PF-4708671

For research use only. Not for use in humans.

Pfizer辉瑞授权生产 目录号：S2163

PF-4708671 Chemical Structure

CAS No. 1255517-76-0

PF-4708671是一种细胞渗透性p70 ribosomal S6 kinase(S6K1亚型)抑制剂，在无细胞试验中Ki/IC50为20 nM/160 nM，作用于S6K1比作用于S6K2选择性高400倍，作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上，是第一个报道的S6K1特异性抑制剂。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1574.66 现货
RMB 876.33 现货
RMB 1179.06 现货
RMB 2197.72 现货
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客户使用Selleck生产的PF-4708671发表文献34篇：

产品安全说明书

S6 Kinase抑制剂选择性比较

生物活性

产品描述 PF-4708671是一种细胞渗透性p70 ribosomal S6 kinase(S6K1亚型)抑制剂，在无细胞试验中Ki/IC50为20 nM/160 nM，作用于S6K1比作用于S6K2选择性高400倍，作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上，是第一个报道的S6K1特异性抑制剂。
靶点
p70 S6K1 [1]
(Cell-free assay)
160 nM
体外研究

PF-4708671是一种哌嗪基嘧啶类似物，是第一个S6K1特异性抑制剂。PF-4708671不显著抑制紧密相关的S6K2亚型或一组其他AGC激酶 (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 或SGK1)的活性。PF-4708671抑制S6K1介导的响应IGF-1（胰岛素样生长因子1）的S6蛋白的磷酸化，对PMA-诱导的底物磷酸化没有作用效果，底物与RSK (p90核糖体S6激酶)和MSK（丝分裂原和应激活化蛋白激酶）激酶高度相关。PF-4708671诱导S6K1的T型环和疏水性基序磷酸化，这种作用依赖于mTORC1 (mTOR复合体1)。PF-4708671不影响mTORC1的活性。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BHT-101 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnRSFNbUUN3ME2wMlgzODJ2IN88US=> NHG1XWFUSU6JRWK=
UACC-893 M{DkTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVO2WpR5UUN3ME21MlE6QDh4IN88US=> MXXTRW5ITVJ?
A427 MmKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrMPFJ3UUN3ME21MlczPTZ5IN88US=> MVnTRW5ITVJ?
OCUB-M NVW3dldsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHCRWpKSzVyPU[uOlYyODJizszN MkPDV2FPT0WU
SW684 M3f2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HtNWlEPTB;Nz61NlI3QCEQvF2= M3XXNnNCVkeHUh?=
SK-LMS-1 MoK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPab|lUUUN3ME25MlAyOzB{IN88US=> M1WzdnNCVkeHUh?=
CP50-MEL-B NV\Nb|RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XNW2lEPTB;OT6zNFQyQSEQvF2= M3fVUHNCVkeHUh?=
NCI-H1651 NVLWUpVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjjTWM2OD1zMD6wNlc3KM7:TR?= NUTmZlk2W0GQR1XS
ABC-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFyLkGwN|ch|ryP NFm5RXVUSU6JRWK=
OE19 M33LN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFyLkG3N|Mh|ryP MnXqV2FPT0WU
DSH1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe1PWhKSzVyPUGwMlg5PzlizszN M3n4NnNCVkeHUh?=
SW13 NFHiXYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkW1TWM2OD1zMT65N|E6KM7:TR?= NYXSUVgxW0GQR1XS
MDA-MB-453 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLMTWM2OD1zMj6xOlA{KM7:TR?= MVnTRW5ITVJ?
647-V MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHFeIs4UUN3ME2xNk4{PTh{IN88US=> NFy4OXpUSU6JRWK=
NCI-H2342 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLYb2RrUUN3ME2xNk4{QTl3IN88US=> NEHmeVNUSU6JRWK=
LB2241-RCC NUPFeXNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF{LkW3O|kh|ryP NWXSNpppW0GQR1XS
UACC-257 MlvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTkeIx1UUN3ME2xN{41PDV|IN88US=> NETWbphUSU6JRWK=
NCI-H661 M{PZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVH0enQ2UUN3ME2xN{43PDR7IN88US=> NIq1WW9USU6JRWK=
FADU NX3TOWNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmraTWM2OD1zMz62PVkzKM7:TR?= NX7tdWgxW0GQR1XS
A2780 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rabWlEPTB;MUOuPFA1OSEQvF2= MnfIV2FPT0WU
NCI-H1793 NEnNU3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mly0TWM2OD1zND60NFg2KM7:TR?= NU[yWZB7W0GQR1XS
TE-8 M1nqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEW0WWFKSzVyPUG1MlM1PjVizszN MXHTRW5ITVJ?
HGC-27 NYK5UlUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX6cpBvUUN3ME2xOk4yPjR2IN88US=> NHXNe2JUSU6JRWK=
MMAC-SF M1vDOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTF5LkO3Nlch|ryP MmPHV2FPT0WU
