parp 1

PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1, and TNKS2, with potential anti-tumor activity that induces apoptosis.

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells.

PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) is an effective inhibito of PARP1 (IC50 = 97 nM).

PROTAC PARP1 degrader is a targeted protein degrader of PARP1 developed using PROTAC technology, and at 10 μM for 24 hours inhibits the proliferation of the MDA-MB-231 breast cancer cell line with an IC50 of 6.12 μM, providing a powerful research tool for studying DNA damage response, PARP1 biology, and degradation-based cancer therapeutics.

PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell cycle in the G2/M phase.PARP-1-IN-3 may be useful for the study of cancer-related diseases. cancer-related diseases.

PARP-1-IN-4 is a potent PARP-1 inhibitor with potential anti-tumor activity, where inhibition of PARP-1 may be applied in cancer treatment.

PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.

PARP1-IN-31 (compound 11f) is a PARP1 inhibitor with an IC₅₀ of 97 nM. It induces apoptosis and inhibits proliferation in lung cancer cell lines (e.g., A549), while upregulating caspase-3 and caspase-9, making it suitable for lung adenocarcinoma research.

PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 of 6.3 nM. When labeled with [18F], PARP1-IN-29 can be utilized for positron emission tomography (PET) imaging, specifically targeting PARP-1 in tumors. This compound is useful in oncology and imaging studies, particularly for detecting PARP-1 activity in cancer.

PARP1-IN-36 (compound 11) is a derivative of 4-carboxamide-isoindolinone and acts as a selective PARP-1 inhibitor with a Kd value of less than 0.01 μM. This compound is utilized in research related to cancer, cardiovascular diseases, neurological injuries, and inflammation.

PARP1-IN-37 (Compound 8) is an orally active and selective inhibitor of poly (ADP-ribose) polymerases 1 and 2 (PARP1/2), with an IC50 value of 24 nM for PARP1. It inhibits PARP activity in cells with an EC50 value of 3.7 μM and holds potential for research on BRCA-mutated tumors, such as breast and ovarian cancers.

PARP1-IN-46 is a potent inhibitor of PARP-1 with an IC50 value of 2.4 nM. It demonstrates significant antiproliferative activity in both rat (C6) and human (U87MG) glioma cells. The compound triggers PARP cleavage, induces DNA damage, and elevates ROS levels. PARP1-IN-46 effectively impedes glioma cell migration, invasion, and colony formation, ultimately inducing apoptosis. It is suitable for research on glioma cells.

PARP1-IN-50 is a selective, orally active PARP-1 inhibitor with an IC50 of 64.98 nM. It inhibits PAR formation and induces DNA double-strand breaks, resulting in DNA damage. PARP1-IN-50 can cause G2/M phase arrest and apoptosis (apoptosis) in cancer cells, demonstrating significant antiproliferative activity against various cancer cell lines. This compound is useful in cancer research, including studies on breast cancer.

PARP1-IN-6, a dual-function inhibitor, targets both tubulin and PARP-1, demonstrating inhibitory concentration (IC50) values of 0.94 μM for tubulin and 0.48 μM for PARP-1.

PARP1-IN-5 is a potent, selective, orally active, low-toxicity PARP-1 inhibitor with an IC50 value of 14.7 nM. PARP1-IN-5 can be used in cancer research.

PARP1-IN-17 is an inhibitor that targets PARP-1 (IC50=19.24 nM ) with a slightly reduced affinity for PARP-2 (IC50=32.58 nM ) and induces apoptosis. It exhibits robust anti-proliferative activity [1].

PARP1 degrader1 (Compound 2c) is a relatively potent PARP1HyT degrader with an intracellular PARP-1 DC50 of 618 nM. It is also a conjugate of HyT-Olaparib. PARP1 degrader1 induces UPR/autophagy, promoting the degradation of PARP-1, and can be utilized in cancer research.

PARP1-IN-30 is a specific and effective PARP1 inhibitor with cytotoxic properties. It precisely inhibits PARP1 in tumor cells lacking breast cancer 1 protein (BRCA1) or BRCA2. PARP1-IN-30 holds potential for use in cancer research.

PARP1/2-IN-4 (compound 3) is an inhibitor of PARP1/2.

PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader specifically targeting PARP1, with a DC50 of 58.14 nM. It demonstrates cytotoxicity in SW-620 and LOVO cancer cells, with IC50 values of 1.63 μM and 2.84 μM, respectively. In BRCA-mutated colon cancer cells, PROTAC PARP1 degrader-3 exhibits synergistic effects with SN-38, with a combination index (CI) of 0.487.

PARP1-IN-33 (Example 6) is a PARP1 inhibitor with an IC50 of 0.41 nM. It demonstrates protective effects on retinal cells, exhibiting an EC50 of 0.02 nM in inhibiting hydrogen peroxide-induced MTS activity in human retinal pigment epithelial cells.

PARP1-IN-34 (compound 30) is a selective PARP1 inhibitor with an IC50 of 0.32 nM. It is a sub-nanomolar PARP1 inhibitor with 1000-fold selectivity over PARP2, having an IC50 of 326 nM, and exhibits anticancer activity.

PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader, demonstrating DC50 values of 180 nM and 240 nM in T47D and MDA-MB-231 cell lines, respectively. It facilitates the ubiquitination and degradation of PARP1 and inhibits its enzymatic activity without causing significant DNA trapping effects. Additionally, PROTAC PARP1 degrader-4 can inhibit tumors with BRCA gene mutations while having minimal impact on the growth of normal cells.

PARP1-IN-35 (compound T26) is a selective, orally active PARP1 inhibitor that can cross the blood-brain barrier, with IC50 values of 0.2 nM for PARP1 and 122 nM for PARP2. It exhibits antiproliferative and anticancer activities and holds potential for breast cancer research.