SBP-3264
Based on 2 publication(s) in Google Scholar
SBP-3264 is a YAP activator and STK/MST inhibitor with IC50 values of 36 nM against STK3/MST2 and 24 nM against STK4/MST1. SBP-3264 modulates the Hippo signaling pathway. SBP-3264 can be used for the research of acute myeloid leukemia.
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- Pureza: 98.50%
- No. CAS: 2869148-13-8
- Fòrmula: C19H20ClN5O
- Peso molecular:369.85
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SBP-3264
MoreVer todos los productos específicos de isoformas YAP
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Actividad biológica
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MST1 24 nM (IC50) |
MST2 36 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
5.8 μM
Compound: 20; SBP-3264
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Antiproliferation activity against human MOLM-13 cells incubated for 72 hrs by celltiter-glo assay
Antiproliferation activity against human MOLM-13 cells incubated for 72 hrs by celltiter-glo assay
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[PMID: 34807584] |
| MV4-11 | IC50 |
3.7 μM
Compound: 20; SBP-3264
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Antiproliferation activity against human MV4-11 cells incubated for 72 hrs by celltiter-glo assay
Antiproliferation activity against human MV4-11 cells incubated for 72 hrs by celltiter-glo assay
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[PMID: 34807584] |
SBP-3264 (Compound 20) potently inhibits purified STK3 and STK4 proteins with IC50 values of 36 nM and 24 nM, respectively, in an ADP-Glo kinase assay[1].
SBP-3264 (2 h) engages intracellular STK3 and STK4 in HEK293 cells with IC50 values of 139 nM and 122 nM, respectively, and shows ≥10-fold selectivity over LRRK2[1].
SBP-3264 (10 μM; 4 h) significantly reduces phosphorylated MOB1 levels in HEK293 cells[1].
SBP-3264 (0.04-10 μM; 4 h) inhibits STK3/4-mediated MOB1 phosphorylation in MOLM 13 AML cells with an IC50 of 413 nM[1].
SBP-3264 (72 h) inhibits proliferation of human AML cell lines, including FLT3-mutated MOLM 13 (IC50 5.8 μM) and MV4:11 (IC50 3.7 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:10 μM
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Incubation Time:4 h
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Result:Produced a significant decrease in relative p-MOB1 levels compared to DMSO-treated control cells.
Confirmed inhibition of STK3/4-mediated Hippo pathway signaling.
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Cell Line:MOLM 13 human AML cells
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Concentration:0.04 μM; 0.1 μM; 0.3 μM; 1.1 μM; 3.3 μM; 10 μM
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Incubation Time:4 h
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Result:Inhibited MOB1 phosphorylation in a concentration-dependent manner, with an IC50 of 413 nM.
Significantly reduced p-MOB1 levels at concentrations ≥0.3 μM.
| Species | Dose | Route | Cmax | Tmax | AUC0-t | T1/2 |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 11.8 μM | 0.25 h | 8.1 μM/L·h | 5.3 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (adult female)[1]
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Dosage:20 mg/kg
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Administration:i.p.; single dose
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Result:Reduced phosphorylated MOB1 (Thr35) levels in mouse liver tissue with statistical significance (p ≤ 0.001) relative to vehicle-treated mice.
Chemical Information
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No. CAS 2869148-13-8
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Appearance Solid
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Peso molecular 369.85
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Fòrmula C19H20ClN5O
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Color Off-white to light yellow
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SMILES
ClC1=CC=CC(C2=CNC3=NC=NC(N4CCC(CC4)NC(C)=O)=C32)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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EMBO J
2024 Oct;43(20):4752-4785. PMID: 39256562 -
Mol Cell Proteomics
Proteomics and Phosphoproteomics Revealed Dysregulated Kinases and Potential Therapy for Liver Fibrosis. [Abstract]2025 May 12:100991. PMID: 40368138
Solvente y solubilidad
DMSO : 62.5 mg/mL (168.99 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (5.62 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.62 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (protect from light). 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 | 2.7038 mL | 13.5190 mL | 27.0380 mL | 67.5950 mL |
| 5 mM | 0.5408 mL | 2.7038 mL | 5.4076 mL | 13.5190 mL | |
| 10 mM | 0.2704 mL | 1.3519 mL | 2.7038 mL | 6.7595 mL | |
| 15 mM | 0.1803 mL | 0.9013 mL | 1.8025 mL | 4.5063 mL | |
| 20 mM | 0.1352 mL | 0.6759 mL | 1.3519 mL | 3.3797 mL | |
| 25 mM | 0.1082 mL | 0.5408 mL | 1.0815 mL | 2.7038 mL | |
| 30 mM | 0.0901 mL | 0.4506 mL | 0.9013 mL | 2.2532 mL | |
| 40 mM | 0.0676 mL | 0.3380 mL | 0.6759 mL | 1.6899 mL | |
| 50 mM | 0.0541 mL | 0.2704 mL | 0.5408 mL | 1.3519 mL | |
| 60 mM | 0.0451 mL | 0.2253 mL | 0.4506 mL | 1.1266 mL | |
| 80 mM | 0.0338 mL | 0.1690 mL | 0.3380 mL | 0.8449 mL | |
| 100 mM | 0.0270 mL | 0.1352 mL | 0.2704 mL | 0.6759 mL |
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