Calu-6 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXXTWM2OD1zOD6xOVE{KM7:TR?= NXjvXmtmW0GQR1XS
HUTU-80 MnnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTF6LkO5OVkh|ryP MWnTRW5ITVJ?
SAS NXrqXIJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\WR2lEPTB;MUiuOlQ2PSEQvF2= MljPV2FPT0WU
IST-MES1 M3\0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF6Lk[1NFgh|ryP M4joXXNCVkeHUh?=
C3A MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDkb4JKSzVyPUG4Mlc6OTlizszN MXPTRW5ITVJ?
ES3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTF6LkizOlQh|ryP MnzQV2FPT0WU
HSC-2 M4HrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O5PGlEPTB;MUmuOlU1OSEQvF2= MoTkV2FPT0WU
T47D Mmm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfzTWZKSzVyPUKwMlE1QDVizszN M{P6XHNCVkeHUh?=
EW-7 NV7kS|lYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJyLki1PFgh|ryP M1:0[nNCVkeHUh?=
LN-405 NUn4NpE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\ETIwxUUN3ME2yNE45QTZ3IN88US=> MWrTRW5ITVJ?
U031 NXuzTmFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37GUWlEPTB;MkGuOFgxOiEQvF2= NY\IbnZ4W0GQR1XS
A549 NWrveHlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu2TWM2OD1{MT64OFkyKM7:TR?= NXSxeZdwW0GQR1XS
RMG-I Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIO3WZNKSzVyPUKyMlI3PjhizszN NYi0bJozW0GQR1XS
BT-474 M2C3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDTcHltUUN3ME2yNk43PTVzIN88US=> NES5bGJUSU6JRWK=
NB69 NFvEO3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTJ|LkG1NkDPxE1? NHj1TYZUSU6JRWK=
NB7 NHHsWVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37Bb2lEPTB;MkSuNVg5KM7:TR?= Mk\3V2FPT0WU
HCC1569 NYnlclg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXSwNWtFUUN3ME2yOE43OTJ3IN88US=> NFvtOmJUSU6JRWK=
MEL-JUSO MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHOOFJ1UUN3ME2yOE43QTB6IN88US=> MoLTV2FPT0WU
MDA-MB-175-VII M2\YbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O1OWlEPTB;MkWuNlUyPyEQvF2= MoH0V2FPT0WU
HCC1419 NH22XlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknDTWM2OD1{NT62NFA{KM7:TR?= NYXJWXNYW0GQR1XS
Ca9-22 M371Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHUNWdKSzVyPUK1MlY1OzJizszN NXnaU2R[W0GQR1XS
KGN MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jYZmlEPTB;MkWuO|U1PyEQvF2= MXTTRW5ITVJ?
LB373-MEL-D MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHG[oFKSzVyPUK2MlE6OzhizszN NYHvTVlrW0GQR1XS
NCI-H1755 NXLWbm1lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;ieI9KSzVyPUK2Mlg5PDFizszN NFXnZ2hUSU6JRWK=
D-423MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:yTWM2OD1{Nz6wO|E2KM7:TR?= Mn7TV2FPT0WU
DK-MG M{SzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJ6Lke4OFYh|ryP Mm\lV2FPT0WU
NCI-H1623 NXfaNpVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;wSlhLUUN3ME2yPE45OzR{IN88US=> NVu2TVI1W0GQR1XS
KU-19-19 NH2xZ45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;LT4RKSzVyPUK4Mlk6PSEQvF2= MWjTRW5ITVJ?
C-33-A MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfvZW5MUUN3ME2yPU4zOTl6IN88US=> M{TO[nNCVkeHUh?=
SCC-4 NFT1fopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\QbpNyUUN3ME2zNE4{OzV2IN88US=> MV;TRW5ITVJ?
MG-63 MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfXdG4xUUN3ME2zNE42QTl2IN88US=> NWPSeYt4W0GQR1XS
LNCaP-Clone-FGC MnLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDEb2dsUUN3ME2zNU41QTJzIN88US=> MWPTRW5ITVJ?
CAPAN-1 NWHkVog2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\iTWM2OD1|MT61Nlg3KM7:TR?= NULYV5FWW0GQR1XS
GI-ME-N NIW0b2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnn5TWM2OD1|MT61N|U{KM7:TR?= Mkj0V2FPT0WU
