dual

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 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-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.

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].

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].

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.

Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.

WH-4-023 (Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK.

Ragaglitazar(NNC-61-0029) is a potent dual PPARα and PPARγ agonist that has shown potent lipid-lowering and insulin sensitizing effects in animal models.Ragaglitazar can be used to study type 2 diabetes.

Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor.

Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.

Proxyphylline (7-(2-Hydroxypropyl)theophylline) is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.

Rupatadine Fumarate (Rinialer) (UR-12592 Fumarate) is a potent dual PAF H1 antagonist with Ki of 0.55 0.1 uM.

(±)-Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.

Sodium 4-nitrophenyl phosphate hexahydrate (4-Nitrophenyl phosphate disodium hexahydrate) is hydrolyzed by alcohol phosphatase (ALP) and can be used to develop a dual-mode immunoassay for the detection of ochratoxin A (OTA).

Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].

Sacubitril Valsartan (LCZ696) is an orally bioavailable, dual angiotensin II receptor and neprilysin inhibitor for the treatment of hypertension and heart failure.

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

Strontium ranelate (S12911), a strontium (II) salt of the ranelic acid, is a medication for osteoporosis. Studies indicate it can also slow the course of osteoarthritis of the knee. The drug is unusual in that it both increases deposition of new bone by osteoblasts and reduces the resorption of bone by osteoclasts. It is therefore promoted as a dual action bone agent (DABA) indicated for use in the treatment of severe osteoporosis.

Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) is a dual agonist of RXRα( EC50=10.4 μM) and PPARγ(EC50=17.7 μM). It blocks TNF-α-induced NF-KB activation.

Br-C10-methyl ester, a PROTAC linker characterized by its alkyl/ether composition, plays a crucial role in the synthesis of a series of PROTACs (MS432). This compound incorporates a dual-ligand system connected via a linker; notably, one ligand interacts with the VHL portion.

Rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.

Norcantharidin (Norcantharadine) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.

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

Adapalene (CD271) is a dual RAR and RXR agonist, utilized in the treatment of skin conditions.

Desmethyl-VS-5584, a dimethyl analog of VS-5584, is a novel and highly selective PI3K mTOR kinase inhibitor used for cancer treatment.

LJ570 is the first PPARα/γ dual agonist (PPARα,PPARγ with EC50s of 1.05 and 0.12 μM, respectively[)

TNF/IFNγ-IN-1 (TGA) is a dual inhibitor of TNF and IFN-γ. TNF/IFNγ-IN-1 has potential antioxidant and anti-inflammatory activities for neurodegenerative diseases such as Alzheimer.

BI-69A11 ((E)-3-(1H-Benzo[d]imidazol-2-yl)-1-(6-chloro-2-hydroxy-4-phenylquinolin-3-yl)prop-2-en-1-one) is a dual AKT and NFkB pathway inhibitor. It enhances the susceptibility of colon cancer cells to mda-7/IL-24-induced growth inhibition by targeting Akt.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.

KX2-361 is a orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma

(S)-HH2853 is a potent dual inhibitor of EZH1 and EZH2, inhibiting EZH2_Y641F with an IC50 of <100 nM.(S)-HH2853 has potential antitumor activity and can be used in the study of autoimmune diseases.

CpCDPK1/TgCDPK1-IN-2 is a dual inhibitor of CpCDPK1 and TgCDPK1 with IC50 values of 12 and 5 nM for CpCDPK1 and TgCDPK1, respectively.CpCDPK1/TgCDPK1-IN-2 can be used in the study of diseases associated with infection of toxoplasmas such as Toxoplasma gondii, Cryptosporidium parvum and C. hominus. CpCDPK1/TgCDPK1-IN-2 can be used to study diseases associated with infections of toxoplasma gondii (T. gondii), Cryptosporidium parvum (C. parvum), and Cryptosporidium hominus (C. hominus).

CpCDPK1/TgCDPK1-IN-3 is a dual inhibitor of CpCDPK1 and TgCDPK1 with an IC50 of 0.003 µM for CpCDPK1 and 0.0036 µM for TgCDPK1. CpCDPK1/TgCDPK1-IN-3 can be used to study infections associated with diseases such as Toxoplasma, Cryptosporidium and Cryptosporidium.

Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.

CB2R FAAH modulator-2 (compound 26) is a dual modulator targeting CB2R and FAAH, acting as a CB2R agonist (Ki = 10.8 nM) and FAAH inhibitor (IC50 = 6.2 μM), with a Ki value of 152.9 nM for CB1R. It has research value in cancer, deleterious inflammatory cascades in neurodegenerative diseases, and COVID-19 infection.

Aleglitazar (R1439) (R1439) is a potent dual PPARα γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.

Izonsteride (LY320236) is a selective and potent 5alpha reductase inhibitor with dual action on the type I and type II isoforms of the enzyme.Izonsteride is used in the treatment of oncology and genitourinary disorders, and may be used in the study of prostate cancer.

CGP 20376 is a benzothiazole compound, an anthelmintic, with dual dose-dependent modulation of in vitro effects on the respiratory burst of eosinophils and antifibrillatory properties.

BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative. BMS-599626 is an orally available and selective dual inhibitor of HER1 and HER2 with IC50s of 20 and 30 nM, respectively. BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor response to radiotherapy.

DORA-22 is a dual orexin receptor antagonist, improves mild stress-induced insomnia with minimal effect on memory

PLpro/RBD-IN-1 is a dual inhibitor of SARS-CoV-2 PLpro and the spiny protein RBD, with anti-novel coronavirus activity, and is seen for the study of viral infections.

CpCDPK1/TgCDPK1-IN-1 is a potent dual inhibitor of CpCDPK1 and TgCDPK1, inhibits Abl and Src, and has antiparasitic activity for the study of Toxoplasma infections and cryptosporidiosis.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

BN-82451 2HCl is a dual inhibitor of COX-1 and COX-2 and can be used to study Huntington's chorea and Parkinson's disease.

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

KSK67 is a selective dual antagonist of sigma-2 and histamine H3 receptors with inhibitory effects on H3 receptors, sigma-1, and sigma-2 receptors, with Ki values of 3.2, 1531, and 101 nM, respectively.KSK67 can be used to study injury pain and neuropathic pain.

Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.

CBHcy is a dual-substrate analogue, a specific BHMT inhibitor that causes betaine-homocysteine S-methyltransferase (BHMT) to adopt the same conformation as the ternary complex, potentially inducing the development of cysteinemia.