YKL-5-124
Based on 17 publication(s) in Google Scholar
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
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- Purity: 99.53%
- CAS No.: 1957203-01-8
- 화학식: C28H33N7O3
- 분자량:515.61
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) YKL-5-124
More- Cell. 2025 Oct 30;188(22):6301-6316.e29. [Abstract]
- Cell Discov. 2022 Oct 6;8(1):102. [Abstract]
- J Biomed Sci. 2022 Feb 14;29(1):13. [Abstract]
- Adv Sci (Weinh). 2024 Dec 10:e2413103. [Abstract]
- Int J Biol Sci. 2024 Aug 19;20(11):4513-4531. [Abstract]
- Cell Death Discov. 2025 Mar 4;11(1):86. [Abstract]
- EMBO J. 2025 Sep 8. [Abstract]
- Int J Mol Sci. 2023 Apr 10;24(8):7009. [Abstract]
- mBio. 2025 Dec 10;16(12):e0289825. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- iScience. 2025 Nov 4;28(12):113925. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- J Cancer Res Clin Oncol. 2023 Jul;149(8):5255-5263. [Abstract]
- bioRxiv. 2025 March 19.
- Res Sq. 2024 Jul 29.
- bioRxiv. 2024 Dec 10:2024.12.09.627542. [Abstract]
- bioRxiv. 2023 Apr 23.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
Biological Activity
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CDK7 53.5 nM (IC50) |
CDK7/Mat1/CycH 9.7 nM (IC50) |
CDK2 1300 nM (IC50) |
CDK9 3020 nM (IC50) |
YKL-5-124 (0-2000 nM; 72 hours; HAP1 cells) treatment causes a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells[1].
YKL-5-124 (0-2000 nM; 24 hours; HAP1 WT cells) treatment inhibits CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion[1].
Treatment of cells with YKL-5-124 as a competitor at a concentration of about 30 nM blocks pull-down of CDK7-cyclin H but has no effect on the pull-down of cyclin K-CDK12/13 in HAP1 cells. Treatment with 100 nM YKL-5-124 reduces CDK7-cyclin H binding to bioTHZ1 by >50% at 30 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HAP1 cells
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Concentration:0 nM, 0.2 nM, 0.7 nM, 2 nM, 6.3 nM, 20 nM, 60 nM, 200 nM, 633.3 nM, 2000 nM
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Incubation Time:72 hours
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Result:Caused a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells.
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Cell Line:HAP1 cells
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Concentration:0 nM, 125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM
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Incubation Time:24 hours
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Result:Inhibited CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion.
Chemical Information
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CAS No. 1957203-01-8
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Appearance Solid
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분자량 515.61
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화학식 C28H33N7O3
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Color White to off-white
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SMILES
CC1(C)N(C(N[C@@H](C2=CC=CC=C2)CN(C)C)=O)CC3=C1NN=C3NC(C4=CC=C(NC(C=C)=O)C=C4)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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Journal Impact Factor
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Most Recent
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Cell
2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455 -
Cell Discov
Lineage-coupled clonal capture identifies clonal evolution mechanisms and vulnerabilities of BRAFV600E inhibition resistance in melanoma. [Abstract]2022 Oct 6;8(1):102. PMID: 36202798
YKL-5-124 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Oct 6;8(1):102. [Abstract]
Cell viability curves of the BRAFi-resistant clones in response to an E2F targets inhibitor YKL-5-124 (10-104 nM).
YKL-5-124 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Oct 6;8(1):102. [Abstract]
Colony formation assay of BRAFi-resistant cells treated with YKL-5-124 (10-90 nM).
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J Biomed Sci
O-GlcNAc transferase couples MRE11 to transcriptionally active chromatin to suppress DNA damage. [Abstract]2022 Feb 14;29(1):13. PMID: 35164752
YKL-5-124 purchased from MedChemExpress. Usage Cited in: J Biomed Sci. 2022 Feb 14;29(1):13. [Abstract]
YKL-5-124 (50-1000 nM; 4 h) robustly decreased RNA Pol II phosphorylation in prostate cancer cells.
