Cell Cycle/Checkpoint

TLR7 agonist 12, a purine nucleoside analog, inhibits DNA synthesis and induces apoptosis in lymphoid cancers.

Carbazole belongs to the class of carbazole-based organic compounds. Carbazole can form novel DNA small groove complexes, inhibiting the synthesis of new DNA or RNA.

5’-O-DMT-Ri can be used in the synthesis of oligoribonucleotides[1].

DNA Gyrase-IN-17 (Compound 5C) is an inhibitor of DNA gyrase. It demonstrates significant antimicrobial activity against a range of Gram-positive and Gram-negative strains, including Enterococcus faecium, Escherichia coli, and Pseudomonas aeruginosa, with a MIC value of 62.5 μg/mL. By inhibiting bacterial DNA gyrase, DNA Gyrase-IN-17 disrupts DNA replication. This compound can be useful in the development of antibiotics, particularly for studying resistant strains.

Potent antagonist of the integrin αvβ3-vitronectin interaction (IC50 = 25.72 nM). Blocks proliferation and induces apoptosis in HUVECs; antiangiogenic.

(Gly0.8Nap0.2)20 is a dual-target compound effective against fungal membranes and DNA. It exhibits antimicrobial properties.

5’-O-DMT-PAC-dA can be used in the synthesis of oligoribonucleotides[1].

3'-dUTP trisodium, a nucleotide analogue, inhibits RNA polymerases I/II and UTP integration into RNA (Ki=2.0 μM).

Dihydro-5-azacytidine (DHAC) is a nucleoside analog that interrupts DNA methylation by integrating into DNA. It also exhibits notable antitumor properties.

CPS2: potent, selective PROTAC CDK2 degrader. IC50=24nM, targets acute myeloid leukemia research.

LY2812223: selective mGlu2 agonist; binds mGlu2/mGlu3 (Ki=144/156 nM).

Aclacinomycin A has a wide range of applications in life science related research.

Stigmatellin is an antibiotic derived from the cell mass of the myxobacterium, effective against yeasts (yeasts), filamentous fungi (filamentous fungi), and several Gram-positive bacteria (Gram-positive bacteria). Additionally, it serves as a potent inhibitor of photosynthetic electron (photosynthetic electron) transfer. Stigmatellin utilizes various sugars, polysaccharides, and acids from the citric acid cycle as substrates, inhibiting RNA and protein synthesis. It has two different inhibitory sites: one located on the reducing side of photosystem II and the other at the cytochrome b6/f complex. Stigmatellin holds potential for use in antimicrobial and photosynthesis research.

PY314 is a CHO-expressed humanized monoclonal antibody targeting TREM2 with antitumor activity for the study of metastatic renal cell carcinoma.

BLINK15 is a blood-brain barrier-permeable Cdk5 inhibitor. It reduces CDK5 activity in CDK5/p35 (IC50= 29.34 nM) and CDK5/p25 (IC50= 12.08 nM) complexes. Additionally, BLINK15 exhibits antidiabetic and neuroprotective effects. It lowers blood glucose levels in type 2 diabetes (T2D) mice, enhances cognitive abilities, and diminishes neurodegenerative lesions.

Deoxythymidine-5'-triphosphate (dTTP) is a nucleoside triphosphate involved in DNA synthesis.

2’-Deoxy-2’-fluoro-N3-(n-dodecyl)uridine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.

DSPE-PEG1000-cRGD is a PEG compound composed of DSPE and the αvβ3-targeting peptide (cRGD). The cRGD peptide specifically binds to the αvβ3 receptors present on the surfaces of various cancer cells and angiogenic vascular cells. DSPE-PEG1000-cRGD is applicable in drug delivery.

DSPE-PEG1000-iRGD is a PEG compound made from DSPE and the αv-integrin-targeting peptide (iRGD). The iRGD peptide initially binds to αv-integrins and undergoes proteolytic cleavage within tumors to produce CRGDK/R, which interacts with neuropilin-1, thereby facilitating tumor targeting and penetration. DSPE-PEG1000-iRGD is useful for drug delivery applications.

Fluorocitabine HCl, a cytarabine analog, hydrolyzes into ara-FC and ara-FU, showing antitumor effects in leukemia and solid cancers.

AV-153, a 1,4-dihydropyridine, reduces DNA damage, stimulates repair, and has anti-cancer properties.

α4β1 integrin (VLA-4) ligand (Kd ~ 12 nM). Non-fluorescent derivative of LDV FITC.

CDK5-IN-1: Potent CDK5 inhibitor (<10 nM) used in kidney disease research.

DHFR-IN-8 (compound 6r), a dihydrofolate reductase (DHFR) inhibitor, disrupts purine and thymidylate biosynthesis critical for cell proliferation and growth.

Pyrindamycin A is an antibiotic that inhibits DNA synthesis,and shows antitumor activities against murine leukemia.

MRK-952 is a NUDIX hydrolase inhibitor. NUDIX enzymes play a role in cellular metabolism, homeostasis, and mRNA processing.

N1-(2-Methyl)propyl pseudouridine, a purine analog, targets lymphoid cancer by inhibiting DNA synthesis and inducing apoptosis.

5'-O-TBDMS-N2-ibu-dG: a nucleoside derivative with strong anti-BVDV activity, useful in lead compound synthesis.

Substrate '[pSer2, pSer5, pSer7]-CTD (TFA)' for CDK7 phosphorylates RNA Pol II CTD at ser2, 5, 7.

PAT-LM1 is a human monoclonal antibody that targets NRB54/NONO. It is applicable in the study of hematological malignancies.

DSPE-PEG2000-iRGD is a PEG compound composed of DSPE and the αv-integrin targeting peptide (iRGD). The iRGD peptide binds to αv-integrins and subsequently undergoes proteolytic cleavage within tumors, producing CRGDK/R, which interacts with neuropilin-1. This compound is characterized by its tumor-targeting and tumor-penetrating properties, making DSPE-PEG2000-iRGD suitable for drug delivery applications.

DHODH-IN-16 is an effective inhibitor of dihydroorotate dehydrogenase (DHODH, IC50 = 0.396 nM for human).

TMX-2138 is a CDKs PROTAC degrader, with IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. It enhances the ubiquitination and degradation of CDKs and is utilized for ovarian cancer research.

CDK8-IN-12: selective CDK8 inhibitor (Ki 14 nM), oral anticancer, blocks GSK-3α/β, PCK-θ, halts MV4-11 cell growth.

AR-13324 analog mesylate is an inhibitor of Rho-kinase and a norepinephrine transporter and reduces intraocular pressure in normotensive monkey eyes.

Emofolin sodium, a synthetic folate analogue, inhibits DNA/RNA/protein synthesis by blocking dihydrofolate reductase.

Chrexanthomycin C, orally active, binds DNA (G4C2)4 G4, Kd 2.8 mM, potential in ALS research.

KIF2C-IN-1 (Compound 7S9) is a selective and potent small molecule inhibitor of KIF2C. It stabilizes the interaction between KIF2C and microtubule proteins, preventing the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel in Paclitaxel-resistant triple-negative breast cancer (TNBC) cells and, when combined with Paclitaxel, significantly reduces tumor growth in mouse models.

EC0489, Small molecule-drug conjugate (SMDC) ,a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (

3,6-DMAD hydrochloride functions as an inhibitor for the IRE1α-XBP1 pathway within the unfolded protein response mechanism.

5'-O-DMT-2'-O-TBDMS-rI, a modified nucleoside, finds application in deoxyribonucleic acid (DNA) or nucleic acid synthesis.

CDK2, a Ser/Thr kinase, is akin to yeast cdc28 and human Cdk1, crucial for cell division.

TTK/PLK1-IN-1 (Formula I) is a dual inhibitor of TTK (threonine tyrosine kinase) and PLK1 (polo-like kinase 1), with IC₅₀ values of 7 nM and 72 nM respectively.

SP27, a selective PROTAC, degrades PLK4 with a DC50 of 19.5 nM and may be utilized in breast cancer research [1].

Compound 12: a potent anti-MRSA, inhibits S. aureus/E. coli DNA gyrases/topo IV; IC50: 0.185-0.365/0.341-0.059 μM.

Antibacterial Agent 144 (compound 8e) exhibits superior efficacy against multi-resistant Staphylococcus aureus compared to Chloromycin and Amoxicillin.