阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S7270 | SRPIN340 | <1 mg/mL | 70 mg/mL | 70 mg/mL |
| S7209 | GSK650394 | <1 mg/mL | 76 mg/mL | <1 mg/mL |
| S6499 | PF-6260933 | <1 mg/mL | 59 mg/mL | 2 mg/mL |
| S8388 | ML-7 HCl | <1 mg/mL | 90 mg/mL | <1 mg/mL |
| S8465 | GSK'872 (GSK2399872A) | <1 mg/mL | 76 mg/mL | '''40 mg/mL |
| S8257 | CFI-402257 | ' mg/mL | ||
| S2642 | 1-Naphthyl PP1(1-NA-PP1) | <1 mg/mL | 9 mg/mL | <1 mg/mL |
| S6710 | SGC-GAK-1 | <1 mg/mL | 78 mg/mL | 39 mg/mL |
| S8864 | ZT-12-037-01 | <1 mg/mL | 41 mg/mL | 3 mg/mL |
| S8872 | GSK8612 | <1 mg/mL | 100 mg/mL | 6 mg/mL |
| S8215 | BAY 1217389 | <1 mg/mL | 100 mg/mL | 3 mg/mL |
| S5792 | CID 2011756 | <1 mg/mL | 30 mg/mL | <1 mg/mL |
| S4956 | Benzamidine HCl | 31 mg/mL | 31 mg/mL | 31 mg/mL |
| S8810 | SPHINX31 | <1 mg/mL | 25 mg/mL | 13 mg/mL |
| S8775 | HS-1371 | <1 mg/mL | 13 mg/mL | 4 mg/mL |
| S8366 | CRT0066101 | 82 mg/mL | 25 mg/mL | 2 mg/mL |
| S6088 | 6-(Dimethylamino)purine | -1 mg/mL | 32 mg/mL | -1 mg/mL |
| S8358 | WNK463 | <1 mg/mL | 92 mg/mL | 92 mg/mL |
| S7188 | CID755673 | <1 mg/mL | 43 mg/mL | <1 mg/mL |
Serine/threonin kinase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 |
|---|---|---|---|
| S7270 |
SRPIN340SRPIN340 is a selective SRPK inhibitor with Ki of 0.89 μM for SRPK1, showing no significant inhibitory activity against more than 140 other kinases.. |
Crystal violet staining of the indicated cell lines treated with SRPIN340 at the indicated concentrations.
|
|
| S7209 |
GSK650394GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively. |
BV-2 cells were incubated in the absence or presence of gsk650394 (1 μM) for 30 min, followed by LPS (500 ng/ml) administration for 30 min, and then fixed. NF-κB p65 protein was visualized by indirect immunofluorescence staining using an antibody for NF-κB p65. For nuclear staining, the cells were stained with DAPI. Bar = 20 μm.
|
|
| S6499新 |
PF-6260933PF-6260933 is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity. |
||
| S8388 |
ML-7 HClML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. |
Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
|
|
| S8465 |
GSK'872 (GSK2399872A)GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity. |
(H-K) Cells incubated in the absence or presence of GSK’872, and treated with PM (100 μg/ml) for 24 h. The relative levels of IL6 (H), and IL8 (J) mRNA transcripts were measured by quantitative RT-PCR, and the protein levels of IL6 (I) and IL8 (K) in the culture supernatants, which are in turn were measured by ELISA.
