Search Result
Results for "
Dual inhibitor
" in MedChemExpress (MCE) Product Catalog:
15
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12299
-
|
Dual LCK/SRC inhibitor
|
Src
|
Cancer
|
|
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
|
-
-
- HY-109108A
-
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DS-3201 tosylate
|
Histone Methyltransferase
|
Cancer
|
|
Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma .
|
-
-
- HY-155195
-
|
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Others
|
Cancer
|
|
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .
|
-
-
- HY-12652
-
|
|
mTOR
|
Cancer
|
AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K .
|
-
-
- HY-129426
-
|
|
Akt
|
Cancer
|
|
PDK1/Akt/Flt dual pathway inhibitor is one of a component of KP372-1 (HY-15673 ), and inhibits PDK1/Akt/Flt dual pathway .
|
-
-
- HY-163787
-
|
|
CDK
|
Cancer
|
|
YY173 is a dual inhibitor for CDK4 and CDK6 with IC50 of 7.7 and 88 nM. YY173 inhibits the proliferation of cell Jurkat with an IC50 of 1.46 μM. YY173 can be used for synthesis of PROTAC CDK4/6 degrader 1 (HY-163786) .
|
-
-
- HY-19373
-
|
3DP-10017
|
Thrombin
Factor Xa
|
Cardiovascular Disease
|
|
RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
|
-
-
- HY-101776
-
|
Desmethyl-SB2343
|
mTOR
PI3K
|
Cancer
|
|
Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure .
|
-
-
- HY-144824
-
|
|
Cytochrome P450
Monoamine Oxidase
|
Neurological Disease
Cancer
|
|
Monoamine oxidase/Aromatase-IN-1 (compound 2q) is a highly potent monoamine oxidase (MAO) and aromatase dual inhibitor with IC50s of 39 nM and 31 nM for MAO-B and aromatase, respectively. Monoamine oxidase/Aromatase-IN-1 can be used for researching neurological disorder and breast cancer .
|
-
-
- HY-158763
-
|
TG0205221
|
SARS-CoV
Cathepsin
Virus Protease
|
Infection
|
|
MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19 .
|
-
-
- HY-119374
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity .
|
-
-
- HY-158264
-
-
-
- HY-147922
-
|
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
|
hCAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with Ki values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity .
|
-
-
- HY-147923
-
|
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
|
hCAI/II-IN-3 (compound 5b) is a potent dual hCA I/II inhibitor with Ki values of 51.25, 13.15 and 42.18 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity .
|
-
-
- HY-155160
-
|
|
Lipoxygenase
COX
|
Inflammation/Immunology
|
|
COX-2/15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2/15-LOX with IC50s of 0.075 μM and 1.97 μM, respectively. COX-2/15-LOX-IN-3 can inhibit LPS-induced cell production of promoting cytokines (IL-6, ROS, and NO), with specific anti-inflammatory activity .
|
-
-
- HY-155161
-
|
|
Lipoxygenase
COX
|
Inflammation/Immunology
|
|
COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor of COX-2/15-LOX with IC50s of 0.075 μM and 1.97 μM, respectively. COX-2/15-LOX-IN-4 can inhibit LPS-induced cell production of promoting cytokines (IL-6, ROS) with specific anti-inflammatory activity .
|
-
-
- HY-151211
-
|
|
Btk
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia .
|
-
-
- HY-155493
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and
aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer .
|
-
-
- HY-168088
-
|
|
HDAC
DNA Methyltransferase
|
Cancer
|
|
DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .
|
-
-
- HY-115904
-
|
|
CDK
FLT3
|
Cancer
|
|
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .
|
-
-
- HY-156094
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .
|
-
-
- HY-150774
-
|
|
HDAC
HSP
Apoptosis
|
Cancer
|
|
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
|
-
-
- HY-15496
-
|
ER-806201
|
MEK
FLT3
|
Cancer
|
|
E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
|
-
-
- HY-149016
-
|
|
Microtubule/Tubulin
Farnesyl Transferase
|
Cancer
|
|
Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity .
|
-
-
- HY-144806
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis .
|
-
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
-
- HY-162061
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
ChEs/MAOs-IN-1 (Compound 4i) is a dual inhibitor of cholinesterases (ChEs) and monoamine oxidases (MAOs).ChEs/MAOs-IN-1 has IC50 values of 0.048 μM, 0.89 μM, 3.58 μM, and 0.095 μM for AChE, BChE, MAO-B and MAO-B respectively. ChEs/MAOs-IN-1 can be used in the study of neurodegenerative diseases .
|
-
-
- HY-10371
-
|
LKB1/AAK1 Dual inhibitor
|
Pim
|
Cancer
|
|
Pim1/AKK1-IN-1 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.
|
-
-
- HY-B0703
-
-
-
- HY-151885
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
Dual AChE-MAO B-IN-3 (compound C10) is a potent dual AChE/MAO-B inhibitior, with IC50 values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site of AChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research .
|
-
-
- HY-110378
-
-
-
- HY-139950
-
|
|
Ras
|
Cancer
|
Rasarfin is a dual Ras and ARF6 inhibitor .
|
-
-
- HY-144738
-
|
|
Epoxide Hydrolase
FAAH
|
Inflammation/Immunology
|
|
Dual FAAH/sEH-IN-1 (compound 3) is a high affinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC50 values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase .
|
-
-
- HY-145708
-
-
-
- HY-B0703S
-
-
-
- HY-158695
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
Dual AChE-MAO B-IN-4 (compound 7) is a dual AChE/MAO-B inhibitor, with IC50 values of 261 nM and 15 nM, respectively. Dual AChE-MAO B-IN-4 protects against oxidative damage induced by H2O2 and 6-OHDA in SH-SY5Y cells. Dual AChE-MAO B-IN-4 can penetrate the central nervous system in a cell model that mimics the blood-brain barrier. Dual AChE-MAO B-IN-4 can be used in the study of neurological diseases such as Alzheimer's disease (AD) .
|
-
-
- HY-115875
-
-
-
- HY-13758A
-
|
BMS-247615 dihydrochloride
|
Topoisomerase
|
Cancer
|
|
TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
|
-
-
- HY-13758
-
|
BMS-247615
|
Topoisomerase
|
Cancer
|
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TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
|
-
-
- HY-18208
-
-
-
- HY-114332
-
-
-
- HY-115851
-
-
-
- HY-15516
-
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LX-4211; LP-802034
|
SGLT
|
Metabolic Disease
|
|
Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.
|
-
-
- HY-16273A
-
|
|
Farnesyl Transferase
|
Cancer
|
|
L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC50 values of 2 nM and 98 nM respectively.
|
-
-
- HY-132867
-
|
|
Pim
|
Cancer
|
|
MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.
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-
-
- HY-112247
-
|
|
PPAR
|
Metabolic Disease
|
|
SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites .
|
-
-
- HY-123322
-
-
-
- HY-157965
-
|
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VEGFR
FAK
|
Cancer
|
|
ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research .
|
-
-
- HY-129666
-
|
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Others
|
Neurological Disease
|
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NSC-65847 is a groundbreaking dual inhibitor targeting both viral neuraminidase and Streptococcus pneumoniae neuraminidase.
|
-
-
- HY-100509
-
-
- HY-118779
-
-
- HY-109565
-
|
ASTX660
|
IAP
Apoptosis
|
Cancer
|
|
Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-157090
-
-
- HY-12453
-
-
- HY-101510
-
|
|
Phosphatase
|
Cancer
|
|
F1063-0967 is a Dual-specificity phosphatase 26 (DUSP26) inhibitor with an IC50 of 11.62 μM.
|
-
- HY-18207
-
-
- HY-115952
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2 .
|
-
- HY-160172
-
-
- HY-160172A
-
-
- HY-163128
-
-
- HY-163580
-
-
- HY-163581A
-
-
- HY-168170
-
|
|
VEGFR
EGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-2 (compound 4b) is an dual inhibitor VEGFR-2 and EGFR.
|
-
- HY-101053
-
|
Src Kinase inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-112164
-
-
- HY-10181S
-
-
- HY-122909
-
-
- HY-132893
-
|
|
TAM Receptor
|
Cancer
|
|
AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
|
-
- HY-115870
-
-
- HY-144904
-
|
|
HDAC
|
Cancer
|
|
MC4343 is a potent and dual inhibitor of EZH2 and histone deacetylase. MC4343 has the potential for the research of cancer disease.
|
-
- HY-147910
-
-
- HY-16273
-
-
- HY-160944
-
|
|
Sirtuin
|
Cancer
|
|
hsa62 is a dual inhibitor for SIRT1 and SIRT2, with IC50 of 1.3 and 5.5 μM, respectively .
|
-
- HY-16273B
-
|
|
Farnesyl Transferase
|
Cancer
|
|
L-778123 dihydrochloride is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM, respectively .
|
-
- HY-161978
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-22 (Compound 1-A) is a CDK4 and CDK6 dual inhibitor .
|
-
- HY-107720
-
|
|
NO Synthase
|
Cancer
|
|
ARL-17477 is a dual inhibitor of NOS1and the autophagy-lysosomal system with anticancer activity and can inhibit tumor growth in KRAS-mutated cancers .
|
-
- HY-112807
-
|
|
SGLT
|
Metabolic Disease
|
|
SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively .
|
-
- HY-15869
-
|
INZ
|
Sirtuin
MDM-2/p53
|
Cancer
|
|
Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
|
-
- HY-17603
-
-
- HY-103714A
-
-
- HY-103714
-
-
- HY-124062
-
TAS-114
2 Publications Verification
|
Others
|
Cancer
|
|
TAS-114 is an orally active dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine .
|
-
- HY-122591
-
PTUPB
1 Publications Verification
|
COX
|
Metabolic Disease
Cancer
|
|
PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC50 of 0.9 nM and 1.26 μM, respectively .
|
-
- HY-133794
-
|
|
Drug Metabolite
|
Cancer
|
|
Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor .
|
-
- HY-145029
-
-
- HY-145852
-
-
- HY-146143
-
|
|
Others
|
Infection
|
|
Falcipain-2/3-IN-2 (Compound 12) is a dual falcipain-2 and falcipain-3 inhibitor .
|
-
- HY-10363
-
|
|
Bcr-Abl
Src
|
Cancer
|
|
AP 24149 is a potent Src-Abl dual inhibitor with IC50 values of 9.1, 3.6 nM for Src and Abl, respectively .
|
-
- HY-161025
-
|
|
c-Fms
VEGFR
|
Cancer
|
|
SYHA1813 is a dual inhibitor of CSF1R and VEGFR. SYHA1813 has potent antitumor activity against GBM .
|
-
- HY-168523
-
-
- HY-116277
-
|
|
Others
|
Cancer
|
|
Z118332870 is a potent dual inhibitor of EGFR and BRD4, exhibiting significant potential as a therapeutic agent for overcoming resistance in cancer treatment.
|
-
- HY-14682
-
|
|
IKK
|
Inflammation/Immunology
|
|
GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
|
-
- HY-112147
-
-
- HY-107636
-
DC_AC50
3 Publications Verification
|
Apoptosis
|
Cancer
|
DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones). Inhibiting intracellular copper chaperones as a means of reducing/preventing acquired chemotherapy resistance .
|
-
- HY-112319
-
-
- HY-12039
-
|
Bafetinib analog
|
Bcr-Abl
|
Cancer
|
|
Lyn-IN-1 (Bafetinib analog) is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1.
|
-
- HY-15434
-
-
- HY-B0196
-
-
- HY-B0196A
-
|
Wy 45030 hydrochloride
|
Serotonin Transporter
|
Neurological Disease
Cancer
|
|
Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
|
-
- HY-13461A
-
|
CAY-10572 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
|
-
- HY-P0090
-
|
Salmon calcitonin
|
CGRP Receptor
|
Cancer
|
|
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
|
-
- HY-U00177
-
GDP366
1 Publications Verification
|
Survivin
|
Cancer
|
|
GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
|
-
- HY-111416
-
-
- HY-13461
-
|
CAY10572
|
CDK
|
Cancer
|
|
PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
|
-
- HY-13219
-
-
- HY-155341
-
|
|
FLT3
Haspin Kinase
|
Cancer
|
|
HSK205 is a dual FLT3 and haspin inhibitor, with IC50 of 0.187 nM for FLT3. HSK205 has antitumor activity .
|
-
- HY-12605
-
|
|
Thrombin
|
Metabolic Disease
|
|
SAR107375 is a potent and orally active dual thrombin and factor Xa inhibitor, with Ki values of 1 nM and 8 nM for factor Xa and thrombin, respectively .
|
-
- HY-162124
-
|
|
NAMPT
HDAC
|
Cancer
|
|
HDAC/NAMPT-IN-1 (compound 39h) is a dual inhibitor of HDAC and NAMPT with IC50 values of 0.72-37081 nM and 1618 nM .
|
-
- HY-119937
-
-
- HY-137996
-
|
|
Akt
mTOR
|
Metabolic Disease
|
|
Dehydrovomifoliol is a AKT/mTOR dual inhibitor. Dehydrovomifoliol reduces lipid accumulation and lipogenesis by inhibiting the AKT/mTOR signaling pathway. Dehydrovomifoliol is used in nonalcoholic fatty liver disease research (NAFLD) .
|
-
- HY-144438
-
|
|
Aurora Kinase
LIM Kinase (LIMK)
|
Cancer
|
|
Aurora/LIM kinase-IN-1 (Compound F114) is a potent and dual inhibitor of aurora and lim kinase. Aurora kinases and lim kinases are involved in neoplastic cell division and cell motility, respectively. Aurora/LIM kinase-IN-1 inhibits GBM proliferation and invasion. Aurora/LIM kinase-IN-1 is a promising new scaffold for dual aurora/lim kinase inhibitors that may be used in future agent development efforts for GBM, and potentially other cancers .
|
-
- HY-13068
-
|
E-7050
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
|
-
- HY-11042
-
GNE-477
1 Publications Verification
|
PI3K
mTOR
|
Cancer
|
|
GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
|
-
- HY-104065
-
|
SHR-1258
|
EGFR
|
Cancer
|
|
Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
|
-
- HY-104065A
-
|
(Rac)-SHR-1258
|
Others
|
Cancer
|
|
(Rac)-Pyrotinib ((Rac)-SHR-1258) is the racemate of Pyrotinib (HY-104065). Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.
|
-
- HY-139879
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC50 values of 0.94 and 0.48 μM, respectively.
|
-
- HY-145336
-
|
|
JAK
|
Cancer
|
|
JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 (IC50 = 29 and 41 nM respectively).
|
-
- HY-117608
-
|
|
CDK
DYRK
|
Neurological Disease
Cancer
|
|
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research .
|
-
- HY-117608A
-
|
|
CDK
DYRK
|
Neurological Disease
Cancer
|
|
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research .
|
-
- HY-156722
-
-
- HY-162788
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-121 (compound 15) is a EGFR and VEGFR-2 dual inhibitor with IC50s of 84 and 3.5 nM, respectively .
|
-
- HY-162952
-
|
|
Bcr-Abl
|
Cancer
|
|
cSRC/BCR-ABL1-IN-1 (compund 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor .
|
-
- HY-16736A
-
-
- HY-16736
-
-
- HY-N2426
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Clerodendrin is a nature product could be isolated from Lobelia chinensis. Clerodendrin is a potent dual Interleukin-4 (IL-4) inhibitor and β-hexosaminidase (Hex) inhibitor .
|
-
- HY-N1322
-
|
|
Others
|
Others
|
|
Sanggenol A acts as a dual inhibitor of nitrofuranone reduction mediated by the intestinal microbial nitrification reductases EcNfsA and EcNfsB. In addition, Sanggenol A is also an effective inhibitor of intestinal bacterial β-glucuronidase .
|
-
- HY-145695
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability .
|
-
- HY-15250
-
JZL195
4 Publications Verification
|
FAAH
MAGL
Autophagy
|
Neurological Disease
|
|
JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively .
|
-
- HY-19205A
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
|
-
- HY-13455
-
|
|
Haspin Kinase
DYRK
|
Cancer
|
|
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively .
|
-
- HY-112623
-
-
- HY-13455A
-
|
|
Haspin Kinase
DYRK
|
Cancer
|
|
LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively .
|
-
- HY-N0493
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
Pectolinarigenin is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity . Pectolinarigenin has potent inhibitory activities on melanogenesis .
|
-
- HY-132883
-
|
|
EGFR
|
Cancer
|
|
EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer research.
|
-
- HY-147361
-
|
|
Apoptosis
Lactate Dehydrogenase
|
Cancer
|
|
LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression .
|
-
- HY-N8480
-
-
- HY-155392
-
|
|
HDAC
Sirtuin
|
Cancer
|
|
Mz325 is a dual inhibitor of HDAC and Sirt2, with the IC50 of 9.7 μM to Sirt2, that play an important role in pathogenesis of cancer and neurodegeneration .
|
-
- HY-133490A
-
|
|
Apoptosis
|
Cancer
|
|
ST1074 is a dual CerS2/CerS4 inhibitor that induces apoptosis. ST1074 can be used in cancer research .
|
-
- HY-137966A
-
|
AL-8520 oxalate
|
Carbonic Anhydrase
|
Cancer
|
|
N-Desethyl Brinzolamide oxalate is a dual inhibitor of Carbonic anhydrase II and Carbonic anhydrase IV with IC50s of 1.28 and 128 nM, respectively .
|
-
- HY-123289
-
|
|
JAK
|
Inflammation/Immunology
|
|
CP-690550A is an analogue of Tofacitinib (HY-40354). CP-690550A is a dual inhibitor of JAK2 and JAK3 .
|
-
- HY-18652
-
|
Ro 5126766; CH5126766
|
MEK
Raf
|
Cancer
|
|
Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
|
-
- HY-136383
-
AZA1
1 Publications Verification
Rac1/Cdc42-IN-1
|
Ras
Apoptosis
|
Cancer
|
|
AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion .
|
-
- HY-104065B
-
|
SHR-1258 dimaleate
|
EGFR
|
Cancer
|
|
Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
|
-
- HY-111048
-
Corin
3 Publications Verification
|
Histone Demethylase
HDAC
|
Cancer
|
|
Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
|
-
- HY-111421
-
-
- HY-116437
-
|
|
EGFR
|
Cancer
|
|
Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects .
|
-
- HY-117761
-
|
|
PPAR
|
Metabolic Disease
Cancer
|
|
MHY908 is a potent dual agonist of PPARα and PPARγ . MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity .
|
-
- HY-149654
-
-
- HY-160487
-
|
|
IRAK
|
Cancer
|
|
KME-2780 is a potent and selective dual IRAK1 and IRAK4 inhibitor and can be used for research of dysregulation of innate immune signaling and hematologic malignancies .
|
-
- HY-N10076
-
-
- HY-N12735
-
|
|
NF-κB
NO Synthase
|
Others
|
|
Hymenoxin (compound 7) is a dual inhibitor of iNOS and NF-κB with IC50 of 42.7 μM and 85.5 μM respectively. Hymenoxin can inhibit 16% of oxidative stress at a concentration of 125 μg/mL .
|
-
- HY-146016
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-5 (compound 19a) is a potent and dual PI3K and mTOR inhibitor, with IC50 values of 86.9 nM and 14.6 nM, respectively .
|
-
- HY-128685
-
|
Ac12Az9
|
P-glycoprotein
BCRP
|
Cancer
|
|
FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity .
|
-
- HY-129700
-
|
|
Bcl-2 Family
|
Cancer
|
|
MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor .
|
-
- HY-10158S
-
-
- HY-B0196B
-
|
|
Serotonin Transporter
|
Cancer
|
|
(S)-Venlafaxine is the (S)-configuration of Venlafaxine. Venlafaxine is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant agent .
|
-
- HY-129702
-
|
|
Bcl-2 Family
|
Cancer
|
|
MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor .
|
-
- HY-126288
-
ASTX029
4 Publications Verification
|
ERK
Apoptosis
|
Cancer
|
|
ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity .
|
-
- HY-157089
-
-
- HY-161469
-
-
- HY-139175
-
|
|
Others
|
Others
|
|
ZLY032 is a dual FFA1/PPARδ agonist with the activity of improving glucose and lipid metabolism, alleviating liver fibrosis, and potentially inhibiting metabolic disorders.
|
-
- HY-15198
-
|
|
Raf
PDGFR
FLT3
c-Kit
|
Cancer
|
|
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities .
|
-
- HY-156655A
-
|
STI-1558 sodium
|
SARS-CoV
Cathepsin
|
Infection
|
|
Olgotrelvir sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
|
-
- HY-15889
-
AMG 925
2 Publications Verification
|
FLT3
CDK
|
Cancer
|
|
AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
|
-
- HY-15889A
-
|
|
FLT3
CDK
|
Cancer
|
|
AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
|
-
- HY-138944
-
|
|
SGLT
|
Metabolic Disease
|
|
SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor extract from WO2015032272A1, compound 2 .
|
-
- HY-120823
-
-
- HY-152954
-
|
|
DAPK
|
Inflammation/Immunology
|
|
DRAK1/2-IN-1 (compound 10e) is an active dual DRAK1 and DRAK2 inhibitor with Kd values of 1 μM and 6 μM, respectively .
|
-
- HY-149471
-
|
|
Tyrosinase
|
Cancer
|
|
hTYR/AbTYR-IN-1 (Compound 7) is a hTYR/AbTYR dual inhibitor, with IC50s of 5.4 μM and 3.52 μM for hTYR and AbTYR respectively .
