CCT251545
Modify Date: 2024-01-20 14:00:34
CCT251545 structure
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Common Name | CCT251545 | ||
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| CAS Number | 1661839-45-7 | Molecular Weight | 421.923 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 709.7±60.0 °C at 760 mmHg | |
| Molecular Formula | C23H24ClN5O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 383.0±32.9 °C | |
Use of CCT251545CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.IC50 value: 5 nM [2]Target: WNTin vitro: CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM).[2]in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings. [1] |
| Name | CCT251545 |
|---|---|
| Synonym | More Synonyms |
| Description | CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.IC50 value: 5 nM [2]Target: WNTin vitro: CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM).[2]in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings. [1] |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 709.7±60.0 °C at 760 mmHg |
| Molecular Formula | C23H24ClN5O |
| Molecular Weight | 421.923 |
| Flash Point | 383.0±32.9 °C |
| Exact Mass | 421.166931 |
| LogP | 2.53 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.701 |
| Storage condition | 2-8℃ |
| 2,8-Diazaspiro[4.5]decan-1-one, 8-[3-chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl]- |
| 8-{3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl}-2,8-diazaspiro[4.5]decan-1-one |
| CCT251545 |