FAK
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S2672 | PF-00562271 Besylate | <1 mg/mL | 14 mg/mL | <1 mg/mL |
| S2890 | PF-562271 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2013 | PF-573228 | <1 mg/mL | 26 mg/mL | <1 mg/mL |
| S2820 | TAE226 (NVP-TAE226) | <1 mg/mL | 94 mg/mL | <1 mg/mL |
| S2725 | PF-03814735 | <1 mg/mL | 0.4 mg/mL | <1 mg/mL |
| S5321 | Y15 | 56 mg/mL | 56 mg/mL | <1 mg/mL |
| S7357 | PF-562271 HCl | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S8523 | GSK2256098 | <1 mg/mL | 82 mg/mL | 82 mg/mL |
| S7653 | PND-1186 (VS-4718) | <1 mg/mL | 24 mg/mL | <1 mg/mL |
| S7644 | PF-431396 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7654 | Defactinib (VS-6063, PF-04554878) | <1 mg/mL | 5 mg/mL | <1 mg/mL |
FAK製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2672 |
PF-00562271 BesylatePF-00562271 Besylate is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. |
|
|
| S2890 |
PF-562271PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
Effect of matrix stiffness on the susceptibility of primary HDFs to apoptosis induced by inhibition of mechanotransduction pathways. HDFs (primary human dermal fibroblasts) were cultured on collagen-coated polyacrylamide hydrogels that recapitulated the stiffness of normal (4 kPa) or densely fibrotic (50 kPa) skin for 24 hours and treated with or without the agents indicated for an additional 48 hours. Apoptosis was assessed by annexin V staining. Data are means ± SD from three independent experiments. P value was determined by Student’s t test.
|
|
| S2013 |
PF-573228PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. |
FAK inhibition blunted the increased migration induced by PGC1α depletion. G361 cells were subjected to 24 h transwell migration assays in the presence of DMSO or various doses of FAK inhibitor PF-573228. Images represent three pictures captured with scale bar representing 100 μm. |
|
| S2820 |
TAE226 (NVP-TAE226)TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. |
Targeting the actin cytoskeleton overcomes resistance to HDACi in primary MM. Graphs representing the proportion of cell death induced in MM patients (n=6) treated LBH589 (5 nM), TAE226 (0.5 uM) and combination. |
|
| S2725 |
PF-03814735PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1. |
(A) Immunoblot demonstrating the expression of phospho-FAK in parental (PAR) and mesenchymal (MES) HCC827 cells following exposure to dasatinib (50nM), PF-562271 (1μM), PF-562271 (1μM) and PF-0381473 for 2 and 24 hours.
|
|
| S5321新 |
Y15Y15 is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner. |
||
| S7357 |
PF-562271 HClPF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. |
NO production was increased in the netrin-1-over-expressing and recombinant netrin-1-treated MiaPaCa II cells. FAK inhibitor PF-562271 blocks the netrin-1-induced NO production. (*P < 0.05).
|
|
| S8523 |
GSK2256098GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. |
||
| S7653 |
PND-1186 (VS-4718)PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1. |
(a) Percentage of apoptotic HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 measured by Annexin V and flow cytometry. Values are plotted as mean±SD (*P<0.05; **P<0.01; versus Vehicle, n =3). (b) Representative WB for p21 and caspase-3 in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (0), 0.5 μM or 1 μM PND 1186. β-tubulin is reported as a loading control (n=2). (c) Relative mRNA expression of EZH2 and NOTCH2 genes as measured by qRT-PCR in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 (*P<0.05; **P<0.01; versus Vehicle, n =3). |
|
| S7644 |
PF-431396PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively. |
||
| S7654 |
Defactinib (VS-6063, PF-04554878)Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2. |
c, d MEL-JUSO cells were pre-treated with Defactinib (5 µM); e, f WM1205-LU cells were pre-treated with either inhibitor or a combination of both. Subsequently, cells were treated with trametinib (10 nM) and phosphorylation of key kinases, as well as cell viability were determined (48 h) using multiplex ELISA and resazurin reduction assay, respectively. Data show averaged median fluorescence intensity (MFI) for each protein (means ± S.D. from n = 3 independent experiments) and or cell viability relative to control values of 100% (means + S.E.M. from n = 3 independent experiments). Statistical analysis was performed using two-way ANOVA with post-hoc Tukey test
|
|
| S2360 |
Solanesol (Nonaisoprenol)Solanesol is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. It mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2672 |
PF-00562271 BesylatePF-00562271 Besylate is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. |
|
|
| S2890 |
PF-562271PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
Effect of matrix stiffness on the susceptibility of primary HDFs to apoptosis induced by inhibition of mechanotransduction pathways. HDFs (primary human dermal fibroblasts) were cultured on collagen-coated polyacrylamide hydrogels that recapitulated the stiffness of normal (4 kPa) or densely fibrotic (50 kPa) skin for 24 hours and treated with or without the agents indicated for an additional 48 hours. Apoptosis was assessed by annexin V staining. Data are means ± SD from three independent experiments. P value was determined by Student’s t test.