RERF-LC-MS NXr2fYRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHFb2RKSzVyPUOyMlY4PDdizszN MmTpV2FPT0WU
KLE MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2S5S2lEPTB;M{OuOFM{PCEQvF2= NIn5WHFUSU6JRWK=
KNS-81-FD NXTmUIJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTN|LkWwNFgh|ryP M{\s[HNCVkeHUh?=
DOK NE\hb5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nwdWlEPTB;M{SuOlYyOiEQvF2= NF3QOY1USU6JRWK=
ACHN NF6zXVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK2dmJKSzVyPUO1MlE2QDhizszN NGPkXGxUSU6JRWK=
KYSE-520 NHr6[GtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XFOGlEPTB;M{WuNlM3OSEQvF2= Mlv0V2FPT0WU
SBC-5 NHe4dIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTN3LkWxNVYh|ryP MVHTRW5ITVJ?
NCI-H28 NUi4V2dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnKNoZKSzVyPUO1MlY3QTVizszN MUXTRW5ITVJ?
ES7 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUK4T5hYUUN3ME2zOk4zOjR7IN88US=> NXHrW4pEW0GQR1XS
A172 MmniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHOyZm9KSzVyPUO2MlQyQDdizszN MnTnV2FPT0WU
UM-UC-3 NYCxc404T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XCRWlEPTB;M{euPFc1PiEQvF2= NXXIO|gyW0GQR1XS
LXF-289 M2XSeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3SyU2lEPTB;M{iuNFA1PyEQvF2= NYfMUGkyW0GQR1XS
KP-4 NGHzRnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vzV2lEPTB;M{iuOFc{QSEQvF2= NGX0O29USU6JRWK=
TE-1 Mor3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfJZpNsUUN3ME2zPU43PTh7IN88US=> MXXTRW5ITVJ?
G-402 Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TuTWlEPTB;NECuNFYyKM7:TR?= NVLIZWJlW0GQR1XS
786-0 MnnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPQTWM2OD12MD65NFk3KM7:TR?= NFzEZ3FUSU6JRWK=
K5 M1LTZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWT6[2RJUUN3ME20NU4{Pjh4IN88US=> NVHxR2k5W0GQR1XS
SK-N-DZ NGXuZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTHTWM2OD12MT6zPFI{KM7:TR?= M2PRb3NCVkeHUh?=
OVCAR-4 M163O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTRzLke1Olgh|ryP NWLVdlBqW0GQR1XS
T84 NWC3V4J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\USFhKSzVyPUSyMlEzPjNizszN MmDPV2FPT0WU
GCIY MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTR|LkC4NFMh|ryP M1q1[nNCVkeHUh?=
BB49-HNC M2nOZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7xNJZPUUN3ME20N{4{OzR6IN88US=> NFvmbphUSU6JRWK=
SNU-C2B NFnNeWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojNTWM2OD12Mz62OFM3KM7:TR?= MXnTRW5ITVJ?
TE-6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjvSYhUUUN3ME20N{45QDl2IN88US=> M3vyR3NCVkeHUh?=
23132-87 NGr1S2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTR2LkK5O|gh|ryP MYXTRW5ITVJ?
DMS-53 MoCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTR2LkOzPFQh|ryP MmfBV2FPT0WU
ONS-76 NWLnfJFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M122S2lEPTB;NESuO|Y3OSEQvF2= MXvTRW5ITVJ?
DMS-273 NWHZ[GpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTR2Lkm0N{DPxE1? MXnTRW5ITVJ?
COLO-824 M1TVcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHTfINKSzVyPUS1Mlg4PzVizszN MWXTRW5ITVJ?
DMS-114 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnToTWM2OD12NT64PVI4KM7:TR?= M1zX[nNCVkeHUh?=
YKG-1 NYLGU3hYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nVNmlEPTB;NE[uNFM2PSEQvF2= M1zmR3NCVkeHUh?=
RH-18 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTR4LkO3N|Mh|ryP NEHiRYZUSU6JRWK=
NCI-H1355 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S0VGlEPTB;NE[uOlE5KM7:TR?= MYHTRW5ITVJ?
NCI-H2170 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDoTWM2OD12Nz63OVg1KM7:TR?= M3mxeXNCVkeHUh?=
OC-314 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLEe5NKSzVyPUS3Mlg1PzhizszN MoS2V2FPT0WU
