CDK9-IN-2
Based on 7 publication(s) in Google Scholar
CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.
For research use only. We do not sell to patients.
- Purity: 98.72%
- CAS No.: 1263369-28-3
- Formula: C23H25ClFN5
- Molecular Weight:425.93
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
HY-L009
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Blood Cancer Compound Library
HY-L079
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Cancer Stem Cells Compound Library
HY-L135
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Anti-Hematopathy Compound Library
HY-L171
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Anti-Ovarian Cancer Compound Library
HY-L173
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
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High-Efficiency Gene Editing Compound Library
HY-L244
Publications Citing Use of MedChemExpress (MCE) CDK9-IN-2
More- Cancer Discov. 2017 Mar;7(3):302-321. [Abstract]
- Nat Cancer. 2022 Oct;3(10):1211-1227. [Abstract]
- Cell Host Microbe. 2017 Apr 12;21(4):507-517.e5. [Abstract]
- Cancer Res. 2025 May 14. [Abstract]
- SLAS Discov. 2018 Sep;23(8):850-861. [Abstract]
- PLoS One. 2017 May 16;12(5):e0177871. [Abstract]
- Res Sq. 2026 Jan 6.
Customer Validation & Images
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WB
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WB
Biological Activity
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CDK9 5 nM (IC50, H929 multiple myeloma cell line) |
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Cell Line
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Type | Value | Description | References |
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| 4T1 | IC50 |
0.116 μM
Compound: I-CDK9
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Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| A498 | IC50 |
0.057 μM
Compound: 30; CDK9
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Antiproliferative activity against human A498 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A498 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 38564299] |
| A549 | IC50 |
1.62 μM
Compound: I-CDK9
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| AD293 | IC50 |
0.076 μM
Compound: 30; CDK9
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Antiproliferative activity against human A-293 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
Antiproliferative activity against human A-293 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay
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[PMID: 38564299] |
| BT-549 | IC50 |
0.053 μM
Compound: I-CDK9
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Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| HeLa | IC50 |
0.15 μM
Compound: I-CDK9
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Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| HepG2 | IC50 |
0.473 μM
Compound: I-CDK9
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Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| HK-2 | IC50 |
0.187 μM
Compound: I-CDK9
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Cytotoxicity against HK-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against HK-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| Hs-578T | IC50 |
0.074 μM
Compound: I-CDK9
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Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| L02 | IC50 |
0.278 μM
Compound: I-CDK9
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Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| MCF-10A | IC50 |
0.108 μM
Compound: I-CDK9
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Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| MDA-MB-231 | IC50 |
0.08 μM
Compound: I-CDK9
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
| MRC5 | IC50 |
0.197 μM
Compound: I-CDK9
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Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37837671] |
CDK9-IN-2 (200 nM) reduces the expression of MEPCE indicating that MEPCE is a pharmacodynamic (PD) marker for any CDK9 inhibitor. The expression of MCL1 protein is reduced 2 hours after treatment and is further reduced after 16 hour exposure to CDK9-IN-2 (500 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1263369-28-3
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Appearance Solid
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Molecular Weight 425.93
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Formula C23H25ClFN5
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Color Light yellow to yellow
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SMILES
ClC1=CN=C(N[C@@H]2CC[C@@H](N)CC2)C=C1C3=NC(NCC4=CC(F)=CC=C4)=CC=C3
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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 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cancer Discov
Enhancer Remodeling during Adaptive Bypass to MEK Inhibition Is Attenuated by Pharmacologic Targeting of the P-TEFb Complex. [Abstract]2017 Mar;7(3):302-321. PMID: 28108460
CDK9-IN-2 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2017 Mar;7(3):302-321. [Abstract]
Small molecule inhibitor of CDK9, HY-16462, similarly blocks adaptive PDGFRB and DDR1 upregulation. Attenuation of 24 h 100 nM Trametinib-induced PDGFRB and DDR1 upregulation by co-treatment with 100 nM HY-16462.
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Nat Cancer
Targeting the ALK-CDK9-Tyr19 kinase cascade sensitizes ovarian and breast tumors to PARP inhibition via destabilization of the P-TEFb complex. [Abstract]2022 Oct;3(10):1211-1227. PMID: 36253486 -
Cell Host Microbe
Transcriptional Elongation of HSV Immediate Early Genes by the Super Elongation Complex Drives Lytic Infection and Reactivation from Latency. [Abstract]2017 Apr 12;21(4):507-517.e5. PMID: 28407486 -
Cancer Res
SMARCA4 loss increases RNA Polymerase II pausing and elevates R-loops to inhibit BRCA1-mediated repair in ovarian cancer. [Abstract]2025 May 14. PMID: 40366633 -
SLAS Discov
Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth. [Abstract]2018 Sep;23(8):850-861. PMID: 29742358 -
PLoS One
2017 May 16;12(5):e0177871. PMID: 28520795
CDK9-IN-2 purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 May 16;12(5):e0177871. [Abstract]
Mcl-1 mRNA is similarly reduced. Immunoblot analysis revealed that the highest concentrations of CDK9 inhibitors strongly reduce Mcl-1 protein.
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Solvent & Solubility
DMSO : 50 mg/mL (117.39 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
H929, A2058, A375, U87MG, and NCIH441 cell lines are treated with CDK9-IN-2 at 500 nM (high) or 200 nM (low) at different time points. Five cell lines are analyzed: NCI-H929, a multiple myeloma cell line; NCI-H441 , a lung papillary adenocarcinoma cell line; A375, a melanoma cell line; A2058, a melanoma cell line and U-87-MG, a glioblastoma cell line. Cell lines are grown in the medium recommended by ATCC and treated as follows: NCI-H929: 2 hours: DMSO, 200 nM CDK9-IN-2 or 500nM CDK9-IN-2. NCI-H441 and A375: 0 timepoint: Untreated, harvested when compound is added to the other plates. 2 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates).8 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates).16 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates). A2058 and U-87-MG: 0 timepoint: Untreated, harvested when compound is added to the other plates (3 plates). 2 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates). 8 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates).16 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates). The IC50s arethe analysed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3478 mL | 11.7390 mL | 23.4780 mL | 58.6951 mL |
| 5 mM | 0.4696 mL | 2.3478 mL | 4.6956 mL | 11.7390 mL | |
| 10 mM | 0.2348 mL | 1.1739 mL | 2.3478 mL | 5.8695 mL | |
| 15 mM | 0.1565 mL | 0.7826 mL | 1.5652 mL | 3.9130 mL | |
| 20 mM | 0.1174 mL | 0.5870 mL | 1.1739 mL | 2.9348 mL | |
| 25 mM | 0.0939 mL | 0.4696 mL | 0.9391 mL | 2.3478 mL | |
| 30 mM | 0.0783 mL | 0.3913 mL | 0.7826 mL | 1.9565 mL | |
| 40 mM | 0.0587 mL | 0.2935 mL | 0.5870 mL | 1.4674 mL | |
| 50 mM | 0.0470 mL | 0.2348 mL | 0.4696 mL | 1.1739 mL | |
| 60 mM | 0.0391 mL | 0.1957 mL | 0.3913 mL | 0.9783 mL | |
| 80 mM | 0.0293 mL | 0.1467 mL | 0.2935 mL | 0.7337 mL | |
| 100 mM | 0.0235 mL | 0.1174 mL | 0.2348 mL | 0.5870 mL |
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