,500–3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average ± S.E. of two or more replicates.
(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	100 mg/mL (169.07 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG +2% Tween 80+ddH2O For best results, use promptly after mixing.	4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download BX-795 SDF

Molecular Weight	591.47
Formula	C₂₃H₂₆IN₇O₂S
CAS No.	702675-74-9
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I

In vivo Formulation Calculator (Clear solution)

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

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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

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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.

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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).

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

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The Serial Dilution Calculator Equation

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Computed Result

C1=C0/X	C1:	LOG(C1):
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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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Molarity Calculator

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

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Can you suggest an in vivo formulation of S1274 for animal studies?
Answer:
We recommend to use the vehicle 2% DMSO+30% PEG +2% Tween 80+ddH2O for in vivo study.

PDK Signaling Pathway Map

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BX-795