DNA Damage/DNA Repair

N-Propargyladenosine is an adenosine analogue. Adenosine analogues are mostly used as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Some popular products in this series include Adenosine phosphate, Acadesine, Clofarabine, Fludarabine phosphate, and Vidarabine.

NSC 80467 is a DNA damaging agent that selectively inhibits survivin. NSC 80467 preferentially inhibits DNA synthesis and induces two markers of DNA damage, γH2AX and pKAP1.

Olaparib-d8 is the deuterated form of Olaparib (AZD2281). Olaparib is an orally effective PARP inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 5 and 1 nM, respectively. Olaparib is also an activator of autophagy and mitophagy.

Orobol is a major soy isoflavone with various pharmacological activities, including anti-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K subtypes (for PI3K α/β/γ/K/δ, IC50=3.46-5.27 μM).

OTUB1/USP8-IN-1 is an effective dual inhibitor of OTUB1 and USP8, with IC50 values of 0.17 and 0.28 nM, respectively. It can be used for cancer research.

PARP10/15-IN-2 (Compound 8h) is an effective dual inhibitor of PARP10 and PARP15, with IC50 values of 0.15 μM and 0.37 μM, respectively. It can enter cells and prevent apoptosis.

PARP10/15-IN-3 (Compound 8a) is an effective 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.

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

PARP10-IN-3 is a selective mono-ADP-ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 1.7 μM for both human PARP2 and human PARP15.

PARP11 inhibitor ITK7 (ITK7) is an effective and selective inhibitor of PARP11. It can effectively inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for research on cellular localization.

PARP1-IN-7 is an inhibitor of poly ADP-ribose polymerase-1 (PARP1), used as an anticancer agent.

PARP7-IN-14 (I-1) is an effective selective PARP7 inhibitor with an IC50 value of 7.6 nM. PARP7-IN-14 has anti-cancer activity.

PROTAC CDK12/13 Degrader-1 (7f) is a highly efficient and selective dual degrader of cell cycle-dependent kinases CDK12/CDK13, with DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used for breast cancer research.

(R)-5-O-Benzoyl-1,2-di-O-isopropylidene-alpha-D-xylofuranose is a purine nucleoside analogue. Purine nucleoside analogues have broad anti-tumor activity and target inert lymphoid malignancies. The anticancer mechanism in this process depends on inhibiting DNA synthesis, inducing apoptosis (cell death), etc.

RBN-3143 is an effective NAD+ competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 is used for research on lung inflammation.

Rohinitib is an effective and specific inhibitor of eIF4A. Rohinitib induces apoptosis in acute myeloid leukemia (AML) cell lines and reduces the leukemia burden in AML xenograft mouse models. Rohinitib can be used for research on AML.

SG2057 (DRG16) is a PBD dimer containing a pentadiene bond, which selectively binds to sequences in the minor groove of DNA, forming inter- and intra-strand crosslink adducts. SG2057 is an effective anti-tumor agent.

SK-575 is an efficient and specific protein-hydrolyzing targeted chimeric molecule (PROTAC) PARP1 degrader with an IC50 of 2.30 nM. SK-575 can effectively inhibit the growth of cancer cells carrying BRCA1/2 mutations.

Snail/HDAC-IN-1 is an effective dual-target inhibitor of Snail/HDAC. It has strong inhibitory activity against HDAC1 with an IC50 of 0.405 μM and a strong inhibitory effect on Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and reduces the expression of Snail protein, thereby inducing apoptosis in cells.

Tanuxiciclib is a cell cycle cyclin-dependent kinase (CDK) inhibitor.

Tanuxiciclib trihydrochloride is a cell cycle cyclin-dependent kinase (CDK) inhibitor.

TNG260 is a selective CoREST deacetylase (CoreDAC) inhibitor. TNG260 selectively inhibits HDAC1 10 times more than HDAC3. TNG260 leads to the inhibition of HDAC1 and reverses anti-PD1 resistance driven by STK11 deficiency. TNG260 reduces tumor infiltration of neutrophils. TNG260 exhibits immune-mediated cell killing.

Topoisomerase I inhibitor 8 is a potent inhibitor of topoisomerase I. It is a camptothecin analogue and has toxicity against tumor cells.

Uridine-13C is a 13C-labeled Uridine. Uridine (β-Uridine) is a nucleoside compound composed of Uracil and Ribose, connected by a β-N1-glycosidic bond.