|
-
- HY-122161
-
|
RWJ-355871
|
Cathepsin
|
Inflammation/Immunology
|
|
JNJ-10311795 (RWJ-355871), a potent dual inhibitor of neutrophil cathepsin G (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM), exhibits noteworthy antiinflammatory activity .
|
-
- HY-133794S
-
|
|
Drug Metabolite
|
Cancer
|
|
Dasatinib N-oxide-d8 is the deuterium labeled Dasatinib N-oxide. Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor[1][2].
|
-
- HY-143886
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
AD011 is a dual inhibitor of cACE/NEP. AD011 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD011 has the potential for providing the potent antihypertensive and cardioprotective benefits .
|
-
- HY-143887
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
AD012 is a dual inhibitor of cACE/NEP. AD012 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD012 has the potential for providing the potent antihypertensive and cardioprotective benefits .
|
-
- HY-143888
-
-
- HY-115941
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo .
|
-
- HY-135490
-
-
- HY-N12041
-
|
|
TAM Receptor
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .
|
-
- HY-124654
-
|
|
SARS-CoV
|
Metabolic Disease
|
|
SS148 is a dual inhibitor of nsp14/nsp16 MTase. SS148 significant inhibits nsp10–nsp16 with an IC50 of 1.2 μM .
|
-
- HY-10191
-
|
OSI-906
|
IGF-1R
Insulin Receptor
|
Endocrinology
Cancer
|
|
Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively .
|
-
- HY-112164A
-
|
IDO/TDO inhibitor (R-enantiomer)
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IACS-8968 (R-enantiomer) is the R-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
|
-
- HY-112164B
-
|
IDO/TDO inhibitor (S-enantiomer)
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IACS-8968 (S-enantiomer) is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
|
-
- HY-112314
-
|
|
Src
Bcr-Abl
Apoptosis
|
Cancer
|
|
AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity . AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells .
|
-
- HY-120086
-
-
- HY-126320
-
|
|
EGFR
c-Met/HGFR
|
Cancer
|
|
EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC .
|
-
- HY-12793
-
|
KPT-9274
|
PAK
NAMPT
|
Cancer
|
|
Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively .
|
-
- HY-161016
-
-
- HY-161876
-
-
- HY-10725
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
Tanogitran is a dual inhibitor targeting Factor Xa and thrombin (thrombin), with Ki values of 26 and 2.7 nM, respectively. Tanogitran exhibits anticoagulant activity and can be used for research in thrombotic diseases .
|
-
- HY-160685
-
|
|
VEGFR
|
Others
|
|
GW809897X is a dual inhibitor of Fluc and VEGFR with IC50 of 0.58 μM and 65 nM, respectively. GW809897X is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential impact on Fluc reporter assays .
|
-
- HY-160684
-
|
|
VEGFR
|
Others
|
|
GW701427A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.12 μM and 603 nM, respectively. GW701427A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays .
|
-
- HY-107364
-
|
Mol 211
|
EGFR
PI3K
|
Cancer
|
|
MTX-211 (Mol 211) is a dual inhibitor of EGFR and PI3K with IC50 values of ＜100 nM. MTX-211 can be used for the research of cancer and other diseases .
|
-
- HY-107424
-
BAY-299
2 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
|
BAY-299 is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.
|
-
- HY-112473
-
|
|
Ras
Others
|
Cancer
|
|
NAV-2729 is a dual Arf1/Arf6 activation inhibitor. ADP ribosylation factors (Arfs) are members of the Arf family of GTP-binding proteins of the Ras superfamily.
|
-
- HY-121087
-
BCI-215
2 Publications Verification
|
Phosphatase
|
Cancer
|
|
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells .
|
-
- HY-131669
-
|
Dasatinib carboxylic acid
|
Drug Metabolite
|
Others
Cancer
|
|
Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib (HY-10181). Dasatinib is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor .
|
-
- HY-N2682A
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
(E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors . And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area .
|
-
- HY-115871
-
-
- HY-161350
-
-
- HY-P0090A
-
|
Salmon calcitonin acetate
|
CGRP Receptor
|
Cancer
|
|
Calcitonin (salmon) (acetate) is a dual-action amylin and calcitonin receptor agonist, can stimulate bone formation and inhibit bone resorption .The acetate form can affect the absorption and efficacy of hormones .
|
-
- HY-161702
-
|
|
FABP
|
Metabolic Disease
|
|
RO6806051 (compound12) is a potent dual fatty acid binding protein 4 and 5 (FABP4 and FABP5) inhibitor with good selectivity and absorption, distribution, metabolism and excretion (eADME) properties .
|
-
- HY-163733
-
-
- HY-19876
-
|
Debio-0827
|
Opioid Receptor
Aminopeptidase
Neprilysin
|
Neurological Disease
Metabolic Disease
|
|
PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain .
|
-
- HY-15999
-
|
PRT062070; PRT2070
|
JAK
Syk
|
Cancer
|
|
Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
|
-
- HY-19642A
-
|
MGCD265 hydrochloride
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
|
-
- HY-101438
-
-
- HY-19642
-
|
MGCD265
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
|
-
- HY-144794
-
|
|
Apoptosis
EGFR
FAK
|
Cancer
|
|
EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis .
|
-
- HY-141476
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity .
|
-
- HY-13994
-
|
|
Mps1
Polo-like Kinase (PLK)
|
Cancer
|
|
Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
|
-
- HY-16962
-
CC-115
2 Publications Verification
|
DNA-PK
mTOR
|
Cancer
|
|
CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
|
-
- HY-16962A
-
|
|
DNA-PK
mTOR
|
Cancer
|
|
CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
|
-
- HY-112842
-
MBQ-167
5 Publications Verification
|
Ras
CDK
|
Cancer
|
|
MBQ-167 is a dual Rac/Cdc42 inhibitor, with IC50s of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively.
|
-
- HY-B0196S
-
-
- HY-B0196AS1
-
|
Wy 45030-d6 hydrochloride
|
Serotonin Transporter
|
Neurological Disease
|
|
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
|
-
- HY-131284
-
|
|
Drug Metabolite
|
Others
|
|
(S)-Dehydro Venlafaxine is an inactive S-enantiomer of Dehydro Venlafaxine. Dehydro Venlafaxine is an impurity of Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is a potent serotonin (5-HT) / norepinephrine (NE) reuptake dual inhibitor .
|
-
- HY-132885
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
|
-
- HY-141864
-
|
|
Itk
|
Inflammation/Immunology
|
|
ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
|
-
- HY-142834
-
-
- HY-149284
-
|
|
JAK
HDAC
|
Cancer
|
|
JAK/HDAC-IN-3 (13a) is a dual JAK and HDAC inhibitor, with IC50 values of 25.36 nM, 0.2 μM and 0.43 μM for JAK2, HDAC and HDAC1, respectively .
|
-
- HY-N12075
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Dehydrodiscretamine chloride is a dual inhibitor of AChE and BChE with IC50s of 17.8 and 118.8 μM, respectively. Dehydrodiscretamine chloride has antioxidant activity. Dehydrodiscretamine chloride can be used in study Alzheimer’s disease .
|
-
- HY-19833
-
|
|
Cytochrome P450
|
Cancer
|
|
CFG920 is an orally active, nonsteroidal, reversible dual CYP17 and CYP11B2 inhibitor. CFG920 has the potential for metastatic castration-resistant prostate cancer research .
|
-
- HY-B0161D
-
|
LY248686 hydrochloride
|
Others
|
Others
|
|
(R)-Duloxetine (LY248686) Hydrochloride is a napthalenyloxy-substituted amine utilized in binding studies with human serum albumin, and unlike its enantiomer (S)-Duloxetine, it exhibits limited efficacy as a dual serotonin and norepinephrine reuptake inhibitor (SNRI).
|
-
- HY-147703
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
|
-
- HY-101438A
-
-
- HY-143398
-
|
|
PARP
|
Cancer
|
|
PARP10/15-IN-1 (compound 8l) is a potent inhibitor of dual inhibitor of PARP10 and PARP15, with IC50s of 160 nM and 370 nM, respectively. PARP10/15-IN-1 can be used for cancer .
|
-
- HY-147243
-
|
ANG-3070
|
VEGFR
PDGFR
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases .
|
-
- HY-141584
-
|
|
MDM-2/p53
|
Cancer
|
|
ATSP-7041, a selective dual peptide inhibitor of MDM2 and MDMX, effectively reactivates the p53 tumor suppressor pathway in a mechanism-dependent manner in p53-positive cancers .
|
-
- HY-50698
-
-
- HY-B0196AS
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
Venlafaxine-d10 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine (Wy 45030) hydrochloride is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1][2].
|
-
- HY-103443
-
|
|
EGFR
|
Cancer
|
|
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation .
|
-
- HY-10460
-
|
|
Pyk2
FAK
|
Cancer
|
|
PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively .
|
-
- HY-142645
-
|
|
RSV
|
Infection
|
|
TP0591816 is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins (wild-type, EC50 = 0.27 nM; D486N-mutant, EC50 = 0.70 nM).
|
-
- HY-145723
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
|
-
- HY-145723A
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 hydrochloride is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hydrochloride has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
|
-
- HY-B0196S1
-
-
- HY-156754
-
-
- HY-156796
-
|
|
ADC Cytotoxin
|
Neurological Disease
Cancer
|
|
Akt/ROCK-IN-1 (B12) is a dual inhibitor for Akt and ROCK, with the IC50s of 0.023 nM and 1.47 nM, respectively. Akt/ROCK-IN-1 has antitumor activity for neuroblastoma .
|
-
- HY-106587A
-
|
Clorotepine maleate salt
|
Dopamine Receptor
|
Neurological Disease
|
|
Octoclothepin maleate salt, an orally active neuroleptic agent, is a dual SR-2A and D2DR inhibitor. Octoclothepin maleate salt reveals an intensive central depressant action in a series of observational and instrumental procedures in rodents .
|
-
- HY-161642
-
|
|
Dengue virus
Flavivirus
|
Infection
|
|
DENV-2/ZIKV-IN-1 (Compd 16a) is a dual inhibitor of Dengue virus (DENV) and Zika virus (ZIKV) with EC50s of 1.4 and 2.4 μM, respectively .
|
-
- HY-136860
-
|
(R)-Wy 45030
|
5-HT Receptor
|
Neurological Disease
|
|
(R)-Venlafaxine is the R-enantiomer of venlafaxine (HY-B0196), an orally active and potent dual inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake. (R)-Venlafaxine can be utilized in antidepressant research .
|
-
- HY-155414
-
|
|
Elastase
|
Inflammation/Immunology
|
|
Neutrophil elastase inhibitor 5 (compound 29) is a dual inhibitor of HNE (human neutrophil elastase) and proteinase 3 (PR3) with IC50 values of 4.91 μM and 20.69 μM, respectively. Neutrophil elastase inhibitor 5 can be used in the study of neutrophil inflammatory diseases .
|
-
- HY-149002
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research .
|
-
- HY-145244
-
|
|
Akt
|
Cancer
|
|
APN/AKT-IN-1 is a potent and dual inhibitor of APN and AKT with IC50s of 0.21 and 0.27 μM, respectively. APN/AKT-IN-1 can effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT .
|
-
- HY-157490
-
|
|
PARP
HDAC
|
Cancer
|
|
PARP/HDAC-IN-1 (compound B102) is a potent dual inhibitor of PARP and HDAC. PARP/HDAC-IN-1 inhibits PARP1, PARP2 and HDAC1 with IC50s of 19.01, 2.13, 1690 nM, respectively .
|
-
- HY-100398
-
|
|
PI3K
mTOR
|
Cancer
|
|
PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
|
-
- HY-108709
-
CC-671
1 Publications Verification
|
CDK
|
Cancer
|
|
CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.
|
-
- HY-14882A
-
|
TAK-652 Mesylate; TBR-652 Mesylate
|
CCR
HIV
|
Infection
Inflammation/Immunology
Endocrinology
|
|
Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
|
-
- HY-109108
-
|
DS-3201
|
Histone Methyltransferase
|
Cancer
|
|
Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma .
|
-
- HY-125741
-
|
|
Tie
VEGFR
|
Cancer
|
|
GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity 。
|
-
- HY-115951
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor of EGFR and HER2 with IC50 values of 5.02 µM and 0.83 µM against EGFR and HER2, respectively .
|
-
- HY-N0737A
-
|
Telepathine
|
DYRK
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
|
-
- HY-129496
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca 2+ inward flow .
|
-
- HY-156607
-
|
|
Phosphatase
|
Cancer
|
|
Anticancer agent 143 (compound 369) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 143 can be used in cancer research .
|
-
- HY-156608
-
|
|
Phosphatase
|
Cancer
|
|
Anticancer agent 144 (compound 444) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 144 can be used in cancer research .
|
-
- HY-111477
-
|
(E/Z)-RPL-554
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
(E/Z)-Ensifentrine is a dual inhibitor of PDE3/4. (E/Z)-Ensifentrine reduces the inflammatory cells into the airways. (E/Z)-Ensifentrine has bronchodilatory and anti-inflammatory activities in vitro and in vivo model .
|
-
- HY-116120
-
-
- HY-B0196AR
-
|
Wy 45030 hydrochloride (Standard)
|
Serotonin Transporter
|
Neurological Disease
Cancer
|
|
Venlafaxine (hydrochloride) (Standard) is the analytical standard of Venlafaxine (hydrochloride). This product is intended for research and analytical applications. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
|
-
- HY-101549A
-
|
UNC2371 hydrochloride
|
FLT3
|
Cancer
|
|
MRX-2843 hydrochloride is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
|
-
- HY-15174
-
|
BEZ235 Tosylate; NVP-BEZ 235 Tosylate
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
|
-
- HY-10579
-
|
SC1
|
Ribosomal S6 Kinase (RSK)
ERK
|
Cancer
|
|
Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 μM, respectively.
|
-
- HY-152185
-
|
|
p38 MAPK
|
Cancer
|
|
BSJ-04-122 is a covalent MKK4/7 dual inhibitor. BSJ-04-122 inhibits MKK4 and MKK7 with IC50 values of 4 nM and 181 nM, respectively. BSJ-04-122 can be used for the research of cancer .
|
-
- HY-161145
-
|
|
EGFR
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting EGFR and tubulin. The IC50 for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis .
|
-
- HY-160024
-
|
|
Others
IAP
|
Cancer
|
|
XIAP BIR2/BIR2-3 inhibitor-2 is a dual inhibitor of BIR2 and BIR2-3 with IC 50s less than 1 nM. XIAP BIR2/BIR2-3 inhibitor-2 can used in study cancers .
|
-
- HY-160030
-
|
|
IAP
|
Cancer
|
|
XIAP BIR2/BIR2-3 inhibitor-3 is a dual inhibitor of BIR2 and BIR2-3 with IC50s less than 1 nM. XIAP BIR2/BIR2-3 inhibitor-3 can used in study cancers .
|
-
- HY-160656
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT/NA Reuptake inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 of 660 nM and 70 nM respectively. . 5-HT/NA Reuptake inhibitor-1 has good in vitro human metabolic stability, hERG selectivity and passive membrane permeability .
|
-
- HY-145428
-
|
|
Notch
γ-secretase
|
Cancer
|
|
BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression .
|
-
- HY-12035
-
AMG-208
1 Publications Verification
|
c-Met/HGFR
Cytochrome P450
|
Cancer
|
|
AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity .
|
-
- HY-100544
-
FLLL32
5 Publications Verification
|
STAT
JAK
Apoptosis
|
Cancer
|
|
FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells .
|
-
- HY-16726
-
|
CG100649
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-128343
-
|
|
Histone Demethylase
|
Cancer
|
|
KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively .
|
-
- HY-117421A
-
|
|
Histone Methyltransferase
DNA Methyltransferase
|
Cancer
|
|
CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
|
-
- HY-115502A
-
|
(E)-BCI hydrochloride
|
Phosphatase
|
Inflammation/Immunology
|
|
BCI ((E)-BCI) hydrochloride is a DUSP6 (dual specificity phosphatase 6) inhibitor. BCI hydrochloride shows anti-inflammatory activity and decreases reactive oxygen species (ROS) production. BCI hydrochloride can be used in inflammatory disease research .
|
-
- HY-115502
-
|
(E)-BCI
|
Phosphatase
|
Inflammation/Immunology
|
|
BCI ((E)-BCI) is a DUSP6 (dual specificity phosphatase 6) inhibitor. BCI shows anti-inflammatory activity and decreases reactive oxygen species (ROS) production. BCI can be used in inflammatory disease research .
|
-
- HY-114412A
-
-
- HY-W010144
-
|
|
COX
Lipoxygenase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat . Phenidone is used as a photographic developer .
|
-
- HY-17485
-
|
EB-382
|
Phospholipase
COX
|
Inflammation/Immunology
|
|
Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory agent (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2 .
|
-
- HY-117421
-
|
|
Histone Methyltransferase
DNA Methyltransferase
|
Cancer
|
|
CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
|
-
- HY-116273
-
|
|
Phospholipase
|
Cancer
|
|
ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells .
|
-
- HY-145723B
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 hemifumarate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
|
-
- HY-145723C
-
|
|
FLT3
FGFR
|
Inflammation/Immunology
Cancer
|
|
MAX-40279 hemiadipate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
|
-
- HY-147772
-
-
- HY-143495
-
|
|
RSV
Influenza Virus
|
Infection
|
|
RSV-IN-3 (Compound 1) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza virus A (IAV). RSV-IN-3 shows anti-RSV activity (EC50 = 32.70 μM) .
|
-
- HY-143496
-
|
|
RSV
Influenza Virus
|
Infection
|
|
RSV-IN-4 (Compound 2) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza virus A (IAV). RSV-IN-4 shows anti-RSV activity (EC50 = 11.76 μM) .
|
-
- HY-149256
-
|
|
SARS-CoV
|
Infection
|
|
PLpro/RBD-IN-1 (compound 5) is a dual SARS-CoV-2 PLpro and spike protein RBD inhibitor with IC50s of 7.197 μM and 8.673 μM, respectively .
|
-
- HY-106823
-
-
- HY-161355
-
|
|
Amylases
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-9 (compound 5h) is a dual inhibitor for both α-amylase (IC50 = 16.4 μM) and α-glucosidase (IC50 = 31.6 μM) enzymes .
|
-
- HY-162603
-
|
|
HDAC
DNA/RNA Synthesis
|
Cancer
|
|
HDAC-IN-74 (PA) is a dual HDAC/Rribonucleotide reductase(RR) inhibitor, with IC50 values of 10.80 μM and 9.34 μM for HDAC and HDAC, respectively. HDAC-IN-74 can be used in anticancer research .
|
-
- HY-103443A
-
|
|
EGFR
|
Cancer
|
|
HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation .
|
-
- HY-131479A
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
Threo-dihydrobupropion is a major metabolite of Bupropion, formed via oxidation and reduction exhibit pharmacological activity. Bupropion, a dual dopamine-norepinephrine uptake inhibitor and a nicotine receptor antagonist, is widely used in the management of depression and as a smoking cessation aid .
|
-
- HY-15391
-
|
E-3810
|
VEGFR
FGFR
|
Cancer
|
|
Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively .
|
-
- HY-112708
-
|
PF-06700841
|
JAK
|
Inflammation/Immunology
|
|
Brepocitinib (PF-06700841) is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively .
|
-
- HY-118916
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively .
|
-
- HY-15391A
-
|
|
VEGFR
FGFR
|
Cancer
|
|
Lucitanib (E-3810) dihydrochloride is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively .
|
-
- HY-12036
-
|
|
PI3K
mTOR
Apoptosis
|
Cancer
|
|
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
|
-
- HY-12947
-
|
|
MAP3K
|
Neurological Disease
|
|
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases .
|
-
- HY-P0025
-
-
- HY-101549
-
|
UNC2371
|
FLT3
|
Cancer
|
|
MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
|
-
- HY-114412
-
-
- HY-100865
-
|
DBPR114
|
FLT3
|
Cancer
|
|
BPR1K871 is a potent and selective dual FLT3/AURKA inhibitor with IC50s of 19 nM and 22 nM for FLT3 and AURKA, respectively, acts as a preclinical development candidate for anti-cancer therapy .
|
-
- HY-131063
-
|
|
CDK
|
Cancer
|
|
CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively .
|
-
- HY-12310
-
|
|
DNA Methyltransferase
HDAC
|
Others
|
|
RSC133 exhibits dual activity by inhibiting histone deacetylase and DNA methyltransferase. RSC133 effectively facilitates reprogramming of human somatic cells to pluripotent stem cells and supports the maintenance of an undifferentiated state of human pluripotent stem cells .
|
-
- HY-146663
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-3 (BMC-1) is a dual AChE and BChE inhibitor with IC50 values of 6.08 μM and 0.383 μM against electric eel AChE (elAChE) and equine serum BChE (eqBChE), respectively .
|
-
- HY-146663A
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-3 (BMC-1) hydrochloride is a dual AChE and BChE inhibitor with IC50 values of 6.08 μM and 0.383 μM against electric eel AChE (elAChE) and equine serum BChE (eqBChE), respectively .
|
-
- HY-149659
-
|
|
Others
|
Cancer
|
|
ARUK2007145 is potent, cell-active dual inhibitor of the PI5P4Kα and PI5P4Kγ isoforms (pIC50: 7.3 and 8.1, respectively) .
|
-
- HY-157290
-
|
|
Epigenetic Reader Domain
Src
|
Cancer
|
|
HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .
|
-
- HY-N0493R
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity . Pectolinarigenin has potent inhibitory activities on melanogenesis .
|
-
- HY-126763
-
|
|
Others
|
Others
|
|
ATI22-107 is a dual-pharmacophore compound designed to simultaneously inhibit cardiac phosphodiesterase (PDE-III) and L-type calcium channels (LTCC), with activity that has specific effects on calcium cycling and contractility in cat ventricular myocytes and trabeculae.
|
-
- HY-13018B
-
|
|
IKK
ULK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells .
|
-
- HY-13018
-
|
|
IKK
ULK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells .
|
-
- HY-13018A
-
|
|
IKK
ULK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively . MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells .
|
-
- HY-118916A
-
|
|
Others
|
Cancer
|
|
FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively .
|
-
- HY-146999
-
|
|
Histone Methyltransferase
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer .
|
-
- HY-149310
-
|
|
Ser/Thr Protease
|
Metabolic Disease
|
|
Dim16 is a dual PCSK9/HMG-CoAR inhibitor, with an IC50 value of 19 nM for PCSK9. Dim16 inhibits PCSK9-LDLR binding with an IC50 value of 0.8 nM. Dim16 increases LDL uptake in HepG2 cells .
|
-
- HY-14882
-
|
TAK-652; TBR-652
|
CCR
HIV
|
Infection
Endocrinology
|
|
Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity .
|
-
- HY-U00457
-
|
|
IKK
|
Cancer
|
|
TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC50s of <100 nM.
|
-
- HY-111427
-
|
|
CDK
|
Cancer
|
|
CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
|
-
- HY-112908
-
|
|
HDAC
Proteasome
|
Cancer
|
|
RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
|
-
- HY-128758
-
|
|
DYRK
|
Cancer
|
|
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity .
|
-
- HY-129701
-
|
|
Bcl-2 Family
|
Cancer
|
|
MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively .
|
-
- HY-128758A
-
|
|
DYRK
|
Cancer
|
|
DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity .
|
-
- HY-123846
-
|
|
Phosphatase
|
Cardiovascular Disease
|
|
MLS-0437605 is a selective dual-specificity phosphatase 3 (DUSP3) inhibitor with an IC50 of 3.7 μM. MLS-0437605 is more selective for DUSP3 than DUSP22 and other protein tyrosine phosphatases (PTPs) .
|
-
- HY-147872
-
|
|
VEGFR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-22 (Compound 25) is a dual VEGFR-2 and β-tubulin polymerization inhibitor with an IC50 of 19.82 nM against VEGFR-2. VEGFR-2-IN-22 induces apoptosis .
|
-
- HY-149421
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD7-IN-3 (compound 1-78) is a dual inhibitor of bromodomain-containing proteins BRD7/BRD9 with IC50s of 1.6 μM and 2.7 μM respectively .
|
-
- HY-156423
-
|
|
Microtubule/Tubulin
JAK
|
Cancer
|
|
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells .
|
-
- HY-163136
-
|
|
Autophagy
REV-ERB
|
Cancer
|
|
Autophagy/REV-ERB-IN-1 (compound 24) is a dual inhibitor of autophagy and REV-ERB. Autophagy/REV-ERB-IN-1 has anti-tumor activity with a CC50 value of 2.3 μM on BTB-474 cells.
|
-
- HY-158075
-
|
|
HDAC
DNA Methyltransferase
|
Cancer
|
|
DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC50 values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.
|
-
- HY-169048
-
|
|
CDK
|
Cancer
|
|
CDK2/4-IN-2 (compound 56) is a CDK2 and CDK4 dual inhibitor with IC50s less than 100 nM. CDK2/4-IN-2 can be used in the study of cancer .
|
-
- HY-121693
-
|
MDL101114ZA free base
|
VDAC
RAD51
|
Cancer
|
|
DIDS is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research .
|
-
- HY-156445
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-14 (compound Y-2) is a potent PI3K and mTOR dual inhibitor with IC50s of 171.4 nM and 10.1 nM, respectively. PI3K/mTOR Inhibitor-14 has antitumor activities .
|
-
- HY-160022
-
|
|
IAP
|
Cancer
|
|
XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) is a dual inhibitor of BIR2 and BIR2-3 with IC50s of 1.9 and 0.8 nM, respectively. XIAP BIR2/BIR2-3 inhibitor-1 can used in study cancers .
|
-
- HY-N1996
-
|
|
COX
Lipoxygenase
SARS-CoV
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis. Chebulagic acid is a M2 serine to asparagine 31 mutation (S31N) inhibitor and influenza antiviral. Chebulagic acid also against SARS-CoV-2 viral replication with an EC50 of 9.76 μM.
|
-
- HY-112708A
-
|
PF-06700841 P-Tosylate
|
JAK
|
Inflammation/Immunology
|
|
Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively .
|
-
- HY-126390
-
|
NSC 150117
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway .
|
-
- HY-161141
-
|
|
c-Met/HGFR
|
Cancer
|
|
EGFR/ C-Met-in-2 (Compound H-22) is a dual inhibitor of EGFR/c-Met. EGFR/c-Met-IN-2 inhibits cell proliferation by arresting G2/M phase. EGFR/c-Met-IN-2 has antitumor activity .
|
-
- HY-162143
-
|
|
SphK
Akt
mTOR
|
Cancer
|
|
SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells .
|
-
- HY-160686
-
|
|
Others
|
Others
|
|
GSK248233A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 1.03 μM and 2 nM, respectively. GSK248233A also shows activity against the AGC family. GSK248233A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays .
|
-
- HY-10594
-
|
TAK-442
|
Factor Xa
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Letaxaban (TAK-442) is an orally active and selective direct FXa inhibitor. Letaxaban is a drug with dual anticoagulant and anti-inflammatory activity that works by directly inhibiting FXa and by intervening in the PAR1 signaling pathway. Letaxaban can be used in the study of thrombotic diseases, cardiovascular diseases and inflammation-related diseases .
|
-
- HY-16782
-
|
ARRY-614
|
Tie
p38 MAPK
Autophagy
|
Cancer
|
|
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
|
-
- HY-114356
-
|
|
c-Met/HGFR
|
Cancer
|
|
BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma .
|
-
- HY-128677
-
|
|
Casein Kinase
|
Neurological Disease
|
|
NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms .
|
-
- HY-124036
-
|
|
PI3K
mTOR
|
Cancer
|
|
DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity .
|
-
- HY-120758
-
|
|
Pim
FLT3
Apoptosis
|
Cancer
|
SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively .
|
-
- HY-141701
-
|
|
mTOR
HDAC
|
Cancer
|
|
mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent .
|
-
- HY-144809
-
|
|
Carboxylesterase
|
Metabolic Disease
|
|
Pancreatic lipase/Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) and human carboxylesterase 1A (hCES1A) with IC50 values of 2.13 µM and 0.055 µM against PL and hCES1A .
|
-
- HY-146664
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-4 (BMC-3) is a dual AChE and BChE inhibitor with IC50 values of 792 nM and 2.2 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-4 can cross the BBB .
|
-
- HY-146665
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-5 (BMC-16) is a dual AChE and BChE inhibitor with IC50 values of 266 nM and 10.6 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-5 can cross the BBB .
|
-
- HY-157391
-
-
- HY-168061
-
|
|
Others
|
Infection
|
|
HldA/E-IN-1 (compound 8) is a dual inhibitor of HldA/E, with IC50 values of 17.2 μM and 67.8 μM for HldA/E, respectively. HldA/E-IN-1 can be used in the study of anti-bacterial infection .
|
-
- HY-128582
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM, respectively .
|
-
- HY-149925
-
|
|
Bacterial
DNA/RNA Synthesis
Topoisomerase
|
Infection
|
|
Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor .
|
-
- HY-159129
-
|
|
Cathepsin
Others
|
Cancer
|
|
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsin B, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
|
-
- HY-D0086
-
|
MDL101114ZA
|
VDAC
RAD51
|
Cancer
|
|
DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research .
|
-
- HY-153120A
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-153120
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-152200
-
|
|
HIV Protease
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS) .
|
-
- HY-104065BR
-
|
|
EGFR
|
Cancer
|
|
Pyrotinib dimaleate (Standard) is the analytical standard of Pyrotinib dimaleate. This product is intended for research and analytical applications. Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
|
-
- HY-B0494
-
|
Bufexamic acid
|
HDAC
Aminopeptidase
|
Inflammation/Immunology
Cancer
|
|
Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug .
|
-
- HY-129179
-
|
APG-2575; Bcl-2/Bcl-xl inhibitor 1
|
Bcl-2 Family
|
Cancer
|
|
Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively .
|
-
- HY-128355
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO/TDO-IN-1 (compound 25) is a highly potent and orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50s of 9.7 and 47 nM, respectively .
|
-
- HY-114303
-
|
|
Phosphodiesterase (PDE)
HDAC
|
Neurological Disease
|
|
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease .
|
-
- HY-129681
-
|
|
Bcl-2 Family
|
Cancer
|
|
MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 4.45 and 3.18 μM, respectively .
|
-
- HY-133117
-
|
|
IKK
|
Cancer
|
|
BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy .
|
-
- HY-N2947
-
|
|
P-glycoprotein
|
Infection
Inflammation/Immunology
|
|
Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress .
|
-
- HY-P99166
-
|
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
Cancer
|
|
Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
|
-
- HY-155708
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-13 (compound 5j) is a potent dual inhibitor of AChE and BChE with IC50s of 20.89 and 17.37 μM, respectively. AChE/BChE-IN-13 can be used in Alzheimer’s disease (AD) research .
|
-
- HY-161019
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK1/TYK2-IN-4 is a dual inhibitor of JAK and TYK2, with IC50s of 39 nM and 21 nM, respectively. JAK1/TYK2-IN-4 has oral bioavailability .
|
-
- HY-161515
-
|
|
NAMPT
Epigenetic Reader Domain
|
Cancer
|
|
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
|
-
- HY-117370
-
|
AZ1
|
Deubiquitinase
|
Cancer
|
|
USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model .
|
-
- HY-18204A
-
|
LCZ696
|
Angiotensin Receptor
Neprilysin
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure . Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis .
|
-
- HY-146333
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner .
|
-
- HY-153254
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
BMS905 is an orally active TLR7 and TLR8 dual inhibitor (IC50s: 0.7 and 3.2 nM respectively). BMS905 inhibits TLR7 or TLR8 induced IL-6 production in human/mouse whole blood. BMS905 can be used for research of lupus .
|
-
- HY-112293
-
|
|
EGFR
|
Cancer
|
|
GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research .
|
-
- HY-155768
-
|
|
COX
|
Cancer
|
|
COX-1/2-IN-5 (compound 2a) is a dual inhibitor of COX1/2 (IC50=2.650 μM, 0.958 μM), with anticancer activity. COX-1/2-IN-5 inhibits liver cancer HepG2 with an IC50 of 60.75 μM .
|
-
- HY-163062
-
|
|
Microtubule/Tubulin
Apoptosis
Complement System
|
Cancer
|
|
Tubulin/NRP1-IN-1 (compound TN-2) is a dual inhibitor of Tubulin and NRP1 with IC50s of 0.71 and 0.85 μM, respectively. Tubulin/NRP1-IN-1 significantly inhibits the viability of prostate tumor cell lines and induces apoptosis .
|
-
- HY-162472
-
|
|
ATM/ATR
DNA-PK
|
Cancer
|
|
XRD-0394 is a potent and specific dual inhibitor of ATM and DNA-PKcs with oral activity. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. In addition, XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
|
-
- HY-168265
-
|
|
DYRK
|
Neurological Disease
Cancer
|
|
Dyrk1A-IN-11 (compound 166) is a potent dual-specificity tyrosine phosphorylation- regulated 1A (DYRK1A) inhibitor with an EC50 value of 0.0021 µM. Dyrk1A-IN-11 inhibits the Phospho-Tau (Thr212) with an EC50 value of 0.0361 µM .
|
-
- HY-112416
-
AZD4320
1 Publications Verification
|
Bcl-2 Family
|
Cancer
|
|
AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.
|
-
- HY-19383
-
|
PTP 112
|
Phosphatase
IKK
PPAR
|
Metabolic Disease
|
|
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
|
-
- HY-136256
-
|
DCC-3014
|
c-Fms
c-Kit
|
Cancer
|
|
Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively .
|
-
- HY-136198
-
|
|
Syk
PI3K
|
Cancer
|
|
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression .
|
-
- HY-130794
-
-
- HY-114653
-
|
|
Casein Kinase
SRPK
|
Cancer
|
|
SRPIN803 is a potent CK2 and SRPK1 dual inhibitor, with IC50s of 203 nM and 2.4 μM, respectively. SRPIN803 exhibits antiangiogenic activity. SRPIN803 can be used for the research of age-related macular degeneration .
|
-
- HY-161136
-
|
|
EGFR
STAT
|
Cancer
|
|
EGFR/STAT3-IN-1 (Compound 5k) is a dual inhibitor of EGFR/STAT3 with IC50 values for EGFR and STAT3 are 41 and 3.34 nM, respectively. EGFR/STAT3-IN-1 has antitumor activity .
|
-
- HY-146504
-
|
|
Topoisomerase
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research .
|
-
- HY-13737
-
R1530
1 Publications Verification
|
VEGFR
FGFR
Apoptosis
|
Cancer
|
|
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence .
|
-
- HY-147867
-
|
|
MMP
|
Cancer
|
|
MMP-2/9-IN-1 (Compound 4a) is a potent dual MMP-2 and MMP-9 inhibitor with IC50 values of 56 nM and 38 nM, respectively. MMP-2/9-IN-1 inhibits tumor growth, strongly induces cancer cell apoptosis, inhibits cell migration, and suppresses cell cycle progression leading to DNA fragmentation .
|
-
- HY-15841
-
|
|
Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
|
|
CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397) .
|
-
- HY-130626
-
|
|
RSV
Influenza Virus
|
Infection
|
|
RSV/IAV-IN-1 (compound 14e) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-1 has lesser cytotoxicity than the clinical agent, Ribavirin. RSV/IAV-IN-1 has the potential for the research of RSV and/or IAV infections .
|
-
- HY-130627
-
|
|
RSV
Influenza Virus
|
Infection
|
|
RSV/IAV-IN-2 (compound 14c) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-2 has lesser cytotoxicity than the clinical agent, Ribavirin. RSV/IAV-IN-2 has the potential for the research of RSV and/or IAV infections .
|
-
- HY-145833A
-
|
|
Epoxide Hydrolase
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively .
|
-
- HY-152210
-
|
|
Cathepsin
|
Cancer
|
|
ASPER-29 is Asperphenamate HY-129578 analog. ASPER-29 also is a dual cathepsin L and S inhibitor with IC50 value of 6.03 μM and 5.02 μM, respectively. ASPER-29 can be used for the research of the migration and invasion of cancer .
|
-
- HY-149348
-
|
|
Topoisomerase
PARP
Apoptosis
|
Cancer
|
|
DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance .
|
-
- HY-155773
-
|
|
FAAH
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
VU534 is a NAPE-PLD activator, with an EC50 of 0.30 μM. VU534 is dual inhibitors of FAAH and sEH (IC50 of 1.2 μM). VU534 increases efferocytosis in a NAPE-PLD dependent manner. VU534 has the potential for cardiometabolic diseases study [1] .
|
-
- HY-163187
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
COX-2/LOX-IN-1 (compound 5) is a dual cyclooxygenase-2/lipoxygenase (COX-2/LOX) inhibitor with IC50s of 30 μM and 0.55 μM, for LOX and COX-2, respectively. .
|
-
- HY-162228
-
|
|
COX
Phospholipase
|
Inflammation/Immunology
|
|
VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway .
|
-
- HY-168648
-
|
|
Bacterial
Fungal
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DNA Gyrase/DHFR-IN-1 is a dual inhibitor of bacterial DNA gyrase and DHFR, with IC50s of 182 μM and 3.90 μM for E. coli DNA gyrase and DHFR respectively. DNA Gyrase/DHFR-IN-1 has bactericidal and antifungal activity .
|
-
- HY-W018555
-
|
|
Endogenous Metabolite
Bacterial
|
Infection
Neurological Disease
|
|
D-Cysteine is the D-isomer of cysteine and a powerful inhibitor of Escherichia coli growth. D-cysteine is mediated by D-amino acid oxidase to produce H2S and is a neuroprotectant against cerebellar ataxias. D-Cysteine could inhibit the growth and cariogenic virulence of dual-species biofilms formed by S. mutans and S. sanguinis .
|
-
- HY-124113
-
|
4′‐BR
|
Sirtuin
Apoptosis
|
Cancer
|
|
4'-Bromo-resveratrol is a potent and dual inhibitor Sirtuin-1 and Sirtuin-3. 4'-Bromo-resveratrol inhibits melanoma cell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanoma cells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling .
|
-
- HY-100950
-
|
|
GSK-3
CDK
|
Inflammation/Immunology
Cancer
|
ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities .
|
-
- HY-155571
-
|
|
MDM-2/p53
IAP
|
Cancer
|
|
MDM2/XIAP-IN-3 (compound 3e) is a dual MDM2/XIAP inhibitor. MDM2/XIAP-IN-3 reduces MDM2 and XIAP protein levels and increases p53 expression, thereby inhibiting cancer cell growth and causing cell death .
|
-
- HY-155227B
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK/EGFR-IN-3 is a dual inhibitor of ALK and EGFR. ALK/EGFR-IN-3 inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.1360, 0.0332, and 0.0339 μM, respectively .
|
-
- HY-157212
-
|
|
Apoptosis
PARP
Proteasome
|
Cancer
|
|
PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis .
|
-
- HY-163340
-
|
|
Glucocorticoid Receptor
Androgen Receptor
|
Cancer
|
|
GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .
|
-
- HY-15838
-
ID-8
4 Publications Verification
|
DYRK
|
Cancer
|
|
ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs .
|
-
- HY-108606
-
PI-828
1 Publications Verification
|
PI3K
Casein Kinase
|
Cancer
|
|
PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively .
|
-
- HY-114205
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-137563
-
|
|
Potassium Channel
|
Neurological Disease
|
A2793 is an efficient dual TWIK-related acid-sensitive K + channel (TASK)-1/TRESK inhibitor, with an IC50 of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1 .
|
-
- HY-114205A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-129411
-
|
ACT-519276; OGT2378
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions .
|
-
- HY-15434A
-
|
|
MAP3K
MAP4K
|
Cancer
|
|
NG25 trihydrochloride is a dual TAK1 and MAP4K2 inhibitor (IC50: 149 nM and 21.7 nM respectively). NG25 sensitizes the breast cancer cells to Doxorubicin (HY-15142A), and enhances apoptosis. NG25 trihydrochloride can be used for research of various cancers .
|
-
- HY-123544
-
|
|
MDM-2/p53
|
Cancer
|
|
RDR03871 (compound 2) is a potent dual MDM2/MDM4 inhibitor with IC50 values of 35.4 nM and 10.4 nM for MDM2-p53 and MDM4-p53, respectively .
|
-
- HY-162044
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-1/2-IN-6 (compound 4 h) is a potent dual inhibitor of COX-1 and COX-2 with IC50s of 68 and 91 nM, respectively. COX-1/2-IN-6 can used in study inflammation diseases .
|
-
- HY-161244
-
|
|
SARS-CoV
Cathepsin
Virus Protease
|
Infection
|
|
FGA145 is a dual, selective inhibitor for M pro and human Cathepsin L, with Kis of 3.71 μM, 9.82 μM and 53 nM, for Mal-M pro, pET21-M pro and Cathepsin L, respectively. FGA145 reveals a multitarget effects in the antiviral activity .
|
-
- HY-161311
-
-
- HY-161351
-
|
|
Akt
STAT
Apoptosis
|
Cancer
|
|
STAT3/AKT-IN-1 is a dual inhibitor for the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signalling pathway, exhibits antitumor activity against gastric cancer and induces cell apoptosis in SGC-7901 cells .
|
-
- HY-160682
-
|
|
EGFR
|
Others
|
|
EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
|
-
- HY-161861
-
|
|
VEGFR
Akt
|
Cancer
|
|
VEGFR-2/AKT-IN-1 (compound 17) is a dual inhibitor of VEGFR-2 and AKT, with the IC50s of 0.164 μM and 0.452 μM, respectively. VEGFR-2/AKT-IN-1 has antitumor activity .
|
-
- HY-129808
-
|
|
Others
|
Cardiovascular Disease
Cancer
|
|
VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases .
|
-
- HY-168563
-
|
|
Cholinesterase (ChE)
FAAH
|
Neurological Disease
|
|
BuChE-IN-15 (compound D12) is a selective BuChE/FAAH dual inhibitor with and show IC50 values of 81 and 400 nM for hBuChE and hFFAH, respectively. BuChE-IN-15 possesses good BBB penetration, and shows neuroprotection.BuChE-IN-15 can be used for study of Alzheimer .
|
-
- HY-119316A
-
|
|
HDAC
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
(cis)-CM-414, the cis-isomer of CM-414, is a dual inhibitor of PDE5, HDAC1, HDAC2, HDAC3, and HDAC6 with pIC50 values of 7.47, 6.65, 6.14, 6.55, and 6.84, repectively .
|
-
- HY-13203
-
|
TAE226
|
FAK
Pyk2
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively .
|
-
- HY-77251
-
|
|
MAP4K
MAP3K
|
Cancer
|
|
TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
|
-
- HY-112816
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
|
-
- HY-144648
-
|
|
SARS-CoV
|
Infection
|
|
Mpro/PLpro-IN-1 (Compound 29) is a potent inhibitor of M pro/PL pro. Mpro/PLpro-IN-1 is a dual acting SARS-CoV-2 proteases inhibitor featuring micromolar inhibitory potency versus M pro (IC50 = 1.72 μM) and submicromolar potency versus PL pro (IC50 = 0.67 μM) .
|
-
- HY-129119
-
|
|
Akt
Caspase
|
Cancer
|
|
Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells .
|
-
- HY-16726R
-
|
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (Standard) is the analytical standard of Polmacoxib. This product is intended for research and analytical applications. Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-168171
-
|
|
ERK
Caspase
Apoptosis
|
Cancer
|
|
ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2, lending to DSB accumulation and ERK1/2 expression degradation. ERK1/2 inhibitor 11 lowers the levels of BCL-2, and induces DNA damage by inhibiting PARP and ERK1/2. ERK1/2 inhibitor 11 activates caspase 3 to inducing apoptosis.
|
-
- HY-147908
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR .
|
-
- HY-153968
-
|
|
Xanthine Oxidase
URAT1
|
Metabolic Disease
|
|
URAT1&XO inhibitor 1 (compound 29) is a dual inhibitor of both URAT1 (IC50=~10 μM) and Xanthine Oxidase (IC50=1.01 μM). URAT1&XO inhibitor 1 results hypouricemic effect in potassium oxonate-induced hyperuricemia rat model. URAT1&XO inhibitor 1 is used for hyperuricemia research .
|
-
- HY-N0232
-
|
|
COX
Lipoxygenase
Notch
Reactive Oxygen Species
Bacterial
|
Cancer
|
|
Psoralidin is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties . Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation .
|
-
- HY-121736
-
|
AGI-026
|
Isocitrate Dehydrogenase (IDH)
|
Neurological Disease
|
|
AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
|
-
- HY-145831
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
Inflammation/Immunology
|
|
sEH/AChE-IN-1 (Compound 12a) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-1 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-1 has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-145833
-
|
|
Epoxide Hydrolase
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively .
|
-
- HY-151561
-
|
|
Parasite
|
Infection
|
|
WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile .
|
-
- HY-149874
-
|
|
DGK
|
Inflammation/Immunology
Cancer
|
|
BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research .
|
-
- HY-161348
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
AT-0174 is an orally active dual inhibitor of IDO1/TDO2 (tryptophan 2,3-dioxygenase-2) with IC50 values of 0.17 and 0.25 μM, respectively. AT-0174 has antitumor activity .
|
-
- HY-W024485
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-86 (Compound 2734589) is a dual inhibitor of the methyltransferases nsp14 and nsp16 of SARS-CoV-2. SARS-CoV-2-IN-86 exhibits low toxicity with a LD50 of 700 mg/kg according to toxicity analysis predict .
|
-
- HY-106056
-
|
D 16726
|
Others
|
Cancer
|
|
Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
|
-
- HY-136809
-
|
|
Others
|
Cancer
|
|
PRMT6-IN-2 (compound 2) is a dual inhibitor of protein arginine methyltransferase PRMT6 and CARM1 with an IC50 of 30 nM. PRMT6 is abnormally expressed in many cancer cells, and PRMT6-IN-2-based derivatives have potential anticancer activity.
|
-
- HY-164553
-
|
|
Apoptosis
CDK
|
Cancer
|
|
ZSQ836 is an orally active dual covalent inhibitor of CDK12/CDK13, with an EC50 value of 32 nM against CDK12. ZSQ836 can induce apoptosis and exhibit anticancer activity in vivo. ZSQ836 can be used in the study of ovarian cancer .
|
-
- HY-114766
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting .
|
-
- HY-15486
-
|
|
Phosphatase
HSV
Autophagy
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation . Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis . Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5 .
|
-
- HY-117822
-
|
|
GSK-3
|
Neurological Disease
|
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
|
-
- HY-160687
-
|
|
Others
|
Others
|
|
GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays .
|
-
- HY-162382
-
|
|
PI3K
Akt
mTOR
|
Cancer
|
|
KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response .
|
-
- HY-19322B
-
|
LGH447 dihydrochloride
|
Pim
Apoptosis
|
Cancer
|
|
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis .
|
-
- HY-19322
-
PIM447
5 Publications Verification
LGH447
|
Pim
Apoptosis
|
Cancer
|
|
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis .
|
-
- HY-135401
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
|
|
VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production .
|
-
- HY-142847
-
-
- HY-145832
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
Inflammation/Immunology
|
|
sEH/AChE-IN-2 (Compound 12b) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-2 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-2 has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-146342
-
|
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-3 (Compound 10) is an irreversible fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) dual inhibitor with IC50 values of 179 and 759 nM against FAAH and MAGL, respectively. FAAH/MAGL-IN-3 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability .
|
-
- HY-151978
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
|
Cancer
|
|
ZC0109 is a dual inhibitor of IDO1 and thioredoxin reductase 1 (TrxR1) with IC50s of 50 nM and 3.0 μM, respectively. ZC0109 induces ROS accumulation and cell cycle arrest at G1/S phase, thus leads to cancer cells apoptosis .
|
-
- HY-P99721
-
|
ABT-981
|
Interleukin Related
|
Inflammation/Immunology
|
|
Lutikizumab (ABT-981) is an anti-IL-1α and IL-1β dual variable domain immunoglobulin. Lutikizumab binds and inhibits IL-1α and IL-1β. Lutikizumab can be used for the research of osteoarthritis .
|
-
- HY-146806
-
|
|
MDM-2/p53
|
Cancer
|
|
YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition .
|
-
- HY-149637
-
|
|
Sirtuin
HSP
|
Cancer
|
|
HSP70/SIRT2-IN-1 (Compounds 2a) is a dual inhibitor for SIRT2 and HSP70, with IC50 of 17.3±2.0 μM for SIRT2. HSP70/SIRT2-IN-1 has antitumor activity .
|
-
- HY-149638
-
|
|
Sirtuin
HSP
|
Cancer
|
|
HSP70/SIRT2-IN-2 (Compounds 1a) is a dual inhibitor for SIRT2 and HSP70, with IC50 of 45.1±5.0 μM for SIRT2. HSP70/SIRT2-IN-2 has antitumor activity .
|
-
- HY-157402
-
|
|
Topoisomerase
EGFR
|
Cancer
|
|
Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer .
|
-
- HY-162406
-
|
|
TAM Receptor
|
Cancer
|
|
UNC8969 (compound 43) is a MERTK/AXL dual inhibitor with IC50s of 1.1±0.8 nM for MERTK and 5.3 ± 2.7 nM for AXL. UNC8969 also exerts a T1/2 of 7.3 h with 5 mg/kg i.v. in mice .
|
-
- HY-163722
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
EGFR/DHFR-IN-1 (Compound 10e) is a dual inhibitor of EGFR and DHFR with IC50s of 0.151 and 0.541 µM, respectively. EGFR/DHFR-IN-1 arrests the cell cycle at both G0-G1 and S phases .
|
-
- HY-N0737AR
-
|
|
DYRK
5-HT Receptor
|
Neurological Disease
Cancer
|
|
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
|
-
- HY-126486
-
|
A293
|
Potassium Channel
|
Cardiovascular Disease
|
|
AVE1231 (A293) is a dual-pore potassium channel TASK-1 inhibitor. AVE1231 blocks carbamoylcholine chloride (HY-B1208)-activated IKACh (IC50=8.4 μM). AVE1231 can be used in the study of arrhythmias and atrial fibrillation .
|
-
- HY-10181
-
Dasatinib
Maximum Cited Publications
99 Publications Verification
BMS-354825
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-10181A
-
|
BMS-354825 hydrochloride
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
|
-
- HY-18756
-
|
|
SHP2
Phosphatase
Apoptosis
|
Others
|
|
NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively . NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26) .
|
-
- HY-18756A
-
|
|
SHP2
Phosphatase
Apoptosis
|
Cancer
|
|
NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively . NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26) .
|
-
- HY-137742
-
|
|
ULK
Autophagy
|
Cancer
|
|
SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-10181B
-
|
BMS-354825 monohydrate
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
|
-
- HY-147308
-
|
|
N-myristoyltransferase
|
Cancer
|
|
PCLX-001 is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively. PCLX-001 can induce cell apoptosis, has anti-cancer activity, inhibits early B cell receptor (BCR) signaling, and can be used to study malignant lymphoma .
|
-
- HY-151368
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research .
|
-
- HY-161775
-
|
|
RET
Trk Receptor
|
Cancer
|
|
RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC50=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits cell viability of LC-2 and KM12, with GI50 of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cell cycle at G1 phase .
|
-
- HY-120882
-
|
UBX1967
|
Bcl-2 Family
|
Cancer
|
|
BM-1197 (UBX1967) is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo .
|
-
- HY-122627
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells .
|
-
- HY-N4115
-
|
Su 3118
|
Monocarboxylate Transporter
|
Cardiovascular Disease
Cancer
|
|
Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine .
|
-
- HY-107365
-
|
|
PI3K
mTOR
|
Cancer
|
|
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .
|
-
- HY-119708
-
|
RPL-554
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-112273
-
|
|
Aurora Kinase
|
Cancer
|
|
CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer .
|
-
- HY-112273A
-
|
|
Aurora Kinase
|
Cancer
|
|
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer .
|
-
- HY-103439
-
|
|
EGFR
|
Cancer
|
|
GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity .
|
-
- HY-157087
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/MAO-B-IN-4 (compound 4a) is a selective dual AChE and MAO-B inhibitor. AChE/MAO-B-IN-4 shows no significant inhibition activity against BChE and h-MAO-A. AChE/MAO-B-IN-4 can be used for the Alzheimer’s disease (AD) research .
|
-
- HY-163136A
-
|
|
Autophagy
REV-ERB
|
Cancer
|
|
Autophagy/REV-ERB-IN-1
hydrochloride (Compound 24) is a dual autophagy and REV-ERB inhibitor with
anticancer activity. Autophagy/REV-ERB-IN-1 (hydrochloride) has improved
potency in blocking autophagy, enhanced toxicity against cancer cells.
Autophagy/REV-ERB-IN-1 (hydrochloride) can be used for the research for
melanoma .
|
-
- HY-163282
-
|
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
|
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
|
-
- HY-17485R
-
|
|
Phospholipase
COX
|
Inflammation/Immunology
|
|
Alminoprofen (Standard) is the analytical standard of Alminoprofen. This product is intended for research and analytical applications. Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory agent (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2 .
|
-
- HY-114414
-
|
|
HDAC
mTOR
Apoptosis
|
Cancer
|
|
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
|
-
- HY-162601
-
|
|
Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer .
|
-
- HY-164455
-
|
|
Aurora Kinase
JAK
STAT
|
Inflammation/Immunology
|
|
AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
|
-
- HY-128142
-
|
|
PKD
PKC
|
Cardiovascular Disease
|
|
PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC50 value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure .
|
-
- HY-108586
-
|
|
Potassium Channel
|
Neurological Disease
|
|
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels .
|
-
- HY-105024
-
|
|
Lipoxygenase
COX
|
Inflammation/Immunology
|
|
FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC50 values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity .
|
-
- HY-15999A
-
|
PRT062070 hydrochloride; PRT2070 hydrochloride
|
Syk
JAK
|
Cancer
|
|
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies .
|
-
- HY-10681
-
|
PKI-587; PF-05212384
|
PI3K
mTOR
|
Cancer
|
|
Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively . Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
|
-
- HY-131971
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease .
|
-
- HY-139047
-
|
|
GLUT
|
Cancer
|
|
SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs .
|
-
- HY-142843
-
|
|
ROR
Dihydroorotate Dehydrogenase
|
Inflammation/Immunology
|
|
RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual RORγt/DHODH inhibitor, with IC50s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity .
|
-
- HY-143412
-
|
|
HDAC
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo .
|
-
- HY-146160
-
|
|
PARP
HDAC
|
Cancer
|
|
PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities .
|
-
- HY-150061
-
|
|
PI3K
mTOR
|
Cancer
|
|
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor . NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-152111
-
-
- HY-152204
-
|
|
Cathepsin
|
Cancer
|
|
Cathepsin L/S-IN-1 is a dual inhibitor of Cathepsin L and Cathepsin S with IC50s of 4.10 μM and 1.79 μM, respectively. Cathepsin L/S-IN-1 shows a significant antimetastatic and invasive effects on pancreatic cancer BxPC-3 and PANC-1 cells .
|
-
- HY-154972
-
|
|
Glucosidase
Amylases
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-3 (Compound 17) is an α-Amylase/α-Glucosidase dual inhibitor, with IC50s of 0.70 μM and 1.10 μM. α-Amylase/α-Glucosidase-IN-3 can be used for research of type-II diabetes mellitus .
|
-
- HY-153199
-
|
|
Others
|
Cancer
|
|
MDM2/XIAP-IN-1 (compound 14) is an orally active inhibitor of dual MDM2/XIAP. MDM2/XIAP-IN-1 has anti-cancer activity with an IC50 value of 0.3 μM, which can be used in cance rescrch .
|
-
- HY-155159
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
COX-2/15-LOX-IN-2 is a potent dual COX-2 and 15-LOX inhibitor with IC50 values of 0.065?μM and 1.86?μM, respectively. COX-2/15-LOX-IN-2 has potent antioxidant activity .
|
-
- HY-149557
-
|
|
Glucosidase
Amylases
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-5 (compound 4l) is a dual inhibitor of α-glucosidase (Glucosidase) and α-amylase (Amylases) with IC50s of 5.96 μM and 1.62 μM, respectively. α-Amylase/α-Glucosidase-IN-4 has potential antidiabetic activity .
|
-
- HY-155241
-
|
|
Glucosidase
Amylases
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-4 (compound 5) is a dual inhibitor of α-glucosidase (Glucosidase) and α-amylase (Amylases) with IC50s of 0.15 μM and 1.10 μM, respectively. α-Amylase/α-Glucosidase-IN-4 has potential antidiabetic activity .
|
-
- HY-156380
-
|
|
Amylases
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-6 (compound 5j) is a potent dual inhibitor of α-amylase and α-glucosidase, with IC50s of 17.0 and 40.1 µM, respectively. α-Amylase/α-Glucosidase-IN-6 exhibits anti-hyperglycemic activities .
|
-
- HY-157399
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual EGFR/HER2 inhibitor with IC50s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma .
|
-
- HY-157441
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
AChE/Aβ-IN-4 is a dual inhibitor of acetylcholinesterase (AChE) and β-amyloid (Aβ) aggregation, with the IC50 values of 1.72 ± 0.18 μM and 1.42 ± 0.3 μM, respectively. AChE/Aβ-IN-4 plays an impotant role in neurological disorders, such as Alzheimer’s disease .
|
-
- HY-157388
-
|
|
Histone Methyltransferase
HDAC
|
Cancer
|
|
CARM1/HDAC2-IN-1 (compound CH-1) is a dual inhibitor against CARM1 and HDAC2, with IC50 values of 3.71 nM and 4.07 nM, respectively. CARM1/HDAC2-IN-1 possesses antitumor activity .
|
-
- HY-161068
-
-
- HY-161245
-
|
|
Virus Protease
Cathepsin
|
Infection
|
|
FGA146 is a dual, selective inhibitor for M pro and human Cathepsin L, with Kis of 2.19 μM, 0.96 μM and 0.87 μM, for Mal-M pro, pET21-M pro and Cathepsin L, respectively. FGA146 reveals an antiviral activity against SARS-CoV-2 .
|
-
- HY-113807
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
ZLJ-6 is a dual COX and 5-LOX inhibitor with oral activity. The IC50 values for COX-1, COX-2 and 5-LOX were 0.73, 0.31 and 0.99 μM, respectively. ZLJ-6 has anti-inflammatory and analgesic activity .
|
-
- HY-163357
-
|
|
CDK
MDM-2/p53
|
Cancer
|
|
CDK2/MDM2-IN-1 (III-13) is a dual inhibitor of CDK2/MDM2 with an IC50 value of 2.60 nM for CDK2. CDK2/MDM2-IN-1 has antitumor activity .
|
-
- HY-158975
-
|
|
Casein Kinase
|
Cancer
|
|
VRK1/CK1-IN-1 (compound 36) is a dual inhibitor of vaccinia-related kinase 1 (VRK1) and casein kinase 1 (CK1), with the Ki of 37.9 nM for VRK1 and IC50s of 17 nM and 15 nM for δ and ε isoforms of CK1, respectively .
|
-
- HY-162673
-
|
|
Amylases
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-16 (compound 15) is a potent dual inhibitor of α-amylase and α-Glucosidase with IC50 values of 0.8 and 1.2 μM, respectively. α-Amylase/α-Glucosidase-IN-16 can be used in the study of diabetes mellitus (DM) .
|
-
- HY-159483
-
|
|
Topoisomerase
Autophagy
Glutathione Peroxidase
|
Cancer
|
|
SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH .
|
-
- HY-168514
-
|
|
EGFR
|
Cancer
|
|
SOS1/EGFR-IN-2 (Compound 4) is a SOS1 and EGFR dual inhibitor with IC50s of 8.3 and 14.6 nM, respectively. SOS1/EGFR-IN-2 exhibits significant antiproliferative effect on the cancer cells haboring various KRAS mutants .
|
-
- HY-106004
-
|
BIA 5-1058
|
Dopamine β-hydroxylase
P-glycoprotein
BCRP
|
Cardiovascular Disease
Cancer
|
|
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively . Zamicastat reduces high blood pressure .
|
-
- HY-18161
-
|
|
FLT3
Aurora Kinase
|
Cancer
|
|
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
|
-
- HY-117273
-
|
|
Raf
Autophagy
|
Cancer
|
|
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity .
|
-
- HY-131707
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
|
-
- HY-139744
-
-
- HY-145935
-
|
|
Insulin Receptor
STAT
|
Cancer
|
|
NT219 is a potent and dual inhibitor of insulin receptor substrates 1/2 (IRS1/2) and STAT3. IRS1/2 and STAT3 are major signaling junctions regulated by various oncogenes. NT219 affects IRS1/2 degradation and inhibits STAT3 phosphorylation. NT219 has the potential for the research of cancer diseases .
|
-
- HY-N1996R
-
|
|
COX
Lipoxygenase
SARS-CoV
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Chebulagic acid (Standard) is the analytical standard of Chebulagic acid. This product is intended for research and analytical applications. Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis. Chebulagic acid is a M2 serine to asparagine 31 mutation (S31N) inhibitor and influenza antiviral. Chebulagic acid also against SARS-CoV-2 viral replication with an EC50 of 9.76 μM.
|
-
- HY-137561A
-
|
PLN-74809 hydrochloride
|
Integrin
|
Inflammation/Immunology
|
|
Bexotegrast hydrochloride (PLN-74809 hydrochloride) is a small molecule dual selective inhibitor with activity targeting αVβ1 and αVβ6. Bexotegrast hydrochloride is used for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). Bexotegrast hydrochloride inhibits the activation of TGF-β1 by blocking the function of these integrins, thereby preventing the growth of fibrous tissue in the lungs and bile ducts .
|
-
- HY-146200
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase .
|
-
- HY-153200
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2/XIAP-IN-2 is a dual inhibitor of murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP). MDM2/XIAP-IN-2 degrades MDM2, and inhibits XIAP mRNA translation to inhibits cancer cells. Particularly, MDM2/XIAP-IN-2 inhibits acute lymphoblastic leukemia cell line EU-1 with an IC50 value of 0.3 μM .
|
-
- HY-146239
-
|
|
EGFR
Thymidylate Synthase
|
Cancer
|
|
EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM .
|
-
- HY-155179
-
|
|
PAK
HDAC
|
Cancer
|
|
ZMF-23 is a PAK1/HDAC6 dual inhibitor. ZMF-23 inhibits PAK1 and HDAC6 regulated aerobic glycolysis and migration. ZMF-23 induces TNF-α-regulated necroptosis, and further enhances apoptosis. ZMF-23 inhibits the Warburg effect and cell migration. ZMF-23 can be used for research of triple-negative breast cancer (TNBC) .
|
-
- HY-157480
-
|
|
EGFR
Aurora Kinase
|
Cancer
|
|
EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research .
|
-
- HY-130250
-
|
|
CDK
Apoptosis
|
Cancer
|
|
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
|
-
- HY-128171
-
|
|
FLAP
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s?of? 30 and 170?nM, respectively, and suppressed the activity of isolated sEH (IC50=20?nM) .
|
-
- HY-112816A
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
|
-
- HY-144643
-
|
|
Fungal
HDAC
Cytochrome P450
|
Inflammation/Immunology
|
|
CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis .
|
-
- HY-101798
-
|
|
PI3K
|
Cancer
|
|
MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
|
-
- HY-161886
-
|
|
Others
|
Cancer
|
|
SMARCA2-IN-7 (compound 12), a dual inhibitor of BRM and BRG1 (IC50 < 0.005 for both), has an anti-tumor proliferation effect that inhibits BRG1-deleted SKMEL5 tumor proliferation with a cell proliferation activity AAC50 of 13 nM in SKMEL5. The cell proliferation activity AAC50 of KRT880 in H1299 cells was 42 nM .
|
-
- HY-164489
-
|
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative .
|
-
- HY-169098
-
|
|
HSP
Histone Demethylase
|
Cancer
|
|
HSP90/LSD1-IN-1 (compound 6) is a HSP90/LSD1 dual inhibitor. HSP90/LSD1-IN-1 inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 and 0.30 μM, respectively .
|
-
- HY-169222S
-
|
|
Dihydroorotate Dehydrogenase
ROR
SARS-CoV
|
Infection
|
|
RORγ/DHODH-IN-2 (Compound 1311) is an orally active dual inhibitor of RORγ/DHODH with IC50 values of 11.9 nM and 90 nM, respectively. RORγ/DHODH-IN-2 exhibits antiviral activity by inhibiting the activity of SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC50 values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively .
|
-
- HY-163537
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
|
-
- HY-18955
-
|
|
MEK
Aurora Kinase
Apoptosis
|
Cancer
|
|
BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-112801
-
|
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
|
Cancer
|
|
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively .
|
-
- HY-B1452
-
|
ML-3000
|
COX
Lipoxygenase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins .
|
-
- HY-100501
-
|
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity .
|
-
- HY-136938
-
NEO2734
1 Publications Verification
EP31670
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains . NEO2734 is active in SPOP mutant and wild-type prostate cancer .
|
-
- HY-U00326
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
|
-
- HY-145280
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active .
|
-
- HY-144881
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
(S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC50 of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases .
|
-
- HY-146502
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP10/15-IN-3 (Compound 8a) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.14 µM and 0.40 µM against PARP10 and PARP15, respectively. PARP10/15-IN-3 is able to enter cells and rescue cells from apoptosis .
|
-
- HY-145280A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active .
|
-
- HY-144695
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .
|
-
- HY-144696
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .
|
-
- HY-147698
-
|
|
CDK
Topoisomerase
Apoptosis
|
Cancer
|
|
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
|
-
- HY-146338
-
|
|
HIV
|
Infection
|
|
RPR103611, the betulinic acid derivative, is a potent HIV-1 entry inhibitor with IC50s of 80, 0.27, and 0.17 for CCR5-tropic virus YU2, CXCR4-tropic virus NL4-3 and dual tropic virus 89.6, respectively .
|
-
- HY-150004
-
|
|
c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-3 (Compound 15f) is a dual c-Met and HDAC inhibitor with IC50 values of 12.50 nM and 26.97 nM against c-Met and HDAC1, respectively. c-Met/HDAC-IN-3 induces apoptosis and cause cell cycle arrest in G2/M phase .
|
-
- HY-150755
-
|
|
Topoisomerase
COX
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway .
|
-
- HY-N10701
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-11 (compound 1) is a potent is a dual AChE and BChE inhibitor with IC50 values of 70 and 71 μM for AChE and BChE, respectively. AChE/BChE-IN-11 is a natural product that could be isolated from the leaf of artichoke . AChE/BChE-IN-11 can be used in research of Alzheimer’s disease (AD) research .
|
-
- HY-148868
-
|
|
Akt
PKA
CDK
|
Others
|
|
Akt1&PKA-IN-1 is a potent dual Akt/PKA inhibitor with IC50 values of 0.03 , 0.11 μM, and 9.8 μM for PKAa, Akt, and CDK2, respectively. Akt1&PKA-IN-1 is selective for cyclin-dependent kinase 2 (CDK2) .
|
-
- HY-156435
-
|
|
α-synuclein
|
Neurological Disease
|
|
tau protein/α-synuclein-IN-1 is a dual inhibitor of tau protein and α-synuclein. tau protein/α-synuclein-IN-1 reduces α-syn inclusions development in M17D neuroblastoma cells. tau protein/α-synuclein-IN-1 can be used in study Alzheimer’s disease .
|
-
- HY-163207
-
|
|
Epoxide Hydrolase
HDAC
|
Neurological Disease
|
|
sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC50s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects .
|
-
- HY-115871A
-
|
|
Others
|
Others
|
|
(Rac)-PDE4-IN-4 is the diastereomer mixture of PDE4-IN-4 (HY-115871). PDE4-IN-4 is a dual M3 (pIC50 = 10.2) antagonist-PDE4 (pIC50 = 8.8) inhibitor for the inhaled research of pulmonary diseases .
|
-
- HY-163352
-
|
|
Others
|
Infection
|
|
Chitinase-IN-6 (Compound 4h) is a potent dual-Chitinase inhibitor, with Ki values of 1.82 and 2.00 μM against OfChtI and OfChi-h, respectively. Chitinase-IN-6 exhibits certain growth inhibition effects against Ostrinia furnacalis. Chitinase-IN-6 is a potential novel insecticide candidate friendly to nontarget organisms .
|
-
- HY-163380
-
|
|
Carbonic Anhydrase
|
Neurological Disease
|
|
CA/MAO-B-IN-1 (Compound 78) is a dual inhibitor for human brain carbonic anhydrases (CA) and Monoamine Oxidase-B (MAO-B), with IC50s of 8.8 and 7.0 nM, respectively. CA/MAO-B-IN-1 reveals a human oral absorption of 71.9% through in silico prediction .
|
-
- HY-163736
-
|
|
Lipoxygenase
PGE synthase
|
Inflammation/Immunology
|
|
mPGES-1/5-LOX-IN-1 (compound 3j) is a potent and orally active mPGES-1 and 5-LOX dual inhibitor with IC50 values of 0.92, 1.89 µM, respectively. mPGES-1/5-LOX-IN-1 shows anti-inflammatory impact .
|
-
- HY-159171
-
-
- HY-164309
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
DBCO-PEG3-Glu-Val-Cit-PABC-MMAE is a drug-linker conjugate for ADC. DBCO-PEG3-Glu-Val-Cit-PABC-MMAE contains a potent tubulin inhibitor Monomethyl auristatin E (MMAE, HY-15162) and can be used for synthesis of dual-drug ADC .
|
-
- HY-130247B
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity .
|
-
- HY-B0494R
-
|
|
HDAC
Aminopeptidase
|
Inflammation/Immunology
Cancer
|
|
Bufexamac (Standard) is the analytical standard of Bufexamac. This product is intended for research and analytical applications. Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 μM and 0.22 μM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug .
|
-
- HY-169220S
-
-
- HY-164454
-
|
|
Aurora Kinase
JAK
STAT
|
Inflammation/Immunology
|
|
AJI-100 is a dual-target inhibitor of Aurora kinase A and JAK2 with IC50 values ??of 12.7 nM and 18.5 nM, respectively. AJI-100 directly blocks Aurora kinase A to inhibit T cell mitosis and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-100 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
|
-
- HY-163439
-
|
|
Amylases
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-12 (compound 10k) is a dual inhibitor targeting α-glucosidase and α-amylase with IC50 of 34.52 nM and 24.62 nM, respectively. α-Amylase/α-Glucosidase-IN-12 is an inhibitor designed based on triazolo[4,3-b][1,2,4]triazine and has the potential to be used in diabetes research .
|
-
- HY-128035
-
|
|
Phospholipase
MAGL
|
Cardiovascular Disease
|
|
ML-211 is a carbamate-based dual inhibitor of acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) (IC50=17 nM) and LYPLA2 (IC50=30 nM). ML-211 also inhibits theserine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases .
|
-
- HY-124314
-
|
|
DAGL
MAGL
|
Metabolic Disease
|
|
LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [ 14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM .
|
-
- HY-145734A
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-145734
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-157320
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase .
|
-
- HY-160613
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM .
|
-
- HY-N12625
-
|
|
CDK
DYRK
GSK-3
|
Cancer
|
|
(R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC50s of 1.1, 0.95, >10, >10 and >10 μM, respectively .
|
-
- HY-159565
-
|
|
Bacterial
VEGFR
|
Infection
|
|
VEGFR-2/InhA-IN-1 is a pyrazole-based dual inhibitor of InhA-VEGFR with anti-tuberculosis and anti-angiogenic activities. VEGFR-2/InhA-IN-1 has good antibacterial activity against Mycobacterium tuberculosis H37Rv strain (MIC=6.25 μg/mL) and significantly inhibits VEGFR-2 (IC50=15.27 nM) .
|
-
- HY-168594
-
|
|
Glucosidase
NOD-like Receptor (NLR)
|
Neurological Disease
Metabolic Disease
|
|
α-Glucosidase/NLRP3-IN-1 (Compound 8) is a dual inhibitor of α-glucosidase and NLRP3, exhibiting an IC50 of 6.6 μM against α-glucosidase and inhibiting NLRP3 in multiple cell lines at a concentration of 100 μM. α-Glucosidase/NLRP3-IN-1 demonstrates neuroprotective and antidiabetic properties, and can be utilized in relevant research .
|
-
- HY-13299
-
MK-8033
2 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-13299A
-
|
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-13838
-
|
|
c-Fms
c-Kit
|
Cancer
|
|
PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
|
-
- HY-12975
-
AZ6102
1 Publications Verification
|
PARP
|
Cancer
|
|
AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.
|
-
- HY-100360
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-101093
-
CA-170
1 Publications Verification
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes .
|
-
- HY-128872
-
|
EHP-101; VCE-004.8
|
PPAR
Cannabinoid Receptor
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
Inflammation/Immunology
|
|
Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
|
-
- HY-128932
-
|
MT-141
|
Bacterial
PPAR
Prostaglandin Receptor
Antibiotic
|
Infection
Cardiovascular Disease
Endocrinology
|
|
Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity . Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension .
|
-
- HY-131970
-
|
|
Histone Demethylase
HDAC
|
Cancer
|
|
LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM) .
|
-
- HY-13838A
-
|
|
c-Fms
c-Kit
|
Inflammation/Immunology
Cancer
|
|
PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
|
-
- HY-100360A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-12572
-
|
|
Tie
VEGFR
|
Cancer
|
|
TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively . TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research .
|
-
- HY-142706
-
|
|
Monoamine Oxidase
HDAC
|
Cancer
|
|
MAO A/HDAC-IN-1 is a dual?inhibitor?of monoamine oxidase A (MAO A) and HDAC. MAO A/HDAC-IN-1 can be used for glioma research . MAO A/HDAC-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-144778
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
Bcl-2 Family
|
Cancer
|
|
IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
|
-
- HY-143411
-
|
|
HDAC
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
|
-
- HY-146501
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP10/15-IN-2 (Compound 8h) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.15 µM and 0.37 µM against PARP10 and PARP15, respectively. PARP10/15-IN-2 is able to enter cells and rescue cells from apoptosis .
|
-
- HY-146225
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-2 (compound 5) is a potent α-amylase and α-glucosidase dual inhibitor with IC50 values of 13.02, 13.09 µM for α-amylase and α-glucosidase, respectively. α-Amylase/α-Glucosidase-IN-2 has the potential for the research of diabetic complications .
|
-
- HY-N8707
-
|
|
Parasite
HDAC
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
|
Homobutein a natural chalcones (can be found in many medicinal plants, fruits, vegetables, spices and nuts), is a potent HDACs/NF-κB dual inhibitor with IC50s of 190 and 38 μM, respectively. Homobutein also a chelator of iron (II and III) cations, shows various activities, including anticancer, anti-inflammatory, antiparasite and antioxidation .
|
-
- HY-143324
-
|
|
HDAC
Adenosine Receptor
|
Cancer
|
|
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity .
|
-
- HY-151563
-
|
|
Deubiquitinase
|
Cancer
|
|
OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer .
|
-
- HY-149417
-
|
|
HDAC
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research .
|
-
- HY-157139
-
|
|
Carbonic Anhydrase
Phosphatase
|
Inflammation/Immunology
|
|
ALP/Carbonic anhydrase-IN-1 (Compound 1e) is a dual carbonic anhydrase (CA) and alkaline phosphatase (ALP) inhibitor. ALP/Carbonic anhydrase-IN-1 shows IC50 values of 0.44 µM, 1.61 µM, 0.51 µM, and 0.107 µM for CA-II, CA-IX, CA-XII, and ALP, respectively .
|
-
- HY-163272
-
|
|
Glutathione Peroxidase
CDK
|
Cancer
|
|
GPX4/CDK-IN-1 (Compound B9) is a dual inhibitor of GPX4 and CDK, with IC50 values of 542.5 nM, 191.2 nM and 68.1 nM for GPX4, CDK4 and CDK6, reapectively. GPX4/CDK-IN-1 shows strong cancer cell growth inhibition in vivo .
|
-
- HY-139230
-
|
|
Cannabinoid Receptor
PPAR
|
Metabolic Disease
|
|
OLHHA is a dual CB1 receptor antagonist and PPARα agonist. OLHHA also is a alcohol intake inhibitor with an EC50 value of 0.2 mg/kg. OLHHA reduces both hepatic lipid accumulation and circulating triglyceride levels. OLHHA shows anti-steatotic activity and has the potential for the research of non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-148233S
-
|
|
Casein Kinase
|
Others
|
|
JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure[1][2].
|
-
- HY-159482
-
|
|
Cholinesterase (ChE)
NOD-like Receptor (NLR)
|
Neurological Disease
|
|
SBN-284 (compound 3x) is a dual inhibitor of blood-brain permeable Cholinesterases and the NLRP3 inflammasome and is effective against EeAChE, hAChE and eqBChE, the IC50 values of are 0.37, 0.31, 0.29 μM respectively, and the EC50 of NLRP3 inflamm is 1 μM. SBN-284 can be used in Alzheimer's disease research .
|
-
- HY-168597
-
|
|
FGFR
Apoptosis
VEGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-3 (Compound 8m) is a dual inhibitor of FGFR1/VEGFR2. FGFR1/VEGFR2-IN-3 exhibits anti-proliferative and anti-migratory activities against cancer cells, and is capable of inducing cell apoptosis .
|
-
- HY-163535
-
|
|
HDAC
DNA Methyltransferase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
|
-
- HY-16438
-
|
|
CD47
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity . RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α . RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity .
|
-
- HY-123205
-
|
|
Histamine Receptor
P2X Receptor
5-HT Receptor
|
Inflammation/Immunology
|
|
Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin .
|
-
- HY-123983
-
|
|
Pim
DAPK
|
Cardiovascular Disease
|
|
HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension .
|
-
- HY-155108
-
|
|
Arginase
|
Cancer
|
|
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study .
|
-
- HY-157165
-
|
|
Microtubule/Tubulin
PARP
|
Cancer
|
|
Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase .
|
-
- HY-162868
-
|
|
c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC50 value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G0/G1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
|
-
- HY-123468
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-162829
-
|
|
URAT1
GLUT
|
Metabolic Disease
|
|
hURAT1 inhibitor 1 (compound 27b) is an isomarine-based, orally active dual hURAT1/GLUT9 inhibitor with IC50s of 0.16 μM and 4.47 μM, respectively, and has anti-hyperuricemia effects. hURAT1 inhibitor 1 showed significant uric acid-lowering activity in a hyperuricemia mouse model (10 mg/kg dose). hURAT1 inhibitor 1 had no significant in vitro cytotoxicity or in vivo hepatotoxicity and showed good PK characteristics .
|
-
- HY-123468A
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-50878A
-
|
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-101925
-
CM-272
3 Publications Verification
|
Histone Methyltransferase
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .
|
-
- HY-10412
-
|
KT7515
|
JNK
Mixed Lineage Kinase
MDM-2/p53
|
Neurological Disease
|
|
CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53 .
|
-
- HY-149283
-
|
|
JAK
HDAC
Apoptosis
|
Cancer
|
|
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
|
-
- HY-163006
-
|
|
EGFR
c-Met/HGFR
|
Cancer
|
|
EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFR L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .
|
-
- HY-162649
-
|
|
Toll-like Receptor (TLR)
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
TIC10g is a dual inhibitor for toll-like receptor 7 and 9 (TLR7 and TLR9), which inhibits TLR7 and TLR9 mediated TNF-α release in mouse macrophages (IC50 is 14.5 μM and 6.5 μM) and human B lymphocytes (IC50 is 7.69 μM and 11.5 μM). TIC10g inhibits the activation of NF-κB and MAPK, and exhibits anti-inflammatory activity against systemic lupus erythematosus and rheumatoid arthritis .
|
-
- HY-162719
-
|
|
SARS-CoV
|
Infection
|
|
RH12 is a dual inhibitor for SARS-CoV-2 related RNA-dependent RNA polymerase (RdRp, IC50 is 4.42 nM) and human transmembrane serine protease 2 (TMPRSS2, IC50 is 4.2 nM). RH12 exhibits antiviral efficacy. RH12 inhibits viral replication and absorption, and exhibits a 90.5% virucidal effects on Vero-E6 cells. RH12 inhibits cell viability of Calu-3 with an IC50 of 17.5 nM .
|
-
- HY-10811
-
GNE-493
2 Publications Verification
|
PI3K
mTOR
|
Cancer
|
|
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
|
-
- HY-12680
-
PRN694
1 Publications Verification
|
Itk
|
Inflammation/Immunology
|
|
PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo .
|
-
- HY-13431
-
|
|
DNA-PK
PI3K
mTOR
|
Cancer
|
|
KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively .
|
-
- HY-10220
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 proagent, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis .
|
-
- HY-114331
-
|
|
MAP3K
|
Neurological Disease
|
|
DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
|
-
- HY-128350A
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
|
-
- HY-18307
-
|
|
c-Met/HGFR
|
Cancer
|
|
SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated .
|
-
- HY-75706
-
|
|
PARP
Ligands for Target Protein for PROTAC
|
Cancer
|
|
N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib (HY-10162) containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a PARP inhibitor used for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4 . N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor .
|
-
- HY-124270
-
|
AR-C68397AA
|
Dopamine Receptor
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.
|
-
- HY-144315
-
|
Snail/HDAC-IN-1
|
HDAC
|
Cancer
|
|
CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. CYD19 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
|
-
- HY-146315
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE-IN-6 (compound 22) is a potent dual AChE/BChE inhibitor with IC50 values of 0.809 µM, 2.248 µM and > 100 µM for hBChE, hAChE and hMAO-B, respectively. AChE/BChE-IN-6 penetrates the blood-brain barrier (BBB). AChE/BChE-IN-6 can be used for Alzheimer’s disease (AD) research .
|
-
- HY-147846
-
-
- HY-151366
-
|
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
|
HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC50 of 443 nM against human HDAC8 and a Kd of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6 .
|
-
- HY-151575
-
|
|
GSK-3
|
Infection
|
|
PfGSK3/PfPK6-IN-2 is a potent dual PfGSK3/PfPK6 (Plasmodium falciparum GSK3/PK6) inhibitor (IC50: 172 nM and 11 nM respectively). PfGSK3/PfPK6-IN-2 can be used in the research of Malaria .
|
-
- HY-123298
-
|
|
Src
Akt
Apoptosis
|
Cancer
|
|
Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .
|
-
- HY-149669
-
|
|
PI3K
HDAC
Apoptosis
|
Cancer
|
|
PH14 is a dual PI3K/HDAC inhibitor with IC50 values of 20.3 nM and 24.5 nM for PI3Kα and HDAC3, respectively. PH14 has antiproliferative activity and also induces apoptosis in Jeko-1 cells. PH14 can be used in cancer research, such as lymphoma .
|
-
- HY-163188
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
COX-2/LOX-IN-2 (compound 6) is a dual inhibitor of COX-2/LOX with IC50s of 7.0 μM and 27.5 μM, respectively. COX-2/LOX-IN-2 has antioxidant activity and has the potential to be used in the development of nonsteroidal anti-inflammatory drugs (tNSAIDs) .
|
-
- HY-N0232R
-
|
|
COX
Lipoxygenase
Notch
Reactive Oxygen Species
Bacterial
|
Cancer
|
|
Psoralidin (Standard) is the analytical standard of Psoralidin. This product is intended for research and analytical applications. Psoralidin is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties . Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation .
|
-
- HY-162906
-
|
|
HDAC
FLT3
|
Cancer
|
|
FLT3/HDAC-IN-2 is (compound 25h) a FLT3/HDAC dual inhibitor. FLT3/HDAC-IN-2 has antiproliferative activity against MOLM-13 cells. FLT3/HDAC-IN-2 can be used in acute myeloid leukemia research .
|
-
- HY-153972
-
|
|
URAT1
Xanthine Oxidase
|
Metabolic Disease
Inflammation/Immunology
|
|
URAT1&XO inhibitor 2 (Compound BDEO) is a dual inhibitor of xanthine oxidase and URAT1, with IC50 of 3.3 μM for xanthine oxidase. URAT1&XO inhibitor 2 blocks uptake of uric acid in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. URAT1&XO inhibitor 2 decreases serum urate level and uric acid excretion in hyperuricemic mice. URAT1&XO inhibitor 2 can be used for research of hyperuricemia .
|
-
- HY-162519
-
|
LZ90
|
NAMPT
PD-1/PD-L1
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
LZFPN-90 (LZ90) is a dual NAMPT/PD-L1 targeting compound. LZFPN-90 inhibits PD-1/PD-L1 interaction and NAMPT activity. LZFPN-90 inhibits cell growth in a NAMPT-dependent manner and blocks the cell cycle, subsequently inducing apoptosis. LZFPN-90 exerted target-dependent antitumor activities, affecting metabolic processes and the immune system .
|
-
- HY-10181R
-
|
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-10115A
-
|
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
|
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy .
|
-
- HY-113509
-
|
LXA4
|
Interleukin Related
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
|
-
- HY-113289
-
|
|
Akt
Androgen Receptor
Bacterial
Drug Metabolite
HSV
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
|
-
- HY-147992
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-147994
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-152030
-
|
|
Microtubule/Tubulin
MMP
Apoptosis
|
Cancer
|
|
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer .
|
-
- HY-149275
-
|
|
Pyruvate Kinase
PDK-1
Akt
EGFR
Apoptosis
|
Cancer
|
|
PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway .
|
-
- HY-149270
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-31 (compound 7b) is an orally active and dual inhibitor of COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). COX-2-IN-31 also inhibits transmembrane hCA IX(Ki=48.9 nM) and hCA XII(Ki=5.8 nM) activity. COX-2-IN-31 exhibits anti-inflammatory and analgesic activity .
|
-
- HY-128397
-
|
|
Parasite
Bcr-Abl
Src
|
Infection
|
|
CpCDPK1/TgCDPK1-IN-1 (compound 7p) is a potent CpCDPK1/TgCDPK1 dual inhibitor (IC50: 10 nM and 5.0 nM respectively). CpCDPK1/TgCDPK1-IN-1 also inhibits Abl and Src (IC50: 75 nM and 65 nM respectively). CpCDPK1/TgCDPK1-IN-1 can be used for research of toxoplasmosis .
|
-
- HY-155784
-
|
|
Sirtuin
Reactive Oxygen Species
Keap1-Nrf2
|
Cancer
|
|
SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway .
|
-
- HY-149474
-
|
|
FLT3
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor (IC50: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). HDAC-IN-63 inhibits MV4-11 cell proliferation (IC50: 92 nM. HDAC-IN-63 induces apoptosis and arrests cell cycle in MV4-11 cells. HDAC-IN-63 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-155227
-
|
|
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
|
ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
|
-
- HY-149578
-
|
|
Microtubule/Tubulin
HDAC
|
Cancer
|
|
Tubulin/HDAC-IN-3 (compound 12a) is a potent tubulin/HDAC dual inhibitor. Tubulin/HDAC-IN-3 effectively disrupts tubulin polymerization (IC50: 5.4 μM). Tubulin/HDAC-IN-3 exhibits potent HDAC1/8 inhibitory activities, with IC50 values of 0.155 and 0.177 μM, respectively. Tubulin/HDAC-IN-3 works through blocking cellular cycle, inducing apoptosis and inhibiting colony formation .
|
-
- HY-161083
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
|
-
- HY-162254
-
|
|
EGFR
Ack1
|
Cancer
|
|
EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity .
|
-
- HY-160558
-
|
|
Epigenetic Reader Domain
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively .
|
-
- HY-161868
-
|
|
PARP
HDAC
Apoptosis
|
Cancer
|
|
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase .
|
-
- HY-113695
-
|
|
Angiotensin-converting Enzyme (ACE)
Adrenergic Receptor
|
Cardiovascular Disease
|
|
BW A575C is a dual inhibitor against angiotensin converting enzyme (ACE) and β-adrenoceptor. BW A575C produces a competitive blockade of Isoprenaline (HY-108353)-induced tachycardia in a guinea-pig right atrial. BW A575C also inhibits Angiotensin I (HY-P1032)-induced pressor responses in rats. BW A575C is promising for research of hypertensive diseases .
|
-
- HY-169212
-
|
|
Others
|
Cancer
|
|
I194496 is a potent cystathionine γ-lyase (CSE) inhibitor, with an IC50 of 0.79 mM. I194496 can inhibit the growth of human TNBC cells via the dual targeting PI3K/Akt and Ras/Raf/ERK pathway and suppress the metastasis of human TNBC cells via down-regulating Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways .
|
-
- HY-13334
-
|
NVP-BGT226 maleate
|
PI3K
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
BGT226 (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells .
|
-
- HY-13334A
-
|
NVP-BGT226
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells .
|
-
- HY-144307
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
|
-
- HY-144305
-
|
|
URAT1
GLUT
|
Infection
|
|
KPH2f is a safe, orally active, and effective dual URAT1/GLUT9 inhibitor with IC50s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively. KPH2f shows little effects on OAT1 and ABCG2 (IC50=32.14 and 26.74 μM) .
|
-
- HY-144826
-
|
|
GSK-3
|
Neurological Disease
|
|
ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. ZDWX-25 possesses significant cytotoxic activities against SH-SY5Y and HL-7702 cells. ZDWX-25 can be used for researching alzheimer's disease .
|
-
- HY-144732
-
|
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-147873
-
|
|
iGluR
HDAC
|
Neurological Disease
|
|
NMDAR/HDAC-IN-1 (Compound 9d) is a dual NMDAR and HDAC inhibitor with a Ki of 0.59 μM for NMDAR and IC50 values of 2.67, 8.00, 2.21, 0.18 and 0.62 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. NMDAR/HDAC-IN-1 efficiently penetrates the blood brain barrier .
|
-
- HY-147925
-
|
|
Carbonic Anhydrase
|
Others
|
|
hCAI/II-IN-4 (compound 6d) is a potent dual hCA I/II inhibitor with Ki values of 16.95, 15.22 and 27.04 nM for hCA I, hCA II and hCA Ⅸ, respectively. hCAI/II-IN-4 has anti-hypoxia activities and low toxicity. hCAI/II-IN-4 can be used for acute mountain sickness (AMS) research .
|
-
- HY-151596
-
-
- HY-155151
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK2/3-IN-1 is a potent dual RIPK2/3 kinases inhibitor with IC50 values of 3 nM and 117 nM, respectively. RIPK2/3-IN-1 is against RIPK2 with IC50 value 14 nM in 14-TriLAN-Gly/NOD1 THP-1 cell-based NF-κB reporter assay .
|
-
- HY-126898
-
|
|
Lipoxygenase
PGE synthase
|
Inflammation/Immunology
|
|
5-LO/mPGES1-IN-1 (Compound 16) is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). IC50 values are 0.3 and 0.4 μM, respectively. 5-LO/mPGES1-IN-1 has anti-inflammatory activity .
|
-
- HY-P10223
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 65 and 123 μM, respectively .
|
-
- HY-160557
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC50=28 nM, PLK1 IC50=40 nM) .
|
-
- HY-161967
-
|
|
FLT3
JAK
Apoptosis
|
Cancer
|
|
JAK2/FLT3-IN-3 (11r) is a dual FLT3 and JAK2 inhibitor, with IC50 values of 2.01 nM, 0.51 nM and 104.40 nM for JAK2, FLT3 and JAK3, respectively. JAK2/FLT3-IN-3 (11r) induces apoptosis and possesses antitumor activity .
|
-
- HY-125050
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
KCA-1490 is a dual PDE3/4 inhibitor with IC50 values of 369 nM and 42 nM, respectively. KCA-1490 exhibits potent bronchodilatory and anti-inflammatory activity. KCA-1490 suppresses Histamine (HY-B1204)-induced bronchoconstriction in vivo, which is promising for research of asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-P0090S
-
|
Salmon calcitonin-13C6,15N4 TFA
|
CGRP Receptor
|
Metabolic Disease
|
|
Calcitonin- 13CIC6, 15NIC4 (salmon) (Salmon calcitonin- 13CIC6, 15NIC4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
|
-
- HY-112348
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-124131
-
DS-437
1 Publications Verification
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 .
|
-
- HY-112602
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively . Antitumor activity .
|
-
- HY-111508
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR . Antitumor activity .
|
-
- HY-155073
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
|
-
- HY-10626
-
|
|
LXR
FXR
ROR
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
|
-
- HY-100867A
-
|
TAK-659 monohydrochloride; CB-659 monohydrochloride
|
Syk
FLT3
|
Cancer
|
|
TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-100867
-
|
TAK-659; CB-659
|
Syk
FLT3
|
Cancer
|
|
TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-128350
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
|
-
- HY-130247
-
|
JAK2/FLT3-IN-1
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity .
|
-
- HY-144449
-
|
|
mTOR
HDAC
Apoptosis
Autophagy
|
Cancer
|
|
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC) .
|
-
- HY-146704
-
|
|
Epoxide Hydrolase
COX
|
Cardiovascular Disease
|
|
COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks .
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-
- HY-146977
-
|
|
PDK-1
|
Cancer
|
|
LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC50 of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases .
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-
- HY-146978
-
|
|
PDK-1
|
Cancer
|
|
LDHA/PDKs-IN-2 (compound 20k) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 1.6 and 0.7 μM, respectively. LDHA/PDKs-IN-2 reduces A549 cell proliferation with an EC50 of 15.7 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-147754
-
|
|
Btk
JAK
|
Inflammation/Immunology
|
|
JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research .
|
-
- HY-143325
-
|
|
HDAC
Adenosine Receptor
|
Cancer
|
|
A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor .
|
-
- HY-N12007
-
|
|
OAT
|
Metabolic Disease
|
|
OAT1/3-IN-1 (compound 7) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-1 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-1 can be used to study mercury-induced kidney damage .
|
-
- HY-N12008
-
|
|
OAT
|
Metabolic Disease
|
|
OAT1/3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-2 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-2 can be used to study mercury-induced kidney damage .
|
-
- HY-149734
-
|
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Bacterial
|
Infection
|
|
MA220607 is an antibacterial agent with low hemolytic toxicity and a dual-target mechanism of action (MOA). MA220607 promotes FtsZ protein polymerization, also increases the permeability of bacterial membranes and inhibits biofilm formation. The resistance rate of MA220607 is low, and the MICs against Gram-positive bacteria and Gram-negative bacteria are Table 0.062-2 μg/mL and 0.5-4 μg/mL, respectively) .
|
-
- HY-160005
-
|
NSC 781517
|
Topoisomerase
|
Cancer
|
|
LMP517 (NSC 781517) a indenoisoquinoline, is a potent a dual TOP1 and TOP2 inhibitor. LMP517 shows better antitumor activity than its parent compound LMP744 (HY-U00248) against H82 (Small Cell Lung Cancer) xenografts. LMP517 induces TOP1 cleavage complexes (TOP1ccs) and TOP2ccs .
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-
- HY-162312
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-15805
-
|
|
Src
Btk
|
Cancer
|
|
KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .
|
-
- HY-P10222
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 14.5 and 10.2 μM, respectively .
|
-
- HY-P10221A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CKLIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 2.6 and 2.2 μM, respectively .
|
-
- HY-161523
-
|
|
Xanthine Oxidase
URAT1
|
Metabolic Disease
|
|
XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC50 of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model .
|
-
- HY-163889
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Ferroptosis/apoptosis inducer-1 (compound 4d) is a dual inducer of apoptosis and ferroptosis. Ferroptosis/apoptosis inducer-1 induces apoptosis and ferroptosis by reducing mitochondrial membrane potential and downregulating GPX4. Ferroptosis/apoptosis inducer-1 can significantly inhibit the proliferation and metastasis of triple-negative breast cancer (TNBC) both in vitro and in vivo, playing an important role in cancer research .
|
-
- HY-161957
-
|
|
Topoisomerase
|
Cancer
|
|
Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models .
|
-
- HY-162940
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC50s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .
|
-
- HY-168554
-
|
|
PROTACs
STING
|
Inflammation/Immunology
|
|
STING-IN-10 (P8) is a dual STING PROTAC degrader and inhibitor with a DC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity .(Pink: Target protein ligand (HY-168676); Black: linker (HY-168675); Blue: E3 ligase ligand (HY-W039116))
|
-
- HY-50673
-
|
BEZ235; NVP-BEZ235
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
|
-
- HY-155191
-
|
|
Galectin
|
Inflammation/Immunology
Cancer
|
|
Galectin-3/galectin-8-IN-1 (Compound 53) is a dual Galectin-3 and galectin-8 C-terminal domain inhibitor, with Kd values of 4.12 μM and 6.04 μM respectively. Galectin-3/galectin-8-IN-1 inhibits the MRC-5 lung fibroblast cells migration. Galectin-3/galectin-8-IN-1 can be used for research of cancer and tissue fibrosis .
|
-
- HY-155192
-
|
|
Galectin
|
Inflammation/Immunology
Cancer
|
|
Galectin-3/galectin-8-IN-2 (Compound 57) is a dual Galectin-3 and galectin-8 C-terminal domain inhibitor, with Kd values of 12.8 μM and 2.06 μM respectively. Galectin-3/galectin-8-IN-2 inhibits the MRC-5 lung fibroblast cells migration. Galectin-3/galectin-8-IN-2 can be used for research of cancer and tissue fibrosis .
|
-
- HY-156114
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC50s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 0.39 μM .
|
-
- HY-156115
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 3.16 μM .
|
-
- HY-156116
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 2.74 μM .
|
-
- HY-N11997
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Feralolide is a dihydroisocoumarin isolated from the methanolic extract of aloe vera resin. Feralolide is also a dual inhibitor of AChE and BuChE, with IC50s of 55 μg/mL and 52 μg/mL respectively. Feralolide has antioxidant activity and inhibits 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS). Feralolide could be used in research into cognitive disorders such as Alzheimer's disease, potentially restoring and enhancing memory .
|
-
- HY-155227A
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively .
|
-
- HY-162349
-
|
|
HDAC
PARP
|
Cancer
|
|
PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6) . br/ .
|
-
- HY-161628
-
|
|
Topoisomerase
|
Cancer
|
|
Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
|
-
- HY-14923
-
|
AVE 7688
|
Angiotensin-converting Enzyme (ACE)
|
Metabolic Disease
|
|
Ilepatril, a vasopeptidase inhibitor, was investigated in obese Zucker diabetic fatty (ZDF) rats as a dual inhibitor of angiotensin converting enzyme and neutral endopeptidase for treating Type 2 diabetic nephropathy. Despite stable diabetes (HbA1c >12%), Ilepatril significantly reduced albuminuria in a dose-dependent manner compared to placebo. This study highlights Ilepatril's efficacy in ameliorating nephropathy symptoms in diabetic rats, suggesting its potential as a therapeutic strategy independent of metabolic control for Type 2 diabetic nephropathy .
|
-
- HY-162645
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
|
-
- HY-161996
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Inflammation/Immunology
|
IDO1-IN-25 is a dual inhibitor of IDO1/TDO2, with IC50 values of 0.17 μM and 3.2 μM, respectively. IDO1-IN-25 can effectively inhibit the production of NO in RAW264.7 cells stimulated by lipopolysaccharide (LPS). IDO1-IN-25 can exert anti-inflammatory effects in a mouse ear edema acute inflammation model induced by croton oil .
|
-
- HY-168030
-
|
|
Apoptosis
Ferroptosis
Carbonic Anhydrase
Reactive Oxygen Species
Caspase
Mitochondrial Metabolism
|
Cancer
|
|
hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 and 8.5 nM for hCA IX and hCA XII, respectively. In addition to inhibiting hCA activity, hCAIX-IN-23 releases NO, exhibiting dual antitumor activity. hCAIX-IN-23 induces apoptosis by regulating mitochondrial caspase activity and the ferroptosis pathway (ferroptosis) through the downregulation of hCA IX and iron-regulatory protein expression. hCAIX-IN-23 is useful for renal cancer research .
|
-
- HY-147613
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-6 displays better stability in artificial gastric fluids than gedatolisib. PI3K/mTOR Inhibitor-6 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-6 has the potential for the research of cancer diseases .
|
-
- HY-108347
-
|
|
P-glycoprotein
BCRP
|
Metabolic Disease
|
|
CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
|
-
- HY-150772
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .
|
-
- HY-10424
-
|
PHA-848125
|
CDK
Autophagy
|
Cancer
|
|
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
|
-
- HY-12279
-
|
TGR-1202; RP5264
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .
|
-
- HY-12279C
-
|
TGR-1202 hydrochloride; RP5264 hydrochloride
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .
|
-
- HY-103018
-
|
ASN-002
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-130247A
-
|
JAK2/FLT3-IN-1 TFA
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity .
|
-
- HY-146675
-
|
|
COX
|
Inflammation/Immunology
|
|
COX/5-LOX-IN-1 (compound 6b) is a potent and dual inhibitor of COX/5-LOX with IC50s of 1.07, 0.55, and 0.28 μM for COX-1, COX-2, and 5-LOX enzyme, respectively. COX/5-LOX-IN-1 has the potential for the research of inflammation diseases .
|
-
- HY-146492
-
|
|
VEGFR
Raf
Apoptosis
|
Cancer
|
|
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase .
|
-
- HY-147951
-
|
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
COX-2/5-LOX-IN-3 (compound 5b) is a potent and dual COX-2/5-LOX inhibitor with IC50 values of 45.73, 5.45 and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. COX-2/5-LOX-IN-3 has the potential for the research of inflammation diseases .
|
-
- HY-146108
-
|
|
RSV
|
Infection
|
|
RSV-IN-5 (Compound 4) is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. RSV-IN-5 exhibits potent anti-RSV activities against not only wild-type A2 F protein (EC50=2.0 nM), but also D486N-mutant F protein (EC50=8.1 nM) .
|
-
- HY-143278
-
|
|
Topoisomerase
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-13 (compound 20) is a potent and effective antileukemic topoisomerase II and FLT3 dual inhibitor with IC50 values of 2.26 μM and 2.26 μM, respectively. FLT3-IN-13 arrests cell cycle at G2/M phase and induce apoptosis. FLT3-IN-13 has anticytotoxic activity, particularly against leukemia .
|
-
- HY-12279A
-
|
TGR-1202 tosylate; RP5264 tosylate
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach .
|
-
- HY-150638
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research .
|
-
- HY-151388
-
|
|
Monoamine Oxidase
COMT
|
Neurological Disease
|
|
hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor (IC50s: 2.5 μΜ for hMAO-B, 3.84 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-1 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-1 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD) .
|
-
- HY-151390
-
|
|
Monoamine Oxidase
COMT
|
Neurological Disease
|
|
hMAO-B/MB-COMT-IN-2 is a dual MAO-B/MB-COMT inhibitor (IC50s: 4.27 μΜ for hMAO-B, 2.69 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-2 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-2 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD) .
|
-
- HY-B1452S1
-
|
ML-3000-d6
|
Apoptosis
Lipoxygenase
COX
|
Cancer
|
|
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
|
-
- HY-103018A
-
|
ASN-002 hydrochloride
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-155694
-
|
|
Carbonic Anhydrase
VEGFR
|
Cancer
|
|
hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual Carbonic Anhydrase(CA) IX/XII with Ki values of 4.7 nM and 8.3 nM for hCA XII and hCA IX, respectively. hCA/VEGFR-2-IN-1 (compound 13a) is a potent VEGFR-2 inhibitor with IC50 values 26.3 nM. hCA/VEGFR-2-IN-1 has anticancer activity .
|
-
- HY-157394
-
|
|
Cholinesterase (ChE)
|
Inflammation/Immunology
|
|
eeAChE/eqBuChE-IN-1 (compound 3F) is a reversible dual eeAChE/eqBuChE inhibitor with IC50s of 1.3?μM and 0.81?μM, respectively. eeAChE/eqBuChE-IN-1 exhibits anti-inflammatory activity. eeAChE/eqBuChE-IN-1 also shows neuroprotective effect on Aβ25-35-induced PC12 cell injury .
|
-
- HY-157440
-
|
|
Amyloid-β
Reactive Oxygen Species
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/Aβ-IN-3 (compound AM5) is a dual inhibitor of AChE and Amyloid-β aggregation with IC50<.sub> values of 1.29 and 4.93 μM, respectively. AChE/Aβ-IN-3 has antioxidant properties that scavenge ROS and restore their normal levels. AChE/Aβ-IN-3 can be used in the study of neurological diseases, such as Alzheimer's disease .
|
-
- HY-15268
-
|
|
c-Met/HGFR
PI3K
DNA-PK
mTOR
Bcr-Abl
Src
VEGFR
EGFR
PDGFR
|
Cancer
|
|
PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research .
|
-
- HY-123008
-
|
|
Others
|
Others
|
|
Reproterol hydrochloride is a dual-acting beta2-adrenoceptor agonist and phosphodiesterase inhibitor. Reproterol hydrochloride is more potent than albuterol and feterol in stimulating cAMP production in human monocytes, demonstrating its potential in enhancing airway function. Furthermore, Reproterol significantly inhibited the production of LTB4, indicating its anti-inflammatory properties. Reproterol hydrochloride may have inhibitory effects in respiratory diseases such as asthma and COPD .
|
-
- HY-W700639
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Tolafentrine, a dual-selective phosphodiesterase 3/4 (PDE3/4) inhibitor, has been shown to have significant acute and chronic effects in a unilateral diacetamide-induced rat pulmonary hypertension model. Experiments show that long-term administration can significantly alleviate all unilateral bisacetamide-induced hemodynamic and gas exchange abnormalities, reduce right ventricular hypertrophy, and normalize pulmonary vascular remodeling changes .
