LD5097
LD5097 is a highly effective and selective PROTAC degrader targeting RIPK1. LD5097 can rapidly and efficiently downregulate RIPK1 and significantly enhance TNFα-mediated apoptosis in Jurkat cells. LD5097 significantly increases the levels of cleaved caspase-3/7 and PARP. LD5097 can be used for the study of acute T-lymphoblastic leukemia.
(Pink: RIPK1 ligand (HY-179235); Blue: VHL ligand (HY-47070); Black: linker (HY-179236)).
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- Formule: C74H75F4N13O8S
- Masse moléculaire:1382.53
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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Caspase-3 |
Caspase-7 |
LD5097 (Compound 24b) (24 h) exhibits potent RIPK1 (DC50 = 0.7 nM) degradation activity in Jurkat nLuc-RIPK1 cells[1].
LD5097 (1.6-1000 nM, 24 h) results in a dose-dependent degradation of endogenous RIPK1 after 24 h (DC50 = 2.6 nM) in Jurkat cells[1].
LD5097 exhibits potent degradation of endogenous RIPK1, with DC50 values of 2.8 and 0.8 nM in both MOLM14 and U937 cells, respectively[1].
LD5097 (100 nM, 0.5-24 h) can completely degrade RIPK1 in Jurkat cells within 2 hours[1].
LD5097's (100 nM, 24 h) degradation ability depends on a bifunctional PROTAC mechanism, which requires simultaneous binding to RIPK1 and VHL E3 ligases[1].
LD5097 (100 nM, 72 h) enhances TNFα-mediated apoptosis in Jurkat cells[1].
LD5097 (0-10 μM, 24 h) achieves complete degradation of RIPK1 at 100 nM in Ramos cells but fails to do so even at 10 μM in A20 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat cells
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Concentration:100 nM
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Incubation Time:0.5 h, 1 h, 2 h, 4 h, 6 h, 12 h, 24 h
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Result:Completely degraded RIPK1 in Jurkat cells within 2 hours.
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Cell Line:Jurkat cells
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Concentration:100 nM
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Incubation Time:72 h
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Result:Combined with TNFα significantly induced apoptosis.
Cleaved caspase-3/7 and PARP levels increased.
Apoptosis could be reversed by Z-VAD-FMK (HY-16658B).
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Cell Line:Ramos cells, A20 cells
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Concentration:0 μM, 0.1 μM, 1 μM, 10 μM
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Incubation Time:24 h
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Result:Complete degradation of RIPK1 at 100 nM in Ramos cells, but failed to do so even at 10 μM in A20 cells.
| Species | Dose | Route | CL | T1/2 | Cmax | AUC0-∞ |
|---|---|---|---|---|---|---|
| Mice | 1 mg/kg | i.v. | 2.3 mL/min/kg | 7.3 h | 19633 ng/mL | 7256 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old female nude mice were subcutaneously injected with 2.5 × 106 Jurkat cells suspended in a 1:1 mixture with Matrigel[1].
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Dosage:10 mg/kg
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Administration:I.v., once
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Result:Induced a decrease of more than 70% in RIPK1 protein levels in tumor tissue at both 6 and 24 hours after administration.
Chemical Information
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Masse moléculaire 1382.53
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Formule C74H75F4N13O8S
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SMILES
O=C(N1CCC2=C1C=CC(C3=CN(C4=NC=NC(N)=C34)C5CCN(CC5)C(C6=CC=C(C=C6)C#CC7=CN=C(C=C7)N8CCN(CC8)C(C[C@@H](C9=CC=C(C=C9)C%10=C(N=CS%10)C)NC([C@@H]%11C[C@H](CN%11C([C@@H](NC(C%12(CC%12)F)=O)C(C)(C)C)=O)O)=O)=O)=O)=C2)CC%13=CC=CC(OC(F)(F)F)=C%13
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LD5097 Related Classifications
HY-179234 Related Classifications
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