pan

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

Pan-RAS-IN-1 is an inhibitor of pan-Ras. It disrupts the interaction of Ras proteins and their effectors.

Pan-KRAS degrader 1 (Compound 1) is a broad-spectrum KRAS degrader, exhibiting an inhibitory constant Ki value of 25 nM against KRASG12V as determined by surface plasmon resonance (SPR). Additionally, this compound demonstrates antitumor activity.

Pan-RAS-IN-7 (Compound D101) is a broad-spectrum RAS inhibitor used in the synthesis of antibody-drug conjugates (ADCs). It is also applicable in cancer research.

Pan-KRAS Ligand 1 serves as a ligand for the target protein of PROTAC (Ligand for Target Protein for PROTAC). This compound facilitates the synthesis of PROTAC Pan-KRAS Degrader 4.

IRAK1 4 pan-FLT3 Kinase-IN-1 (Compound 31) is a potent inhibitor of IRAK1, IRAK4, and FLT3 kinases, demonstrating IC50 values of 5 nM for IRAK1, 0.6 nM for IRAK4, and less than 0.5 nM for FLT3. It exhibits favorable pharmacokinetic properties and holds promise for research in acute myeloid leukemia, with survival extension effects comparable to Gilteritinib.

pan-TEAD-IN-1 (Compound 3) is an orally active pan-inhibitor of TEAD, disrupting its interaction with coactivators YAP TAZ by targeting the palmitoylation site of TEAD. This inhibition leads to the downregulation of oncogene transcription, such as Ctgf and Cyr61, within the Hippo signaling pathway. Demonstrating outstanding efficacy, pan-TEAD-IN-1 has an IC50 of 0.36 nM for luciferase and 1.52 nM for H226 cells, along with favorable pharmacokinetic properties (AUC0–∞= 228.7 μg mL·min, T1 2= 183.9 min). The compound significantly inhibits tumor growth in xenograft models of TEAD-dependent cancers, indicating its potential for research in these cancer types.

Pan-Raf RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRafV600E), 8.86 nM (ARaf), 5.78 nM (BRafWT), and 1.65 nM (CRaf). It exhibits antiproliferative activity against various cancer cell lines and can be utilized in cancer research.

pan-KRAS-IN-17 (Example 34) is an inhibitor that targets multiple forms of the KRAS protein.

Pan-BET/BD2-IN-1 (compound 6b) is a selective BET protein inhibitor with BRDT-1Ki of 1.05 μM and BRD4-1Ki of 0.68 μM. It effectively inhibits the growth of MM.1S cancer cells with an IC50 value of 2.6 μM.

IRAK1/4/pan-FLT3 Kinase-IN-2 (compound 27) is a potent dual inhibitor of IRAK1/4 and FLT3 with IC50 values of 10 nM, 0.7 nM, and < 0.5 nM, respectively. This compound enhances survival in mice models of acute myeloid leukemia.

PAN endonuclease-IN-2 (compound T-31) is a PAN endonuclease inhibitor (IC50: 0.15 μM) and has antiviral properties with broad-spectrum anti-influenza activity. PAN, as the N-terminal PA subunit of the polymerase-RNA complex, possesses a cap-dependent endonuclease (CEN) active site, facilitating RNA cleavage and initiating the synthesis of new RNA molecules. PAN endonuclease-IN-2 targets both influenza HA and RdRp complexes, thereby disrupting viral entry into host cells and impeding viral replication.

pan-KRAS-IN-8 (Compound 38) is an inhibitor of the human tumor mutated gene KRAS. It effectively suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.07 nM and 0.18 nM, respectively.

Pan-KRAS-IN-10 (Compound 58) acts as an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells, specifically AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.7 and 0.24 nM, respectively.

pan-KRAS-IN-7 (Compound 25) is an inhibitor of the human tumorigenic mutant gene KRAS. It effectively suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with an IC50 of 0.35 nM and 0.51 nM, respectively.

Pan-KRAS-IN-8 (Compound 52) is an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 values of 0.24 nM and 0.30 nM, respectively.

pan-KRAS-IN-13 (compound 2) is a potent inhibitor of KRAS, exhibiting IC50 values of 2.75 nM and 2.89 nM for its G12D and G12V mutations, respectively.

pan-KRAS-IN-14 (compound 20) is a Pan-KRAS inhibitor with an IC50 value of 2.3 nM.

Pan-RAS-IN-5 (compound 7A) is a molecular glue that facilitates the formation of a ternary complex with cyclophilin A (CYPA) and RAS(ON) protein. This complex inhibits the binding of RAF downstream of RAS, demonstrating antitumor activity.

pan-HER-IN-1 (Compound C5) is an irreversible, orally active Pan-HER inhibitor that exhibits IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFR T790M/L858R, and 3.5 nM for HER2, respectively. pan-HER-IN-1 induces apoptosis and demonstrates antitumor activities.

pan-HER-IN-2 (Compound C6) is an orally active, reversible, broad-spectrum HER inhibitor that targets EGFR (IC50: 0.72 nM), HER4 (IC50: 2.0 nM), EGFRT790M (IC50: 8.2 nM), and L858R (IC50: 75.1 nM). pan-HER-IN-2 induces apoptosis and possesses anti-tumor effects.

Pan-RAF kinase inhibitor 1 is a potent inhibitor of the Pan-RAF kinase pair, which regulates MAPK signaling and affects the proliferation of RAS-mutated tumor cells. Pan-RAF kinase inhibitor 1 has shown research potential for the study of cancer diseases.

Pan-Trk-IN-2 is a small molecule Trks inhibitor that exhibits promising antitumor effects.

Pan-Trk-IN-3 is a potent, broad-spectrum inhibitor of Trk and its drug-resistant mutants, acting on TrkA (IC50: 2 nM), TrkB (IC50: 3 nM), TrkC (IC50: 2 nM), TrkAG595R (IC50: 21 nM), TrkAG667C (IC50: 26 nM), TrkAG667S (IC50: 5 nM), TrkAF589L (IC50: 7 nM) and TrkCG623R (IC50: 6 nM), TrkAG667S (IC50: 5 nM), TrkAF589L (IC50: 7 nM) and TrkCG623R (IC50: 6 nM). Pan-Trk-IN-3 induces apoptosis and has significant anti-tumour effects.