NCI-H2030 M2rU[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPpVFlKSzVyPUS3Mlg6ODZizszN M{HHcnNCVkeHUh?=
22RV1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\ETWM2OD12Nz65NFE2KM7:TR?= MmXjV2FPT0WU
G-401 NIO3U3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn60TWM2OD12OD60OFE2KM7:TR?= MmPGV2FPT0WU
YAPC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW4ZVVKSzVyPUS5MlgxPzNizszN MVLTRW5ITVJ?
SW1573 Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTVyLkK0N|Uh|ryP NWW0enJwW0GQR1XS
COLO-792 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfFNGNCUUN3ME21NE43OjN5IN88US=> MoroV2FPT0WU
KNS-62 NIKyS|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f5XWlEPTB;NUCuO|UxQCEQvF2= NHrYUphUSU6JRWK=
NB5 NFHTSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTVzLkS1NFkh|ryP NXXaN5BiW0GQR1XS
CP66-MEL Ml3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fpUGlEPTB;NUGuOlQxQCEQvF2= M1vJUHNCVkeHUh?=
CaR-1 NIjuPZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPLTWM2OD13Mj6wOlA3KM7:TR?= MVPTRW5ITVJ?
CAL-54 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTV{LkGxNFIh|ryP MmrEV2FPT0WU
8305C MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mni0TWM2OD13Mj6zNVUh|ryP MU\TRW5ITVJ?
Calu-3 MoiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHVTWM2OD13Mj6zO|M{KM7:TR?= NXv6bJNCW0GQR1XS
AU565 NVr5fYpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;n[m9pUUN3ME21Nk42PTB7IN88US=> M3nNRXNCVkeHUh?=
CW-2 NFjibZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrkU5hKSzVyPUWyMlg3PTRizszN MYjTRW5ITVJ?
BEN MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTsbZgyUUN3ME21N{44QDZ{IN88US=> MYrTRW5ITVJ?
NCI-H1975 NWjPZ4dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXIR5lKSzVyPUWzMlg6PjZizszN MXLTRW5ITVJ?
HCT-116 NUP2bJNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHCXIZKSzVyPUW0MlA{OjdizszN NUL0Nmp7W0GQR1XS
SH-4 NWDlc4tZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzGTWM2OD13ND6xN|gh|ryP M1GyZ3NCVkeHUh?=
NCI-H1693 NIXseHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vabWlEPTB;NUSuNlExOyEQvF2= MUDTRW5ITVJ?
BPH-1 M17oOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTV3LkK4PVIh|ryP NH\lcWZUSU6JRWK=
CAMA-1 M2C5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHVVJkyUUN3ME21OU45OTF4IN88US=> MYXTRW5ITVJ?
A388 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrLWpRbUUN3ME21Ok4xQTh3IN88US=> MXrTRW5ITVJ?
C2BBe1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rqN2lEPTB;NU[uNlY{PCEQvF2= M3[zcHNCVkeHUh?=
GAMG MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT1TWM2OD13Nj61PVU2KM7:TR?= Mlq0V2FPT0WU
MKN28 M4\6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mln4TWM2OD13Nj64NFE{KM7:TR?= MkG1V2FPT0WU
VA-ES-BJ NV;acHFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjwUoVKSzVyPUW2Mlg4PDVizszN Ml;6V2FPT0WU
HuCCT1 M{f6NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILudm1KSzVyPUW3MlA1QTJizszN NEDS[VRUSU6JRWK=
BFTC-905 NYOyUpd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj3R2lmUUN3ME21O{4zQDl6IN88US=> MorvV2FPT0WU
LS-123 M3zmUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLFZWtKSzVyPUW3MlU3PjhizszN MmSwV2FPT0WU
LB996-RCC NUnqVllXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjjTWM2OD13OD6wNlg4KM7:TR?= MlruV2FPT0WU
NCI-H1048 M{nqdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XYcmlEPTB;NUiuNlE5QCEQvF2= NILIXGFUSU6JRWK=
COR-L105 M2PkZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX6xS3dxUUN3ME21PE44OzN5IN88US=> Mmq4V2FPT0WU
OVCAR-8 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP3clV[UUN3ME21PU4yPzF4IN88US=> NI\UV3lUSU6JRWK=
SK-N-FI NIq0UpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vZTGlEPTB;NUmuN|IxPyEQvF2= NXPPdHp6W0GQR1XS
