GSPT1 degrader-1
GSPT1 degrader-1 is a highly selective degrader targeting GSPT1. GSPT1 degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G0/G1 phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research.
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- CAS. Nr.: 3037491-05-4
- Formel: C28H33ClN4O5
- Molecular Weight:541.04
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
eRF3a/GSPT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | IC50 |
0.006 μM
Compound: 9q
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Antiproliferative activity against human MOLT-4 cells measured after 72 hrs by CCK-8 method
Antiproliferative activity against human MOLT-4 cells measured after 72 hrs by CCK-8 method
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[PMID: 37418973] |
| MV4-11 | IC50 |
0.027 μM
Compound: 9q
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Antiproliferative activity against human MV4-11 cells measured after 72 hrs by CCK-8 method
Antiproliferative activity against human MV4-11 cells measured after 72 hrs by CCK-8 method
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[PMID: 37418973] |
| U-937 | IC50 |
0.019 μM
Compound: 9q
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Antiproliferative activity against human U-937 cells measured after 72 hrs by CCK-8 method
Antiproliferative activity against human U-937 cells measured after 72 hrs by CCK-8 method
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[PMID: 37418973] |
In Vitro
GSPT1 degrader-1 (Compound 9q) (0-300 nM; 0-24 h) potently induces dose- and time-dependent degradation of GSPT1 in U937 acute myeloid leukemia cells, with a DC50 of 35 nM and the half-life of GSPT1 shortened to 6.3 h[1].
GSPT1 degrader-1 (0-300 nM; 6 h) potently induces dose-dependent degradation of GSPT1 in MOLT-4 acute lymphoblastic leukemia cells and MV4-11 acute myeloid leukemia cells[1].
GSPT1 degrader-1 (100 nM; 6 h) induces the degradation of GSPT1 in U937 acute myeloid leukemia cells via the ubiquitin-proteasome system[1].
GSPT1 degrader-1 (72 h) potently inhibits the proliferation of U937, MOLT-4 and MV4-11 leukemia cells, with IC50 values of 0.019, 0.006 and 0.027 μM, respectively[1].
GSPT1 degrader-1 (0-100 nM; 24 h) induces dose-dependent G0/G1 phase arrest and apoptosis in U937 acute myeloid leukemia cells, accompanied by decreased levels of CDK6 and cyclin B1, as well as increased levels of activated caspase-3 and activated caspase-9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937 acute myeloid leukemia cells
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Concentration:0, 3.7, 11.1, 33.3, 100, 300 nM (6 h incubation); 100 nM (0-24 h incubation); 100 nM (co-treated with 10 μM cycloheximide, 0-24 h incubation)
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Incubation Time:6 h (0-300 nM); 0, 2, 4, 6, 8, 12, 24 h (100 nM); 0-24 h (100 nM + 10 μM cycloheximide)
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Result:Induced dose-dependent GSPT1 degradation, achieving a maximal degradation rate of 81.65% at 300 nM after 6 h.
Observed time-dependent degradation with significant depletion starting at 4 h and maximal degradation at 24 h with 100 nM treatment.
Shortened the biological half-life of GSPT1 from 53.4 h to 6.3 h when protein synthesis was blocked with cycloheximide.
Potently degraded GSPT1 with a DC50 of 35 nM in U937 cells.
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Cell Line:MOLT-4 acute lymphocytic leukemia cells, MV4-11 acute myeloid leukemia cells
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Concentration:0, 3.7, 11.1, 33.3, 100, 300 nM
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Incubation Time:6 h
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Result:Effectively induced dose-dependent degradation of GSPT1 in both MOLT-4 and MV4-11 leukemia cell lines.
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Cell Line:U937 acute myeloid leukemia cells
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Concentration:100 nM (with 2 h pretreatment of 5 μM MG-132 (HY-13259) or 5 μM MLN-4924 (HY-70062))
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Incubation Time:6 h (with 2 h pretreatment)
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Result:Increased the ubiquitination level of GSPT1 in U937 cells.
Allowed full rescue of GSPT1 protein levels from degradation when cells were pretreated with either the proteasome inhibitor MG-132 or the NEDD8-activating enzyme inhibitor MLN-4924.
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Cell Line:U937 acute myeloid leukemia cells
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Concentration:0, 10, 30, 100 nM
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Incubation Time:24 h
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Result:Induced dose-dependent G0/G1 phase arrest.
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Cell Line:U937 acute myeloid leukemia cells
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Concentration:0, 10, 30, 100 nM
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Incubation Time:24 h
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Result:Induced apoptosis.
Chemical Information
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CAS. Nr. 3037491-05-4
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Molecular Weight 541.04
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Formel C28H33ClN4O5
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SMILES
CC1=C(CN(C)CCOC)C=C(NC(CCC2=CC=C3CN(C4CCC(NC4=O)=O)C(C3=C2)=O)=O)C=C1Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GSPT1 degrader-1 Related Classifications
HY-155552 Related Classifications
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