|
|
| S8257新 |
CFI-402257CFI-402257 is a potent highly selective, and orally active small-molecule inhibitor of Mps1 with Ki value of 0.09 ± 0.02 nM. |
||
| S2642新 |
1-Naphthyl PP1(1-NA-PP1)1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
||
| S6710新 |
SGC-GAK-1SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase. |
||
| S8864新 |
ZT-12-037-01ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM. |
||
| S8872新 |
GSK8612GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified. |
||
| S8215 |
BAY 1217389BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1) with IC50 values below 10 nmol/L while showing an excellent selectivity profile. |
||
| S5792 |
CID 2011756CID 2011756 is an inhibitor of protein kinase D (PKD) with IC50 values of 3.2, 0.6, and 0.7 μM for PKD1, PKD2, and PKD3, respectively. |
||
| S4956 |
Benzamidine HClBenzamidine is an inhibitor of serine proteases with Ki values of 35, 350, and 220 µM for trypsin, plasmin, and thrombin, respectively. |
||
| S8810 |
SPHINX31SPHINX31 is a SRPK1 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold). |
||
| S8775 |
HS-1371HS-1371 is a potent RIP3 kinase inhibitor with an IC50 of 20.8 nM. It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro. |
||
| S8366 |
CRT0066101CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple. |
||
| S6088 |
6-(Dimethylamino)purine6-Dimethylaminopurine is a serine threonine protein kinase inhibitor. It inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes. |
||
| S8358 |
WNK463WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4). |
||
| S7188 |
CID755673CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs. |
| 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 |
|---|---|---|---|
| S7270 |
SRPIN340SRPIN340 is a selective SRPK inhibitor with Ki of 0.89 μM for SRPK1, showing no significant inhibitory activity against more than 140 other kinases.. |
Crystal violet staining of the indicated cell lines treated with SRPIN340 at the indicated concentrations.
|
|
| S7209 |
GSK650394GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively. |
BV-2 cells were incubated in the absence or presence of gsk650394 (1 μM) for 30 min, followed by LPS (500 ng/ml) administration for 30 min, and then fixed. NF-κB p65 protein was visualized by indirect immunofluorescence staining using an antibody for NF-κB p65. For nuclear staining, the cells were stained with DAPI. Bar = 20 μm.
|
|
| S6499新 |
PF-6260933PF-6260933 is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity. |
||
| S8388 |
ML-7 HClML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. |
Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
|
|
| S8465 |
GSK'872 (GSK2399872A)GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity. |
(H-K) Cells incubated in the absence or presence of GSK’872, and treated with PM (100 μg/ml) for 24 h. The relative levels of IL6 (H), and IL8 (J) mRNA transcripts were measured by quantitative RT-PCR, and the protein levels of IL6 (I) and IL8 (K) in the culture supernatants, which are in turn were measured by ELISA.
|
|
| S8257新 |
CFI-402257CFI-402257 is a potent highly selective, and orally active small-molecule inhibitor of Mps1 with Ki value of 0.09 ± 0.02 nM. |
||
| S2642新 |
1-Naphthyl PP1(1-NA-PP1)1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
||
| S6710新 |
SGC-GAK-1SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase. |
||
| S8864新 |
ZT-12-037-01ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM. |
||
| S8872新 |
GSK8612GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified. |
||
| S8215 |
BAY 1217389BAY 1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1) with IC50 values below 10 nmol/L while showing an excellent selectivity profile. |
||
| S5792 |
CID 2011756CID 2011756 is an inhibitor of protein kinase D (PKD) with IC50 values of 3.2, 0.6, and 0.7 μM for PKD1, PKD2, and PKD3, respectively. |
||
| S4956 |
Benzamidine HClBenzamidine is an inhibitor of serine proteases with Ki values of 35, 350, and 220 µM for trypsin, plasmin, and thrombin, respectively. |
||
| S8810 |
SPHINX31SPHINX31 is a SRPK1 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold). |
||
| S8775 |
HS-1371HS-1371 is a potent RIP3 kinase inhibitor with an IC50 of 20.8 nM. It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro. |
||
| S8366 |
CRT0066101CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple. |
||
| S6088 |
6-(Dimethylamino)purine6-Dimethylaminopurine is a serine threonine protein kinase inhibitor. It inhibits the germinal vesicle breakdown and the meiotic maturation of oocytes. |
||
| S8358 |
WNK463WNK463 is a pan-WNK-kinase inhibitor. It potently inhibits the in vitro kinase activity of all four WNK family members (WNK1, WNK2, WNK3, and WNK4). |
||
| S7188 |
CID755673CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs. |