MES-SA MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vvOGlEPTB;NUmuOFUxQSEQvF2= MVHTRW5ITVJ?
SCC-9 M{[xSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{K3[2lEPTB;NUmuOFc2OyEQvF2= NGTIZ5RUSU6JRWK=
EFO-27 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDhTWM2OD13OT65OFMh|ryP NWnkNHQzW0GQR1XS
GT3TKB MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTZyLk[wOFgh|ryP NWjUOXRbW0GQR1XS
HCC38 NWfSTFVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzSOFMxUUN3ME22NU41Ozd7IN88US=> MljMV2FPT0WU
MLMA M4jKSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofuTWM2OD14MT62NVY{KM7:TR?= MlLiV2FPT0WU
D-566MG NFHySWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzVTWM2OD14Mz61NlI1KM7:TR?= NIXzcI5USU6JRWK=
SF295 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTZ|Lk[2OVUh|ryP MnfXV2FPT0WU
ES4 M13ISGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTZ2LkS3NVkh|ryP MkPSV2FPT0WU
CAKI-1 NILwb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTZ2LkW3NlEh|ryP M131bHNCVkeHUh?=
OAW-28 NHT2TI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M371TmlEPTB;NkSuPVY1PyEQvF2= NXfGWoF[W0GQR1XS
NCI-H460 MofpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r5d2lEPTB;NkWuNFg6PyEQvF2= M4X6[3NCVkeHUh?=
JAR M2TTV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrLTWM2OD14NT61OVE3KM7:TR?= Ml\oV2FPT0WU
SNU-449 NYTIVHFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTZ3Lke2NVYh|ryP M2LDTHNCVkeHUh?=
D-392MG M{mxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTZ3Lkm0N|Qh|ryP M4fFTHNCVkeHUh?=
EW-22 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIm2WoNKSzVyPU[2MlM6PSEQvF2= MVnTRW5ITVJ?
GCT M1TUNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP4Z4FKSzVyPU[3MlA1PDNizszN NFqwO2JUSU6JRWK=
NOS-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHwTWM2OD14Nz62PFY4KM7:TR?= MkPxV2FPT0WU
RH-1 MnvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYe4Z3dCUUN3ME22PE42PTV7IN88US=> M2ezd3NCVkeHUh?=
HuH-7 NWLROWRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT5eoxKSzVyPU[5MlExODJizszN Mnv4V2FPT0WU
NUGC-3 NXqweHFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfQS|JKSzVyPUewMlk3PDRizszN MYfTRW5ITVJ?
IST-SL1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvpSpVKSzVyPUexMlI{OjRizszN M1\RXHNCVkeHUh?=
SHP-77 NXrlVWF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HFd2lEPTB;N{KuNVE6KM7:TR?= M1P6WXNCVkeHUh?=
SW1116 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHLTWM2OD15Mj6xOFA4KM7:TR?= NVjOVoNNW0GQR1XS
LK-2 NHTSV2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTd{Lki2NVIh|ryP M{H5NHNCVkeHUh?=
U-2-OS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PwVGlEPTB;N{OuNVgzQCEQvF2= MWDTRW5ITVJ?
KYSE-150 M4TNPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTd|Lk[xNVgh|ryP NHLIZ2VUSU6JRWK=
U251 M{XQTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\hSmlEPTB;N{OuPFE3QCEQvF2= M2nE[HNCVkeHUh?=
HT-1080 NUjrVmZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH1SopKSzVyPUe0MlI2PzRizszN NELrb5RUSU6JRWK=
NCI-H1437 M{P5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvKZYlHUUN3ME23OE43OzJ4IN88US=> Ml7OV2FPT0WU
HPAF-II MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPpblJKSzVyPUe0MlY1OTVizszN MV;TRW5ITVJ?
Becker MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL5XZEyUUN3ME23OU4yOTB3IN88US=> MmfxV2FPT0WU
PANC-10-05 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV6zRXlZUUN3ME23OU4zQDZ3IN88US=> MX7TRW5ITVJ?
TYK-nu NHPDNnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjXTWM2OD15NT6zNVAzKM7:TR?= M4\tN3NCVkeHUh?=
SKG-IIIa NEDBe3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUn3NY03UUN3ME23OU4{OzRzIN88US=> Mm\RV2FPT0WU
NCI-H1993 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DyeGlEPTB;N{WuO|M6PyEQvF2= NXO2d4RTW0GQR1XS
