dual inhibitor

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.

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

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.

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.

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

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

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].

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.

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.

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.

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.

(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.

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

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.

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.

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.

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

ER-34122, a novel orally available dual 5-lipoxygenase/cyclooxygenase inhibitor, exhibits potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model.

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.

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.

Homobutein (3-O-Methylbutein) is a dual inhibitor of HDACs and NF-κB with IC50s of 190 and 38 μM. Homobutein is an iron chelator with anticancer, anti-inflammatory, antiparasite, and antioxidation activities.

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.

N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine is a novel 2,6-naphthyridine identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor[1].

Ladostigil (Ladostigil free base) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) with inhibitory effects on MAO-B and AChE, with IC50 values of 37.1 and 31.8 μM, respectively.Ladostigil possesses anti-inflammatory, antioxidant, and neuroprotective activities, and may be used in studies of depression and Alzheimer's disease.

Roxindole (EMD 49980) is a selective dopamine autoreceptor and 5-HT1A dual agonist and inhibitor of 5-hydroxytryptamine (5-HT) uptake with antipsychotic and antidepressant activity.Roxindole can be used to study Parkinson's and neurodivergence.

Daniquidone (Batracylin) is a potent dual inhibitor of DNA topoisomerase I and DNA topoisomerase II with cytotoxic and antiproliferative activity that induces DNA fragmentation for the study of neoplasms, immune disorders, and lymphatic disorders.

QL-X-138 HCl is a novel selective and highly potent BTK/MNK dual-kinase inhibitor with anticancer activity that binds covalently to BTK and noncovalently to MNK. QL-X-138 HCl inhibited BTK, MNK1, and MNK2 kinases. QL-X-138 HCl has anti-dengue virus 2 activity and shows anti-proliferative activity in acute myeloid leukemia cells. QL-X-138 HCl can be used to study lymphoma and leukemia.

Tubulin inhibitor 35 (Tubulin IN 35) is a potent dual inhibitor of topoisomerase I and microtubule protein polymerization with antitumor activity, inhibits migration and invasion of MGC-803 and RKO cell lines, interrupts the cell cycle and induces apoptosis.

CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.

XR-11576 HCl is a novel orally active dual topoisomerase I and II inhibitor with antitumor activity.

PI3Kα mTOR-IN-1 is a potent dual inhibitor of PI3Kα mTOR, with an IC50 of 7 nM for PI3Kα in a cell assay and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα [in a cell-free assay], respectively.

mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.

UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3.

RS-601 is a potent dual leukotriene D4/thromboxane A2 inhibitor that inhibits antigen-induced airway hyperresponsiveness (AHR) and shows asthmatic effects in a guinea pig model of asthma.

mTOR/HDAC-IN-1 HCl is a potent dual inhibitor of mTOR and HDAC with potential anti-inflammatory, anti-proliferative, autophagy and apoptosis-inducing effects for cancer research.

OTUB1 USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1 USP8-IN-1 may be used in the study of leukaemia.

KDM4-IN-2 is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [1].

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

DIDS, an anion exchange inhibitor, acts by blocking reversibly and later irreversibly, exchangers such as chloride-bicarbonate exchanger. It is also a RAD51 inhibitor.