| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C28H33ClN4O5 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSPT1 degrader-1 is a highly selective degrader of GSPT1 that promotes its degradation via the ubiquitin-proteasome system. It induces G0/G1 phase arrest and apoptosis and inhibits proliferation in leukemia cells, lowering levels of CDK6 and Cyclin B1 while raising levels of activated caspase-3 and caspase-9, supporting its use in leukemia research[1]. It has the molecular formula C28H33ClN4O5 and a molecular weight of 541.04 g/mol.
Physical & Chemical Properties
| CAS Number | 3037491-05-4 |
|---|---|
| Molecular Formula | C28H33ClN4O5 |
| Molecular Weight | 541.04 g/mol |
| SMILES | CC1=C(CN(C)CCOC)C=C(NC(CCC2=CC=C3CN(C4CCC(NC4=O)=O)C(C3=C2)=O)=O)C=C1Cl |
| Target | eRF3a/GSPT1 |
| Signaling Pathway | PROTAC; Apoptosis; Cell Cycle/DNA Damage |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
In U937 acute myeloid leukemia cells, dose- and time-dependent degradation of GSPT1 is potently induced by GSPT1 degrader-1 (0-300 nM; 0-24 h), with a DC50 of 35 nM; the half-life of GSPT1 is shortened to 6.3 h[1]. Dose-dependent GSPT1 degradation is potently induced by GSPT1 degrader-1 (0-300 nM; 6 h) in MOLT-4 acute lymphoblastic leukemia cells as well as in MV4-11 acute myeloid leukemia cells[1]. GSPT1 degradation in U937 acute myeloid leukemia cells is induced by GSPT1 degrader-1 (100 nM; 6 h) through the ubiquitin-proteasome system[1]. Proliferation of U937, MOLT-4 and MV4-11 leukemia cells is potently inhibited by GSPT1 degrader-1 (72 h), with IC50 values of 0.019, 0.006 and 0.027 μM, respectively[1]. In U937 acute myeloid leukemia cells, GSPT1 degrader-1 (0-100 nM; 24 h) induces dose-dependent G0/G1 phase arrest and apoptosis, together with lower levels of CDK6 and cyclin B1 and higher levels of activated caspase-3 and activated caspase-9[1].
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 or 5 μM MLN-4924) |
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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