Cyclin G-associated Kinase (GAK) Inhibitor

LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC₅₀ of 3.3 nM and a K_i of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC₅₀=14 nM) and a modest inhibitor of GAK (IC₅₀=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research.

KMG-732 is a dual-target inhibitor that targets GAK and β-tubulin, with K_d values of 12.0 nM and 19.3 μM, respectively. KMG-732 exhibits broad-spectrum antiproliferative activity in various human cancer cell lines and directly binds to purified tubulin in vitro. KMG-732 reduces the phosphorylation level of AP2M1, induces G₂/M phase cell cycle arrest, disrupts the microtubule network, and inhibits cancer cell migration and invasion. KMG-732 shows significant antitumor activity in organoid and in vivo xenograft models. KMG-732 can be used for cancer research.

BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC₅₀ value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC₅₀ values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain.

NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK₁) receptor antagonist with IC₅₀ of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK₂, NK₃ receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.

6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase).

ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17 IC₅₀ 0.939 μM and HDAC2 IC₅₀ 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer.

CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer.

EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with K_D values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells.

BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC₅₀ value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC₅₀ values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain.

ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.

BMT-090605 (hydrochloride) (Standard) is the analytical standard of BMT-090605 (hydrochloride) (HY-101290A). This product is intended for research and analytical applications. BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain.

AAK1-IN-7 (Compound 16) is a dual AAK1/GAK inhibitor (EC₅₀ values are 40 and 80 nM, respectively). AAK1-IN-7 inhibits the phosphorylation of AP2-µ2 subunit at T156. AAK1-IN-7 has weak antiviral activity against RNA viruses.

GAK-IN-3 is a cyclin G-associated kinase (GAK) inhibitor with an IC₅₀ of 207 nM and a K_i of 66 nM. GAK-IN-3 inhibits kinase activity in the nanomolar range by binding to GAK’s ATP-binding site. GAK-IN-3 acts as a cytotoxic agent that reduces viability of Ewing sarcoma cells. GAK-IN-3 can be used for the research of ewing sarcoma.

AAK1-IN-8 (Compound 18) is a pan-NAK inhibitor. AAK1-IN-8 inhibits AAK1 and GAK (EC₅₀ values are 50 and 190 nM, respectively). AAK1-IN-8 inhibits the phosphorylation of AP2-µ2 subunit at T156.