2. PROTAC Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. PROTACs Survivin PARP
  4. PROTAC survivin degrader-1

PROTAC survivin degrader-1 is an orally active, CNS-penetrant survivin-targeting PROTAC. PROTAC survivin degrader-1 induces degradation of survivin via the ubiquitin proteasome system. PROTAC survivin degrader-1 can be used for the research of glioblastoma.
(Pink: Ligands for Target Protein for PROTAC ligand (HY-186213); Blue: Ligands for E3 Ligase ligand (HY-W453715); Black: linker).

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

PROTAC survivin degrader-1

PROTAC survivin degrader-1 Chemical Structure

CAS No. : 3079079-69-6

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PROTAC survivin degrader-1 Related Antibodies

Top Publications Citing Use of Products

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

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Description

PROTAC survivin degrader-1 is an orally active, CNS-penetrant survivin-targeting PROTAC. PROTAC survivin degrader-1 induces degradation of survivin via the ubiquitin proteasome system. PROTAC survivin degrader-1 can be used for the research of glioblastoma[1]. (Pink: Ligands for Target Protein for PROTAC ligand (HY-186213); Blue: Ligands for E3 Ligase ligand (HY-W453715); Black: linker).

In Vitro

PROTAC survivin degrader-1 (compound 11) (0.03-3 μM; 24 h) reduces survivin protein levels in U87 and CL261 glioblastoma cells[1].
PROTAC survivin degrader-1 (0.01-1.0 μM; 48 h) induces a DNA damage response in GL261 glioblastoma cells and potentiates the DNA damage, cell killing, and apoptotic effects of 2Gy irradiation[1].
PROTAC survivin degrader-1 (0.5 μM; 2 weeks) potentiates the cytotoxic effect of 0Gy, 2Gy, 4Gy, 6Gy, and 8Gy irradiation in GL261 glioblastoma cells[1].
PROTAC survivin degrader-1 (10-100 nM; 24 h) induces proteasome-dependent survivin degradation in U87 glioblastoma cells[1].

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

PROTAC survivin degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: GL261 glioblastoma cell line
Concentration: 0.01; 0.1; 0.5; 1.0 μM
Incubation Time: 48 h
Result: Increased ATM and CHK1 phosphorylation levels, indicating induction of a DNA damage response.
Potentiated the DNA damage response when combined with 2Gy irradiation.
Increased cleaved PARP levels, enhancing cancer cell killing.
Increased levels of cleaved Caspase 3 and Caspase 9, enhancing apoptosis.

Western Blot Analysis[1]

Cell Line: U87 glioblastoma cell line
Concentration: 10; 100 nM
Incubation Time: 24 h
Result: Reduced survivin protein levels when treated alone.
Prevented the PROTAC-induced reduction of survivin protein levels when co-treated with MG132 (HY-13259).
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-last AUC0-inf MRT0-last MRT0-inf
Mice[1] 206 mg/kg p.o. 125 ng/mL 6 h 1.23 h 680 ng·h/mL 687 ng·h/mL 4.74 h 4.84 h
Molecular Weight

884.35

Formula

C48H43ClFN7O7
CAS No.
SMILES

N#CC1=C(C2=CC(OCC3=CC=CC=C3)=CC=C2)C=C(C4=C(O)C=C(N5CCC(CC5)CN6CCN(CC6)C7=CC=C8C(N(C9C(NC(CC9)=O)=O)C(C8=C7F)=O)=O)C(Cl)=C4)NC1=O
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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PROTAC survivin 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:

PROTAC survivin degrader-13079079-69-6PROTAC survivin degrader1PROTAC survivin degrader 1PROTACsSurvivinPARPpoly ADP ribose polymeraseirradiationmale C57BL/6J miceDNA damage responseglioblastomasurvivinGL261 glioblastoma cellsubiquitin proteasome systemU87 glioblastoma cellsmale Sprague-Dawley ratsblood-brain barrierInhibitorinhibitorinhibit

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