Search Result
Results for "
Activator Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1412
Inhibitors & Agonists
2
Biochemical Assay Reagents
89
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-122098
-
PAI-749
|
PAI-1
|
Cardiovascular Disease
|
Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nM. Diaplasinin has antithrombotic efficacy.
|
-
- HY-149725
-
|
MMP
|
Neurological Disease
|
proMMP-9 selective inhibitor-1 (compound 33) is a highly potent and selective inhibitor of proMMP-9 activation.
|
-
- HY-N1330
-
-
- HY-N11924
-
|
PPAR
AMPK
|
Metabolic Disease
|
Foenumoside B is a triterpene saponin isolated from Lysimachia foenum-graecum. Foenumoside B activates AMPK signaling, inhibits PPARγ-induced adipogenesis, and shifts lipid metabolism toward lipolysis. Foenumoside B can be used in the study of obesity and obesity-related metabolic diseases.
|
-
- HY-N10227
-
-
- HY-P5786
-
-
- HY-156574
-
|
DGK
|
Cancer
|
DGKζ-IN-4 is a DGK-zeta inhibitor. DGKζ-IN-4 can be used as an active component of pharmaceutical compositions. DGKζ-IN-4 is used to treat cancers associated with immune cell activation or cancers resistant to anti-PD-1 antibody/anti-PD-11 antibody treatment.
|
-
- HY-N10754
-
|
Cytochrome P450
mTOR
|
Cancer
Infection
Cardiovascular Disease
|
Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca 2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme.
|
-
- HY-113492
-
-
- HY-117724
-
|
PAI-1
|
Cardiovascular Disease
|
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay.
|
-
- HY-120035
-
|
Proteasome
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation.
|
-
- HY-142163
-
|
Others
|
Cardiovascular Disease
|
S62798 is a selective and potent inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) with an IC50 value of 6 mM.
|
-
- HY-148480
-
|
Keap1-Nrf2
|
Cardiovascular Disease
|
Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4).
|
-
- HY-108356
-
|
Apoptosis
|
Cancer
|
NS3694, a diarylurea compound, is an apoptosome inhibitor. NS3694 inhibits apoptosome formation and caspase activation.
|
-
- HY-156081
-
|
Apoptosis
Keap1-Nrf2
|
Metabolic Disease
|
Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis.
|
-
- HY-N10782
-
-
- HY-121667
-
|
ROCK
|
Cancer
|
Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation.
|
-
- HY-N0277
-
-
- HY-N3425
-
|
AMPK
|
Others
|
Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation.
|
-
- HY-154973
-
|
Mitochondrial Metabolism
AMPK
|
Cancer
Metabolic Disease
|
AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research.
|
-
- HY-155363
-
|
AMPK
|
Metabolic Disease
|
AMPK activator 13 is a potent activator of AMPK. AMPK activator 13 inhibits mitotic clonal expansion of 3T3-L1 cells by activating AMPK pathway and enhances cell mitochondrial oxygen consumption rate. AMPK activator 13 can be used in study obesity.
|
-
- HY-156375
-
|
PDK-1
Pyruvate Kinase
|
Cancer
|
PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM).
|
-
- HY-17032A
-
YM-08054
|
5-HT Receptor
|
Neurological Disease
|
Indeloxazine hydrochloride is a 5-HT receptor and norepinephrine (NE) reuptake inhibitor. Indeloxazine hydrochloride is an antidepressant and cerebral activator.
|
-
- HY-114304
-
COH000
1 Publications Verification
|
E1/E2/E3 Enzyme
|
Cancer
|
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
|
-
- HY-14754
-
S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
|
Ras
Autophagy
|
Cancer
|
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
|
-
- HY-107753
-
|
Ras
|
Cancer
Inflammation/Immunology
|
XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules.
|
-
- HY-145879
-
|
Keap1-Nrf2
|
Cancer
|
Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells.
|
-
- HY-N7563
-
|
EBV
|
Cancer
Infection
|
α-Toxicarol is a potent inhibitor of EBV.α-Toxicarol significantly inhibits mouse skin tumor in vivo. α-Toxicarol inhibits the TPA-induced EBV-EA activation.
|
-
- HY-130789
-
|
EBV
|
Infection
|
Cimigenol-3-one inhibits Epstein-Barr virus early antigen (EBV-EA) activation.
|
-
- HY-135825
-
|
Autophagy
|
Neurological Disease
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
|
-
- HY-N3254
-
Murpanidin; (+)-Murpanidin
|
HSV
|
Infection
|
Minumicrolin is a plant growth inhibitor. Minumicrolin can be isolated from Murraya paniculata. Minumicrolin inhibits Epstein-Barr virus early antigen (EBV-EA) activation.
|
-
- HY-101112
-
|
Others
|
Inflammation/Immunology
|
Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cell activation.
|
-
- HY-19635A
-
|
PAK
|
Cancer
|
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
|
-
- HY-18723
-
|
Piezo Channel
Akt
ERK
Potassium Channel
|
Cardiovascular Disease
|
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
|
-
- HY-112956
-
|
Others
|
Inflammation/Immunology
|
Drotrecogin alfa activated (DrotAA) is recombinant human activated protein C (APC). Drotrecogin alfa activated prevents smoke-induced increases in pulmonary microvascular permeability and proinflammatory cytokine IL-1β in rats. Drotrecogin alfa activated inhibits coagulation and inflammation and promotes fibrinolysis. Drotrecogin alfa activated can be used for severe sepsis reaearch.
|
-
- HY-136172
-
|
Ras
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
|
-
- HY-148553
-
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 36 is an anti-inflammatory agent. Anti-inflammatory agent 36 inhibits LPS-induced macrophage activation.
|
-
- HY-N4231
-
|
NF-κB
|
Inflammation/Immunology
|
Lucyoside B inhibits the production of inflammatory mediators via both NF-κB and activator protein-1 pathways in activated macrophages.
|
-
- HY-15336
-
Tyrphostin AG 555
|
EGFR
Reverse Transcriptase
|
Cancer
|
AG 555 (Tyrphostin AG 555), a potent antiretroviral agent, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
|
-
- HY-10484
-
MLN4924 hydrochloride
|
NEDD8-activating Enzyme
|
Cancer
|
Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM.
|
-
- HY-70062
-
MLN4924
|
NEDD8-activating Enzyme
|
Cancer
|
Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM.
|
-
- HY-15723A
-
-
- HY-P2271
-
|
Apelin Receptor (APJ)
|
Cancer
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation.
|
-
- HY-134975
-
|
c-Myc
|
Cancer
|
NY2267 is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM. NY2267 inhibits Myc- and Jun-induced transcriptional activation.
|
-
- HY-N1380
-
-
- HY-101047
-
Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
|
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
|
-
- HY-B0167
-
-
- HY-15542A
-
FRAX597
5 Publications Verification
|
PAK
|
Cancer
|
FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
|
-
- HY-12364
-
|
Fatty Acid Synthase (FASN)
|
Cancer
|
C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator.
|
-
- HY-121896
-
|
SHP2
|
Cancer
|
DSHN is a potent small heterodimer partner (SHP) activator. DSHN inhibits Ccl2 expression and secretion by inhibiting p65 activation of Ccl2 promoter activity. DSHN can be used in research of cancer.