|
|
| S2013 |
PF-573228PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. |
FAK inhibition blunted the increased migration induced by PGC1α depletion. G361 cells were subjected to 24 h transwell migration assays in the presence of DMSO or various doses of FAK inhibitor PF-573228. Images represent three pictures captured with scale bar representing 100 μm. |
|
| S2820 |
TAE226 (NVP-TAE226)TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. |
Targeting the actin cytoskeleton overcomes resistance to HDACi in primary MM. Graphs representing the proportion of cell death induced in MM patients (n=6) treated LBH589 (5 nM), TAE226 (0.5 uM) and combination. |
|
| S2725 |
PF-03814735PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1. |
(A) Immunoblot demonstrating the expression of phospho-FAK in parental (PAR) and mesenchymal (MES) HCC827 cells following exposure to dasatinib (50nM), PF-562271 (1μM), PF-562271 (1μM) and PF-0381473 for 2 and 24 hours.
|
|
| S5321新 |
Y15Y15 is a small-molecule FAK scaffolding inhibitor that directly inhibits FAK autophosphorylation in a dose- and time-dependent manner. |
||
| S7357 |
PF-562271 HClPF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. |
NO production was increased in the netrin-1-over-expressing and recombinant netrin-1-treated MiaPaCa II cells. FAK inhibitor PF-562271 blocks the netrin-1-induced NO production. (*P < 0.05).
|
|
| S8523 |
GSK2256098GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. |
||
| S7653 |
PND-1186 (VS-4718)PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1. |
(a) Percentage of apoptotic HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 measured by Annexin V and flow cytometry. Values are plotted as mean±SD (*P<0.05; **P<0.01; versus Vehicle, n =3). (b) Representative WB for p21 and caspase-3 in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (0), 0.5 μM or 1 μM PND 1186. β-tubulin is reported as a loading control (n=2). (c) Relative mRNA expression of EZH2 and NOTCH2 genes as measured by qRT-PCR in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 (*P<0.05; **P<0.01; versus Vehicle, n =3). |
|
| S7644 |
PF-431396PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively. |
||
| S7654 |
Defactinib (VS-6063, PF-04554878)Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2. |
c, d MEL-JUSO cells were pre-treated with Defactinib (5 µM); e, f WM1205-LU cells were pre-treated with either inhibitor or a combination of both. Subsequently, cells were treated with trametinib (10 nM) and phosphorylation of key kinases, as well as cell viability were determined (48 h) using multiplex ELISA and resazurin reduction assay, respectively. Data show averaged median fluorescence intensity (MFI) for each protein (means ± S.D. from n = 3 independent experiments) and or cell viability relative to control values of 100% (means + S.E.M. from n = 3 independent experiments). Statistical analysis was performed using two-way ANOVA with post-hoc Tukey test
|
|
| S2360 |
Solanesol (Nonaisoprenol)Solanesol is a long-chain polyisoprenoid alcohol compound with inhibitory activities toward FAK. It mainly accumulates in solanaceous crops, including tobacco, tomato, potato, eggplant, and pepper plants. |
