SJPYT-195
Based on 1 Customer Validation
SJPYT-195 is a molecular glue degrader targeting GSPT1, with a DC50 of 310 nM. SJPYT-195 mediates CRBN-dependent and proteasome-dependent degradation of GSPT1 by forming a stable ternary complex with CRBN and GSPT1. As a secondary effect of GSPT1 degradation, SJPYT-195 induces a decrease in PXR protein levels. SJPYT-195 is applicable to research related to acute myeloid leukemia.
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- Purity : 98.07%
- CAS No.: 2973762-16-0
- 화학식: C35H34N6O8
- 분자량:666.68
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Eukaryotic Release Factor (eRF) Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
eRF3a/GSPT1 310 nM (DC50) |
PXR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| SNU-C4 | CC50 |
3.3 nM
Compound: 18; SJPYT-195
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Cytotoxicity against PXR knock in human SNU-C4 cells measured after 72 hrs by celltiter-glo assay
Cytotoxicity against PXR knock in human SNU-C4 cells measured after 72 hrs by celltiter-glo assay
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[PMID: 35978691] |
In Vitro
SJPYT-195 (0.001-100 μM; 24 h) dose-dependently reduces HiBiT-FKBPF36V-PXR protein levels in HepG2 cells cotransfected with CRBN[1].
SJPYT-195 (10 μM; 24 h) reduces PXR RNA levels in SNU-C4 3xFLAG-PXR KI cells after 24 h treatment with 10 μM, with no substantial reduction seen at 12 h with 5 μM[1].
SJPYT-195 (0.00001-10 μM) weakly binds the purified PXR ligand binding domain in a TR-FRET assay[1].
SJPYT-195 (5 μM; 12 h) selectively downregulates GSPT1, GSPT2, ZFP91, CYP1A1, and BRIP1, and upregulates FOS in SNU-C4 3xFLAG-PXR KI cells[1].
SJPYT-195 (0.00001-10 μM) binds purified CRBN with an EC50 of 31 nM in a TR-FRET assay[1].
SJPYT-195 is a potent, proteasome- and CRBN-dependent molecular glue degrader of GSPT1 in SNU-C4 3xFLAG-PXR KI cells, with a GSPT1 DC50 < 10 nM and cell proliferation IC50 of 440 nM.
SJPYT-195 (0.003-50 μM; 2-48 h) mediates proteasome-dependent degradation of endogenous 3xFLAG-PXR in SNU-C4 3xFLAG-PXR KI cells with a DC50 of 310 nM after 24 h treatment, and reduces PXR protein levels over a 48 h time course[1].
SJPYT-195 (0.001-10 μM; 24 h) mediates CRBN- and proteasome-dependent degradation of GSPT1 in SNU-C4 3xFLAG-PXR KI cells at concentrations lower than those needed for PXR reduction[1].
SJPYT-195 (0.00001-100 μM; 72 h) is cytotoxic to SNU-C4 3xFLAG-PXR KI cells with a CC50 of 440 nM after 72 h treatment, with cytotoxicity partially mediated by GSPT1 degradation[1].
SJPYT-195 (10 μM; 24 h) induces complete loss of GSPT1 protein in SNU-C4 3xFLAG-PXR KI cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU-C4 3xFLAG-PXR KI colorectal cancer cells
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Concentration:0.003-50 μM (24 h incubation); 10 μM (2-48 h incubation); 10 μM (24 h incubation with MG-132)
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Incubation Time:2-48 h
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Result:Potently and efficaciously reduced endogenous 3xFLAG-PXR protein with a half maximal degradation concentration (DC50) of 310 nM and maximum degradation efficacy (DMax) of 85% after 24 h treatment.
Decreased PXR protein levels gradually over time, with substantial reduction observed by 24 h.
Rescued PXR protein levels by co-treatment with the proteasome inhibitor MG-132.
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Cell Line:SNU-C4 3xFLAG-PXR KI cells
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Concentration:10 μM (2-48 h incubation); 5 μM (12 h incubation)
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Incubation Time:2-48 h
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Result:Drastically reduced PXR RNA levels after 24 h treatment.
Showed negligible reduction of PXR RNA levels after 12 h treatment.
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Cell Line:SNU-C4 3xFLAG-PXR KI cells
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Concentration:0.001-10 μM (24 h incubation); 10 μM (24 h incubation with MG-132); 0.01-10 μM (24 h incubation after CRBN siRNA transfection)
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Incubation Time:24 h
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Result:Depleted GSPT1 protein at concentrations lower than those required to reduce PXR.
Rescued GSPT1 loss by co-treatment with MG-132.
Prevented GSPT1 degradation via siRNA-mediated CRBN knockdown.
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Cell Line:SNU-C4 3xFLAG-PXR KI cells; SNU-C4 3xFLAG-PXR KI cells stably expressing empty vector, HA-GSPT1, or HA-GSPT1G575N
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Concentration:0.00001-100 μM
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Incubation Time:72 h
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Result:Exhibited a half maximal cytotoxic concentration (CC50) of 440 nM in parental SNU-C4 3xFLAG-PXR KI cells.
Rendered cells partially resistant to induced cytotoxicity via overexpression of the degradation-resistant GSPT1G575N mutant.
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Cell Line:SNU-C4 3xFLAG-PXR KI cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced 100% loss of GSPT1 protein relative to DMSO control.
Chemical Information
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CAS No. 2973762-16-0
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Appearance Solid
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분자량 666.68
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화학식 C35H34N6O8
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Color White to off-white
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SMILES
O=C(C1=C(C)N(C2=CC(OC)=CC=C2OC)N=N1)NC3=CC(OC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=CC(C(C)(C)C)=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 50 mg/mL (75.00 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. 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. 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)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.12 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (2.50 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
In Vivo Dissolution Calculator
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.
순도&문서
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Data Sheet (290 KB)
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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)
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Handling Instructions (2659 KB)
References
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.5000 mL | 7.4999 mL | 14.9997 mL | 37.4993 mL |
| 5 mM | 0.3000 mL | 1.5000 mL | 2.9999 mL | 7.4999 mL | |
| 10 mM | 0.1500 mL | 0.7500 mL | 1.5000 mL | 3.7499 mL | |
| 15 mM | 0.1000 mL | 0.5000 mL | 1.0000 mL | 2.5000 mL | |
| 20 mM | 0.0750 mL | 0.3750 mL | 0.7500 mL | 1.8750 mL | |
| 25 mM | 0.0600 mL | 0.3000 mL | 0.6000 mL | 1.5000 mL | |
| 30 mM | 0.0500 mL | 0.2500 mL | 0.5000 mL | 1.2500 mL | |
| 40 mM | 0.0375 mL | 0.1875 mL | 0.3750 mL | 0.9375 mL | |
| 50 mM | 0.0300 mL | 0.1500 mL | 0.3000 mL | 0.7500 mL | |
| 60 mM | 0.0250 mL | 0.1250 mL | 0.2500 mL | 0.6250 mL |
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