|
-
- HY-110367A
-
|
Src
|
Others
|
LCB 03-0110, a thienopyridine derivative, is a potent pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor. LCB 03-0110 suppresses scar formation by inhibiting fibroblast and macrophage activation.
|
-
- HY-100472
-
|
Caspase
|
Cancer
|
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.
|
-
- HY-101796
-
|
Others
|
Cancer
|
NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect.
|
-
- HY-10249
-
|
Akt
AMPK
Autophagy
|
Cancer
|
GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
|
-
- HY-N8617
-
|
Caspase
|
Cancer
|
Trijuganone C, a natural product extracted from Salvia miltiorrhiza, inhibits the proliferation of cancer cells through induction of apoptosis mediated by mitochondrial dysfunction and caspase activation.
|
-
- HY-15027
-
-
- HY-P1376
-
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-N10458
-
|
NF-κB
|
Inflammation/Immunology
|
Asperbisabolane L, a sesquiterpenoid, exerts the anti-inflammatory activity by inhibiting the NF-κB-activated pathway. Asperbisabolane L inhibits the translocation of NF-κB from cytoplasm to the nucleus. Asperbisabolane L also inhibits NO production in LPS-activated BV-2 microglia cells.
|
-
- HY-14452
-
125B11
|
Fatty Acid Synthase (FASN)
|
Cancer
|
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-15870
-
|
AP-1
|
Cancer
Inflammation/Immunology
|
SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).
|
-
- HY-15542B
-
|
PAK
|
Cancer
|
FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
|
-
- HY-N4182
-
|
Akt
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
|
-
- HY-19635
-
G-5555
5 Publications Verification
|
PAK
|
Cancer
|
G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
|
-
- HY-W006230
-
|
Others
|
Cancer
|
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
|
-
- HY-10255A
-
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-N6688
-
|
Potassium Channel
Bacterial
Antibiotic
|
Infection
|
Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
|
-
- HY-P3452
-
|
Tyrosinase
|
Inflammation/Immunology
|
Tetrapeptide-30 is a skin-brightening peptide consisting of four amino acids. Tetrapeptide-30 can act as a tyrosinase inhibitor, lightening hyperpigmentation and evening out skin tone by reducing the amount of tyrosinase and inhibiting melanocyte activation.
|
-
- HY-B0289
-
-
- HY-N10445
-
|
CD3
CD28
|
Inflammation/Immunology
|
Maydispenoid A is a potent immunosuppressor. Maydispenoid A can inhibit anti-CD3/anti-CD28 mAbs activated and lipopolysaccharide activated murine splenocyte proliferation.
|
-
- HY-13764
-
-
- HY-110105
-
|
Potassium Channel
|
Neurological Disease
|
NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
|
-
- HY-101918
-
|
Others
|
Cardiovascular Disease
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-N0896
-
1-O-Acetylbritannilactone
|
NF-κB
COX
|
Cancer
Inflammation/Immunology
|
Inulicin (1-O-Acetylbritannilactone) is an active compound that inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
|
-
- HY-12372
-
|
IAP
Caspase
|
Cancer
|
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation.
|
-
- HY-N5101
-
-
- HY-133987
-
|
NF-κB
|
Inflammation/Immunology
|
AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
|
-
- HY-B1197
-
-
- HY-10255
-
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-14452A
-
125B11 hydrobromide
|
Fatty Acid Synthase (FASN)
|
Cancer
|
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-135388
-
ent-SCH 58235
|
Drug Metabolite
|
Cardiovascular Disease
|
ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-N3464
-
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity.
|
-
- HY-19706
-
ARS-853
2 Publications Verification
|
Ras
Apoptosis
|
Cancer
|
ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
|
-
- HY-136059
-
|
Keap1-Nrf2
Autophagy
|
Cancer
Cardiovascular Disease
|
Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-P1260
-
-
- HY-148712
-
|
Apoptosis
Sirtuin
|
Cancer
|
SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 μM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity.
|
-
- HY-18749
-
-
- HY-N10446
-
|
CD3
CD28
|
Inflammation/Immunology
|
Maydispenoid B is a potent immunosuppressor. Maydispenoid B can inhibit anti-CD3/anti-CD28 mAbs activated and lipopolysaccharide activated murine splenocyte proliferation.
|
-
- HY-B0167S
-
-
- HY-103666
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.
|
-
- HY-10255AS
-
SU 11248-d10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-B0167A
-
-
- HY-100602
-
HJC0152
1 Publications Verification
|
STAT
Apoptosis
|
Cancer
|
HJC0152 is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
|
-
- HY-U00434
-
-
- HY-N0441
-
-
- HY-101214
-
-
- HY-13626
-
ES-285
|
PKC
|
Cancer
|
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation.
|
-
- HY-153675
-
|
PIN1
|
Metabolic Disease
|
BCPA is a Pin1 regulator without cytotoxicity. BCPA attenuates the reduction of Pin1 protein to inhibit receptor activator of RANKL-induced osteoclastogenesis. BCPA regulates osteoclast activation, used to osteoporosis research.
|
-
- HY-N9239
-
|
Others
|
Others
|
Turmeronol A is a sesquiterpenoid compound.
Turmeronol A has anti-inflammatory activity. Turmeronol A prevents macrophage
activation and the production of inflammatory mediators by inhibiting the
activation of NFκB. Turmeronol A can be used to prevent chronic inflammatory
diseases .
|
-
- HY-N9297
-
(+)-Oxyphyllenone A
|
NO Synthase
|
Inflammation/Immunology
|
Oxyphyllenone A is an inhibitor of NO Synthase. Oxyphyllenone A inhibits the NO production in lipopolysaccharide-activated macrophages with an IC50 of 28 μM.
|
-
- HY-P1260A
-
-
- HY-143510
-
|
mTOR
|
Cancer
|
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
|
-
- HY-18965
-
|
PKC
|
Cardiovascular Disease
|
TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
|
-
- HY-12364B
-
|
Fatty Acid Synthase (FASN)
|
Cancer
|
(−)-C75 is a isoform of C75 (HY-12364), which is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator.
|
-
- HY-139667
-
|
Pyruvate Kinase
|
Neurological Disease
|
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
|
-
- HY-P99371
-
AK002; Anti-Siglec-8 Reference Antibody (lirentelimab)
|
Apoptosis
|
Inflammation/Immunology
|
Lirentelimab (AK002) is a humanized IgG1 monoclonal antibody that targets sialic acid-binding Ig-like lectin 8 (SIGLEC8). Lirentelimab induces cell apoptosis of IL-5-activated eosinophils and inhibits IgE-mediated mast cell activation. Lirentelimab can be used for the research of eosinophilic gastritis and duodenitis.
|
-
- HY-W015445
-
|
p38 MAPK
|
Metabolic Disease
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-W067427
-
|
IKK
|
Cancer
|
BAY32-5915 is a potent IKKα inhibitor with an IC50 value of 60 nM. BAY32-5915 has not affect Doxorubicin (HY-15142A)-induced NF-κB activation.
|
-
- HY-118131
-
|
Ser/Thr Protease
|
Infection
|
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages.
