カゼインキナーゼ
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 | ||
| S1105 | LY294002 | <1 mg/mL | 36 mg/mL | 21 mg/mL |
| S2248 | Silmitasertib (CX-4945) | <1 mg/mL | 16 mg/mL | <1 mg/mL |
| S6544 | SR-3029 | <1 mg/mL | 47 mg/mL | <1 mg/mL |
| S5265 | TBB | -1 mg/mL | 86 mg/mL | -1 mg/mL |
| S6536 | TTP 22 | <1 mg/mL | 66 mg/mL | 8 mg/mL |
| S2249 | PF 4800567 | <1 mg/mL | 72 mg/mL | <1 mg/mL |
| S6734 | PF-670462 | 82 mg/mL | 82 mg/mL | 28 mg/mL |
| S6578 | Longdaysin | <1 mg/mL | 67 mg/mL | 67 mg/mL |
| S7642 | D 4476 | <1 mg/mL | 79 mg/mL | <1 mg/mL |
| S8237 | IC261 | <1 mg/mL | 62 mg/mL | <1 mg/mL |
| S5516 | Ellagic Acid hydrate | -1 mg/mL | 2 mg/mL | -1 mg/mL |
亜型選択性的な製品
Casein 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 |
|---|---|---|---|
| S1105 |
LY294002LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis. |
Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
|
|
| S2248 |
Silmitasertib (CX-4945)Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1/2. |
|
|
| S6544新 |
SR-3029SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively. |
||
| S5265 |
TBBTBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively. |
||
| S6536新 |
TTP 22TTP22 is a casein kinase 2 (CK2) inhibitor with an IC50 value of 100 nM. It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM. |
||
| S2249新 |
PF 4800567PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM). |
||
| S6734新 |
PF-670462PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively. |
||
| S6578新 |
LongdaysinLongdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7. |
||
| S7642 |
D 4476D 4476 is a potent, selective, and cell-permeant CK1 (casein kinase 1) inhibitor with IC50 of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an ALK5 inhibitor with IC50 of 500 nM. |
Western blot of signaling effects. 48 hrs after transfection cells were serum‐starved for 12 h before stimulation with Wnt5a for 30 min or 120 min (200 ng/ml) in the presence or absence of casein kinase inhibitor D4476 (100 μM).
|
|
| S8237 |
IC261IC261 is a novel inhibitor of CK1. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM. |
||
| S5516 |
Ellagic Acid hydrateEllagic acid is a potent inhibitor of protein kinase CK2 with IC50s of 0.04, 2.9 and 3.5 μM for CK2, Lyn and PKA respectively. It shows potent antioxidant, anti-mutagenic and antidepressant properties. |
| 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 |
|---|---|---|---|
| S1105 |
LY294002LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis. |
Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
|
|
| S2248 |
Silmitasertib (CX-4945)Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1/2. |
|
|
| S6544新 |
SR-3029SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively. |
||
| S5265 |
TBBTBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively. |
||
| S6536新 |
TTP 22TTP22 is a casein kinase 2 (CK2) inhibitor with an IC50 value of 100 nM. It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM. |
||
| S2249新 |
PF 4800567PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM). |
||
| S6734新 |
PF-670462PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively. |
||
| S6578新 |
LongdaysinLongdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7. |
||
| S7642 |
D 4476D 4476 is a potent, selective, and cell-permeant CK1 (casein kinase 1) inhibitor with IC50 of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an ALK5 inhibitor with IC50 of 500 nM. |
Western blot of signaling effects. 48 hrs after transfection cells were serum‐starved for 12 h before stimulation with Wnt5a for 30 min or 120 min (200 ng/ml) in the presence or absence of casein kinase inhibitor D4476 (100 μM).
|
|
| S8237 |
IC261IC261 is a novel inhibitor of CK1. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM. |
||
| S5516 |
Ellagic Acid hydrateEllagic acid is a potent inhibitor of protein kinase CK2 with IC50s of 0.04, 2.9 and 3.5 μM for CK2, Lyn and PKA respectively. It shows potent antioxidant, anti-mutagenic and antidepressant properties. |
