2. PROTAC Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. PROTACs RIP kinase Apoptosis Caspase PARP
  4. 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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LD5097

LD5097 Chemical Structure

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LD5097 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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RIPK1 RIPK2 RIPK3

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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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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

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[1]. (Pink: RIPK1 ligand (HY-179235); Blue: VHL ligand (HY-47070); Black: linker (HY-179236)).

IC50 & Target[1]

Caspase-3

 

Caspase-7

 

In Vitro

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.

LD5097 Related Antibodies

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 100 nM
Incubation Time: 0.5 h, 1 h, 2 h, 4 h, 6 h, 12 h, 24 h
Result: Completely degraded RIPK1 in Jurkat cells within 2 hours.

Apoptosis Analysis[1]

Cell Line: Jurkat cells
Concentration: 100 nM
Incubation Time: 72 h
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).

Western Blot Analysis[1]

Cell Line: Ramos cells, A20 cells
Concentration: 0 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Complete degradation of RIPK1 at 100 nM in Ramos cells, but failed to do so even at 10 μM in A20 cells.
Parmacokinetics
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
In Vivo

LD5097 (Compound 24b) (10 mg/kg, i.v., once) significantly degrades RIPK1 in Jurkat cell xenograft mice tumor[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 10 mg/kg
Administration: I.v., once
Result: Induced a decrease of more than 70% in RIPK1 protein levels in tumor tissue at both 6 and 24 hours after administration.
Molecular Weight

1382.53

Formula

C74H75F4N13O8S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LD5097 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:

LD5097LD 5097LD-5097PROTACsRIP kinaseApoptosisCaspasePARPReceptor-interacting protein kinasesRIPKpoly ADP ribose polymeraseRIPK1 DegradersPROTACJurkat Xenograft ModelInhibitorinhibitorinhibit

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