|
-
- HY-B0069
-
F-ara-A; NSC 118218
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
STAT
Apoptosis
|
Cancer
|
Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.
|
-
- HY-10255AS1
-
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-N3054
-
-
- HY-15300
-
-
- HY-101047S
-
Erythrosphingosine-d7; erythro-C18-Sphingosine-d7; trans-4-Sphingenine-d7
|
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].
|
-
- HY-N1380S
-
-
- HY-P0190A
-
|
Potassium Channel
|
Others
|
Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels.
|
-
- HY-N6258
-
|
AMPK
Apoptosis
|
Metabolic Disease
|
Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
|
-
- HY-10162
-
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
|
-
- HY-N1380S3
-
-
- HY-108599
-
DCP-LA
2 Publications Verification
FR236924
|
PKC
CaMK
Phosphatase
Apoptosis
|
Neurological Disease
|
DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca( 2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis.
|
-
- HY-136427
-
|
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
|
-
- HY-N1380S4
-
-
- HY-N1380S2
-
-
- HY-148189
-
LXY-05-029
|
AMPK
|
Metabolic Disease
|
Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis.
|
-
- HY-122082
-
|
Others
|
Inflammation/Immunology
|
Methopterin inhibits osteoclasts proliferation. Methopterin inhibits the activation and bone resorption function of osteoclasts, and induced osteoclasts apoptosis.
|
-
- HY-100447
-
-
- HY-139858
-
-
- HY-128642
-
|
FAP
|
Cancer
|
FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
|
-
- HY-141432
-
|
E1/E2/E3 Enzyme
|
Cancer
|
Cbl-b-IN-3 (Compound 23) is a casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 of < 1 nM. Cbl-b is an E3 ubiquitin ligase that negatively regulates T-cell activation.
|
-
- HY-B0099S
-
MCI-186-d5
|
MMP
Apoptosis
|
Neurological Disease
|
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
|
-
- HY-139553
-
ATI-450; CDD-450
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.
|
-
- HY-16592
-
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
Bacterial
|
Cancer
Infection
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-15253
-
PAI-039; Tiplasinin
|
PAI-1
Apoptosis
|
Metabolic Disease
Cancer
|
Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
|
-
- HY-116626
-
|
NF-κB
p38 MAPK
MMP
|
Cancer
|
SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
|
-
- HY-N3807
-
|
Acyltransferase
ERK
NF-κB
|
Cancer
Infection
Cardiovascular Disease
|
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
|
-
- HY-112473
-
|
Others
|
Cancer
|
NAV-2729 is a dual Arf1/Arf6 activation inhibitor.
|
-
- HY-105198
-
-
- HY-15840
-
C24
|
AMPK
|
Cancer
|
YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
|
-
- HY-N8041
-
|
HSV
|
Infection
|
Mogroside III A2 is a cucurbitane glycoside. Mogroside III A2 can inhibit Epstein-Barr virus early antigen (EBV-EA) activation. Mogroside III A2 shows weak inhibitory effects on activation of NOR 1.
|
-
- HY-148853
-
|
Interleukin Related
|
Others
|
SRI-42127 is a HuR translocation inhibitor. HuR is an RNA regulator that binds to AREs, and HuR translocations promote the production of inflammatory cytokines in glial cells. However, SRI-42127 can destroy mRNA stability and inhibit gene promoter activation. SRI-42127 also inhibits microglial cell activation and attenuates recruitment/chemotaxis of neutrophils and monocytes.
|
-
- HY-15002
-
AST 487
4 Publications Verification
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-B0289S
-
-
- HY-129390
-
ICP-022
|
Btk
|
Cancer
|
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
|
-
- HY-153098
-
-
- HY-N1260
-
(-)-Scutebarbatine A
|
Apoptosis
|
Cancer
|
Scutebarbatine A inhibits the proliferation of HCC cells and triggers their apoptosis via the activation of MAPK and ER stress.
|
-
- HY-U00458
-
TX-803
|
Akt
|
Cancer
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-15252
-
-
- HY-P99166
-
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
|
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-131265
-
|
PPAR
PAK
NF-κB
|
Cancer
Inflammation/Immunology
|
Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
|
-
- HY-10162S1
-
AZD2281-d8; KU0059436-d8
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-15027S
-
Mesalamine-d3 (hydrochloride); 5-ASA-d3 (hydrochloride); Mesalazine-d3 (hydrochloride)
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
5-Aminosalicylic Acid-d3 (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
|
-
- HY-128403
-
|
Btk
|
Inflammation/Immunology
|
BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM.
|
-
- HY-12357
-
-
- HY-127041
-
|
Others
|
Infection
|
Virstatin inhibits the pili system synthesis and prevents A. baumannii biofilm formation. Virstatin also inhibits dimerization of the transcriptional activator ToxT.
|
-
- HY-N0822
-
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
AIM2
|
Cancer
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-137888A
-
oATP trisodium salt
|
P2X Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis.
|
-
- 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-P0190
-
|
Potassium Channel
|
Cardiovascular Disease
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
|
-
- HY-148174
-
|
DGK
|
Cancer
|
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation.
|
-
- HY-P1026
-
-
- HY-116278
-
|
STAT
|
Cancer
|
HJC0149 is a potent and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3).
|
-
- HY-101790
-
-
- HY-128642A
-
|
FAP
|
Cancer
|
FAPI-2 TFA is a fibroblast activation protein (FAP) inhibitor with potential use in cancer research.
|
-
- HY-N0897
-
Corylifol-A; Corylinin
|
STAT
|
Others
|
Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
|
-
- HY-152860
-
|
p38 MAPK
|
Cancer
|
Darizmetinib is an inhibitor of mitogen-activated protein kinase kinase (MAP2K).
|
-
- HY-15530
-
-
- HY-50703
-
MK-2461
1 Publications Verification
|
c-Met/HGFR
|
Cancer
|
MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
|
-
- HY-155182
-
|
Autophagy
HDAC
|
Inflammation/Immunology
Neurological Disease
|
HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain.
|
-
- HY-N3552
-
|
NF-κB
|
Inflammation/Immunology
|
Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages.
|
-
- HY-103697
-
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-P4243
-
|
Ser/Thr Protease
|
Others
|
Dansyl-Glu-Gly-Arg-Chloromethylketone is a protease inhibitor, and inhibits serine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone inhibits activated porcine factor IX.
|
-
- HY-P5146
-
-
- HY-142125
-
|
Xanthine Oxidase
Reactive Oxygen Species
Apoptosis
|
Cancer
Inflammation/Immunology
|
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways.
|
-
- HY-B1546
-
Benzylamiloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-B1546A
-
Benzylamiloride hydrochloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-B0111
-
Dihydrospirorenone
|
Progesterone Receptor
Androgen Receptor
|
Cancer
Endocrinology
|
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
|
-
- HY-107460
-
|
Ephrin Receptor
|
Cancer
|
LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC.
|
-
- HY-149555
-
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
DNL343 is a brain-penetrating activator of eukaryotic initiation factor 2B (eIF2B) that inhibits the abnormal integrated stress response (ISR). DNL343 inhibits ISR activity in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 has inhibitory potential in studies of vanishing white matter disease (VWMD) driven by eIF2B LOF and chronic ISR activation.
