Cell Cycle/Checkpoint

CDK1-IN-6 (Ligand 3) is an effective inhibitor of CDK1 and shows potential for use in cancer research.

Gallium maltolate is a ribonucleoside-diphosphate reductase inhibitor.

Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-

TMX-2039 is a pan-CDK inhibitor that targets cell cycle CDKs (CDK1, CDK2, CDK4, CDK5, and CDK6) and transcription CDKs (CDK7 and CDK9), with IC50 values of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5, and 25 nM, respectively. It serves as a ligand for the target protein in PROTAC applications.

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.

MGB-BP-3 is a synthetic antibiotic with bactericidal activity that inhibits bacterial DNA replication and can be used to study recurrent C. difficile infections.

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

2',3'-Dideoxyuridine is a purine nucleoside analog with potential antitumor activity.

WRN inhibitor 11 (Example 17) is an orally effective inhibitor of WRN helicase, with an IC50 of 63 nM.

C16Y, a short peptide, serves as an inhibitor for the integrins αvβ3 and α5β1. It targets the cell membrane and exerts its antitumor activity by inhibiting angiogenesis.

EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).

5-Methylcytosine is a methylated nucleotide base found in eukaryotic DNA.

SRI-29329 is a potent, specific inhibitor of CDC-like kinase (with IC50 of 78 nM, 16 nM and 86 nM for CLK1, CLK2 and CLK4, respectively).

3-AP (Triapine) is a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR).

Human PD-L1 Inhibitor V is a peptide that binds to the human PD-1 protein with an affinity characterized by a dissociation constant (Kd) of 3.32 μM, effectively

T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.

AZ5576 is a potent and highly selective CDK9 inhibitor. AZ5576 can be used for the research of Hematological Malignancy [1].

PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0/G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)

SCH900776 S-isomer (MK-8776 S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM).

Senexin C is a CDK8/19 inhibitor with anticancer activity.Senexin C inhibits the growth of MV4-11 leukemia cells.

DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor with an IC50 value of 48 μM.

Aminopurvalanol A is a competitive, selective and cell-permeable inhibitor of cyclin-dependent kinase (CDK) that potently inhibits Cyclin A/cdk2, Cyclin B/cdk1

Sintilimab (IBI308), an IgG4 monoclonal antibody, blocks PD-1, enhancing T-cell anti-tumor response; treats Hodgkin's, lung, and esophageal cancers.

Atuveciclib S-Enantiomer is a (S)-form of BAY-1143572; a potent, selective CDK9 inhibitor with an IC50 of 16 nM.

PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor(IC50 of 92.3 nM).

CFI-402257 is a selective inhibitor of Mps1/TTK kinase (Mps1 Ki = 0.09 nM; EC50 = 6.5 nM)and can be used in studies about hepatocellular carcinoma diseases.

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC

Damnacanthal is a natural anthraquinone with potential anticancer property, inhibiting a variety of protein kinases such as LIMK1, LIMK2 and Lck.

RNA polymerase II-IN-1 (19iv), an amatoxin, inhibits Pol II at 36.66 nM IC50, is more toxic to cancer cells, less to normal cells than α-Amanitin.

SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50

Aurora A Inhibitor 3 (Compound 5h) effectively inhibits Aurora-A kinase, exhibiting an IC50 of 0.78 μM, and demonstrates cytotoxicity against MCF-7 and MDA-MB-

Proguanil (Chloroguanide) is a prophylactic antimalarial drug that acts primarily through its active metabolite, Cycloguanil, which inhibits the DHFR enzyme .

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3, modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

5-Aza-7-deazaguanine is a non-natural substituted nucleobase with potential antiviral activity, used in cancer and bacterial infection research.

8-Azaguanosine is a purine nucleoside analog with a broad spectrum of antitumor activity and is used in the study of a variety of tumor diseases.

BI8622 is a HUWE1 antagonist that restores levels of RP2 mutants in retinal cell lines and inhibits cellular activation of NLRP3 and AIM2 inflammatory vesicles.

(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that inhibits the transcription of anti-apoptotic and pro-survival proteins.

Nicotinamide N-oxide, a metabolite of nicotinamide and precursor to NAD+, is reduced by liver enzyme xanthine oxidase.

AS2863619 is an oral inhibitor of cyclin-dependent kinase(CDK8) and CDK19. Inhibition of CDK8/19 enhances STAT5 activation.Cost-effective and quality-assured.

