SJ6986
Based on 1 publication(s) in Google Scholar
SJ6986 is an orally active GSPT1/2 molecular glue degrader, with a DC50 of 9.7 nM at 4 h and 2.1 nM at 24 h for GSPT1 degradation in MV4-11 cells. SJ6986 recruits GSPT1/2 to the CRBN E3 ligase complex, inducing ubiquitination and proteasomal degradation of GSPT1/2. SJ6986 triggers activation of the integrated stress response pathway and apoptosis downstream of GSPT1 degradation. SJ6986 serves as a chemical probe for investigating the functions of GSPT1/GSPT2 in vitro and in vivo. SJ6986 can be used for research on acute leukemia and medulloblastoma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.35%
- No. CAS: 2765625-93-0
- Fòrmula: C20H14F3N3O7S
- Peso molecular:497.40
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Almacenamiento: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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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
Publications Citing Use of MedChemExpress (MCE) SJ6986
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Customer Validation & Images
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WB
Ver todos los productos específicos de isoformas Eukaryotic Release Factor (eRF)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
eRF3a/GSPT1 |
eRF3b/GSPT2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MV4-11 | EC50 |
1.5 nM
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Antiproliferative activity against human MV4-11 (KMT2A-rearranged acute myeloid leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
Antiproliferative activity against human MV4-11 (KMT2A-rearranged acute myeloid leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
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34042448 |
| MHH-CALL-4 | EC50 |
0.4 nM
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Antiproliferative activity against human MHH-CALL-4 (CRLF2-rearranged JAK2-mutated acute lymphoblastic leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
Antiproliferative activity against human MHH-CALL-4 (CRLF2-rearranged JAK2-mutated acute lymphoblastic leukemia) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
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34042448 |
| MB002 cell | EC50 |
726 nM
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Antiproliferative activity against human MB002 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
Antiproliferative activity against human MB002 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
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34042448 |
| MB004 cell | EC50 |
336 nM
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Antiproliferative activity against human MB004 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
Antiproliferative activity against human MB004 (TP53-mutated Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
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34042448 |
| HD-MB03 | EC50 |
3583 nM
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Antiproliferative activity against human HD-MB03 (TP53 wild-type Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
Antiproliferative activity against human HD-MB03 (TP53 wild-type Group 3 medulloblastoma) cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay.
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34042448 |
| MV4-11 | DC50 |
9.7 nM
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Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 4 hrs, measured by immunoblot analysis.
Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 4 hrs, measured by immunoblot analysis.
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34042448 |
| MV4-11 | DC50 |
2.1 nM
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Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis.
Induction of GSPT1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis.
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34042448 |
| MV4-11 | DC50 |
30 nM
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Induction of IKZF1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis.
Induction of IKZF1 protein degradation in human MV4-11 cells incubated for 24 hrs, measured by immunoblot analysis.
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34042448 |
| MHH-CALL-4 | DC50 |
15 nM
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Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 4 hrs, measured by immunoblot analysis.
Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 4 hrs, measured by immunoblot analysis.
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34042448 |
| MHH-CALL-4 | DC50 |
3.5 nM
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Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis.
Induction of GSPT1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis.
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34042448 |
| MHH-CALL-4 | DC50 |
117 nM
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Induction of IKZF1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis.
Induction of IKZF1 protein degradation in human MHH-CALL-4 cells incubated for 24 hrs, measured by immunoblot analysis.
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34042448 |
| HEK-293T | EC50 |
0.1 nM
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Induction of HiBit-tagged GSPT1 protein degradation in human HEK293T cells incubated for 4 hrs, measured by Nano-Glo HiBiT lytic detection system.
Induction of HiBit-tagged GSPT1 protein degradation in human HEK293T cells incubated for 4 hrs, measured by Nano-Glo HiBiT lytic detection system.
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34042448 |
In Vitro
SJ6986 (Compound 6) inhibits the proliferation of MV4-11, MHH-CALL-4, MB002, MB004 and HD-MB03 cells after 72 h, with EC50 values of 1.5, 0.4, 726, 336 and 3583 nM[1].
SJ6986 (0.001-10 μM; 4 h, 24 h) rapidly degrades GSPT1 in MV4-11 cells, with a DC50 of 9.7 nM at 4 h and 2.1 nM at 24 h; it also induces delayed and less potent degradation of IKZF1, with a DC50 of 30 nM at 24 h[1].