|
-
- HY-111673
-
8-CPT-cAMP sodium; 8-(p-Chlorophenylthio)-cAMP sodium
|
PKA
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator.
|
-
- HY-153128
-
|
DOCK
|
Inflammation/Immunology
|
DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC50=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation.
|
-
- HY-122714
-
|
PAI-1
|
Cancer
|
SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma.
|
-
- HY-Z0816
-
|
Calcium Channel
|
Others
|
Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders.
|
-
- HY-19356
-
Roc-A
|
NF-κB
HSP
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
|
-
- HY-10162S3
-
AZD2281-d4-1; KU0059436-d4-1
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-P99274
-
BI 836845; Anti-Human IGF1 and IGF2 Recombinant Antibody
|
IGF-1R
|
Cancer
|
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a humanized monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation.
|
-
- HY-14266
-
TMC120; R147681
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
|
-
- HY-N0516
-
Vitexicarpin
|
STAT
|
Inflammation/Immunology
|
Casticin is a methyoxylated flavonol isolated from Vitex rotundifolia, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
|
-
- HY-10590
-
-
- HY-14645A
-
(1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ
|
Keap1-Nrf2
|
Inflammation/Immunology
|
(+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
|
-
- HY-153671
-
|
Others
|
Infection
|
4'-Methyl-β-naphthoflavone is a metabolite of Naphthoflavones (benzoflavones) in fungal. Naphthoflavones are activators or inhibitors of CYP-450.
|
-
- HY-112125A
-
-
- HY-139401
-
|
FAP
|
Cancer
|
FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).
|
-
- HY-123399
-
-
- HY-16511
-
WX-671
|
Ser/Thr Protease
PAI-1
|
Cancer
|
Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
|
-
- HY-50714
-
MK-591 sodium
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
|
-
- HY-100965
-
-
- HY-131958
-
|
AMPK
|
Cancer
|
D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth.
|
-
- HY-101180
-
Ceramide 2
|
Phosphatase
Mitochondrial Metabolism
Apoptosis
Autophagy
|
Endocrinology
Metabolic Disease
|
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation, autophagy and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
|
-
- HY-N0518
-
|
PAI-1
|
Cardiovascular Disease
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-N1990
-
|
PPAR
|
Inflammation/Immunology
Cardiovascular Disease
|
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
|
-
- HY-18085G
-
-
- HY-B1221
-
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-Y1832
-
2-Vanillin
|
Fungal
|
Cancer
Infection
|
o-Vanillin (2-Vanillin) is a nature product, could be extracted from Vanilla planifolia, Pinus koraiensis fruit. o-Vanillin is a potent antifungal agent. o-Vanillin inhibits the growth of mycelia by disrupting the integrity of cell walls and cell membranes. o-Vanillin inhibits Doxorubicin (HY-15142A)- and 4-hydroperoxycyclophosphamide-induced NF-κB activation.
|
-
- HY-131035
-
|
Histone Acetyltransferase
|
Cancer
|
Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.
|
-
- HY-N10393
-
|
PKC
HSP
|
Cancer
|
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor.
|
-
- HY-N1140
-
|
MAP3K
p38 MAPK
AP-1
NF-κB
|
Cancer
Infection
Inflammation/Immunology
|
Torilin is a sesquiterpene with antimicrobial, anticancer, and anti-inflammatory properties. Torilin inhibits LPS-induced NO release, as well as inhibiting iNOS, PGE2, COX-2, NF-α, IL-1β, IL-6, and GM-CSF. Torilin suppresses NF-kB and AP-1 translocation, inhibits TAK1 kinase activation. Subsequently results suppression of MAPK-mediated JNK, p38, ERK1/2, and AP-1 (ATF-2 and c-jun) activation and IKK-mediated I-κBα degradation, p65/p50 activation, and translocation.
|
-
- HY-N1147
-
Tagitinin D
|
Others
|
Inflammation/Immunology
|
Tirotundin (Tagitinin D) is a potent anti-inflammatory agent. Tirotundin inhibits the activation of NF-Kβ.
|
-
- HY-N1533
-
-
- HY-145944
-
|
Apoptosis
|
Cancer
|
ASR-488 activates the mRNA-binding protein CPEB1, induces apoptosis and inhibits bladder cancer growth.
|
-
- HY-143477
-
-
- HY-N2506
-
|
Others
|
Cardiovascular Disease
|
Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation.
|
-
- HY-N1244
-
Sarmentosine; Sarmentosine (glycoside)
|
Apoptosis
mTOR
Keap1-Nrf2
|
Cancer
|
Sarmentosin is an activator of Nrf2. Sarmentosin inhibits mTOR signaling and induces autophagy-dependent apoptosis in human HCC cells.
|
-
- 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-128586
-
-
- HY-78131B
-
(R)-Ibuprofen
|
NF-κB
|
Inflammation/Immunology
Cancer
|
(R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
|
-
- HY-100407
-
|
mGluR
|
Neurological Disease
|
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
|
-
- HY-114398
-
BAY-293
1 Publications Verification
|
Ras
|
Cancer
|
BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
|
-
- HY-103697A
-
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-156520
-
|
Apoptosis
|
Inflammation/Immunology
|
Immunosuppressant-1 (Compound 31) inhibits anti-CD3/anti-CD28 co-stimulated T-cell proliferation. Immunosuppressant-1 has immunosuppressive activity, and induces apoptosis by activating caspase-3 and PARP in activated lymph node cells.
|
-
- HY-W019721
-
|
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A. Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc).
|
-
- HY-10119
-
SCH 530348
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-13417A
-
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
|
Cancer
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-13417
-
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
|
Cancer
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-117102
-
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
|
-
- HY-14993
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-14994
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-148258
-
-
- HY-15027S1
-
-
- HY-136477
-
PGV-1
|
Apoptosis
COX
VEGFR
NF-κB
|
Cancer
|
Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
|
-
- HY-P5154
-
|
Potassium Channel
|
Neurological Disease
|
Tamapin is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin is a selctive blocker of SK2 (Potassium Channel). Tamapin inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin can be isolated from the Indian red scorpion (Mesobuthus tamulus).
|
-
- HY-10119A
-
SCH 530348 sulfate
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-122542
-
|
PAI-1
|
Cardiovascular Disease
|
PPACK is a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK also inhibits the binding of rt-PA to plasma protease inhibitors.
|
-
- HY-100671
-
|
Histone Acetyltransferase
STAT
|
Cancer
Inflammation/Immunology
|
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
|
-
- HY-P990091
-
SAR 445088
|
Complement System
|
Inflammation/Immunology
|
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a.
|
-
- HY-149472
-
|
PI3K
NF-κB
|
Inflammation/Immunology
|
Anti-osteoporosis agent-4 (Compound 11h) inhibits differentiation of primary osteoclasts. Anti-osteoporosis agent-4 attenuates RANKL-induced osteoclastogenesis. Anti-osteoporosis agent-4 inhibits osteoclast formation with an IC50 value of 358.29 nM. Anti-osteoporosis agent-4 inhibits PI3K/AKT and IκBα/NF-κB signaling pathway activation.
|
-
- HY-N11020
-
|
EBV
|
Infection
Inflammation/Immunology
|
Cabenoside D (compound 8) is a triterpenoid glycoside, which can be isolated from the methanol extract of lichen root. Cabenoside D shows anti-inflammatory activity and inhibits inflammation induced by 12-O-tetracylacyl hormone-13-acetate (TPA) in mice. Cabenoside D also inhibits TPA-induced Epstein-Barr virus (EBV) early antigen (EBV-EA) activation.
|
-
- HY-147187
-
|
STAT
Apoptosis
Bcl-2 Family
Survivin
|
Cancer
|
MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells.
|
-
- HY-15004
-
AUZ 454
3 Publications Verification
K03861
|
CDK
|
Cancer
|
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
|
-
- HY-108635
-
PAF (C16)
|
p38 MAPK
MEK
ERK
Endogenous Metabolite
|
Inflammation/Immunology
Cardiovascular Disease
|
C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
|
-
- HY-19354
-
Aglafolin; Rocaglamide U; (-)-Methyl rocaglate
|
Others
|
Cardiovascular Disease
|
Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor).
|
-
- HY-15251
-
-
- HY-P9969
-
EMD 72000
|
EGFR
|
Cancer
|
Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth.
|
-
- HY-N2283
-
|
ERK
Akt
Endogenous Metabolite
|
Cancer
|
Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
|
-
- HY-136352
-
|
Others
|
Others
|
Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
|
-
- HY-50910
-
CCI-779
|
mTOR
Autophagy
Apoptosis
Bacterial
|
Cancer
|
Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model.
|
-
- HY-N8759
-
|
Others
|
Inflammation/Immunology
|
Vogeloside is an iridoid that can be isolated from the roots of Triosteum pinnatifidum. Vogeloside inhibits nitric oxide production in LPS-activated macrophages.
|
-
- HY-126421
-
-
- HY-12524
-
Bikinin
1 Publications Verification
Abrasin
|
GSK-3
|
Others
|
Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
|
-
- HY-N6946
-
|
Others
|
Inflammation/Immunology
|
Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. Mitraphylline inhibits lipopolysaccharide-mediated activation of primary human neutrophils.
|
-
- HY-101790A
-
|
NEDD8-activating Enzyme
|
Cancer
|
ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
|
-
- HY-112469
-
|
ERK
Insulin Receptor
|
Metabolic Disease
|
ERK Inhibitor II (Negative control) is an effective inhibitor of extracellular signal-regulated kinase (ERK). ERK Inhibitor II (Negative control) inhibits the activation of insulin receptor, which can be used in the study of diabetes.
|
-
- HY-125567
-
|
CXCR
|
Inflammation/Immunology
|
Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
|
-
- HY-16561
-
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-P1740
-
|
Integrin
Apoptosis
|
Inflammation/Immunology
|
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation.
|
-
- HY-155477
-
|
E1/E2/E3 Enzyme
|
Cancer
|
Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ligase Cbl (IC50: 15 nM). Cbl-b refers to Casitas B-lineage lymphoma proto-oncogene-b, which inhibits T-cell, natural killer (NK) cell, and B-cell activation. Cbl-b-IN-15 activates T cell function with EC50=0.41 μM.
|
-
- HY-155971
-
|
Autophagy
|
Cancer
Inflammation/Immunology
|
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cell activation (VISTA). VISTA-IN-2 induces VISTA degradation in cells through an autophagic mechanism. VISTA-IN-2 rescues VISTA-mediated immunosuppression, and enhances antitumor activity of immune cells. VISTA-IN-2 also activates the antitumor immunity and inhibits tumor growth in a CT26 mouse model.
|
-
- HY-110247
-
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
|
-
- HY-155516
-
|
Potassium Channel
|
Inflammation/Immunology
|
KV1.3-IN-1 (Compound trans-18) is a KV1.3 channel inhibitor (IC50: 230 nM and 26.12 nM in Ltk? cells and PHA-activated T-lymphocytes respectively). KV1.3-IN-1 impairs intracellular Ca 2+ signaling. KV1.3-IN-1 inhibits T-cell activation, proliferation, and colony formation.
|
-
- HY-114363A
-
|
c-Met/HGFR
|
Cancer
|
SRI 31215 (TFA) is a Matriptase/Hepsin/hepatocyte growth factor activator (HGFA) triplex inhibitor and mimics the activity of HAI-1/2 (endogenous inhibitors of HGF activation). SRI 31215 has potent inhibitory activity against matriptase, hepsin and HGFA with IC50 values of 0.69 μM, 0.65 μM and 0.30 μM, respectively. SRI 31215 can be used for the research of cancer.
|
-
- HY-114842
-
|
Others
|
Cancer
|
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50=18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the efficacy of Platinum (Pt)-based chemotherapy in lung and ovarian cancer. RPA plays essential roles in both nucleotide excision repair (NER) and homologous recombination (HR), along with its role in DNA replication and DNA damage checkpoint activation.
|
-
- HY-15027S2
-
Mesalamine-13C6; 5-ASA-13C6; Mesalazine-13C6
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
|
-
- HY-B1816
-
-
- 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-139553A
-
(R)-ATI-450; (R)-CDD-450
|
Others
|
Inflammation/Immunology
|
(R)-Zunsemetinib is the inactive isomer of Zunsemetinib (HY-139553), and can be used as an experimental control. Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.
|
-
- HY-50694
-
ICA-17043
|
Potassium Channel
|
Others
|
Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
|
-
- HY-151631
-
|
Bacterial
|
Infection
|
MRV03-070 is an inhibitor of colibactin-activating peptidase ClbP with an IC50 value of 69 nM, acts like biosynthetic precursor precolibactin.
|
-
- HY-102066
-
AZD-7451
|
Trk Receptor
|
Cancer
|
Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.
|
-
- HY-111789
-
TAK-981
|
E1/E2/E3 Enzyme
|
Cancer
Inflammation/Immunology
|
Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
|
-
- HY-N10359
-
-
- HY-117962A
-
|
Guanylate Cyclase
|
Metabolic Disease
|
BI 703704 is a potent soluble guanylate cyclase (sGC) activator. BI 703704 inhibits the progression of diabetic nephropathy in the ZSF1 rat.
|
-
- HY-13694
-
-
- HY-B0809S
-
-
- HY-B0099
-
MCI-186
|
MMP
Apoptosis
|
Neurological Disease
|
Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
|
-
- HY-N2117
-
-
- HY-15477A
-
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-15477
-
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-126382
-
|
NF-κB
|
Inflammation/Immunology
|
Hesperidin methylchalcone (Hesperidin methyl chalcone) inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone inhibits inflammation and pain. Hesperidin methylchalcone exhibits vasoprotective activity.
|
-
- HY-17376
-
-
- HY-N2065
-
|
NF-κB
Ferroptosis
|
Cancer
Inflammation/Immunology
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-18935A
-
Curaxin-137 hydrochloride; CBL-C137 hydrochloride
|
MDM-2/p53
NF-κB
|
Cancer
|
CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
|
-
- HY-103097
-
|
Phospholipase
|
Others
|
ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
|
-
- HY-105118A
-
CGS-9343B; KW 5617
|
Calmodulin
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR.
