YKL-5-124

Name: YKL-5-124
Brand: MedChemExpress
SKU: HY-101257
Rating: 5.0 (6 reviews)

Cat. No.: HY-101257 Purity: 98.03%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

YKL-5-124 Chemical Structure

CAS No. : 1957203-01-8

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 289	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 289	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 121	In-stock	Estimated Time of Arrival: December 31
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 696	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of YKL-5-124:

YKL-5-124 TFA In-stock

5 Publications Citing Use of MCE YKL-5-124

Cell Viability Assay

: YKL-5-124 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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Description

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.

Molecular Weight

515.61

Formula

C₂₈H₃₃N₇O₃

CAS No.

1957203-01-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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: ≥ 2.08 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.
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.
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: ≥ 2.08 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

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.03%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (251 KB) HNMR (309 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

Complete Stock Solution Preparation Table

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

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-5-1241957203-01-8Inhibitorinhibitorinhibit

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YKL-5-124

Customer Review

Other Forms of YKL-5-124:

YKL-5-124 Related Antibodies

5 Publications Citing Use of MCE YKL-5-124

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

Customer Review

YKL-5-124 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

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