YKL-5-124 TFA
Based on 17 publication(s) in Google Scholar
YKL-5-124 TFA 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 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.74%
- CAS No.: 2748220-93-9
- 화학식: C30H34F3N7O5
- 분자량:629.63
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 TFA
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). 2025 Feb;12(5):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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Cell Proliferation/Viability Assay
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 WT 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. 2748220-93-9
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Appearance Solid
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분자량 629.63
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화학식 C30H34F3N7O5
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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.FC(F)(C(O)=O)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 TFA 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 TFA 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 TFA 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]2025 Feb;12(5):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 TFA 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 TFA 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 TFA 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 (158.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (79.41 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (3.97 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 (3.97 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.5882 mL | 7.9412 mL | 15.8823 mL | 39.7059 mL |
| 5 mM | 0.3176 mL | 1.5882 mL | 3.1765 mL | 7.9412 mL | |
| 10 mM | 0.1588 mL | 0.7941 mL | 1.5882 mL | 3.9706 mL | |
| 15 mM | 0.1059 mL | 0.5294 mL | 1.0588 mL | 2.6471 mL | |
| 20 mM | 0.0794 mL | 0.3971 mL | 0.7941 mL | 1.9853 mL | |
| 25 mM | 0.0635 mL | 0.3176 mL | 0.6353 mL | 1.5882 mL | |
| 30 mM | 0.0529 mL | 0.2647 mL | 0.5294 mL | 1.3235 mL | |
| 40 mM | 0.0397 mL | 0.1985 mL | 0.3971 mL | 0.9926 mL | |
| 50 mM | 0.0318 mL | 0.1588 mL | 0.3176 mL | 0.7941 mL | |
| 60 mM | 0.0265 mL | 0.1324 mL | 0.2647 mL | 0.6618 mL | |
| DMSO | 80 mM | 0.0199 mL | 0.0993 mL | 0.1985 mL | 0.4963 mL |
| 100 mM | 0.0159 mL | 0.0794 mL | 0.1588 mL | 0.3971 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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