PROTAC PARP1 degrader
- Product Name
- PROTAC PARP1 degrader
- CAS No.
- 2369022-68-2
- Chemical Name
- PROTAC PARP1 degrader
- Synonyms
- PROTAC PARP1 degrader;2-(4-(1-(1-(4-((4R,5S)-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)-2-oxopiperazin-1-yl)-2-oxo-6,9,12,15-tetraoxa-3-azaheptadecan-17-yl)-1H-1,2,3-triazol-4-yl)phenyl)-2H-indazole-7-carboxamide;2-(4-{1-[14-(2-{4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1H-imidazole-1-carbonyl]-2-oxopiperazin-1-yl}acetamido)-3,6,9,12-tetraoxatetradecan-1-yl]-1H-1,2,3-triazol-4-yl}phenyl)-2H-indazole-7-carboxamide;2H-Indazole-7-carboxamide, 2-[4-[1-[17-[4-[[(4R,5S)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-oxo-1-piperazinyl]-16-oxo-3,6,9,12-tetraoxa-15-azaheptadec-1-yl]-1H-1,2,3-triazol-4-yl]phenyl]-
- CBNumber
- CB48054607
- Molecular Formula
- C58H63Cl2N11O10
- Formula Weight
- 1145.09
- MOL File
- 2369022-68-2.mol
PROTAC PARP1 degrader Property
- Density
- 1.39±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- form
- Solid
- pka
- 14.32±0.46(Predicted)
- color
- White to off-white
PROTAC PARP1 degrader Chemical Properties,Usage,Production
Uses
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader consists of E3 ubiquitinase ligand MDM2 ligand (HY-128836), blue part; target protein ligand PAPR1 ligand (HY-171543), red part; PROTAC linker N3-PEG4-C2-NH2 (HY-128834), black part[1][2].
Biological Activity
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
IC 50
PARP1; MDM2
References
[1]. Zhao Q, et al. Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule. Chem Commun (Camb). 2019 Jan 2;55(3):369-372.
PROTAC PARP1 degrader Preparation Products And Raw materials
Raw materials
Preparation Products
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