|
-
- HY-124748
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Inflammation/Immunology
|
ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis.
|
-
- HY-124748A
-
|
Protease Activated Receptor (PAR)
Apoptosis
|
Inflammation/Immunology
|
ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.
|
-
- HY-P5154A
-
|
Potassium Channel
|
Neurological Disease
|
Tamapin TFA is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin TFA is a selctive blocker of SK2 (Potassium Channel). Tamapin TFA inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin TFA can be isolated from the Indian red scorpion (Mesobuthus tamulus).
|
-
- HY-139504
-
CC-99677
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1.
|
-
- HY-119039
-
|
TAM Receptor
|
Cancer
Inflammation/Immunology
|
RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis.
|
-
- HY-114372
-
|
Lipoxygenase
Caspase
Apoptosis
|
Cancer
|
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
|
-
- HY-124822
-
|
AMPK
|
Cancer
Metabolic Disease
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders.
|
-
- HY-14266S
-
TMC120-d11; R147681-d11
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
|
-
- HY-132878
-
|
Others
|
Infection
|
FgGpmk1-IN-1 is a novel fusarium graminearum mitogen-activated protein kinase (FgGpmk1) inhibitor with an EC50 value of 3.46 μg/mL.
|
-
- HY-N8816
-
|
NF-κB
|
Inflammation/Immunology
|
Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM.
|
-
- HY-15718A
-
-
- 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-108634
-
-
- HY-148507
-
|
MEK
|
Cancer
|
GSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis.
|
-
- HY-100611
-
-
- HY-N10926
-
|
AP-1
|
Cancer
|
(+)-Glaucarubinone is a potent AP-1 (activator protein-1) inhibitor with an EC50 value of 0.13 µM. (+)-Glaucarubinone shows noncytotoxic.
|
-
- HY-120675
-
SSTC3
1 Publications Verification
|
Casein Kinase
Wnt
|
Cancer
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-14165
-
-
- HY-N0773
-
Saponaretin; Homovitexin
|
JNK
NF-κB
|
Inflammation/Immunology
|
Isovitexin is a flavonoid isolated from passion flower, Cannabis and, and the palm, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
|
-
- HY-147287
-
|
PSMA
|
Cancer
|
Glu-urea-Glu-NHS ester (compound 21) is an activated N-hydroxysuccinamide (NHS) ester of Glu-urea-Glu which can be used as a pharmacophore for linking with prostate specific membrane antigen (PSMA) inhibitors.
|
-
- HY-32735
-
PG490
|
NF-κB
Apoptosis
|
Cancer
|
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.
|
-
- HY-B1221S1
-
|
Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
Flufenamic acid- 13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-15186
-
GDC-0068; RG7440
|
Akt
Apoptosis
|
Cancer
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.
|
-
- HY-10201
-
Bay 43-9006
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
|
-
- HY-121629
-
|
PDK-1
|
Cancer
|
PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
|
-
- HY-P1740A
-
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation.
|
-
- HY-B1221S
-
|
Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-10201A
-
Bay 43-9006 Tosylate
|
Raf
VEGFR
FLT3
Autophagy
Ferroptosis
Apoptosis
|
Cancer
|
Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
|
-
- HY-N1504
-
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-15098
-
Apoptosis Activator VII
|
HSP
Apoptosis
|
Cancer
|
Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
|
-
- HY-138558
-
-
- HY-149860
-
|
FAP
|
Cancer
|
FAP-IN-1 is a fibroblast activation protein (FAP) inhibitor with an IC50 value of 3.3 nM. FAP-IN-1 can be used for the research of cancer.
|
-
- HY-16642A
-
-
- HY-47979
-
|
FAP
|
Others
|
FAP-IN-2 is a derivative of 99mTc-labeled isonitrile-containing fibroblast activation protein (FAPI) inhibitor, that can be used for tumor imaging.
|
-
- HY-10072
-
|
NF-κB
AP-1
|
Inflammation/Immunology
|
SPC 839 (compound 10) is an orally active inhibitor of AP-1 and NF-kB mediated transcriptional activation with IC50 of 0.008 μM.
|
-
- HY-19700
-
|
MEK
ERK
Endogenous Metabolite
|
Others
|
trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
|
-
- HY-13296
-
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
|
-
- HY-19084
-
-
- HY-118019
-
-
- HY-N0629
-
-
- HY-12496
-
NS-1619
1 Publications Verification
|
Potassium Channel
Apoptosis
|
Cancer
Cardiovascular Disease
|
NS-1619 is an opener of large conductance Ca 2+-activated K + (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.
|
-
- HY-130354
-
Bt2cGMP sodium
|
Potassium Channel
|
Cardiovascular Disease
|
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
|
-
- HY-103308
-
|
Potassium Channel
|
Neurological Disease
|
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease.
|
-
- 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-156671
-
|
Ras
|
Cancer
|
RMC-4998 is a molecular glue compound with good antitumor activity. RMC-4998 is able to form a ternary complex with CYPA and an activated KRAS G12C mutant. Furthermore, CYPA binding to KRAS G12C blocks the interaction between activated KRAS mutants and downstream effector proteins, thereby inhibiting signaling that promotes cell proliferation.
|
-
- HY-145263
-
|
Ser/Thr Protease
|
Cancer
|
VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer.
|
-
- HY-P1281
-
|
Potassium Channel
|
Neurological Disease
|
Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability.
|
-
- HY-16561R
-
trans-Resveratrol (Standard); SRT501 (Standard)
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-16561S1
-
trans-Resveratrol-13C6; SRT501-13C6
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
|
-
- HY-16561S
-
trans-Resveratrol-d4; SRT501-d4
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
|
-
- HY-100227
-
E 64c
2 Publications Verification
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-N1490
-
14-dehydro Andrographolide; AP10
|
NF-κB
|
Inflammation/Immunology
Cancer
|
14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
|
-
- HY-122908
-
AZD5718
|
FLAP
|
Cardiovascular Disease
|
Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
|
-
- HY-N6781
-
|
Phosphodiesterase (PDE)
|
Cancer
Infection
|
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
|
-
- HY-13772
-
AD-32
|
PKC
Antibiotic
|
Cancer
Inflammation/Immunology
|
Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
|
-
- HY-N0754
-
|
HSP
|
Inflammation/Immunology
|
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
|
-
- HY-B0649S1
-
-
- HY-155646
-
|
NF-κB
|
Inflammation/Immunology
|
Anti-inflammatory agent 48 is an anti-inflammatory agent based on its role in inhibiting the NF-κB signaling pathway and activating HO-1 expression.
|
-
- HY-139303
-
|
Others
|
Endocrinology
|
LUF5771 is a potent allosteric recombinant luteinizing hormone (recLH) and Org 43553 inhibitor. LUF5771 is able to partially activate the LH receptor with low efficacy.
|
-
- HY-120261
-
-
- HY-147005
-
|
CRAC Channel
|
Cardiovascular Disease
|
piCRAC-1 is a potent, photoinducible Ca 2+ release-activated Ca 2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage.
