parp-10

PARP10-IN-3 is a potent and selective mono-Adp-ribotransferase PARP10 inhibitor that inhibits human PARP10 (IC50:480 nM). PARP10-IN-3 also inhibited human PARP2 and human PARP15 with IC50 values of 1.7 μM.

PARP10-IN-2 is a potent inhibitor of PARP10, a mono-ADP-ribosyltransferase, with an IC50 value of 3.64 μM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 27 μM and 11 μM, respectively.

OUL35 (NSC-39047) is a selective PARP-10 inhibitor, and small-molecule ARTD10 inhibitor. OUL35 has been shown to rescue cells from ARTD10-induced cell death.

OUL232 is a potent single ARTs PARP7, PARP10, PARP11, PARP12, PARP14 and PARP15 inhibitor for cancer and tumour research.

PARP10/15-IN-3 (Compound 8a) is a potent dual inhibitor of PARP10 and PARP15 with IC50 values of 0.14 μM and 0.40 μM, respectively. It can enter cells and prevent apoptosis [1].

PARP10/15-IN-1 (compound 8l) is a dual inhibitor of PARP10 and PARP15, with IC50 values of 160 nM and 370 nM, respectively. It is applicable in cancer research[1].

PARP10/15-IN-2 (Compound 8h) is a dual inhibitor of PARP10 and PARP15, with IC50 values of 0.15 μM and 0.37 μM, respectively. It can penetrate cells and prevent apoptosis [1].

ARTD10/PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly ADP-ribose polymerase-1 (ARTD1/PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.

ARTD10/PARP10-IN-2 is a potent, non-selective inhibitor of mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1, exhibiting IC50 values of 2.0 μM and 9.7 μM, respectively.

RBN012759 inhibits PARP14 protein with an IC50 value of 0.003 μM and is more than 300-fold selective over all PARP family members.[2]

TIQ-A is a PARP1 inhibitor which involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is triggered by DNA damage and its excessive activation has been proposed as a causative factor in many pathological conditions includi

ART-IN-1 (compound 7) is a selective inhibitor of PARP with IC50 values of 19 μM for PARP2, 22 μM for TNKS2, 2.4 μM for PARP10, >100 μM for PARP14, and 1.1 μM for PARP15 [1].

ME0328 is a potent, selective PARP inhibitor with an IC50 of 0.89 μM for PARP3, showing approximately 7-fold selectivity over PARP1.

RBN-3143 is a potent inhibitor of NAD+-competitive catalytic PARP14 (IC50= 4 nM), which inhibits ADP-ribosylation mediated by PARP14 and stabilizes PARP14 in cell lines, demonstrating research potential for lung inflammation.

OUL245, a 7-Hydroxy derivative, selectively inhibits PARP2 with an IC50 of 44 nM. Additionally, it exhibits inhibition against other PARP and TNKS enzymes, displaying IC50 values ranging from 2.9 to 8.8 μM.

YCH1899, an orally active PARP inhibitor, demonstrates potent inhibition of PARP1/2 with an IC50 of less than 0.001 nM. It shows marked antiproliferative efficacy against Olaparib-resistant (Capan-1/OP) and Talazoparib-resistant (Capan-1/TP) cells with IC50 values of 0.89 nM and 1.13 nM, respectively. Moreover, YCH1899 possesses favorable pharmacokinetic attributes in rats [1].

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.

BET-IN-20 (compound 10), a BRD4 BD1 inhibitor (IC 50 =1.9 nM), exhibits significant anticancer properties. It promotes apoptosis in acute myeloid leukemia (AML) cells and arrests the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits both c-Myc and CDK6, and enhances PARP cleavage [1].

B102 (PARP/HDAC-IN-1) is a dual inhibitor of PARP and HDAC, exhibiting IC50 values of 19.01 nM for PARP1, 2.13 nM for PARP2, 1.69 μM for HDAC1, and greater than 10 μM for HDAC6 in enzymatic assays. It possesses antiproliferative and antitumor properties and induces DNA damage and apoptosis in vitro.

PROTACPARP1 degrader-2 (Compound 72) is a potent PROTAC degrader of PARP, achieving a DC50 of less than 10 nM in MDA-MB-231 cells. Additionally, this compound effectively inhibits the viability of MDA-MB-436 cells with an IC50 of less than 100 nM.