Art. -Nr.: HY-161828

JWZ-5-13

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JWZ-5-13 is a CDK7 PROTAC degrader. JWZ-5-13 inhibits the proliferation of cancer cells. JWZ-5-13 is applicable to the research of ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia and non-small cell lung cancer.
(Pink: CDK7 ligand (HY-161830); Blue: VHL ligand (HY-112078); Black: linker (HY-Y0925)).

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Reinheit: 98.19%
CAS. Nr.: 3103763-70-5
Formel: C₅₄H₆₆N₁₀O₆S
Molecular Weight:983.23

Speicherung:

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

JWZ-5-13 Chemical Structure

CAS. Nr.: 3103763-70-5

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Fluorescent Dye

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

JWZ-5-13 is a CDK7 PROTAC degrader. JWZ-5-13 inhibits the proliferation of cancer cells. JWZ-5-13 is applicable to the research of ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia and non-small cell lung cancer^[1]. (Pink: CDK7 ligand (HY-161830); Blue: VHL ligand (HY-112078); Black: linker (HY-Y0925)).

IC₅₀ & Target

VHL

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	332 nM Compound: 17; JWZ-5-13	Antiproliferative activity against human A549 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A549 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 39004018]
Jurkat	IC₅₀	160 nM Compound: 17; JWZ-5-13	Antiproliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 39004018]
MOLT-4	IC₅₀	89 nM Compound: 17; JWZ-5-13	Antiproliferative activity against human MOLT-4 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLT-4 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 39004018]
OVCAR-3	IC₅₀	780 nM Compound: 17; JWZ-5-13	Antiproliferative activity against human OVCAR-3 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OVCAR-3 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 39004018]
SU-DHL-5	IC₅₀	52 nM Compound: 17; JWZ-5-13	Antiproliferative activity against human SU-DHL-5 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-5 cells assessed as cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 39004018]

In Vitro

JWZ-5-13 (Compound 17) potently inhibits the kinase activity of CDK7/Cyclin H/MNAT1 in cell-free assays, with an IC₅₀ of 20.1 nM^[1].
JWZ-5-13 (10 nM-5 μM; 0.5-24 h) induces dose-dependent degradation of CDK7 in Jurkat cells^[1].
JWZ-5-13 (0.1-5.0 μM; 6 h) potently degrades CDK7 in a variety of human cancer cell lines, including OVCAR3, SUDHL5, Molt4 and A549 cells^[1].
JWZ-5-13 (10 nM-5 μM; 6 h) induces the degradation of CDK7, accompanied by downregulated expression of its binding partners Cyclin H and MAT1^[1].
JWZ-5-13 (72 h) potently inhibits the proliferation of various human cancer cell lines, with IC₅₀ values ranging from 52 nM (SUDHL5), 89 nM (Molt4), 160 nM (Jurkat) to 332 nM (A549) after 72 h of treatment^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

Jurkat human T lymphocyte cells
Concentration:

0.1 μM (time-course); 10-5000 nM (6 h dose-response); 0.1, 1 μM (16 h)
Incubation Time:

0.5, 1, 2, 4, 8, 16, 24 h (0.1 μM); 6 h (10-5000 nM); 16 h (0.1, 1 μM)
Result:

Induced detectable CDK7 degradation as early as 0.5 h, with sustained degradation through 24 h at 0.1 μM.
Induced dose-dependent CDK7 degradation at 10-5000 nM for 6 h, with near-complete degradation observed at concentrations ≥100 nM.
Induced up to 95% reduction in CDK7 protein levels at 0.1 or 1 μM for 16 h.

Western Blot Analysis^[1]

Cell Line:

OVCAR3 ovarian adenocarcinoma, SUDHL5 B-cell lymphoma, Molt4 T lymphoblast, A549 lung adenocarcinoma cells
Concentration:

0.1-5.0 μM
Incubation Time:

6 h
Result:

Induced robust CDK7 degradation in all tested cell lines.

