LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity.

LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity.

Trimelamol (CB10-375; NSC283162) is a highly efficient acid-catalyzed DNA interstrand crosslinker with low neurotoxicity due to its limited BBB penetration. Trimelamol exhibits anti-tumor activity and overcomes platinum resistance. Trimelamol is investigated for lung and ovarian cancer research[1][2][3][4][5].

KW-2450 tosylate is an orally active Aurora A and B kinases, IGF-1R, and IR tyrosine kinases inhibitor. KW-2450 tosylate induces Apoptosis. KW-2450 tosylate also exhibits anticancer activity against triple-negative breast cancer.

502U83 is an anti-cancer agent. 502U83 can inhibit DNA and RNA synthesis (IC50 ≈ 30 µM). 502U83 can be used for research on cancers such as leukemia.

CU-TZD-20 is a PARP-1 inhibitor. CU-TZD-20 has a high affinity for binding to the PARP-1 catalytic domain and good structural stability. CU-TZD-20 competitively occupies NAD+ binding sites and forms stable interactions with key catalytic residues. CU-TZD-20 can be used for cancer research.

(Rac)-IBR120 is the racemate of IBR120. IBR120 is a RAD51 inhibitor that has significant growth inhibition activity against MDA-MB-468 cells. (Rac)-IBR120 can be used for the research of difficult-to-treat cancers like triple negative breast cancer.

BAY-1112054 (BAY-958) (hydrochloride) is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-1112054 (hydrochloride) shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-1112054 (hydrochloride) exhibits good metabolic stability. BAY-1112054 (hydrochloride) effectively inhibits tumor growth in mouse xenograft models without significant toxicity.

NU6301 is a NU6102 (a CDK2 inhibitor) prodrug. NU6301 can rapidly generate NU6102 in mouse plasma. NU6301 has anticancer activity against endometrial cancer.

TrkA Inhibitor (Compound 18) is a CDK2 inhibitor with an IC50 of 0.69  μM over CDK1. TrkA Inhibitor can be used for chemotherapy-induced alopecia research.

GSK4418959 enantiomer is an enantiomer of GSK4418959. GSK4418959 (IDE275) is a non-covalent, reversible, selective and orally active WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer.

3′-Azido-2′,3′-dideoxy-GTP (AZddGTP) is a selective telomerase inhibitor with a Ki value of 1.5 μM. 3′-Azido-2′,3′-dideoxy-GTP can be incorporated into the 3′-terminus of DNA by telomerase. 3′-Azido-2′,3′-dideoxy-GTP inhibits telomerase activity in HeLa cells in vitro.

8-ET-NAD+ (sodium) is the derivative of NAD+. 8-ET-NAD+ (sodium) can be used in screening of PARP1 gatekeeper mutations. 8-ET-NAD+ (sodium) can be studied in research on cancer.

CGP-6809 is an orally active DNA inhibitor. CGP-6809 exhibits antitumor activity against various transplantable tumors in mice and rats, including melanoma, prostate cancer, and rectal cancer. CGP-6809 can be used in research on various cancers, including melanoma, prostate cancer, and rectal cancer.

OUL312 is a potent PARP10 inhibitor (IC50 = 20 nM), showing more than 75-fold greater selectivity for PARP15(IC50 = 1500 nM). OUL312 is also at least 18-fold higher than all other human enzymes in the family. OUL312 has a good ADME profile, is able to enter cells, is not toxic, and effectively rescues human cells from PARP10-induced apoptosis at sub-micromolar concentrations. OUL312 can be used for the study of cervical cancer.

iRucaparib-TP3 is a selective PARP1 degrader (DC50=36 nM). iRucaparib-TP3 is promising for research of oncology (e.g., BRCA-mutated cancers) and neurodegenerative diseases.

CEP-6800 is an inhibitor of PARP-1 with chemopotentiating ability. CEP-6800 attenuates irinotecan- and Temozolomide-induced poly(ADP-ribose) accumulation in LoVo as well as HT29 xenografts. CEP-6800 can suppress Calu-6 tumor growth. CEP-6800 can be studied in anti-cancer research.

PARP14 inhibitor 2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC50 value of <30 nM. PARP14 inhibitor 2 inhibits the mono-ADP-ribosyltransferase activity of PARP14 and regulates IFN-γ and IL-4 signaling, reversing protumor macrophage polarization and inhibiting anti-tumor inflammatory responses. PARP14 inhibitor 2 is promising for research of PARP14-related diseases such as tumors, atopic dermatitis and autoimmune diseases.

Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer.

NSC 727357 is a DNA intercalator and topoisomerase inhibitor with antitumor activity. NSC 727357 can inhibit cells proliferation and induce G1 phase arrest. NSC 727357 can be used for the research of cancer, such as melanoma.

SG3683 is a DNA-targeted cytotoxic agent belonging to pyrrolobenzodiazepine (PBD) dimers. SG3683 exerts antitumor activity with an IC50 value of 0.74 nM in MDA-MB-436 cells. SG3683 is promising for research of cancers, such as breast cancer.

YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC).

NISC-6 is a novel dual Topo-IIα/Akt inhibitor. NISC-6 has inhibitory activity against various cells, such as UACC903 (IC50 = 2.5 µM) and CHL-1 (IC50 = 0.8 µM) cells. NISC-6 dose dependently induces early and late apoptosis. NISC-6 can be used for research on melanoma.

INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases.

AKI-001 is an inhibitor of aurora kinase with cellular potency of IC50 of less than 100 nM. AKI-001 shows low nanomolar potency against Aurora A and Aurora B enzymes.

RBN010860 (example 150) is a potent PARP7 inhibitor with an IC50 of <0.1 μM. RBN010860 can be used for the study of cancer.

Dalpiciclib (isethionate) is a CDK4/6 inhibitor. Dalpiciclib (isethionate) inhibits the kinase activity of CDK4 and CDK6, thereby blocking the G1-to-S phase transition of the cell cycle and suppressing abnormal cell proliferation. Dalpiciclib (isethionate) can be used for the study of breast cancer.

NK-611 is an epipodophyllotoxin derivative. NK-611 induces DNA double-strand breaks by inhibiting topoisomerase II (IC50 = 56 μM). NK-611 does not inhibit microtubule polymerization, thus avoiding the side effects of the parent compound, Podofilox. NK-611 exhibits broad-spectrum antitumor activity and demonstrates potent efficacy in in vivo models of leukemia. NK-611 can be used in cancer research.

F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer.

GI-149893 is a selective topoisomerase I (TopoI) inhibitor. GI-149893 prevents DNA religation and induces irreversible DNA damage in tumor cells. GI-149893 is promising for research of cancers (e.g., colon carcinoma HT-29/SW-48, breast MX-1, prostate PC-3 xenografts).