Cell Cycle/Checkpoint

Isocytosine ,with CAS No. 108-53-2, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Isocytosine provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

PROTAC CDK9 Degrader-8 (Compound 21) is a potent degrader of CDK9 with an IC50 of 0.01 μM, utilized in cancer research [1].

CDK4/6-IN-5 inhibits CDK4/6; Ki: 0.2 nM (CDK4/D1) & 4.4 nM (CDK6/D3). (WO2019207463A1, A93)

Lamifiban trifluoroacetate is an antagonist of the nonpeptide platelet fibrinogen receptor (GPIIb/IIIa).

CDK12-IN-2 selectively inhibits CDK12 (IC50: 52 nM) with minimal effect on CDK2, CDK7, and CDK9, useful for CDK12 research.

Edatrexate (CGP 30694), a Methotrexate analog, combats MTX-resistant tumors and researches various cancers.

SM311 (Compound 10) is a potent, selective, and irreversible inhibitor of LIMK1, with an EC50 of 0.045 μM and over 30-fold selectivity for LIMK1 over LIMK2. It can inhibit cofilin phosphorylation and actin cytoskeleton regulation. SM311 shows potential for research in neurodegenerative disorders such as Fragile X Syndrome (FXS) and Alzheimer's disease, as well as in tumor invasion.

13-TP is an inhibitor of SARS-CoV-2. It effectively suppresses in vitro RNA synthesis catalyzed by the central replication-transcription complex (C-RTC, nsp12-nsp7-nsp82) of SARS-CoV-2. 13-TP fully inhibits RdRp polymerase activity and obstructs the complete extension of some primer RNAs.

Tubercidin5'-triphosphate (7-Deazaadenosine 5'-triphosphate) tetrasodium is a nucleoside analogue and serves as an active metabolite of Tubercidin.

DHFR-IN-11 (compound 6b) is a DHFR inhibitor with demonstrated inhibitory efficacy against the M.

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.

WAY-647802 is a CDK inhibitor.

N6-Ethyl-2’-beta-C-ethynyl adenosine is a purine nucleoside analog.

LB-80317, a DNA polymerase inhibitor, is used potentially for the potential treatment of hepatitis B virus infection.

FOXM1-IN-4 (compound36) hydrochloride is a 5-HT7 receptor antagonist and FOXM1 regulator, with a Ki of 92 nM for the 5-HT7 receptor and high selectivity over 5-HT1A, 5-HT2A, and 5-HT6 receptors. This compound blocks 5-HT7 receptor signaling pathways, decreases total and phosphorylated FOXM1 protein levels, and downregulates cyclin B1 and cdc25B expression. It induces cell cycle arrest at the G2/M phase, reduces the proportion of cells in the G0/G1 phase, and inhibits clonogenic capacity. FOXM1-IN-4 (hydrochloride) suppresses cancer cell proliferation and can be used in research related to triple-negative breast cancer.

N6-Methyl-2’-O-(2-methoxyethyl) adenosine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.

TFMU-ADPr triethylamine is a substrate for PARG activity measurement, releasing a fluorophore to indicate PAR hydrolase activity.

Py-MAA-Val-Cit-PAB-DX8951, a purine toxin, serves as an intermediate in the synthesis of antibody-drug conjugates [1].

YKL-5-124 TFA is a potent CDK7 inhibitor (IC50: 53.5 nM), more than 100x selective over CDK9/2, not active on CDK12/13, and disrupts the cell cycle.

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)