CDK8/19-IN-51 is a CDK8 and CDK19 inhibitor with anticancer activity, used in research on colorectal and gastric cancers.

KOdiA-PC is a truncated oxidized phospholipid and a CD36-targeting ligand found on oxLDL. It inhibits activation of TLR4 signaling components.

Envafolimab (ASC 22) is a humanized antibody targeting PD-L1, with anticancer activity, blocking the PD-L1 and PD-1 interaction.

LY2880070 is a new checkpoint kinase 1 (CHK1) inhibitor for cancer therapy.

WAY-647802 is a CDK inhibitor.

Madrasin (DDD00107587) is a potent and cell penetrant splicing inhibitor that interferes with the early stages of spliceosome assembly.

PD-1/PD-L1-IN-51 (Compound III-4) is an inhibitor of PD-1/PD-L1 (IC50: hPD-L1 at 2.9 nM). It binds directly to PD-L1, blocking the interaction between PD-1 and PD-L1, and enhancing the release of IFN-γ. Additionally, PD-1/PD-L1-IN-51 exhibits antitumor activity.

CCT 137690 is a highly specific and oral-available aurora kinase inhibitor, for aurora A(IC50=15 nM ), B(IC50=25 nM) and C(IC50=19 nM).

5'-O-DMT-N4-Bz-5-Me-dC (DMT-NBZ-5-METHYL DC) is a modified nucleoside used in the synthesis of nucleoside phosphoramidites.

Efalizumab: humanized monoclonal antibody CD11a; modulates T cell activation/adhesion; for plaque psoriasis, psoriatic arthritis research.

SR 11302 is an inhibitor of activator protein-1 (AP-1).

Nedaplatin, a cisplatin derivative, induces tumor DNA damage (IC50: 94 μM) through platinum-DNA cross-links, causing apoptosis.

A-205804 is a specific and effective inhibitor of E-selectin( IC50=20 nM ) and ICAM-1(IC50=25 nM) expression.

N-6-Furfurylguanosine (kinetin riboside) is a purine nucleoside analog with cytotoxicity, inhibiting the growth of cancer cells.

Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity.

Uridine-5-acetic acid (5-Carboxymethyluridine) is a nucleoside formed during RNA transfer processes in yeast and wheat embryos.

PolQi2 is a Polθ inhibitor that suppresses the helicase activity of Polθ, and when combined with AZD7648.

CHK1 inhibitor (GDC-0575 analog) is a CHK1 inhibitor.

Saccharin 1-methylimidazole (SMI) is a general-purpose activator used for DNA and RNA synthesis.

THZ1 (CDK7 inhibitor) is a selective inhibitor of CDK7, binding to the Cys residue located at the outer end of the classical kinase domain. Cost-effective and quality-assured.

Antiviral agent 36 (compound 27), a potent inhibitor of both dengue (DENV) and Zika (ZIKV) viruses, demonstrates replication inhibition with EC50 values of 100

m-Se3 is a potent, selective inhibitor of c-MYC transcription with demonstrated capability to inhibit tumor growth and exhibit anti-cancer activity [1].

CDK2-IN-4 is a potent and selective inhibitor of CDK2 with an IC50 of 44 nM for CDK2/cyclin A.

Bersiporocin is a novel prolyl-tRNA synthetase (PRS) inhibitor that exerts antifibrotic effects through downregulation of collagen synthesis in IPF.

ON-013100 is an antineoplastic drug. ON-013100 also acts as a mitotic inhibitor that could inhibit Cyclin D1 expression.

ICAM-1-IN-1 is a potent and selective E-selectin(IC50 = 7 nM) and ICAM-1(IC50 = 5 nM) inhibitor.

CDK9-IN-40 is an inhibitor of CDK2 (Cyclin-dependent kinase 2). It effectively inhibits CDK2/Cyclin E1, with an IC50 of ≤ 10 nM.

MYCi361 (NUCC-0196361) is an inhibitor of MYC (binding to MYC with Kd of 3.2 μM).

Dimethylenastron, an Eg5 inhibitor, arrests cells with monopolar spindles to which all chromosomes attach in a syntelic manner.

Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively).

HAMNO (NSC-111847) is a protein interaction inhibitor of replication protein A (RPA).

BML-259 inhibits CDK5/CDK2 (IC50: 64/98 nM) for cancer and neurodegeneration research.

WRN inhibitor 14 (compound S35) is an orally administered WRN inhibitor with anticancer properties. It effectively suppresses tumor growth in the SW48 xenograft model in BALB/c nude mice.