JSH-150
Based on 1 publication(s) in Google Scholar
JSH-150 is a highly selective and potent CDK9 inhibitor with an IC50 of 1 nM.
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- Pureté: 98.08%
- CAS No.: 2247481-21-4
- Formule: C24H33ClN6O2S
- Masse moléculaire:505.08
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) JSH-150
More
Activité biologique
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | GI50 |
0.044 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| A-431 | GI50 |
0.019 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| CHO | GI50 |
1.1 μM
Compound: 40; JSH-150
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Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay
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[PMID: 30253346] |
| COLO 205 | GI50 |
0.014 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| GISTT1 | GI50 |
0.0021 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| HL-60 | GI50 |
0.056 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| MOLM-13 | GI50 |
0.012 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| MOLM-14 | GI50 |
0.0011 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| MV4-11 | GI50 |
0.012 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| MV4-11 | IC50 |
12 nM
Compound: 37; JSH-150
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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
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[PMID: 38564299] |
| OCI-AML-3 | GI50 |
0.0066 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| Ramos | GI50 |
0.013 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| SKM-1 | GI50 |
0.012 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| SK-N-BE(2)-M17 | GI50 |
0.034 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
| U-937 | GI50 |
0.002 μM
Compound: 40; JSH-150
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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
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[PMID: 30253346] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2247481-21-4
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Appearance Solid
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Masse moléculaire 505.08
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Formule C24H33ClN6O2S
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Color Off-white to yellow
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SMILES
COCCN[C@@H]1CC[C@@H](NC2=NC=C(Cl)C(C3=CSC(NCC4(C#N)CCOCC4)=N3)=C2)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
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Most Recent
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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
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
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.
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.
Pureté et documentation
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Fiche technique (278 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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, 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 |
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