SJ6986 (0.001-10 μM; 4 h, 24 h) rapidly degrades GSPT1 in MHH-CALL-4 cells, with a DC50 of 15 nM at 4 h and 3.5 nM at 24 h; it also induces delayed and weak degradation of IKZF1, with a DC50 of 117 nM at 24 h[1].
The antiproliferative activity of SJ6986 (72 h) in MV4-11 cells is completely dependent on the degradation of GSPT1[1].
SJ6986 (1 μM; 4 h) selectively degrades GSPT1 and GSPT2 in MV4-11 cells[1].
SJ6986 (1 h) potently binds to the CRBN-DDB1 complex in a cell-free competitive fluorescence polarization assay, with an IC50 of 15 nM[1].
SJ6986 (4 h) efficiently degrades HiBit-tagged GSPT1 in HEK293T cells, with an EC50 of 0.1 nM after 4 h of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.001, .01, 0.1, 1, 10 μM
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Incubation Time:4 h; 24 h
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Result:Induced dose-dependent GSPT1 degradation with a DC50 of 9.7 nM and 90% maximal degradation at 100 nM after 4 h.
Did not significantly reduce IKZF1 levels after 4 h.
Induced GSPT1 degradation with a DC50 of 2.1 nM and nearly complete degradation after 24 h.
Induced IKZF1 degradation with a DC50 of 30 nM after 24 h.
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Cell Line:MHH-CALL-4 cells
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Concentration:0.001, .01, 0.1, 1, 10 μM
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Incubation Time:4 h; 24 h
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Result:Induced dose-dependent GSPT1 degradation with a DC50 of 15 nM after 4 h.
Did not significantly reduce IKZF1 levels after 4 h.
Induced GSPT1 degradation with a DC50 of 3.5 nM and nearly complete degradation after 24 h.
Induced IKZF1 degradation with a DC50 of 117 nM and maximal degradation less than 50% after 24 h.
Parmacokinetics
Chemical Information
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No. CAS 2765625-93-0
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Appearance Solid
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Peso molecular 497.40
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Fòrmula C20H14F3N3O7S
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Color White to yellow
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SMILES
O=S(C1=CC=CC=C1OC(F)(F)F)(NC2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3=O)=O)C=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Leukemia
Targeting of IRAK4 and GSPT1 enhances therapeutic efficacy in AML via c-Myc destabilization. [Abstract]2025 Sep;39(9):2163-2173. PMID: 40670672
SJ6986 purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Sep;39(9):2163-2173. [Abstract]
Immunoblots for c-MYC and GSPT1 in THP1 and HL60 cells cultured with CA-4948 (10 µM) or vehicle for 14 days and then treated with the indicated GSPT1 degraders (SJ6986; 10 µM; CC-885, 0.5 nM) for 24 h.
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (201.05 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, 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: ≥ 2.5 mg/mL (5.03 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.
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.
Pureza y Documentación
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Ficha de datos (290 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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. 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 | 2.0105 mL | 10.0523 mL | 20.1045 mL | 50.2614 mL |
| 5 mM | 0.4021 mL | 2.0105 mL | 4.0209 mL | 10.0523 mL | |
| 10 mM | 0.2010 mL | 1.0052 mL | 2.0105 mL | 5.0261 mL | |
| 15 mM | 0.1340 mL | 0.6702 mL | 1.3403 mL | 3.3508 mL | |
| 20 mM | 0.1005 mL | 0.5026 mL | 1.0052 mL | 2.5131 mL | |
| 25 mM | 0.0804 mL | 0.4021 mL | 0.8042 mL | 2.0105 mL | |
| 30 mM | 0.0670 mL | 0.3351 mL | 0.6702 mL | 1.6754 mL | |
| 40 mM | 0.0503 mL | 0.2513 mL | 0.5026 mL | 1.2565 mL | |
| 50 mM | 0.0402 mL | 0.2010 mL | 0.4021 mL | 1.0052 mL | |
| 60 mM | 0.0335 mL | 0.1675 mL | 0.3351 mL | 0.8377 mL | |
| 80 mM | 0.0251 mL | 0.1257 mL | 0.2513 mL | 0.6283 mL | |
| 100 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5026 mL |
SJ6986 Related Classifications
HY-132199 Related Classifications
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