ck-1-in-1

CK1-IN-1 (PUN51207) is a casein kinase 1 (CK1) inhibitor. CK1-IN-1 has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

EGFRT790M/L858R/ACK1-IN-1 (Compound 21a) is a dual inhibitor targeting EGFRT790M/L858R and ACK1 with IC50 values of 23 nM and 263 nM, respectively. This compound effectively inhibits cell proliferation and exhibits antitumor activity.

VRK1/CK1-IN-1 (compound 36) is a dual inhibitor targeting vaccinia-related kinase 1 (VRK1) and casein kinase 1 (CK1), with a Ki of 37.9 nM for VRK1. It exhibits IC50 values of 17 nM and 15 nM for CK1 δ and ε isoforms, respectively.

CK2/PIM1-IN-1 is an inhibitor of CK2 (IC50: 3.787 μM) and PIM1 (IC50: 4.327 μM), developed for researching proliferative disorders like cancer and other kinase-associated conditions.

YTHDF2-IN-1 (Compound CK-75) is an inhibitor of YT521-B homology domain family 2 (YTHDF2) with a dissociation constant (Kd) of 26.2 μM, and it effectively blocks the interaction between YTHDF2 and m6A RNA. It suppresses colony formation in JAR cells and exhibits antiproliferative activity in various cancer cell lines, with an IC50 in the micromolar range. Additionally, YTHDF2-IN-1 induces apoptosis in K562 cells and causes cell cycle arrest at the G0/G1 phase.

GSK-3β/CK-1δ-IN-1 (8d) is a dual inhibitor of GSK-3β and CK-1δ that can cross the blood-brain barrier, with IC50 values of 0.77 μM and 0.57 μM, respectively. GSK-3β/CK-1δ-IN-1 (8d) is applicable in neuroblastoma research.

CK-17 is an interleukin-1 antagonist and an IL-1 blocker, which inhibits fibroblast proliferation in a concentration-dependent manner.

Cosibelimab (CK-301; TG-1501) is a fully human, high-affinity monoclonal antibody that inhibits PD-L1 by preventing interaction between PD-L1 and PD-1. Cosibelimab (CK-301; TG-1501), which contains a functional Fc domain, effectively induces antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) against PD-L1-positive cell lines, including lymphoma cells. Cosibelimab (CK-301; TG-1501) is therefore valuable for immuno-oncology investigations involving immune checkpoint signaling, Fc-mediated immune effector functions, and tumor immune microenvironment regulation.

Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective inhibitor of gingipain-K, effectively extending plasma thrombin time (TT) in proportion to dosage and duration [1].

CK-963 is an activator of cardiac troponin (cTnC) with a K i of 11.5 μM, exhibiting activity in enhancing cardiac contractility in Sprague-Dawley rats [1].

Ilexsaponin A (Standard) is a reference standard for research and analysis in studies involving Ilexsaponin A. 1. Ilexsaponin A (Ilexsaponin A1) shows protective effects on ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway.

Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.