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Adv Sci (Weinh)
Dual Inhibition of CDK4/6 and CDK7 Suppresses Triple-Negative Breast Cancer Progression via Epigenetic Modulation of SREBP1-Regulated Cholesterol Metabolism. [Abstract]2024 Dec 10:e2413103. PMID: 39656925 -
Int J Biol Sci
Olaparib combined with CDK12-IN-3 to promote genomic instability and cell death in ovarian cancer. [Abstract]2024 Aug 19;20(11):4513-4531. PMID: 39247812 -
Cell Death Discov
CeDaD-a novel assay for simultaneous tracking of cell death and division in a single population. [Abstract]2025 Mar 4;11(1):86. PMID: 40038265
YKL-5-124 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 4;11(1):86. [Abstract]
YKL-5-124 (10-10-10-5 M; 48 h) concentration-dependent reduced HCT116 cell growth.
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EMBO J
Resistance to CDK7 inhibitors directed by acquired mutation of a conserved residue in cancer cells. [Abstract]2025 Sep 8. PMID: 40921851
YKL-5-124 purchased from MedChemExpress. Usage Cited in: EMBO J. 2025 Sep 8. [Abstract]
Growth inhibition for YKL-5-124 (10-2-104 nM) was carried out using Sam-selected D97N knock-in cells (22Rv1-CDK7-D97N, LNCaP-CDK7-D97N) alongside parental Samsensitive cells.
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Int J Mol Sci
Re-Evaluating the Relevance of the Oxygen-Glucose Deprivation Model in Ischemic Stroke: The Example of Cdk Inhibition. [Abstract]2023 Apr 10;24(8):7009. PMID: 37108171 -
mBio
Functional insight into cyclin-dependent kinase (CDK)7 via chemical inhibition of the priority fungal pathogen Cryptococcus neoformans. [Abstract]2025 Dec 10;16(12):e0289825. PMID: 41171060 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
iScience
2025 Nov 4;28(12):113925. PMID: 41321622 -
iScience
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]2024 May 16;27(6):110011. PMID: 38868181 -
J Cancer Res Clin Oncol
2023 Jul;149(8):5255-5263. PMID: 36401094
YKL-5-124 purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Jul;149(8):5255-5263. [Abstract]
OSMI-4 (20 µM; 4 days) and YKL-5-124 (1, 5, 10, 50, 400 nM; 4 days) demonstrate highly signifcant combinatorial toxicity on three CRPC models.
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bioRxiv
2024 Dec 10:2024.12.09.627542. PMID: 39713309 -
용액&용해도
DMSO : 100 mg/mL (193.95 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)
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: ≥ 2.08 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (4.03 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
순도&문서
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Data Sheet (276 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 | 1.9395 mL | 9.6973 mL | 19.3945 mL | 48.4863 mL |
| 5 mM | 0.3879 mL | 1.9395 mL | 3.8789 mL | 9.6973 mL | |
| 10 mM | 0.1939 mL | 0.9697 mL | 1.9395 mL | 4.8486 mL | |
| 15 mM | 0.1293 mL | 0.6465 mL | 1.2930 mL | 3.2324 mL | |
| 20 mM | 0.0970 mL | 0.4849 mL | 0.9697 mL | 2.4243 mL | |
| 25 mM | 0.0776 mL | 0.3879 mL | 0.7758 mL | 1.9395 mL | |
| 30 mM | 0.0646 mL | 0.3232 mL | 0.6465 mL | 1.6162 mL | |
| 40 mM | 0.0485 mL | 0.2424 mL | 0.4849 mL | 1.2122 mL | |
| 50 mM | 0.0388 mL | 0.1939 mL | 0.3879 mL | 0.9697 mL | |
| 60 mM | 0.0323 mL | 0.1616 mL | 0.3232 mL | 0.8081 mL | |
| 80 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6061 mL | |
| 100 mM | 0.0194 mL | 0.0970 mL | 0.1939 mL | 0.4849 mL |
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