|
-
- HY-B0649
-
-
- HY-N2337
-
11β-Hydroxyprogesterone
|
Endogenous Metabolite
|
Cardiovascular Disease
|
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
|
-
- HY-N0436
-
|
NF-κB
|
Infection
Inflammation/Immunology
|
Engeletin is a flavanonol glycoside isolated from Smilax glabra Roxb. , inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-156769
-
-
- HY-N6046
-
|
NF-κB
|
Cancer
Inflammation/Immunology
|
Kamebakaurin is a natural compound isolated from Rabdosia excisa. Kamebakaurin is a potent inhibitor of NF-κB activation by directly targeting DNA-binding activity of p50.
|
-
- HY-B0795
-
|
mTOR
Autophagy
|
Cancer
|
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
|
-
- HY-P99482
-
A 623; AMG 623
|
TNF Receptor
|
Inflammation/Immunology
|
Blisibimod (A 623) is a potent and selective tetravalent inhibitor of B-cell activating factor (BAFF). Blisibimod can be used for the research of systemic lupus erythematosus (SLE).
|
-
- HY-N0826
-
-
- HY-10999
-
GSK1120212; JTP-74057
|
MEK
Autophagy
Apoptosis
|
Cancer
|
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
|
-
- HY-107415
-
|
Raf
|
Cancer
|
PLX7922, a RAF inhibitor, can bind with BRAF V600E. PLX7922 inhibits pERK in BRAF V600E cell lines, and activates pERK in mutant NRAS cell lines.
|
-
- HY-N2119
-
|
NF-κB
|
Inflammation/Immunology
|
Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba. Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1.
|
-
- HY-18849
-
|
ERK
|
Cancer
|
ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 WT and Erk2 DS1 activation loop phosphorylation, with IC50 of 5 μM and 42 nM, respectively.
|
-
- HY-N4171
-
|
Apoptosis
|
Inflammation/Immunology
|
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
|
-
- HY-N0141
-
(-)-Parthenolide
|
NF-κB
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
|
-
- HY-123506
-
|
Src
|
Inflammation/Immunology
Neurological Disease
|
Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models.
|
-
- HY-W404002
-
|
Prolyl Endopeptidase (PREP)
|
Metabolic Disease
|
BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2
|
-
- HY-N7018
-
|
Others
|
Inflammation/Immunology
|
20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the agent discovery of nerve inflammation diseases associated with microglia activated by LPS.
|
-
- HY-16124
-
TLK-286; TER286
|
DNA-PK
Apoptosis
|
Cancer
|
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies.
|
-
- HY-14600
-
BRL 49653C
|
PPAR
TRP Channel
Autophagy
Ferroptosis
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
|
-
- HY-107818
-
|
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
|
-
- HY-103238
-
|
AMPK
STAT
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity.
|
-
- HY-120231
-
|
MALT1
|
Cancer
|
Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression.
|
-
- HY-111662
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis.
|
-
- HY-144765
-
|
NF-κB
Apoptosis
|
Inflammation/Immunology
Neurological Disease
|
NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research.
|
-
- HY-121377
-
-
- HY-137974
-
|
STAT
Apoptosis
|
Cancer
|
8-Epixanthatin is a potential colchicine binding site inhibitor isolated from Xanthium chinese Mill. 8-Epixanthatin can inhibit the activation of STAT3, induce apoptosis, and has anti-tumor activity.
|
-
- HY-112391
-
|
JAK
STAT
|
Cancer
|
SD-1029 is a JAK2/STAT3 inhibitor. SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation.
|
-
- HY-17592
-
|
Parasite
Bacterial
|
Cancer
Infection
|
Bithionol is an antibacterial, anthelmintic, and algaecide agent. Bithionol is also a potent inhibitor of soluble adenylyl cyclase through binding to the allosteric activator site (IC50: 4 μM).
|
-
- HY-N1469
-
-
- HY-N0014
-
-
- HY-N3436
-
-
- HY-N1208
-
O-Acetylspiradine G; Spiradine G acetate
|
Others
|
Cardiovascular Disease
|
Spiradine F is a main alkaloidal component of spiraea japonioa L. fil. Spiradine F derivative can inhibit platelet-activating factor (PAF)-induced platelet aggregation.
|
-
- HY-144813
-
|
Cathepsin
|
Cancer
Inflammation/Immunology
|
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
|
-
- HY-151196
-
|
Others
|
Cardiovascular Disease
|
FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability.
|
-
- HY-101255
-
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
|
-
- HY-133558
-
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
|
-
- HY-N0168A
-
|
p38 MAPK
Apoptosis
Autophagy
|
Cancer
Neurological Disease
|
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
|
-
- HY-N3245
-
-
- HY-19770
-
|
ROR
|
Inflammation/Immunology
|
GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
|
-
- HY-13595
-
Chrysophanic acid
|
EGFR
|
Cancer
|
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
|
-
- HY-12212
-
RTA 408
|
Keap1-Nrf2
STING
Apoptosis
|
Cancer
Inflammation/Immunology
|
Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
|
-
- HY-155657
-
|
Src
|
Inflammation/Immunology
|
BT424 is a specific HCK inhibitor. BT424 can regulate macrophage activation and autophagy in vitro. BT424 ameliorates inflammation and kidney fibrosis in UUO model.
|
-
- HY-121134
-
|
Reactive Oxygen Species
|
Cancer
Neurological Disease
|
Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition.
|
-
- HY-153343
-
|
DGK
|
Cancer
|
BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer.
|
-
- HY-N10062
-
|
RANKL/RANK
|
Others
|
Amakusamine inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinuclear osteoclasts with an IC50 value of 10.5 μM in RAW264.7 cells.
|
-
- HY-10257
-
BAY 11-7083
|
NF-κB
Ferroptosis
Apoptosis
|
Cancer
|
BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
|
-
- HY-N3720
-
6-Demethoxycapillarisin
|
PEPCK
|
Metabolic Disease
|
Demethoxycapillarisin (6-Demethoxycapillarisin) inhibits PEPCK mRNA levels (IC50: 43 μM) by activation of the PI3K pathway. Demethoxycapillarisin decreases glucose production.
|
-
- HY-N0708
-
-
- HY-121160
-
SM1213; Therafectin
|
Bacterial
|
Cancer
Infection
|
Amiprilose (SM1213; Therafectin) is a potent inhibitor against Hepatocellular carcinoma (HCC). Amiprilose induces lymphokine-induced macrophage activation directly to kill Listeria monocytogenes.
|
-
- HY-18286
-
|
TSH Receptor
|
Endocrinology
|
NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
|
-
- HY-149989
-
|
Ack1
Akt
|
Cancer
|
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity.
|
-
- HY-10108
-
|
PI3K
Casein Kinase
DNA-PK
Apoptosis
Autophagy
|
Cancer
Infection
|
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator.
|
-
- HY-N9921
-
|
Pyroptosis
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
Antcin A is a potent NLRP3 inhibitor that inhibits the assembly and activation of the NLRP3 inflammasome. Antcin A can inhibit Kupffer cell pyroptosis and has liver protective activity. Antcin A can be used to study inflammation, such as non-alcoholic fatty liver disease.
|
-
- HY-12005
-
FTY720
|
LPL Receptor
PAK
|
Inflammation/Immunology
Cancer
|
Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
|
-
- HY-130723
-
|
AMPK
|
Cancer
|
AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549).
