Art. -Nr.: HY-X0150

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JSH-150

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JSH-150 is a highly selective and potent CDK9 inhibitor with an IC₅₀ of 1 nM.

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Reinheit: 98.08%
CAS. Nr.: 2247481-21-4
Formel: C₂₄H₃₃ClN₆O₂S
Molecular Weight:505.08

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

JSH-150 Chemical Structure

CAS. Nr.: 2247481-21-4

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

JSH-150 is a highly selective and potent CDK9 inhibitor with an IC₅₀ of 1 nM.

IC₅₀ & Target^[1]

CDK9/cyclinT1

1 nM (IC₅₀)

CDK16/Cyclin Y

292 nM (IC₅₀)

Cdk1/cyclin B

1.34 μM (IC₅₀)

CDK14/Cyclin Y

1.68 μM (IC₅₀)

CDK7/Cyclin H/MNAT1

1.72 μM (IC₅₀)

cdk2/cyclin A

2.86 μM (IC₅₀)

Cdk5/p25

4.64 μM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	GI₅₀	0.044 μM Compound: 40; JSH-150	Antiproliferative activity against human A375 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human A375 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
A-431	GI₅₀	0.019 μM Compound: 40; JSH-150	Antiproliferative activity against human A431 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human A431 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
CHO	GI₅₀	1.1 μM Compound: 40; JSH-150	Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
COLO 205	GI₅₀	0.014 μM Compound: 40; JSH-150	Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
GISTT1	GI₅₀	0.0021 μM Compound: 40; JSH-150	Antiproliferative activity against human GISTT1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human GISTT1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
HL-60	GI₅₀	0.056 μM Compound: 40; JSH-150	Antiproliferative activity against human HL60 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human HL60 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MOLM-13	GI₅₀	0.012 μM Compound: 40; JSH-150	Antiproliferative activity against human MOLM13 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MOLM13 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MOLM-14	GI₅₀	0.0011 μM Compound: 40; JSH-150	Antiproliferative activity against human MOLM14 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MOLM14 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MV4-11	GI₅₀	0.012 μM Compound: 40; JSH-150	Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MV4-11	IC₅₀	12 nM Compound: 37; JSH-150	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured for 72 hrs by cellTiter-Glo assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured for 72 hrs by cellTiter-Glo assay	[PMID: 38564299]
OCI-AML-3	GI₅₀	0.0066 μM Compound: 40; JSH-150	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
Ramos	GI₅₀	0.013 μM Compound: 40; JSH-150	Antiproliferative activity against human Ramos cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human Ramos cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
SKM-1	GI₅₀	0.012 μM Compound: 40; JSH-150	Antiproliferative activity against human SKM1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human SKM1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
SK-N-BE(2)-M17	GI₅₀	0.034 μM Compound: 40; JSH-150	Antiproliferative activity against human BE(2)-M17 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human BE(2)-M17 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
U-937	GI₅₀	0.002 μM Compound: 40; JSH-150	Antiproliferative activity against human U937 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human U937 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]

In Vitro

The antiproliferative effect of JSH-150 is examined ton a panel of established cancer cell lines. JSH-150 exhibits potent antiproliferative activities in solid tumor cell lines such as A375 (melanoma), A431 (squamous), BE(2)M17 (neuroblastoma), GIST-T1 (GIST) and COLO205 (colon cancer) with GI₅₀ values from 0.002 to 0.044 μM. In the leukemia cell lines including acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL) and B cell lymphoma cell lines, JSH-150 also displays strong growth inhibition efficacies with GI₅₀s ranging from single to double digit nM. In addition, JSH-150 is much less sensitive in normal CHO cells (GI₅₀: 1.1 μM) compared with the cancer cell lines^[1].

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

In Vivo

Treatment of JSH-150 at all dosages, i.e., 10, 20 and 30 mg/kg/day, can almost completely suppress the tumor progression in the first two weeks and does not affect the animal’s weight indicating that there is no general cytotoxicity at these doses. After stopping the treatment of JSH-150, the tumors of the animals treated with 10 mpk drug dosage start to grow again. However, this tumor recurrence is not observed in the 20 and 30 mpk dosage groups during the following week after administration of JSH-150 is stopped and p values are quantified on the 21st day, which are 0.042, 0.0035 and 0.0028, respectively. The PK properties of JSH-150 are evaluated in different species including mice, Sprague-Dawley rats and beagle dogs through intravenous injection and oral administration. JSH-150 is absorbed rapidly in dogs and mice (T_max=1.33 h and 2.00 h respectively) but slowly in rats (T_max=3.33 h). JSH-150 also displays different half-lives in three different species via oral administration (T_1/2=1.55 h in mice, 3.37 h in rats and 20.37 h in dogs), which indicates that it is metabolized very slowly in dogs compared with mice and rats. In addition, JSH-150 exhibits acceptable bioavailability in mice, rats and dogs (F=45.01%, 45.10% and 39.15%, respectively). The PK properties indicated that JSH-150 is suitable for oral administration^[1].

