PARP1 PROTAC 180055

Chemical Structure : PARP1 PROTAC 180055

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货号: PC-23651Not For Human Use, Lab Use Only.

PARP1 PROTAC 180055 is a potent, PARP1-specific degradation PROTAC compound with DC50 of 180 nM and 240 nM in T47D and MDA-MB-231 cell lines, respectively.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

PARP1 PROTAC 180055 is a potent, PARP1-specific degradation PROTAC compound with DC50 of 180 nM and 240 nM in T47D and MDA-MB-231 cell lines, respectively.
180055 exhibits significant degradation potency towards PARP1 protein in 12 more cell lines, encompassing breast cancer cell lines (MDA-MB-468), ovarian cancer cell lines (IGROV1, A2780, Hey, CAOV1, OVK18, OC316, OVCAR3), colorectal cancer cell line (RKO), human acute T-lymphoblastic leukemia cell line (MOLT4), prostate cancer cell line (DU 145), as well as human osteosarcoma cell line (U-2 OS).
180055 is dependent on the ubiquitin-proteasome system, and does not affect other members of the PARP family, Tankyrase and PARP2.
180055 inhibits the catalytic activity of PARP1.
180055 protects cells from gene toxicity-induced cell death.
180055 (40 mg/kg) effectively degraded PARP1 in tumors derived from MOLT4-xenografted mice and mouse model of A2780 tumor xenografts with BRCA mutations, inhibits tumor growth.

物理化学性质&存储条件

分子量	920.16
分子式	C51H62FN7O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N1-(4-(8-fluoro-1-oxo-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-5-yl)benzyl)-N10-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-N1-methyldecanediamide

参考文献

1. Chen L, et al. Cell Death Dis. 2024 Dec 18;15(12):898.