YKL-5-124 TFA

Name: YKL-5-124 TFA
Brand: MedChemExpress
SKU: HY-101257B
Rating: 5.0 (7 reviews)

Cat. No.: HY-101257B Purity: 99.44%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

YKL-5-124 TFA Chemical Structure

CAS No. : 2748220-93-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 353	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 353	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 255	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 435	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 870	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1390	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2220	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of YKL-5-124 TFA:

CDK7-IN-1 Get quote
YKL-5-124 Get quote

6 Publications Citing Use of MCE YKL-5-124 TFA

Cell Viability Assay

: YKL-5-124 TFA purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2022 Nov 18. [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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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CDK7

53.5 nM (IC₅₀)

CDK7/Mat1/CycH

9.7 nM (IC₅₀)

CDK2

1300 nM (IC₅₀)

CDK9

3020 nM (IC₅₀)

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 WT 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.

Molecular Weight

629.63

Formula

C₃₀H₃₄F₃N₇O₅

CAS No.

2748220-93-9

Appearance

Solid

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.FC(F)(C(O)=O)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5882 mL	7.9412 mL	15.8823 mL
5 mM	0.3176 mL	1.5882 mL	3.1765 mL
10 mM	0.1588 mL	0.7941 mL	1.5882 mL

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (79.41 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.44%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (254 KB) HNMR (418 KB) LCMS (129 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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
DMSO	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.

YKL-5-124 TFA Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YKL-5-1242748220-93-9CDKCyclin dependent kinaseCDK7CDK7/Mat1/CycHtranscriptioncovalentcell-cyclearrestPol-IIphosphorylationT-loopirreversibleInhibitorinhibitorinhibit

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YKL-5-124 TFA

Customer Review

Other Forms of YKL-5-124 TFA:

YKL-5-124 TFA Related Antibodies

6 Publications Citing Use of MCE YKL-5-124 TFA

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

YKL-5-124 TFA Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

YKL-5-124 TFA Related Classifications

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