S-117 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoD0TWM2OD15NT63OVUh|ryP M1fnU3NCVkeHUh?=
HuO9 MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXFTWM2OD15Nj6wNFQ5KM7:TR?= M2XqZ3NCVkeHUh?=
CAL-51 M1PMemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYi4UlBzUUN3ME23Ok4yODB4IN88US=> NW\zWpdyW0GQR1XS
BT-20 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLmTWM2OD15Nj6yNVY5KM7:TR?= MYnTRW5ITVJ?
LB831-BLC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnPdYRqUUN3ME23Ok4{OjF5IN88US=> NEnmW3pUSU6JRWK=
LB1047-RCC MkDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPhTWM2OD15Nj63OlE6KM7:TR?= M2njeXNCVkeHUh?=
ES8 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGm0VWJKSzVyPUe4MlAxPzNizszN NEn3WFZUSU6JRWK=
UMC-11 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFq1TJBKSzVyPUe4MlA5QDRizszN MkLrV2FPT0WU
NCI-H226 NIHMeWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLBRWdDUUN3ME23PE4yOzF3IN88US=> MYnTRW5ITVJ?
IGROV-1 MnvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzyTWM2OD15OD61OVUh|ryP NFnnZVFUSU6JRWK=
BHY M1TrcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4eweWlEPTB;N{muOVk3KM7:TR?= Mm\sV2FPT0WU
MKN45 MkjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnexTWM2OD16MD6zNVc1KM7:TR?= Mlz1V2FPT0WU
IA-LM MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRThyLkO1NVEh|ryP M4DkUnNCVkeHUh?=
WM-115 M2DOXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL6RZpKSzVyPUixMlQyOTRizszN MoPIV2FPT0WU
VMRC-RCZ MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL5e3pKSzVyPUixMlQ1OjVizszN NUL5SnRbW0GQR1XS
NCI-H2291 NIDk[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\i[oJKSzVyPUixMlY5PDJizszN MnPMV2FPT0WU
MCF7 NY\G[XhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DpSWlEPTB;OEOuNlg6PyEQvF2= MXPTRW5ITVJ?
639-V NH6ybGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z4OWlEPTB;OESuOlEzQSEQvF2= M2Xne3NCVkeHUh?=
RT4 MmnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTh3LkK0NFMh|ryP MWLTRW5ITVJ?
NCI-H2405 NFTkdGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXKyS4E2UUN3ME24OU4zQTl5IN88US=> NVjnWGJ3W0GQR1XS
CAL-33 MmPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fGR2lEPTB;OEWuOlMyPSEQvF2= MkTrV2FPT0WU
BT-549 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXvRodKSzVyPUi1Mlk{QDJizszN MVrTRW5ITVJ?
HT-1197 NHLZPWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETod5ZKSzVyPUi4MlExPzdizszN NGHVNGpUSU6JRWK=
G-361 M2T2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTh6LkG0O|Qh|ryP NYfPOXB2W0GQR1XS
LS-411N M{HRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz5TWM2OD16OT6zN|g5KM7:TR?= MYHTRW5ITVJ?
HT-144 MofZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPwWZE5UUN3ME24PU42QTl{IN88US=> NXOwO2dVW0GQR1XS
DJM-1 NUDIcWpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTh7Lki4OFUh|ryP NETzS2JUSU6JRWK=
CAL-12T Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTlyLke4PVUh|ryP MkLNV2FPT0WU
MKN7 NFPqe|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPXXnNQUUN3ME25NU4{PTVzIN88US=> M1LK[HNCVkeHUh?=
HuP-T3 NITnTpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO1TWM2OD17Nj6xNFA1KM7:TR?= MV\TRW5ITVJ?
SK-MG-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlH1TWM2OD17Nj6xN|Q5KM7:TR?= MlXHV2FPT0WU
NCI-H2347 NF7XW2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTl6LkGwOFIh|ryP MUfTRW5ITVJ?
SW872 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4noS2lEPTB;MUCwMlQ2PiEQvF2= NI\YRpFUSU6JRWK=
COLO-829 NXHPOXpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvuU5gyUUN3ME2xNFAvPTV|IN88US=> Mm\4V2FPT0WU
MC-IXC Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlP1TWM2OD1zMECuOlE2KM7:TR?= NUjMN5FHW0GQR1XS

