CDK8/19-IN-1
Based on 1 Customer Validation
CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
For research use only. We do not sell to patients.
- Purity: 98.08%
- CAS No.: 1818427-07-4
- Formula: C19H18N4O4S2
- Molecular Weight:430.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CDK8/CycC 0.46 nM (IC50) |
CDK19/CycC 0.99 nM (IC50) |
CDK9 270 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Calu-1 | GI50 |
0.43 nM
Compound: 52h
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Growth inhibition of human Calu1 cells after 196 hrs by CellTiter-Glo luminescence assay
Growth inhibition of human Calu1 cells after 196 hrs by CellTiter-Glo luminescence assay
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[PMID: 28302507] |
| MV4-11 | GI50 |
1.6 nM
Compound: 52h
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Growth inhibition of human MV411 cells after 196 hrs by CellTiter-Glo luminescence assay
Growth inhibition of human MV411 cells after 196 hrs by CellTiter-Glo luminescence assay
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[PMID: 28302507] |
| RPMI-8226 | GI50 |
2.5 nM
Compound: 52h
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Growth inhibition of human RPMI8226 cells after 196 hrs by CellTiter-Glo luminescence assay
Growth inhibition of human RPMI8226 cells after 196 hrs by CellTiter-Glo luminescence assay
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[PMID: 28302507] |
CDK8/19-IN-1 (52h) is a potent CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively. CDK8/19-IN-1 also weakly inhibits CDK2, with 62% inhibition at 1 μM. CDK8/19-IN-1 (1 μM) shows >50% inhibition against GSK3β, PLK1, ASK1, CK1δ, PKA, ROCK1, PKCθ, CDC7. CDK8/19-IN-1 shows Kds of 25, 46, 81, 86, 97, 160 and >3000 nM for CDK19, CDK8, DYRK1B, HASPIN, YSK4, HIPK1 and EPHA3, respectively. CDK8/19-IN-1 displays potent antitumor activity, with GI50 of 0.43-2.5 nM for colon, multiple myeloma, acute myelogenous leukemia (AML), lung cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1818427-07-4
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Appearance Solid
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Molecular Weight 430.50
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Formula C19H18N4O4S2
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Color Off-white to light yellow
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SMILES
O=C(C1=C2CCC3=C(SN=C3)C2=C(OC4=CC=C(C(NCCOC)=O)N=C4)S1)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (116.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3229 mL | 11.6144 mL | 23.2288 mL | 58.0720 mL |
| 5 mM | 0.4646 mL | 2.3229 mL | 4.6458 mL | 11.6144 mL | |
| 10 mM | 0.2323 mL | 1.1614 mL | 2.3229 mL | 5.8072 mL | |
| 15 mM | 0.1549 mL | 0.7743 mL | 1.5486 mL | 3.8715 mL | |
| 20 mM | 0.1161 mL | 0.5807 mL | 1.1614 mL | 2.9036 mL | |
| 25 mM | 0.0929 mL | 0.4646 mL | 0.9292 mL | 2.3229 mL | |
| 30 mM | 0.0774 mL | 0.3871 mL | 0.7743 mL | 1.9357 mL | |
| 40 mM | 0.0581 mL | 0.2904 mL | 0.5807 mL | 1.4518 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1614 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9679 mL | |
| 80 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7259 mL | |
| 100 mM | 0.0232 mL | 0.1161 mL | 0.2323 mL | 0.5807 mL |
CDK8/19-IN-1 Related Classifications
HY-111427 Related Classifications
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