Western Blot Analysis^[1]

Cell Line:

Jurkat cells (wild-type and VHL-knockout)
Concentration:

0.01, 0.1, 0.5, 1 μM (6 h); 0.1 μM (6 h, with 2 h pretreatment with inhibitors/ligands)
Incubation Time:

6 h (JWZ-5-13 alone); 6 h (JWZ-5-13 with 2 h pretreatment)
Result:

Induced dose-dependent CDK7 degradation in Jurkat cells at 0.01-1 μM for 6 h.
Had its induced CDK7 degradation rescued by pretreatment with MG132, MLN-4924, YKL-5-167, or (S,R,S)-AHPC-Me.
Showed completely abrogated CDK7 degradation in VHL-knockout Jurkat cells compared to wild-type controls.

Western Blot Analysis^[1]

Cell Line:

Jurkat cells, OVCAR3 cells
Concentration:

10, 50, 100, 500 nM (Jurkat CDK profiling); 0.1 μM (OVCAR3 proteomics); 0.1, 0.5, 1, 5 μM (CDK7 complex component profiling; LONRF2 profiling)
Incubation Time:

6 h
Result:

Barely affected protein levels of CDK1, 2, 4, 5, 6, 8, or 9 in Jurkat cells at concentrations up to 500 nM.
Identified only three significantly changed proteins (≥1.75-fold change) in OVCAR3 cells treated with 0.1 μM: CDK7 (downregulated), Cyclin H (downregulated), and MAT1 (downregulated via Western blot confirmation).
Induced dose-dependent downregulation of Cyclin H and MAT1 in both Jurkat and OVCAR3 cells.
Did not induce degradation of LONRF2 in Jurkat cells at concentrations up to 5 μM.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-last	CL_{_obs}	V_{ss_obs}
Mice^[1]	3 mg/kg	i.v.	3.76 h	0.083 h	17100 μM	6120 μM·h	8.3 mL/min/kg	0.345 L/kg
Mice^[1]	10 mg/kg	i.p.	2.82 h	1.0 h	3390 μM	19400 μM·h	8.7 mL/min/kg	/

Chemical Information

CAS. Nr. 3103763-70-5
Appearance Solid
Molecular Weight 983.23
Formel C₅₄H₆₆N₁₀O₆S
Color White to off-white
SMILES

O=C(NC1=NNC2=C1CN(C(N[C@@H](C3=CC=CC=C3)CN(C)C)=O)C2(C)C)C4=CC=C(C#CCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)C=C4
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (101.71 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

1.0171 mL

5.0853 mL

10.1706 mL

5 mM

0.2034 mL

1.0171 mL

2.0341 mL

10 mM

0.1017 mL

0.5085 mL

1.0171 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: ≥ 2.5 mg/mL (2.54 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.54 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (2.54 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.

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 (279 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Ji W, et al. Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7). Eur J Med Chem. 2024;276:116613. [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	1.0171 mL	5.0853 mL	10.1706 mL	25.4264 mL
	5 mM	0.2034 mL	1.0171 mL	2.0341 mL	5.0853 mL
	10 mM	0.1017 mL	0.5085 mL	1.0171 mL	2.5426 mL
	15 mM	0.0678 mL	0.3390 mL	0.6780 mL	1.6951 mL
	20 mM	0.0509 mL	0.2543 mL	0.5085 mL	1.2713 mL
	25 mM	0.0407 mL	0.2034 mL	0.4068 mL	1.0171 mL
	30 mM	0.0339 mL	0.1695 mL	0.3390 mL	0.8475 mL
	40 mM	0.0254 mL	0.1271 mL	0.2543 mL	0.6357 mL
	50 mM	0.0203 mL	0.1017 mL	0.2034 mL	0.5085 mL
	60 mM	0.0170 mL	0.0848 mL	0.1695 mL	0.4238 mL
	80 mM	0.0127 mL	0.0636 mL	0.1271 mL	0.3178 mL
	100 mM	0.0102 mL	0.0509 mL	0.1017 mL	0.2543 mL

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JWZ-5-13

PROTAC Library

MCE Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JWZ-5-13

PROTAC Library

MCE Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JWZ-5-13 Related Classifications

HY-161828 Related Classifications