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pS6 / S6 / pS6K / S6K1 / pAKT / AKT ; 

PubMed: 28626016     


Western blot of cell lysates from neurons treated with PF-4708671, rapamycin, and Torin-2, individually or in combination for the indicated times.

p-mTOR / mTOR / p-p70S6K / p70S6K ; 

PubMed: 30423811     


As determined using Western blotting, the phospho-p70S6K (p-p70S6K) inhibitor (PF-4708671) reduced the expression of phospho-mTOR (p-mTOR) and p-p70S6K in SCC-4 and SCC-25 cells. SCC-4 and SCC-25 cells were not treated as negative control (NC) or treated with 20 µM PF-4708671 for 6 h (6 h), 12 h (12 h), 18 h (18 h), 1 day (1 d), 2 days (2 d), and 3 days (3 d). Western blot analysis was performed to examine the expression levels of p-mTOR, mTOR, p-p70S6K, p70S6K, and β-actin.

28626016 30423811
Growth inhibition assay
Cell viability; 

PubMed: 30423811     


Inhibitory effects of various doses (0.5, 1, 2, 5, 10, 20, and 40 µM) of PF-4708671 on SCC-4 (B) and SCC-25 (C) cells were assessed using MTT assay after 72 h of treatment. Data presented are the mean and standard error of the mean of three independent experiments. * p < 0.05, ** p < 0.01, and *** p < 0.001 indicate the statistical significance of differences between cells with and without treatment. t (red ** and *** for SCC-4 and blue *, ** and *** for SCC-25).

30423811

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 30 mg/mL (76.84 mM)
Ethanol 8 mg/mL (20.49 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
30% PEG400+0.5% Tween80+5% propylene glycol
 30 mg/mL

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

化学数据

分子量 390.41
化学式

C19H21F3N6
CAS号 1255517-76-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

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

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

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

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

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

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

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

    Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for S2163 is suitable for i.p. or not?

  • 回答：

    The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one. It is a suspension.

Selleck产品目录册

S6 Kinase Signaling Pathway Map

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    LY2584702 Tosylate是一种选择性的，ATP竞争性p70S6K抑制剂，IC50为 4 nM。Phase 1。

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂， IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性，对GSK-3β的选择性是对CDKs选择性的350倍。CHIR-99021 可作为Wnt/β-catenin的激活剂并诱导自噬。

  • BI-D1870

    BI-D1870是一种ATP-竞争性S6 ribosome抑制剂，在无细胞试验中作用于RSK1/2/3/K4，IC50分别为31 nM/24 nM/18 nM/15 nM，作用于RSK比作用于MST2，GSK-3β，MARK3，CK1和Aurora B选择性高10到100倍。BI-D1870 显示除了抗癌的属性包括活性氧的生成、提高内质网应激反应和诱导自噬。

  • Rapamycin (AY-22989)

    Rapamycin (AY-22989, Rapamune, Sirolimus, NSC-2260804)是一种特定的 mTOR 抑制剂，在 HEK293细胞中，IC50 为 ~0.1 nM。

  • MK-2206 2HCl

    MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，在无细胞试验中IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。MK-2206 2HCl 在肿瘤细胞中可诱导自噬和凋亡。Phase 2。

    Features:MK-2206是第一个进入临床研究阶段的Akt小分子变构抑制剂。

  • CHIR-99021 (CT99021) HCl

    CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂，IC50为10 nM/6.7 nM。其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy，并可增强 GR，RORα和自噬相关蛋白等表达。

  • LY294002

    LY294002 (SF 1101, NSC 697286) 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。

    Features:LY294002是选择性的, 可渗透细胞的特定PI3K抑制剂，可作用于酶的ATP结合位点，且抑制自体吞噬的螯合作用。

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA, NSC 66389) 是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。3-Methyladenine (3-MA)可成功应用于抑制线粒体自噬。现配现用（加热助溶）。

  • Everolimus (RAD001)

    Everolimus (RAD001, SDZ-RAD)是一种mTOR抑制剂，作用于FKBP12，在无细胞试验中IC50为1.6-2.4 nM。Everolimus 可诱导细胞凋亡及自噬并抑制肿瘤细胞的增殖。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID