2. Apoptosis Cell Cycle/DNA Damage
  3. Apoptosis CDK Caspase
  4. 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.

For research use only. We do not sell to patients.

GSPT1 degrader-1

GSPT1 degrader-1 Chemical Structure

CAS No. : 3037491-05-4

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GSPT1 degrader-1 Related Antibodies

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target

GSPT1[1]
Cellular Effect
Cell Line Type Value Description References
MOLT-4 IC50
0.006 μM
Compound: 9q
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
[PMID: 37418973]
MV4-11 IC50
0.027 μM
Compound: 9q
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
[PMID: 37418973]
U-937 IC50
0.019 μM
Compound: 9q
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
[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.

GSPT1 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: U937 acute myeloid leukemia cells
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)
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)
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.

Western Blot Analysis[1]

Cell Line: MOLT-4 acute lymphocytic leukemia cells, MV4-11 acute myeloid leukemia cells
Concentration: 0, 3.7, 11.1, 33.3, 100, 300 nM
Incubation Time: 6 h
Result: Effectively induced dose-dependent degradation of GSPT1 in both MOLT-4 and MV4-11 leukemia cell lines.

Western Blot Analysis[1]

Cell Line: U937 acute myeloid leukemia cells
Concentration: 100 nM (with 2 h pretreatment of 5 μM MG-132 (HY-13259) or 5 μM MLN-4924 (HY-70062))
Incubation Time: 6 h (with 2 h pretreatment)
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.

Cell Cycle Analysis[1]

Cell Line: U937 acute myeloid leukemia cells
Concentration: 0, 10, 30, 100 nM
Incubation Time: 24 h
Result: Induced dose-dependent G0/G1 phase arrest.

Apoptosis Analysis[1]

Cell Line: U937 acute myeloid leukemia cells
Concentration: 0, 10, 30, 100 nM
Incubation Time: 24 h
Result: Induced apoptosis.
Molecular Weight

541.04

Formula

C28H33ClN4O5
CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GSPT1 degrader-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSPT1 degrader-13037491-05-4ApoptosisCDKCaspaseCyclin dependent kinaseGSPT1 degraderU937 cellsMOLT-4 cellsMV4-11 cellsapoptosisleukemiaInhibitorinhibitorinhibit

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