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.

ddATP (2',3'-Dideoxyadenosine 5'-triphosphate) tetrasodium is an active metabolite of 2',3'-dideoxyadenosine and an inhibitor of chain elongation by DNA polymerase (DNA polymerase). ddATP tetrasodium can be used in Sanger sequencing and research related to viral infections.

Clofarabine-5'-triphosphate is the metabolite of Clofarabine by deoxycytidine kinase (dCK) phosphorylation. Clofarabine-5'-triphosphate exhibits cytotoxicity in cancer cells through inhibition of DNA synthesis and DNA repair.

Clofarabine-5'-diphosphate trisodium (Clofarabine-DP trisodium) is the trisodium salt form of Clofarabine-5'-diphosphate. Clofarabine-5'-diphosphate trisodium is the metabolite of ClofarabineA0005) by deoxycytidine kinase (dCK) phosphorylation. Clofarabine-5'-diphosphate trisodium can be further phorphorylated into Clofarabine-5'-triphosphate, and exhibits cytotoxicity in cancer cells through inhibition of DNA synthesis and DNA repair.

Clofarabine-5'-diphosphate (Clofarabine-DP) is the metabolite of Clofarabine by deoxycytidine kinase (dCK) phosphorylation. Clofarabine-5'-diphosphate can be further phorphorylated into Clofarabine-5'-triphosphate, and exhibits cytotoxicity in cancer cells through inhibition of DNA synthesis and DNA repair.

Ap4dT is an inhibitor for human adenylate kinase isozyme 1 (hAK1), that inhibits the ATP and ADP synthesis with IC50s of 42 μM and 38 μM.

AHL-Pu-2 is the clickable electrophilic purine. AHL-Pu-2 can be used to directly quantify protein-RNA interactions on proteins through photoaffinity competition with 4-thiouridine (4SU)-labeled RNA in cells.

Adenosyl-(3′→5′)-uridine (ApU) is a nucleotide, which is composed of an adenine base and a uracil sugar molecule through a 3'-5' phosphodiester bond. Adenosyl-(3′→5′)-uridine (ApU) participates in the biological processes, such as gene expression regulation, signal transduction, and protein synthesis.

2'-(2-Nitrobenzyl)-ATP is an rATP analog. 2'-(2-Nitrobenzyl)-ATP acts as a transcription terminator, inhibiting further RNA chain elongation by T7 RNA polymerase.

NNISC-2 (compound 4) is a DNA intercalator-linker conjugate of Naph-Se-TMZ, which is composed of DNA intercalator Nitro-Naphthalimide-C2-acylamide and a linker.

Nitro-Naphthalimide-C2-acylamide is a DNA intercalator. Nitro-Naphthalimide-C2-acylamide can be used for the synthesis of PROTAC-like Naph-Se-TMZ can significantly improve the survival rate of mice and inhibit tumor growth. DOTA-XYIMSR-01 shows promise for research in the field of anti-cancer therapy.

HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies).

YY2201 is a highly potent and selective ATR inhibitor with an IC50 of 8 nM. YY2201 shows >200-fold more selective for ATR than mTOR. YY2201 inhibits tumor progression in broad-spectrum cancer types (such as lung cancer).

(S)-WSD0628 (Compound 28) is the S-isomer of WSD0628. 4-Methylphenoxyacetic acid-Oxindole-CF3 can be utilized in PROTAC synthesis.

OSI-7904L (GW1843) is a noncompetitive inhibitor of thymidylate synthase (TS). OSI-7904L is an antifolate compound and a substrate for folylpolyglutamate synthetase. OSI-7904L has cytotoxicity against solid tumor lines, and the toxicity can be selectively blocked by folic acid.

Thioparib is a next-generation potent, orally bioavailable pan-PARP inhibitor with IC50 of 0.13/0.006 nM (PARP1/2), overcomes multiple PARPi resistance both in vitro and in vivo.

Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM.

SW394703 is a novel DDB1-dependent molecular glue degrader for cyclin K, SW394703 is toxic to HCT116 cells (IC50=1.2 uM).

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).

TH 287 is a first-in-class MTH1 inhibitor (IC50 value 5.0 nM) that selectively and effectively kills U2OS and other cancer cell lines, with considerably less toxicity towards several primary or immortalized cells.

PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. MM2 is the binding site of RMI complex on Fanconi anemia complementation group M protein (FANCM). PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.

TH588 represents a highly selective and cell-permeable small molecule inhibitor targeting MTH1 (NUDT1), a member of the nudix hydrolase family, with potent inhibitory activity (IC₅₀ ≈5 nM).

RX-3117 is an orally available and potent DNA synthesis inhibitor with potential antineoplastic activity.

​​Flavopiridol hydrochloride​​ is a potent pan-cyclin-dependent kinase (CDK) inhibitor with a unique ATP-competitive mechanism.

NCGC00131308 is a small molecule inhibitor that effectively disrupts IQGAP1-Cdc42 interaction in breast cancer cells, shows EC50 of 4.47 uM in biochemical HTRF assays.

XPW1 is a potent and selective CDK9 inhibitor with excellent anti-ccRCC activity and low toxicity.

A83B4C63 is a highly potent small-molecule inhibitor targeting the DNA repair enzyme polynucleotide kinase 3'-phosphatase (PNKP), exhibiting strong binding affinity with a ​Kd of 80 nM. Due to its limited aqueous solubility, A83B4C63 was formulated into ​nano-encapsulated carriers, enhancing its therapeutic potential—particularly in ​PTEN-deficient colorectal cancer (CRC).

BS-181 is a highly selective inhibitor of CDK7, exhibiting potent activity with an IC50 value of 21 nM. It demonstrates remarkable specificity, showing over 40-fold greater selectivity for CDK7 compared to other cyclin-dependent kinases, including CDK1, CDK2, CDK4, CDK5, CDK6, and CDK9. This exceptional selectivity positions BS-181 as a valuable tool for studying CDK7-specific biological functions and exploring its therapeutic potential in diseases where CDK7 plays a critical role, such as cancer. Its precision in targeting CDK7 underscores its utility in both research and drug development efforts.

AZD2461 is indeed a novel poly (ADP-ribose) polymerase (PARP) inhibitor that has been investigated for its potential to overcome resistance mechanisms associated with other PARP inhibitors, such as Olaparib. One of the key resistance mechanisms to Olaparib is mediated by P-glycoprotein (Pgp), an efflux pump that can reduce intracellular concentrations of the drug, thereby diminishing its efficacy.

TH7528 is a SAMHD1 inhibitor with IC50 of 4.5 μM/2.8 μM/2.6 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively.