PARP Degrader

Apoptosis inducer 34 (Compound 4) is a small molecule compound that induces apoptosis by directly activating the intrinsic apoptotic pathway. Apoptosis inducer 34 promotes Apaf-1 oligomerization to form mature apoptosomes, thereby activating caspase-9 and caspase-3. It significantly activates the apoptotic pathway in Jurkat cells by enhancing the cytochrome c-dependent apoptotic signaling pathway, inducing PARP cleavage and chromosomal DNA fragmentation. Furthermore, Apoptosis inducer 34 exhibits low toxicity to normal cells, demonstrating potential for selective targeting of cancer cells. Apoptosis inducer 34 is a promising candidate for studying cancer related to apoptotic pathways.

PARP1 degrader-3 is a selective PARP1 degrader derived from Olaparib (HY-10162) bearing a bicyclo[1.1.1]pentane (BCP) hydrophobic tag. PARP1 degrader-3 degrades PARP1 with a DC₅₀ of 4.31 μM. PARP1 degrader-3 induces PARP1 degradation primarily through the ubiquitin-proteasome system, and the HSP70/HSP90-associated protein quality control pathway may be involved in this process. PARP1 degrader-3 can be used for colorectal cancer-related research.

CPP-13 is a selective PARP1 PROTAC degrader with a DC₅₀ of 0.48 nM. CPP-13 induces CRBN-dependent ubiquitination and proteasomal degradation of PARP1. CPP-13 induces DNA damage. CPP-13 inhibits the growth of BRCA-deficient breast cancer and pancreatic cancer. CPP-13 can be used in studies related to BRCA-deficient breast cancer and BRCA-deficient pancreatic cancer.

PROTAC PARP1 degrader-3 is a PARP1 PROTAC degrader with a DC₅₀ of 58.14 nM. PROTAC PARP1 degrader-3 promotes the ubiquitination and degradation of PARP1 via the ubiquitin-proteasome system. PROTAC PARP1 degrader-3 acts synergistically with SN-38 (HY-13704) to inhibit colorectal cancer. PROTAC PARP1 degrader-3 can be used in studies related to colorectal cancer.

XZ8078 is a potent, selective dual-target PROTAC degrader against PARP1 and IKZF3. In Capan-1 cells, XZ8078 exhibits a DC₅₀ of 23.01 nM for PARP1 degradation and a DC₅₀ of 23.20 nM for IKZF3 degradation. XZ8078 upregulates DNA damage markers in a concentration-dependent manner, induces cell cycle arrest, upregulates activated caspases and triggers apoptosis. XZ8078 inhibits tumor growth in both AZD5305-sensitive and AZD5305-resistant xenograft models. XZ8078 can be used for cancer-related research.