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

Chemical Information

CAS. Nr. 2247481-21-4
Appearance Solid
Molecular Weight 505.08
Formel C₂₄H₃₃ClN₆O₂S
Color Off-white to yellow
SMILES

COCCN[C@@H]1CC[C@@H](NC2=NC=C(Cl)C(C3=CSC(NCC4(C#N)CCOCC4)=N3)=C2)CC1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Int J Biol Macromol

CDK2-based CDK7 mimic as a tool for structural analysis: Biochemical validation and crystal structure with SY5609. [Abstract]

2024 Dec 27:139117. PMID: 39733900

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (197.99 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

1.9799 mL

9.8994 mL

19.7988 mL

5 mM

0.3960 mL

1.9799 mL

3.9598 mL

10 mM

0.1980 mL

0.9899 mL

1.9799 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (4.95 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 (4.95 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 (4.95 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

Protokoll

Cell Assay^[1]

The A375 (melanoma), A431 (squamous), BE(2)M17 (neuroblastoma), BE(2)M17 (neuroblastoma), CRL-2234 (hepatoma), COLO205 (colon cancer), A549 (lung adenocarcinoma), Ramos (B cell lymphoma), MV4-11 (AML), Ramos (B cell lymphoma), U937 (AML), CHL (hamster lung cell), and CHO (hamster ovary cell) cell lines are used. OCI-AML-3 (AML), SKM-1 (AML), MEC-1 (CLL), MEC-2 (CLL) and HL-60 (human promyelocytic leukemia cells) are used. Human GIST-T1 cells are used. MOLM-13 and MOLM14 cell lines are used. All the cells are grown in a humidified incubator at 37°C under 5% CO2. A375, A431, GIST-T1, A549, Colo205 and CHO cells are maintained in DMEM supplemented with 10% FBS, 1% Penicillin/Streptomycin. BE(2)M17 cells are cultured with 1:1 mixture of ATCC-formulated Eagle's minimum essential medium, and F12 Medium. MV4-11, MEC-1 and MEC-2 are grown in IMDM supplemented with 10% FBS, 1% Penicillin/Streptomycin. CRL-2234, U2932, U937, Ramos, MOLM13, MOLM14, OCI-AML-3, SKM-1, HL-60 and CHL are grown in RPMI 1640 medium supported with 10% FBS and 1% Penicillin/Streptomycin. Adherent cells are grown in tissue culture flasks until they are 85-95% confluent prior to use. For suspension cells, cells are collected by spin down at 800 rpm/min for 5 min before use. Cells are grown in 96-well culture plates (3000 cells/well). The compounds (e.g., JSH-150) at various concentrations are added into the plates. Cell proliferation is determined after treatment with compounds (e.g., JSH-150) for 72 h. Cell viability is measured using the Cell Titer-Glo assay and luminescence is measured in a multilabel reader^[1].

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

Animal Administration^[1]

Mice^[1]
Five-week-old female nu/nu mice are used. Prior to implantation, cells are harvested during exponential growth. Five million MV4-11 cells in PBS are formulated as a 1:1 mixture with Matrigel and injected into the subcutaneous space on the right flank of nu/nu mice. Daily oral administration is initiated when MV4-11 tumors have reached a size of 200-400 mm³. Animals are then randomized into treatment groups of 5 mice each for efficacy studies. JSH-150 is delivered daily in a HKI solution (0.5% methocellulose/0.4% Tween80 in ddH₂O) by oral gavage. A range of doses of JSH-150 or its vehicle as control are administered. Female nu/nu mice bearing established MV4-11 tumor xenografts are treated with JSH-150 at 10, 20, and 30 mg/kg/d dosage or vehicle. Body weight is measured daily and tumor growth is measured every day after JSH-150 treatment. Tumor volume is calculated^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Beilei Wang, et al. Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor. Eur J Med Chem. 13 September 2018.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9799 mL	9.8994 mL	19.7988 mL	49.4971 mL
	5 mM	0.3960 mL	1.9799 mL	3.9598 mL	9.8994 mL
	10 mM	0.1980 mL	0.9899 mL	1.9799 mL	4.9497 mL
	15 mM	0.1320 mL	0.6600 mL	1.3199 mL	3.2998 mL
	20 mM	0.0990 mL	0.4950 mL	0.9899 mL	2.4749 mL
	25 mM	0.0792 mL	0.3960 mL	0.7920 mL	1.9799 mL
	30 mM	0.0660 mL	0.3300 mL	0.6600 mL	1.6499 mL
	40 mM	0.0495 mL	0.2475 mL	0.4950 mL	1.2374 mL
	50 mM	0.0396 mL	0.1980 mL	0.3960 mL	0.9899 mL
	60 mM	0.0330 mL	0.1650 mL	0.3300 mL	0.8250 mL
	80 mM	0.0247 mL	0.1237 mL	0.2475 mL	0.6187 mL
	100 mM	0.0198 mL	0.0990 mL	0.1980 mL	0.4950 mL

Keywords

JSH-150

1 Cited Publications

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JSH-150

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) JSH-150

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JSH-150

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) JSH-150

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JSH-150 Related Classifications

Art. -Nr.: HY-X0150