dual

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

BCI-215 causes selective cancer cell cytotoxicity in part through non-redox-mediated activation of MAPK signaling

SYN1143 (AMG-1) is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol/L, respectively.

Dual FAAH/sEH-IN-1 is a dual inhibitor of sEH (soluble epoxide hydrolase) (IC50: 9.6 nM) and FAAH (fatty acid amide hydrolase) (IC50: 7 nM) with high affinity and anti-inflammatory activity.

Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.

DualCathepsinL/JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1/2/3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL/JAK-IN-1 is applicable in research on acute lung injury (ALI).

Dual AChE-MAO B-IN-4 (compound 7) is a dual inhibitor of AChE and MAO-B, with IC50 values of 261 nM and 15 nM, respectively. It offers protection against oxidative damage induced by H2O2 and 6-OHDA in SH-SY5Y cells and can penetrate the central nervous system in a model simulating the blood-brain barrier. This compound is applicable in research on neurological disorders such as Alzheimer's disease (AD).

Dual FXR/PPARδ agonist-2 is a dual agonist for FXR and PPARδ, derived from the hybridization of the FXR agonist GW-4064 and the PPARδ agonist GW-0742. It exhibits potent dual-target activity, with an EC50 of 12.28 nM for FXR activation and a 69% activation rate of PPARδ at a concentration of 100 nM. Additionally, dual FXR/PPARδ agonist-2 demonstrates antifibrotic effects in a mouse model of pulmonary fibrosis.

Dual GO/LDHA-IN-1 is an orally effective dual-target inhibitor of glycolate oxidase (GO) and lactate dehydrogenase A (LDHA), with Ki values of 390 nM and 40 nM, respectively. It decreases liver LDHA levels, urinary oxalate excretion, and renal calcium oxalate crystal deposition. Dual GO/LDHA-IN-1 is applicable for research in primary hyperoxaluria type 1.

Dual AChE-MAO B-IN-2 is a potent dual inhibitor of AChE (IC50: 0.12 μM) and MAO B (IC50: 0.01 μM) with potential for Alzheimer's disease studies.

Dual AChE-MAO B-IN-1 (compound 15) is a safe, metabolically stable neuroprotective agent. This potent, orally active, CNS-permeable inhibitor demonstrates IC50 values of 550 nM for human AChE and 8.2 nM for MAO-B, indicating low in vitro activity against these enzymes.

Dual AChE-MAO B-IN-3 (Compound C10) is a potent inhibitor of both AChE and MAO-B, with IC50 values of 0.58 μM and 0.41 μM, respectively. It targets the catalytic anionic site and peripheral anionic site of AChE, making it relevant for Alzheimer's disease (AD) research [1].

GIP/GLP-1 dual receptor agonist-1 (compound 4), a receptor agonist for both GIP and GLP-1, shows potential for researching metabolic disorders and fatty liver diseases, such as nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD) [1].

Dual photoCORM 1 (compound 5), a metal-free, photoactive, dual carbon monoxide releasing molecule (CORM), demonstrates efficient cellular uptake and enables real-time tracking of CO release via a colorimetric change in B16F10 cancer cells [1].

GIP/GLP-1 dual receptor agonist-1 (Compound 4) (sodium) functions as a GIP/GLP-1 receptor agonist. This compound is applicable for research into metabolic disorders and liver diseases, including non-alcoholic steatohepatitis (NASH) and non-alcoholic fatty liver disease (NAFLD).

GNF4877 is a small molecule inhibitor, a potent dual-specificity kinase inhibitor targeting DYRK1A (IC50=6 nM) and GSK3β (IC50=16 nM). This compound promotes β-cell proliferation by blocking NFATc nuclear export (EC50=0.66 μM for mouse R7T1 cells) and is primarily used for research on β-cell regeneration related to diabetes.

Cilnidipine (FRC-8653)(FRC8653) is a dual L- and N-type calcium channel blocker and displays antihypertensive, sympatholytic and neuroprotective activity.

GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

Harmine (Telepathine) is an alkaloid isolated from seeds of Peganum harmala.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Harmine hydrochloride (telepathine hydrochloride) is extracted from Peganum Harmala Genus.

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.