Art. -Nr.: HY-101257

YKL-5-124

17 Cited Publications

Kundenbewertung

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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Reinheit: 99.53%
CAS. Nr.: 1957203-01-8
Formel: C₂₈H₃₃N₇O₃
Molecular Weight:515.61

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

YKL-5-124 Chemical Structure

CAS. Nr.: 1957203-01-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK7

53.5 nM (IC₅₀)

CDK7/Mat1/CycH

9.7 nM (IC₅₀)

CDK2

1300 nM (IC₅₀)

CDK9

3020 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Cell Cycle Analysis^[1]

Cell Line:

HAP1 cells
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
Incubation Time:

72 hours
Result:

Caused a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells.

Western Blot Analysis^[1]

Cell Line:

HAP1 cells
Concentration:

0 nM, 125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM
Incubation Time:

24 hours
Result:

Inhibited CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion.

Chemical Information

CAS. Nr. 1957203-01-8
Appearance Solid
Molecular Weight 515.61
Formel C₂₈H₃₃N₇O₃
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (17)

All WBCell Proliferation/Viability Assay

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Journal Impact Factor

Cell

RNA Pol II inhibition activates cell death independently from the loss of transcription. [Abstract]

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).
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.
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.
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.
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

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
iScience

CDK7 is a novel therapeutic target in fibrolamellar carcinoma. [Abstract]

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

Castration-resistant prostate cancer cells are dependent on the high activity of CDK7. [Abstract]

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.
bioRxiv

2025 March 19.
Res Sq

2024 Jul 29.
bioRxiv

Pol II degradation activates cell death independently from the loss of transcription. [Abstract]

2024 Dec 10:2024.12.09.627542. PMID: 39713309
bioRxiv

2023 Apr 23.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9395 mL

9.6973 mL

19.3945 mL

5 mM

0.3879 mL

1.9395 mL

3.8789 mL

10 mM

0.1939 mL

0.9697 mL

1.9395 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Olson CM, et al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

YKL-5-124

17 Cited Publications

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YKL-5-124

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) YKL-5-124

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YKL-5-124

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) YKL-5-124

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YKL-5-124 Related Classifications

HY-101257 Related Classifications