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-
- HY-123205R
-
|
|
Histamine Receptor
P2X Receptor
5-HT Receptor
|
Inflammation/Immunology
|
|
Oxatomide (Standard) is the analytical standard of Oxatomide. This product is intended for research and analytical applications. Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin .
|
-
- HY-100034
-
|
DA-3003-1
|
Phosphatase
Histone Methyltransferase
|
Cancer
|
|
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
|
-
- HY-137561
-
|
PLN-74809
|
Integrin
|
Inflammation/Immunology
|
|
Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung .
|
-
- HY-115906
-
|
|
FLT3
MNK
Apoptosis
|
Cancer
|
|
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase .
|
-
- HY-147939
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Cancer
|
|
AChE/BuChE-IN-3 is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC50s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease .
|
-
- HY-151263
-
|
|
HDAC
G-quadruplex
|
Cancer
|
|
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer .
|
-
- HY-149418
-
|
|
HDAC
Cholinesterase (ChE)
Tau Protein
|
Neurological Disease
|
|
BChE/HDAC6-IN-2 (compound 29a) is a dual inhibitor of BChE and HDAC6 with IC50s of 1.8 nM and 71.0 nM, respectively. BChE/HDAC6-IN-2 has prominently neuroprotective effects and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is also an effective chelator of metal ion (Fe2+ and Cu2+). BChE/HDAC6-IN-2 inhibits phosphorylation of tau, and exhibits moderate immunomodulatory effect.
|
-
- HY-149633
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
Apoptosis
|
Cancer
|
|
EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .
|
-
- HY-133233
-
|
1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). The IC50 value for thioetheramide-PC is 2 μM at a substrate concentration of 0.5 mM.1 In addition to binding to the catalytic site of sPLA2, thioetheramide-PC also binds to the activator site of this enzyme. The binding of thioetheramide-PC to the activator site is tighter than its binding to the catalytic site. The result of this dual interaction is that at low concentrations thioetheramide-PC may activate phospholipase activity rather than inhibiting it.
|
-
- HY-161859
-
|
|
VEGFR
STAT
|
Cancer
|
|
VEGFR-2/STAT-3-IN-1 (Compound 9f) is a dual inhibitor for VEGFR-2 (IC50=26.3 nM) and STAT-3 (IC50=5.63 nM). VEGFR-2/STAT-3-IN-1 inhibits the proliferation of cancer cells PANC1 and PC3 with IC50 of 0.14 and 0.10 µM. VEGFR-2/STAT-3-IN-1 induces apoptosis in PC3 .
|
-
- HY-155108B
-
|
|
Arginase
|
Cancer
|
|
OATD-02 hydrochloride is the hydrochloride salt form of OATD-02 (HY-155108). OATD-02 hydrochloride an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and Arginase2. OATD-02 hydrochloride is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 hydrochloride bolishes tumor immunosuppression induced by both arginases. OATD-02 hydrochloride can be used for melanoma study .
|
-
- HY-159513
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-2/Mcl-1-IN-4 (compound 20) is a dual inhibitor targeting Bcl-2 (Ki=0.49 μM) and Mcl-1 (Ki=0.51 μM). Bcl-2/Mcl-1-IN-4 significantly inhibits cancer cell proliferation and effectively induces apoptosis in U937 cells. Bcl-2/Mcl-1-IN-4 can be used in cancer research .
|
-
- HY-161968
-
|
|
EGFR
PI3K
|
Cancer
|
|
EGFR/PI3Kα-IN-1 (compound 30k) is a dual EGFR/PI3Kα inhibitor with IC50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. EGFR/PI3Kα-IN-1 can inhibit tumor cell proliferation and has anticancer activity .
|
-
- HY-116191
-
|
|
PI3K
mTOR
|
Cancer
|
|
WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
|
-
- HY-168049
-
|
|
PPAR
Akt
|
Metabolic Disease
|
|
ZLY06 is an orally active dual agonist of peroxisome proliferator-activated receptor (PPAR) δ and γ (PPAR δ: EC50=341 nM; PPAR γ: EC50=237 nM). ZLY06 induces hepatic lipid accumulation by inhibiting the phosphorylation of AKT1, mediating the upregulation of CD36. In addition, ZLY06 significantly improves glucose and lipid metabolism without increasing body weight, and alleviates fatty liver by promoting β-oxidation of fatty acids and inhibiting hepatic lipogenesis .
|
-
- HY-128932R
-
|
|
Bacterial
PPAR
Prostaglandin Receptor
Antibiotic
|
Infection
Cardiovascular Disease
Endocrinology
|
|
Cefminox (sodium) (Standard) is the analytical standard of Cefminox (sodium). This product is intended for research and analytical applications. Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity . Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension .
|
-
- HY-126249
-
|
|
Aurora Kinase
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM .
|
-
- HY-W011266
-
|
|
PDGFR
|
Cancer
|
|
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
|
-
- HY-136310
-
|
|
Others
|
Cancer
|
|
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 µM and 0.6 µM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways .
|
-
- HY-111140
-
|
|
PGE synthase
Lipoxygenase
|
Inflammation/Immunology
|
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells .
|
-
- HY-12279B
-
|
TGR-1202 sulfate; RP-5264 sulfate
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach .
|
-
- HY-147060
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .
|
-
- HY-151809
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 19 nM and 17 nM, respectively. CYP4A11/CYP4F2-IN-1 has potential for the research of renal diseases .
|
-
- HY-152142
-
|
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
|
-
- HY-149819
-
|
|
HDAC
CDK
|
Cancer
|
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
|
-
- HY-155152
-
|
|
P-glycoprotein
BCRP
|
Cancer
|
|
P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
|
-
- HY-138215
-
|
|
ERK
|
Cancer
|
|
ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo .
|
-
- HY-N11728
-
|
|
Amylases
Glucosidase
|
Metabolic Disease
|
|
2,7"-Phloroglucinol-6,6'-bieckol is an orally active dual α-amylase/α-glucosidase inhibitor with IC50 values of 6.94 μM and 23.35 μM respectively. 2,7"-Phloroglucinol-6, 6'-bieckol alleviates postprandial hyperglycemia in diabetic mice. 2,7"-Phloroglucinol-6,6'-bieckol can be used in diabetes research .
|
-
- HY-161094
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-12 is a dual inhibitor of metal β-lactamases (MβLs (NDM-1, IMP-1)) and serine β-lactamases (SβLs (OXA-48, KPC-2)), with IC50 values of 0.64 μM, 1.32 μM, 1.01 μM, and 0.57 μM, respectively. Metallo-β-lactamase-IN-12 has antibacterial activity .
|
-
- HY-162332
-
|
|
Apoptosis
EGFR
JNK
|
Cancer
|
|
EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2 with IC50s of 2.7 and 3.0 μM, respectively. EGFR-PK/JNK-2-IN-1 can induce apoptosis and induce cell cycle arrest at different cell phases. EGFR-PK/JNK-2-IN-1 can be used for the research of cancer .
|
-
- HY-163371
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .
|
-
- HY-161470
-
|
|
Histone Demethylase
E1/E2/E3 Enzyme
DNA/RNA Synthesis
Caspase
Apoptosis
|
Cancer
|
|
WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-163710
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2 IN-5 (compound 9) is an indolone-phenylsulfonamide and a potential dual inhibitor of cancer-related hCA IX/XII and VEGFR-2. The IC50 values of hCA/VEGFR-2-IN-5 for VEGFR-2, hCA IX and hCA XII are 0.38 μM, 40 and 3.2 nM, respectively. hCA/VEGFR-2-IN-5 has antitumor activity .
|
-
- HY-162803
-
|
|
Apoptosis
c-Met/HGFR
STAT
|
Cancer
|
|
c-Met-IN-24 (compound 3g) is a dual-target inhibitor of STAT-3 ( =4.7 μM) and c-MET ( =12.67 μM) with anticancer activity. c-Met-IN-24 arrests the G2/M cell cycle and induces apoptosis in SNB-75 cells. c-Met-IN-24 can be used in the study of central nervous system cancers .
|
-
- HY-112828
-
|
|
DAGL
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
LEI105 is a potent, highly selective and reversible dual diacylglycerol lipase (DAGL)-α/DAGL-β inhibitor. LEI105 reduces 2-arachidonoylglycerol levels in Neuro2A cells. LEI105 also reduces cannabinoid CB1-receptor-mediated short-term synaptic plasticity in a mouse hippocampal slice model. LEI105 is promising for research of diseases, such as obesity, related metabolic disorders and neuroinflammation .
|
-
- HY-143471
-
|
PLK1/BRD4-IN-1
|
Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
Androgen Receptor
c-Myc
|
Cancer
|
|
WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .
|
-
- HY-155523
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
|
Cancer
|
|
Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with an IC50 of 0.403 μM, 0.591μM, 3.552μM, 0.459μM for HDAC1/2/3/6. Tubulin/HDAC-IN-2 blocks cell cycle arrest at G2 phase, induces cell apoptosis. Tubulin/HDAC-IN-2 inhibits the growth of hematoma and solid tumor cells, reduces tumor metastasis, and also inhibits tumor growth in a liver tumor allograft mouse model .
|
-
- HY-50878AS
-
|
PF-02341066-d9 hydrochloride
|
c-Met/HGFR
Autophagy
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Isotope-Labeled Compounds
|
Cancer
|
|
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-163943
-
|
|
SARS-CoV
PIKfyve
|
Infection
|
|
UNI418 is a dual inhibitor of PIKfyve and PIP5K1C with antiviral activity against SARS-CoV-2 (EC50=1.4 μM). UNI418 blocks ACE2-mediated SARS-CoV-2 viral endocytosis by inhibiting PIP5K1C (IC50=60.1 nM; Kd=61 nM). In addition, UNI418 inhibits the proteolytic activation of proteases regulated by PIKfyve (Kd=0.78 nM) to prevent SARS-CoV-2 from entering host cells .
|
-
- HY-158319
-
|
|
Apoptosis
Isocitrate Dehydrogenase (IDH)
NAMPT
|
Cancer
|
|
Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC50=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively .
|
-
- HY-128879A
-
|
|
Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
|
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
|
-
- HY-128879
-
|
|
Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
|
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
|
-
- HY-112258
-
|
|
DNA/RNA Synthesis
|
Infection
|
|
IMP-1088 is a potent human N-myristoyltransferases NMT1 and NMT2 dual inhibitor with IC50s of <1 nM for HsNMT1 and HsNMT2. IMP-1088 has a Kd of <210 pM for HsNMT1. IMP-1088 efficiently blocks rhinovirus replication by blocking rhinovirus virus-encoded protein (VP0) N-myristoylation. IMP-1088 protects host cells from the cytotoxic effects of viral infection .
|
-
- HY-131447
-
KY19382
1 Publications Verification
A3051
|
GSK-3
Wnt
β-catenin
|
Metabolic Disease
|
|
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases .
|
-
- HY-134581
-
|
M5049
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
|
-
- HY-134581A
-
|
M5049 hydrochloride
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research .
|
-
- HY-10620
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer .
|
-
- HY-146789
-
|
|
PI3K
|
Cancer
|
|
PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies .
|
-
- HY-146491
-
|
|
VEGFR
Raf
Apoptosis
|
Cancer
|
|
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase .
|
-
- HY-146285
-
|
|
Histone Demethylase
Histone Methyltransferase
|
Cancer
|
|
LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
|
-
- HY-151810
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases .
|
-
- HY-106720
-
|
YM 09538
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
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-
- HY-149411
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Inflammation/Immunology
Cancer
|
|
IDO1/TDO-IN-6 (compound 11) is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively. IDO1/TDO-IN-6 has inhibitory effects on IDO1 and TDO, with Ki values of 1.9 and 3.1 μM, respectively. IDO1/TDO-IN-6 can be used in cancer and immunology research .
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-
- HY-156523
-
|
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MAP4K
|
Cancer
|
|
TNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM，respectively，in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition .
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-
- HY-162169
-
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|
Amylases
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-8 (Compound 7p) is a potent dual inhibitor of α-amylase and α-glucosidase, with IC50s of 10.19 and 10.33 μM, respectively. α-Amylase/α-Glucosidase-IN-8 has good anti-oxidant activity(IC50 = 14.93 μM). α-Amylase/α-Glucosidase-IN-8 can be used for the research of diabetes .
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-
- HY-163355
-
|
|
COX
Lipoxygenase
NF-κB
|
Inflammation/Immunology
|
|
COX-2/15-LOX-IN-5 (Compound 4f) is a dual inhibitor of COX-2/15-LOX. COX-2/15-LOX-IN-5 attenuates increased NF-κB activation in RAW 264.7 macrophages mediated by lipopolysaccharide (HY-D1056). COX-2/15-LOX-IN-5 has anti-inflammatory and antioxidant activities .
|
-
- HY-169078
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
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-
- HY-162962
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/TDO-IN-7 (Compound 43b), an isoquinoline derivative, is a potent dual IDO1/TDO inhibitor, with IC50s of 0.31 μM and 0.08 μM, respectively. IDO1/TDO-IN-7 displays acceptable pharmacokinetic profiles and potent antitumor efficacy with low toxicity in B16-F10 tumor model .
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-
- HY-106720A
-
|
YM 09538 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Amosulalol (YM 09538) hydrochloride is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol hydrochloride exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol hydrochloride decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
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-
- HY-167950
-
|
|
Others
|
Metabolic Disease
|
|
PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC50 of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy .
|
-
- HY-146293
-
|
|
HDAC
HSP
|
Cancer
|
|
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
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-
- HY-151201
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase/17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-3 irreversibly inhibits hSTS activity with anIC50 value of 27 nM. Steroid sulfatase/17β-HSD1-IN-3 can be used in the study of endometriosis and other estrogen-dependent diseases .
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-
- HY-151202
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase/17β-HSD1-IN-4 (compound 37) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-4 irreversibly inhibits hSTS activity with anIC50 value of 63 nM. Steroid sulfatase/17β-HSD1-IN-4 can be used in the study of endometriosis and other estrogen-dependent diseases .
|
-
- HY-149269
-
|
|
COX
Carbonic Anhydrase
LOX-1
|
Inflammation/Immunology
|
|
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
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-
- HY-157169
-
|
AMU302
|
Pim
mTOR
Akt
PI3K
|
Cancer
|
|
IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629) .
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-
- HY-163105
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .
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-
- HY-163288
-
|
|
Histone Methyltransferase
HSP
Apoptosis
|
Cancer
|
|
EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB) .
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-
- HY-14243
-
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Anaplastic lymphoma kinase (ALK)
Insulin Receptor
VEGFR
Tie
|
Cancer
|
|
CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC50 value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma .
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-
- HY-147614
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-7 (Compound 19i) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-7 shows 4.7-fold higher potency than the positive control gedatolisib (0.3 vs. 1.4 μM, IC50 values). PI3K/mTOR Inhibitor-7 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-7 has the potential for the research of cancer diseases .
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-
- HY-N10009
-
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NF-κB
TNF Receptor
COX
ERK
p38 MAPK
Sirtuin
|
Inflammation/Immunology
|
|
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
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-
- HY-149250
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with Kis of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity .
|
-
- HY-103160A
-
|
|
Adenosine Deaminase
Phosphodiesterase (PDE)
Influenza Virus
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
|
EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
|
-
- HY-D0976
-
|
|
P2X Receptor
HIV
|
Infection
|
|
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
|
-
- HY-10399
-
|
TV-3326
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-121496
-
|
|
Toll-like Receptor (TLR)
Influenza Virus
|
Infection
Inflammation/Immunology
Cancer
|
|
3M-011 is a potent dual toll-like receptor TLR7/8 agonist and a cytokine inducer. 3M-011 significantly inhibits H3N2 influenza viral replication in the nasal cavity. 3M-011 is also a potent adjuvant to radiotherapy that induces local and profound systemic immune responses during radiotherapy. 3M-011 strongly has antitumor action .
|
-
- HY-144654
-
|
|
HDAC
Topoisomerase
|
Cancer
|
|
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy .
|
-
- HY-143497
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity .
|
-
- HY-144694
-
|
|
HSP
HDAC
Fungal
|
Infection
|
|
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1 .
|
-
- HY-145851
-
|
|
HDAC
Topoisomerase
Apoptosis
|
Cancer
|
|
Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells .
|
-
- HY-151108
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Neurological Disease
Inflammation/Immunology
|
|
IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders .
|
-
- HY-151170
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/ MDM4 inhibitor and p53 activator with the IC50 values of 70.7 nM for MDM2- p53 and 81.4 nM for MDM4-p53 complexes. MDM2/4-p53-IN-2 regulates the cell cycle, induces cell apoptosis and has anticancer activity .
|
-
- HY-151464
-
|
|
SHP2
Phosphatase
HDAC
|
Inflammation/Immunology
Cancer
|
|
SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch .
|
-
- HY-151900
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SARS-CoV-2 Mpro-IN-4 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 900 nM and 60 nM respectively. SARS-CoV-2 Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 8.2 nM .
|
-
- HY-151901
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM .
|
-
- HY-10399A
-
|
TV-3326 hydrochloride
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149630
-
|
|
VEGFR
HDAC
Apoptosis
|
Cancer
|
|
VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC50s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect .
|
-
- HY-161372
-
|
|
PARP
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
|
-
- HY-158328A
-
-
- HY-133095
-
|
|
STAT
PPAR
|
Inflammation/Immunology
|
|
BML-260 is a potent inhibitor of dual-specific phosphatases JSP-1 and DUSP22. BML-260 can activate UCP1 and thermogenesis in adipocytes in a JSP-1-independent manner. The effect of BML-260 on adipocytes is partially achieved through the activation of CREB, STAT3, and PPAR signaling pathways. BML-260 can be used in the research of inflammatory and proliferative disorders associated with JNK signaling dysfunction as well as obesity .
|
-
- HY-162828
-
|
|
STAT
HDAC
|
Cancer
|
|
STAT3/HDAC-IN-2 (compound 18) is a dual inhibitor of STAT3 and HDAC, inducing autophagy and apoptosis. STAT3/HDAC-IN-2 is an amphiphilic hydroxamic acid hybrid based on the natural product isopropanol lactone (IAL) and is a nanoscale anticancer agent. STAT3/HDAC-IN-2 can self-assemble in water to form nanoparticles, which have higher tumor tissue accumulation, cellular uptake and anticancer properties compared to the free state .
|
-
- HY-111164
-
|
|
p38 MAPK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 with anti-inflammatory and anti-allodynic activities. CBS-3595 reduces the production of the proinflammatory cytokine IL-6 and increases the levels of the anti-inflammatory cytokine IL-10 in rats. CBS-3595 reduces paw oedema formation in the Complete Freund’s adjuvant (CFA) (HY-153808)-induced arthritis rat model. CBS-3595 is promising for research of autoimmune diseases .
|
-
- HY-169299
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines .
|
-
- HY-113509S
-
|
LXA4-d5
|
Interleukin Related
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3].
|
-
- HY-108543
-
|
|
Phosphatase
Apoptosis
|
Cancer
|
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)) . NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway .
|
-
- HY-148572
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
NAMPT
|
Cancer
|
|
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel .
|
-
- HY-155965
-
|
|
VEGFR
PARP
Apoptosis
|
Cancer
|
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-155760
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
|
-
- HY-120826
-
|
|
Monoamine Oxidase
Adenosine Receptor
|
Neurological Disease
|
|
A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
|
-
- HY-158138
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
|
-
- HY-159169
-
|
|
COX
Epoxide Hydrolase
Lipoxygenase
|
Inflammation/Immunology
|
|
5-LOX/sEH-IN-1 (Compound 8o) is a dual 5-LOX/sEH-IN-1 inhibitor with cardioprotective effects, exhibiting IC50 values of 3.05 μM and 2.20 nM respectively, and 5-LOX/sEH-IN-1 can also inhibit the activity of COX-2 (IC50=10.50 μM). 5-LOX/sEH-IN-1 has analgesic and anti-inflammatory effects, while reducing ulcer pathogenicity, and can be used to develop anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects .
|
-
- HY-155169
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Others
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Inflammation/Immunology
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hLTA4H/hLTA4S-IN-1 is a possible dual inhibitor that has the activity of inhibiting both human leukotriene hydrolase (hLTA4H) and human leukotriene C4 synthase (hLTC4S). hLTA4H/hLTA4S-IN-1 was identified by computer-assisted methods and is able to effectively interfere with the leukotriene biosynthesis pathway in cells. hLTA4H/hLTA4S-IN-1 can be used to study inflammatory responses .
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- HY-100401A
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CS-505
|
Acyltransferase
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Cardiovascular Disease
|
|
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
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- HY-100401
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CS-505 free base
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Acyltransferase
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Cardiovascular Disease
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Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
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- HY-143494
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RSV
Influenza Virus
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Infection
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|
RSV/IAV-IN-3 (compound 14'i) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza A virus (IAV) with EC50 values of 2.92 µM and 1.90 µM,respectively. RSV/IAV-IN-3 has antiviral effect against H1N1 and H3N2 with EC50 values of 3.25 µM and 1.50 µM in MDCK cells, respectively. RSV/IAV-IN-3 significantly inhibits the activity of luciferase in a dose-dependent manner, with an EC50 of 3.89 µM. RSV/IAV-IN-3 inhibits IAV infectivity and RdRp activity. RSV/IAV-IN-3 inhibits IAV and RSV replication at the post-entry stage .
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- HY-142696
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CDK
Pim
Apoptosis
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Cancer
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CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity .
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- HY-155580
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Monoamine Oxidase
HSP
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Cancer
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MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape [1].
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- HY-10261
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BIBW 2992
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EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
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|
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-10261A
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BIBW 2992MA2
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
|
|
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-100769
-
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YL0919
|
5-HT Receptor
|
Neurological Disease
|
|
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A?receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .
|
-
- HY-124645
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Flavivirus
Dengue virus
Btk
MNK
|
Infection
Cancer
|
|
QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC50s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies .
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- HY-10400
-
|
TV-3326 hemitartrate
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Monoamine Oxidase
Cholinesterase (ChE)
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Neurological Disease
|
|
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease . Ladostigil (hemitartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-10261D
-
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BIBW 2992 oxalate
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EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
|
Cancer
|
|
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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-
- HY-12927
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|
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CXCR
|
Inflammation/Immunology
|
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
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-
- HY-143332
-
|
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Epigenetic Reader Domain
|
Cancer
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|
TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research .
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-
- HY-155727
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Sirtuin
Apoptosis
|
Cancer
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|
Sirt1/2-IN-2 (compound hsa55) is a dual inhibitor of SIRT1/2 with IC50s of 1.8 μM (SIRT1) and 2.4 μM (SIRT2), respsectivley. Sirt1/2-IN-2 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-2 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines .
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- HY-155728
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Sirtuin
Apoptosis
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Cancer
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Sirt1/2-IN-3 (compound PS9) is a dual inhibitor of SIRT1/2 with IC50s of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respsectivley. Sirt1/2-IN-3 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-3 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines .
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-
- HY-161302
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Apoptosis
DNA/RNA Synthesis
PARP
|
Cancer
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|
Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
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-
- HY-169075
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HDAC
CDK
Apoptosis
|
Cancer
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CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
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-
- HY-125876
-
|
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PROTACs
Bcl-2 Family
|
Cancer
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|
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
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- HY-15648F
-
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Histone Demethylase
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Cancer
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GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 .
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-
- HY-155758
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VEGFR
Carbonic Anhydrase
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Cancer
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hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
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-
- HY-155763
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VEGFR
Carbonic Anhydrase
|
Cancer
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|
hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
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-
- HY-156444
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
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-
- HY-162319
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|
|
Apoptosis
HDAC
Microtubule/Tubulin
Reactive Oxygen Species
|
Cancer
|
|
Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity .
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-
- HY-162643
-
|
|
PD-1/PD-L1
PARP
|
Cancer
|
|
Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics .
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-
- HY-158310
-
|
|
EGFR
Ras
|
Cancer
|
|
SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM) .
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-
- HY-156091
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC50 of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT(Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC50=0.17 μM) and has good anti-cancer activity .
|
-
- HY-156798
-
ADS032
1 Publications Verification
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
ADS032 is a dual inhibitor of NLRP1 and NLRP3 that can rapidly, reversibly and stably inhibit inflammasome formation. ADS032 can reduce NLPR1 and NLRP3 activation of human macrophages and bronchial epithelial cells to secrete and mature IL-1β and TNF-α, and reduce NLRP3-induced ASC speck formation. ADS032 protected mice against the deadly influenza A virus, reducing inflammation in the lungs and improving survival. ADS032 inhibits Nigericin (HY-127019)-induced IL-1β secretion with IC50s of 94.6 μM (No wash out) and 354 μM (Wash out) respectively .
|
-
- HY-163434
-
|
|
EGFR
Histone Methyltransferase
|
Cancer
|
|
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
|
-
- HY-162910
-
|
|
Xanthine Oxidase
HDAC
Autophagy
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
HDAC-IN-79 (compound 4) is an orally active dual xanthine oxidase-HDAC inhibitor (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM;), with significant in vivo anti-hyperuricemia and anti-tumor activities. HDAC-IN-79 is the most potent cell growth inhibitor (IC50=0.706 μM) of leukemia HL60 cells, induces apoptosis and autophagy, and can regulate the expression levels of signature biomarkers associated with intracellular HDAC inhibition .
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-
- HY-W023758
-
|
4-(4-Bromo-1H-pyrazol-5-yl)pyridine
|
Others
|
Cancer
|
|
HDGFRP2/PSIP1-IN-1 (compound BPP) is a dual inhibitor targeting the PWWP domain of hepatocarcinogenic growth factor-related protein 2 (HDGFRP2) and its homologous protein PSIP1, hinder the development and progression of diffuse intrinsic pontine glioma (DIPG). HDGFRP2/PSIP1-IN-1 binds to HDGFRP2 with a Kd value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a Kd value of 27 μM; meanwhile, it has a Kd value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .
|
-
- HY-128679
-
|
|
IKK
|
Cancer
|
|
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
|
-
- HY-129453
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
|
-
- HY-143462
-
|
|
HDAC
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
|
-
- HY-146336
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis .
|
-
- HY-151635
-
|
|
PI3K
VEGFR
Apoptosis
|
Cancer
|
|
PI3K/VEGFR2-IN-1 is a potent dual PI3K/VEGFR2 inhibitor with IC50 values of 2.21 and 68 μM for PI3K and VEGFR2, respectively. PI3K/VEGFR2-IN-1 induces apoptosis. PI3K/VEGFR2-IN-1 can be used in research of cancer .
|
-
- HY-149617
-
|
|
Cytochrome P450
PD-1/PD-L1
|
Infection
|
|
CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target (CYP51/PD-L1) inhibitor, with IC50 values of 0.17 and 0.021 μM, respectively. CYP51/PD-L1-IN-4 exhibits excellent antifungal and antidrug-resistant fungal activity in vitro. CYP51/PD-L1-IN-4 can be used for fungal infections research .
|
-
- HY-163116
-
|
|
COX
Carbonic Anhydrase
|
Neurological Disease
Inflammation/Immunology
|
|
Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), and has anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 67 has IC50s of 10.4 μM and 50 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 67 binding to different isoforms of carbonic anhydrase are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII) .
|
-
- HY-163117
-
|
|
COX
Carbonic Anhydrase
|
Neurological Disease
Inflammation/Immunology
|
|
Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), with anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 68 has IC50s of 12.6 μM and 60 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 68 binding to different isoforms of carbonic anhydrase are 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII) .
|
-
- HY-158696
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
BChE/MAO-B-IN-1 (compound 7) is a dual BChE/MAO-B inhibitor with IC50 values of 375 nM and 20 nM, respectively. BChE/MAO-B-IN-1 protects against oxidative damage induced by H2O2 and 6-OHDA in SH-SY5Y cells. BChE/MAO-B-IN-1 can penetrate the central nervous system in a cell model that mimics the blood-brain barrier. BChE/MAO-B-IN-1 can be used in the study of neurological diseases such as Alzheimer's disease (AD) .
|
-
- HY-161667
-
|
|
GSK-3
HDAC
|
Neurological Disease
|
|
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-162606
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases .
|
-
- HY-163786
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
|
-
- HY-155577
-
|
|
Monoamine Oxidase
HSP
|
Cancer
|
|
MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research .
|
-
- HY-15648B
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
|
-
- HY-162772
-
|
|
Isocitrate Dehydrogenase (IDH)
Apoptosis
|
Cancer
|
|
IDH1/2-IN-1 (Compound 6b) serves as a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC50 values of 0.22 μM and 1.6 μM, respectively. IDH1/2-IN-1 effectively inhibits tumor growth by suppressing tumor cell proliferation and enhancing host defense through the activation of antioxidant enzymes. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating robust antitumor activity. IDH1/2-IN-1 holds potential for research in leukemia .
|
-
- HY-130709
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand .
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-
- HY-146276
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
|
-
- HY-152254
-
|
|
FAAH
Cannabinoid Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
|
-
- HY-152253
-
|
|
FAAH
Cannabinoid Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
|
-
- HY-162367
-
|
|
FLT3
Checkpoint Kinase (Chk)
|
Cancer
|
|
FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-159564
-
|
|
COX
NO Synthase
|
Inflammation/Immunology
|
|
iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitory activity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
|
-
- HY-169076
-
|
|
FLT3
HDAC
Apoptosis
|
Cancer
|
FLT3/HDAC-IN-1 is a dual inhibitor of FLT3/HDAC, with IC50 values of 30.4, 52.4, and 14.7 nM for FLT3, HDAC1, and HDAC3, respectively. FLT3/HDAC-IN-1 can induce apoptosis in MV-4-11 cells and has anti-proliferative effects on FLT3 mutant-transformed BaF3 cells. FLT3/HDAC-IN-1 is being researched for its potential in treating hard-to-treat solid tumors and hematological malignancies .
|
-
- HY-149493
-
|
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8 + killing T cells.IHMT-PI3K-455 is used in cancer research .
|
-
- HY-149454
-
|
|
P2Y Receptor
|
Cancer
|
|
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
|
-
- HY-151563A
-
|
|
Deubiquitinase
|
Cancer
|
|
OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
|
-
- HY-159519
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
|
-
- HY-114796
-
|
|
Others
|
Inflammation/Immunology
|
|
tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
|
-
- HY-124322
-
|
|
Beta-secretase
|
Neurological Disease
Inflammation/Immunology
|
|
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
|
-
- HY-135906
-
|
|
Casein Kinase
ERK
Pim
DYRK
Apoptosis
|
Cancer
|
|
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-152146
-
|
|
Apoptosis
FGFR
HDAC
|
Cancer
|
|
HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity .
|
-
- HY-10261E
-
|
(R)-BIBW 2992
|
EGFR
c-Met/HGFR
p38 MAPK
|
Cancer
|
|
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-155066
-
|
|
PI3K
mTOR
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
|
-
- HY-157295
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC50 values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .
|
-
- HY-118264
-
|
|
Angiotensin-converting Enzyme (ACE)
Neprilysin
|
Cardiovascular Disease
|
|
MDL-100240 is a dual-acting angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) inhibitor. MDL-100240 can significantly lower blood pressure, reverse left ventricular hypertrophy, and effectively prevent hypertrophy and dilatation of the aorta and resistance arteries, with an effect comparable to that of ramipril (HY-B0279). In addition, MDL-100240 can also reduce aldosterone levels, but has no significant effect on atrial natriuretic peptide and cGMP. In 3-month-old transgenic rats, MDL-100240 can reduce adrenomedullin concentrations, prevent and reverse severe hypertension and cardiovascular damage, and enhance bradykinin effects.
|
-
- HY-148862
-
|
|
Calcium Channel
Monoamine Transporter
|
Inflammation/Immunology
|
|
Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain .
|
-
- HY-148863
-
|
|
Calcium Channel
Monoamine Transporter
|
Inflammation/Immunology
|
|
Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain .
|
-
- HY-117049
-
|
|
CDK
DYRK
|
Neurological Disease
|
|
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively) . Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model .
|
-
- HY-146749
-
|
|
FLT3
Trk Receptor
Apoptosis
|
Cancer
|
|
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
|
-
- HY-151364
-
|
|
HDAC
|
Cancer
|
|
HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
|
-
- HY-121465
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Stearoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is a dual antagonist of fatty acid amide hydrolase (FAAH) and the transient receptor potential vanilloid-type 1 (TRPV1) channel, reducing both acute and chronic peripheral pain. The effects of replacing the arachidonoyl portion with the saturated 18-carbon stearoyl moiety have not been studied. However, replacement of arachidonate with saturated 11- or 12-carbon fatty acids produces compounds that potently inhibit capsaicin-induced TRPV1 channel activation (IC50=0.76 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC50 > 50 μM).
|
-
- HY-146295
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2/5-LOX-IN-2 (5b) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-2 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-2 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 5.40, 0.01 and 1.78 μM, respectively .
|
-
- HY-146294
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2/5-LOX-IN-1 (compound 3a) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-1 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-1 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 12.13, 0.4 and 4.96 μM, respectively .
|
-
- HY-150609
-
|
|
SHP2
Phosphatase
CDK
|
Cancer
|
|
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-149209
-
|
|
PROTACs
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
|
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
|
-
- HY-150537
-
|
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
|
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-104042
-
|
AG-881
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
|
-
- HY-101034
-
|
CHMFL-ABL-KIT-155
|
Bcr-Abl
c-Kit
Apoptosis
PDGFR
Discoidin Domain Receptor
|
Cancer
|
|
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
|
-
- HY-11080
-
PKI-179
1 Publications Verification
|
PI3K
mTOR
|
Cancer
|
|
PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo .
|
-
- HY-11080A
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo .
|
-
- HY-143885
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells .
|
-
- HY-147825
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
|
-
- HY-156150
-
|
|
Fungal
Cytochrome P450
PD-1/PD-L1
|
Infection
|
|
CYP51/PD-L1-IN-2 (compound L20) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-2 is a dual inhibitor of CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.017 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-2 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
|
-
- HY-156151
-
|
|
Fungal
Cytochrome P450
PD-1/PD-L1
|
Infection
|
|
CYP51/PD-L1-IN-3 (compound L21) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-3 is a dual inhibitor of CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-3 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
|
-
- HY-156149
-
|
|
Fungal
Cytochrome P450
PD-1/PD-L1
|
Infection
|
|
CYP51/PD-L1-IN-1 (compound L11) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-1 is a dual inhibitor of CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-1 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
|
-
- HY-149254
-
|
|
Phosphatase
Aldose Reductase
|
Metabolic Disease
|
|
PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC50 value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels .
|
-
- HY-159510
-
|
|
Apoptosis
VEGFR
Microtubule/Tubulin
Reactive Oxygen Species
|
Cancer
|
|
VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) with anti-tumor activity. VEGFR-2-IN-51 induces tumor cell apoptosis by reducing mitochondrial membrane potential and increasing reactive oxygen species (ROS) levels. VEGFR-2-IN-51 exerts anti-angiogenic effects by blocking the VEGFR-2/PI3K/AKT signaling pathway. In addition, VEGFR-2-IN-51 has significant anti-proliferative activity against the gastric cancer cell line MGC-803 (IC50=0.005 μM) .
|
-
- HY-164445
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
|
-
- HY-146159
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects .
|
-
- HY-149255
-
|
|
Phosphatase
Aldose Reductase
|
Metabolic Disease
|
|
PTP1B/AKR1B1-IN-2 (Compound 7f) is a dual PTP1B/AKR1B1 inhibitor (IC50s: 3.2 and 2.1 μM, Kis: 4.0 and 0.9μM). PTP1B/AKR1B1-IN-2 is an insulin-mimetic agent. PTP1B/AKR1B1-IN-2 improves glucose uptake in murine C2C12 myoblasts. PTP1B/AKR1B1-IN-2 can be used for research of Type 2 diabetes mellitus (T2DM) .
|
-
- HY-P10302A
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
|
-
- HY-161995
-
|
|
Apoptosis
Necroptosis
FGFR
VEGFR
PDGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
|
-
- HY-163679
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
|
-
- HY-117947
-
|
|
Others
|
Cancer
|
|
(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
|
-
- HY-121562
-
|
|
Others
|
Neurological Disease
|
|
SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.
|
-
- HY-162812
-
|
|
Apoptosis
Cholinesterase (ChE)
Tau Protein
Ferroptosis
Histamine Receptor
|
Neurological Disease
|
|
H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D0086
-
|
MDL101114ZA
|
Dyes
|
|
DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0090
-
|
Salmon calcitonin
|
CGRP Receptor
|
Cancer
|
|
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
|
-
- HY-P0025
-
NIM811
Maximum Cited Publications
12 Publications Verification
(Melle-4)cyclosporin; SDZ NIM811
|
Cyclophilin
Mitochondrial Metabolism
HCV
|
Infection
Inflammation/Immunology
|
|
NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is an orally bioavailable mitochondrial permeability transition and cyclophilin dual inhibitor, which exhibits potent in vitro activity against hepatitis C virus (HCV) .
|
-
- HY-P0090S
-
|
Salmon calcitonin-13C6,15N4 TFA
|
CGRP Receptor
|
Metabolic Disease
|
|
Calcitonin- 13CIC6, 15NIC4 (salmon) (Salmon calcitonin- 13CIC6, 15NIC4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
|
-
- HY-P10221A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CKLIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 2.6 and 2.2 μM, respectively .
|
-
- HY-P10302A
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GLP-1R/GIPR agonist-1 soduim is the sodium salt form of GLP-1R/GIPR agonist-1 (HY-P10302). GLP-1R/GIPR agonist-1 soduim is a dual agonist for glucagon-like peptide-1 receptor (GLP-1R, EC50 is 0.57 nM) and glucose-dependent insulin releasing peptide receptor (GIPR, EC50 is 0.75 nM). GLP-1R/GIPR agonist-1 soduim lowers blood sugar by mimicking the action of endogenous hormones GLP-1 and GIP, enhancing insulin secretion while inhibiting glucagon secretion. GLP-1R/GIPR agonist-1 soduim can be used in the study of metabolic diseases such as diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
|
-
- HY-P0090A
-
|
Salmon calcitonin acetate
|
CGRP Receptor
|
Cancer
|
|
Calcitonin (salmon) (acetate) is a dual-action amylin and calcitonin receptor agonist, can stimulate bone formation and inhibit bone resorption .The acetate form can affect the absorption and efficacy of hormones .
|
-
- HY-141584
-
|
|
MDM-2/p53
|
Cancer
|
|
ATSP-7041, a selective dual peptide inhibitor of MDM2 and MDMX, effectively reactivates the p53 tumor suppressor pathway in a mechanism-dependent manner in p53-positive cancers .
|
-
- HY-P10223
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 65 and 123 μM, respectively .
|
-
- HY-P10222
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 14.5 and 10.2 μM, respectively .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99166
-
|
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
Cancer
|
|
Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
|
-
- HY-P99568
-
|
RC18
|
Inhibitory Antibodies
|
Inflammation/Immunology
|
|
Telitacicept (RC18) is a fully human TACI-Fc fusion protein. Telitacicept is a dual B lymphocyte stimulator (BLyS)/APRIL (a proliferation-inducing ligand) inhibitor that effectively blocks proliferation of B lymphocytes. Telitacicept can be used in research of B-cell autoimmune disease .
|
-
- HY-P99721
-
|
ABT-981
|
Interleukin Related
|
Inflammation/Immunology
|
|
Lutikizumab (ABT-981) is an anti-IL-1α and IL-1β dual variable domain immunoglobulin. Lutikizumab binds and inhibits IL-1α and IL-1β. Lutikizumab can be used for the research of osteoarthritis .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10181S
-
|
|
|
Dasatinib-d8 is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.
|
-
-
- HY-B0196S
-
|
|
|
Venlafaxine-d6 is the deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
|
-
-
- HY-B0196AS1
-
|
|
|
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
|
-
-
- HY-B0703S
-
|
|
|
Eslicarbazepine acetate-d4 is deuterated labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
|
-
-
- HY-10158S
-
|
|
|
Bosutinib-d8 is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively[1][2].
|
-
-
- HY-133794S
-
|
|
|
Dasatinib N-oxide-d8 is the deuterium labeled Dasatinib N-oxide. Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor[1][2].
|
-
-
- HY-B0196AS
-
|
|
|
Venlafaxine-d10 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine (Wy 45030) hydrochloride is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1][2].
|
-
-
- HY-B0196S1
-
|
|
|
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
|
-
-
- HY-169222S
-
|
|
|
RORγ/DHODH-IN-2 (Compound 1311) is an orally active dual inhibitor of RORγ/DHODH with IC50 values of 11.9 nM and 90 nM, respectively. RORγ/DHODH-IN-2 exhibits antiviral activity by inhibiting the activity of SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC50 values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively .
|
-
-
- HY-169220S
-
|
|
|
RORγ/DHODH-IN-1 (compound 1404), a deuterium labeled compound, is a dual RORγ and DHODH inhibitor with IC50 values of 9.7 nM and 100 nM, repaectively. RORγ/DHODH-IN-1 blocks the replication of SARS-CoV-2, HCMV, and non-enveloped DNA virus (HAdV5) .
|
-
-
- HY-148233S
-
|
|
|
JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure[1][2].
|
-
-
- HY-P0090S
-
|
|
|
Calcitonin- 13CIC6, 15NIC4 (salmon) (Salmon calcitonin- 13CIC6, 15NIC4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
|
-
-
- HY-B1452S1
-
|
|
|
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
|
-
-
- HY-50878AS
-
|
|
|
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
-
- HY-113509S
-
|
|
|
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-10399A
-
|
TV-3326 hydrochloride
|
|
Alkynes
|
|
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10400
-
|
TV-3326 hemitartrate
|
|
Alkynes
|
|
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease . Ladostigil (hemitartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-159129
-
|
|
|
Azide
|
|
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsin B, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
|
-
- HY-169098
-
|
|
|
Alkynes
|
|
HSP90/LSD1-IN-1 (compound 6) is a HSP90/LSD1 dual inhibitor. HSP90/LSD1-IN-1 inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 and 0.30 μM, respectively .
|
-
- HY-164309
-
|
|
|
DBCO
|
|
DBCO-PEG3-Glu-Val-Cit-PABC-MMAE is a drug-linker conjugate for ADC. DBCO-PEG3-Glu-Val-Cit-PABC-MMAE contains a potent tubulin inhibitor Monomethyl auristatin E (MMAE, HY-15162) and can be used for synthesis of dual-drug ADC .
|
-
- HY-142706
-
|
|
|
Alkynes
|
|
MAO A/HDAC-IN-1 is a dual?inhibitor?of monoamine oxidase A (MAO A) and HDAC. MAO A/HDAC-IN-1 can be used for glioma research . MAO A/HDAC-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10399
-
|
TV-3326
|
|
Alkynes
|
|
Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-159169
-
|
|
|
Azide
|
|
5-LOX/sEH-IN-1 (Compound 8o) is a dual 5-LOX/sEH-IN-1 inhibitor with cardioprotective effects, exhibiting IC50 values of 3.05 μM and 2.20 nM respectively, and 5-LOX/sEH-IN-1 can also inhibit the activity of COX-2 (IC50=10.50 μM). 5-LOX/sEH-IN-1 has analgesic and anti-inflammatory effects, while reducing ulcer pathogenicity, and can be used to develop anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects .
|
-
- HY-159564
-
|
|
|
Azide
|
|
iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitory activity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
|
-
- HY-159519
-
|
|
|
Azide
|
|
EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-113289
-
|
|
|
Cholesterol
|
|
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
|
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