Ceftezole (GR69153) is a broad-spectrum cephalosporin antibiotic and an α-glucosidase inhibitor. Ceftezole inhibits bacterial cell lysis by inhibiting cell wall synthesis and binding to penicillin-binding proteins (PBPs). Ceftezole exhibits in vivo anti-diabetic activity in diabetic mice. Ceftezole can be used in antibacterial and anti-diabetic research.

CE-1037 (MDL 201,404YA) is a selective inhibitor of human neutrophil elastase (HNE) (Ki: 0.45 nM). CE-1037 prevents the pulmonary hemorrhage induced by intratracheal instillation of HNE. CE-1037 can be used for research of pulmonary diseases, such as COPD.

CDK9-IN-49 is a CDK9 inhibitor with an IC50 of 7.32 nM. CDK9-IN-49 inhibits the proliferation of various cancer cells. CDK9-IN-49 can be used in the research of cancers such as acute myeloid leukemia and prostate cancer.

CDK9-IN-48 is a CDK9 inhibitor with an IC50 of 1.37 nM. CDK9-IN-48 inhibits the proliferation of various cancer cells. CDK9-IN-48 can be used in the research of cancers such as acute myeloid leukemia and prostate cancer.

CDK9-IN-46 (Compound Formula I) is a CDK9 inhibitor. CDK9-IN-46 can be used for the research of cancer.

CDK8-IN-2 is an orally active CDK8 inhibitor of an IC50 values of 0.010 μM. CDK8-IN-2 shows a CDK19 IC50 value of 0.026 μM. CDK8-IN-2 inhibits phospho-STAT1, a pharmacodynamic biomarker of CDK8. CDK8-IN-2 inhibits WNT pathway activity. CDK8-IN-2 can be used for the research of colorectal carcinoma.

CDK7-IN-33 (formula Ⅰ) is a pyrimidine derivative and also a CDK7 kinase inhibitor. CDK7-IN-33 is applicable to the research of cancer, inflammation, cardiovascular diseases, infectious diseases, immune diseases and metabolic diseases.

SHOC2-RAS PPI-IN-1 (compound 6) is a non-covalent competitive inhibitor that disrupts the SHOC2-RAS protein-protein interaction. It exhibits an IC50 of 0.048 μM and a KD of 0.065 μM against NRASQ61R. The compound inhibits the SMP phosphatase complex, resulting in elevated CRAFS259 phosphorylation and subsequent blockade of the MAPK signaling pathway (evidenced by reduced pMEK and pERK levels). This inhibition induces tumor cell cycle arrest and apoptosis. SHOC2-RAS PPI-IN-1 serves as a research tool for investigating NRASQ61R-mutant malignancies including melanoma and colorectal cancer.

CDK4-IN-4 (example 30) is a selective CDK4 inhibitor (IC50＜10 nM) that can be used in cancer research.

CDK2-IN-55 (Compound 12c) is a CDK2 inhibitor with an IC50 value of 4.7 nM. CDK2-IN-55 also has a strong inhibitory effect on CDK1 (IC50 = 26.3 nM), moderate inhibitory effects on Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM), and very weak inhibitory activities on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM). CDK2-IN-55 shows strong anti-proliferative activity against various cancer cell lines, inducing cell cycle arrest and apoptosis. CDK2-IN-55 can be used for research on colorectal cancer, lung cancer, and cervical cancer.

CDK2-IN-54 (Formula I) is a CDK2 inhibitor. CDK2-IN-54 can be used in cancer research such as triple-negative breast cancer, ovarian cancer, bladder cancer, and uterine cancer.

CDK2-IN-52 (Compound Cpb No 39) is a selective cyclin-dependent kinase 2 (CDK2) inhibitor with a DC50 value of 1-10 nM. CDK2-IN-52 induces cell cycle arrest and suppresses tumor cell proliferation. CDK2-IN-52 is promising for research of CDK2-overexpressing malignancies such as breast and ovarian cancers.

CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer.

CDK2-IN-21 (example 30) is a potent cyclin-dependent kinase 2 (CDK2) inhibitor with an IC50 of 0.24 µM. CDK2-IN-21 can be used for cancer research.

CDK12-IN-9 is a potent and selective CDK12 inhibitor with an IC50 of 2.2 nM. CDK12-IN-9 inhibits pSER2 (a downstream marker of CDK12/13 activity). CDK12-IN-9 can be used for the research of cancer.

CDK12 ligand-3 is a molecular glucose degrading agent that targets the CDK12 protein (DC50 = 35 nM). CDK12 ligand-3 degrades CDK12, CDK13 and their regulatory subunit Cyclin K in a concentration dependent manner, and inhibits RNA polymerase II CTD (Ser2) phosphorylation. CDK12 ligand-3 exhibits potent anti proliferative activity against Jurkat cells. CDK12 ligand-3 can be used for research on cancers such as leukemia.

CDH11-IN-1 is a CDH11 inhibitor. CDH11-IN-1 regulates CDH11-mediated biological pathways. CDH11-IN-1 can be used for research on cancer and rheumatoid arthritis.

CDC14A/B-IN-2, phosphotyrosine mimetic, is a competitive human CDC14A/B phosphatase inhibitor with IC50 values of 10.4 and 11.2 μM, and Ki values of 5.8 and 7.3 μM. CDC14A/B-IN-2 shows at least 20-fold selectivity over other protein tyrosine phosphatases. CDC14A/B-IN-2 can be used for the research of cancer.

CDA-IN-5 (Compound M-09) is a Chitin deacetylase inhibitor with a Ki of 27.5 μM against PstCDA. CDA-IN-5 is an antifungal agent. CDA-IN-5 can inhibit infection by Rhizoctonia solani, Pyricularia oryzae, and Botrytis cinerea and exhibits moderate control efficacy against rice sheath blight.

CD38-IN-5 (compound 1) is a CD38 inhibitor that selectively inhibits CD38 hydrolase with an IC50 of 4.0 μM. CD38-IN-5 does not inhibits CD38 cyclase. CD38-IN-5 is highly effective at promoting NK cell-mediated tumor toxicity. CD38-IN-5 increases NADH+ and IFNγ levels in activated PBMCs. CD38-IN-5 can be used for the study of cancer.

CCT368772 (compound 35) is a selective kinesin HSET inhibitor (HSET ADP-Glo IC50 = 0.019 μM). CCT368772 exhibits selectivity over Eg5 (Eg5 ADP-Glo IC50 >200 μM). CCT368772 (compound 152) can be used for the study of hyperproliferative diseases and disorders such as cancer.

CCR2 antagonist 6 (Example 98) is a CCR2 antagonist (Kb: 0.215 μM for CCR2, 0.174 μM for hCCR2B). CCR2 antagonist 6 can be used in the research of inflammation and autoimmune diseases.

CC-M-1 is a potent and selective PI3K/mTOR inhibitor. CC-M-1 inhibits PI3Kα/β/γ/δ and mTOR with IC50 values of 0.68, 1.02, 1.03, 8.03, and 15 nM, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines, including HCT-116 (IC50 = 0.38 μM) and HT-29 (IC50 = 1.70 μM). CC-M-1 can be used for colorectal cancer (CRC) research.

CCL17-IN-2 (Compound Ex.128) is a CCL17 secretion inhibitor with an EC50 of 0.3 nM. CCL17-IN-1 can be used in the research of autoimmune diseases, dermatological conditions, and respiratory disorders.

CCL17-IN-1 (Compound Ex.132) is a CCL17 secretion inhibitor with an EC50 of 0.2 nM. CCL17-IN-1 can be used in the research of autoimmune diseases, dermatological conditions, and respiratory disorders.

CC-11 is an orally active small molecule drug conjugate (SMDC) that links the PI3K/mTOR inhibitor with the extracellular heat shock protein 90 (EHSP90) targeting ligand through a cleavable linker. CC-11 exhibits strong HSP90 binding activity (IC50 = 15 nM) and inhibits PI3Kα kinase activity (IC50 = 0.54 nM). CC-11 has anti-proliferative activity against colon cancer cells. CC-11 shows significant efficacy in the HCT-116 xenograft tumor model. CC-11 can be used for research on colon cancer.

Cbz-QFR-kbt is a ketone-based benzothiazole ketone inhibitor of TMPRSS2, with an IC50 value of 0.42 nM. Cbz-QFR-kbt also has inhibitory activity against Matriptase, Hepsin, HGFA, and Factor Xa, with IC50 values of 1, 1.3, 85, and 85 nM respectively. Cbz-QFR-kbt shows significant inhibitory effects against SARS-CoV-2 and H1N1 (IC50 = 60 nM). Cbz-QFR-kbt can be used in antiviral research.

CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders in studies related to prostate cancer and other cancers.

CBP/p300 ligand-Linker Conjugate 3 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for CBP/p300 and a PROTAC linker, which recruits E3 ligases. CBP/p300 ligand-Linker Conjugate 3 can be used for synthesis of PROTAC CBP/P300 Degrader-2.

CBP/p300 ligand 10 (Compound 3-E) is a CBP/p300 degrader. CBP/p300 ligand 10 also serves as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) and can be used to synthesize the PROTAC CBP/p300 Degrader-2.