|
-
- HY-130723A
-
|
AMPK
|
Cancer
|
AMPK activator 2 (compound 7a) hydrochloride, a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 hydrochloride inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549).
|
-
- HY-P3412
-
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease.
|
-
- HY-P1934A
-
|
Fungal
IFNAR
Reactive Oxygen Species
|
Cancer
Inflammation/Immunology
Infection
|
Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay.
|
-
- HY-150587
-
|
ERK
NF-κB
|
Inflammation/Immunology
|
Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver.
|
-
- HY-100487
-
MLN7243
|
E1/E2/E3 Enzyme
NF-κB
Apoptosis
|
Cancer
|
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
|
-
- HY-119160
-
|
PAI-1
|
Cancer
Inflammation/Immunology
|
TM5007 is a poent and orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) with an IC50 of 29 μM. TM5007 enhance fibrinolysis activity and inhibits coagulation. TM5007 also prevents the fibrotic process initiated by bleomycin in mouse lung.
|
-
- HY-P4136
-
|
ERK
|
Cancer
|
Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM.
|
-
- HY-108534
-
AW 464
|
TrxR
|
Cancer
Inflammation/Immunology
|
PMX464 (AW 464), a thiol-reactive quinol, is the inhibitor of thioredoxin-thioredoxin reductase (Trx/TrxR) system. PMX464 can inhibit NF-κB-mediated proinflammatory activation of human type II alveolar epithelial cells.
|
-
- HY-103269
-
BAI1
4 Publications Verification
|
Bcl-2 Family
Apoptosis
|
Cancer
|
BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
|
-
- HY-12357S
-
ETC-1002-d5; ESP-55016-d5
|
ATP Citrate Lyase
AMPK
|
Metabolic Disease
|
Bempedoic acid-d5 is the deuterium labeled Bempedoic acid[1]. Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor[1]. Bempedoic acid (ETC-1002) activates AMPK[2].
|
-
- HY-13412
-
HOE-642
|
Potassium Channel
Sodium Channel
|
Cardiovascular Disease
|
Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1.
|
-
- HY-19634
-
|
Sirtuin
|
Cancer
|
YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells.
|
-
- HY-P2641
-
|
MMP
|
Cancer
|
Peptide 74 is a synthetic peptide containing the prodomain sequence of matrix metalloproteinase (MMP). Peptide 74 inhibits the activated form of the 72-kDa type IV collagenase in vitro.
|
-
- HY-101860
-
-
- HY-P2228
-
|
HDAC
Apoptosis
|
Cancer
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
|
-
- HY-139701
-
|
Others
|
Cancer
|
NI-Pano (CH-03) is a novel hypoxia-activated KDAC inhibitor. NI-Pano (CH-03) is reduced in an O2-dependent manner to release panobinostat.
|
-
- HY-148052
-
|
RIP kinase
|
Cancer
|
RIPK3-IN-2 is a RIP3 inhibitor. RIPK3-IN-2 can be used in diseases caused by or associate with activated necrotic pathways research.
|
-
- HY-151619
-
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
sEH inhibitor-12 (compound 34) is a sEH inhibitor with an IC50 value of 0.7 μM. sEH inhibitor-12 inhibits the 5-lipoxygenase-activating protein (FLAP)-mediated leukotriene (LT) biosynthesis with an IC50 value of 2.9 μM. sEH inhibitor-12 can be used for the research of inflammation.
|
-
- HY-156154
-
|
Pyroptosis
|
Cancer
|
Caspase-3 activator 1 (compound 4b) is a Ru(III) metal complex that inhibits gastric tumor growth and metastasis. Caspase-3 activator 1 mediates caspase-3 cleavage, which in turn causes Caspase-3 to cleave gasdermin E (GSDME) to produce the GSDME-N terminus, causing gastric tumor cell membrane perforation. Caspase-3 activator 1 is capable of inducing pyroptosis and pyroptosis-induced immune responses and can be assembled with decitabine DCT (HY-A0004) into a 4b-DCT-Lip lipid delivery system.
|
-
- HY-P4133
-
|
ERK
MEK
|
Cancer
|
MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable.
|
-
- HY-119931
-
-
- HY-109079A
-
DWP14012 hydrochloride; Fexuprazan hydrochloride
|
Proton Pump
|
Metabolic Disease
|
Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
|
-
- HY-N0039
-
-
- HY-N0883
-
Gamabufagin
|
VEGFR
|
Cancer
|
Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.
|
-
- HY-127002A
-
|
Src
|
Cancer
|
Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
|
-
- HY-109079
-
DWP14012; Fexuprazan
|
Proton Pump
|
Metabolic Disease
|
Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
|
-
- HY-117958
-
HJC0197
1 Publications Verification
|
Ras
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
|
-
- HY-124151
-
2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
|
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
|
-
- HY-142694
-
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation.
|
-
- HY-N0492S
-
-
- HY-134205A
-
|
Keap1-Nrf2
|
Metabolic Disease
Neurological Disease
|
CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
|
-
- HY-116868
-
Anecortave
|
PAI-1
|
Cardiovascular Disease
|
Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases.
|
-
- HY-133114
-
EZM-K
|
Keap1-Nrf2
Autophagy
|
Cancer
Cardiovascular Disease
|
Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.
|
-
- HY-112800
-
|
Phosphatase
|
Metabolic Disease
|
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
|
-
- HY-118532
-
AG30
|
EGFR
|
Cancer
|
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
|
-
- HY-B0151
-
3β-Hydroxy-5-pregnen-20-one
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
|
-
- HY-10256A
-
SB 203580 hydrochloride; RWJ 64809 hydrochloride
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator.
|
-
- HY-113205
-
15-keto-PGE2
|
PPAR
STAT
Prostaglandin Receptor
Endogenous Metabolite
|
Cancer
|
15-keto-Prostaglandin E2 is an endogenous metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to its Cys259 residue. 15-keto-Prostaglandin E2 can bind and stabilize EP2 and EP4 receptor. 15-keto-Prostaglandin E2 inhibits breast cancer cell growth and progression. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth.
|
-
- HY-N11768
-
|
Toll-like Receptor (TLR)
Interleukin Related
NF-κB
|
Inflammation/Immunology
|
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model.
|
-
- HY-B1505
-
Theophyllineacetic acid; Theophylline-7-acetic acid
|
Adenosine Receptor
Protein Arginine Deiminase
Phosphodiesterase (PDE)
|
Cancer
|
Acefylline (Theophyllineacetic acid), a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator, which inhibits rat lung cAMP phosphodiesterase isoenzymes.
|
-
- HY-135715
-
|
Others
|
Others
|
(E)-UK122 TFA is the isomer of UK122 TFA. UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM.
|
-
- HY-144812
-
|
Cathepsin
|
Cancer
Inflammation/Immunology
|
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
|
-
- HY-157147
-
-
- HY-13324
-
RTA 402; NSC 713200; CDDO Methyl ester
|
Keap1-Nrf2
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
|
-
- HY-P9952
-
LymphoStat B
|
TNF Receptor
|
Inflammation/Immunology
|
Belimumab (LymphoStat B) is a human IgG1λ monoclonal antibody that inhibits B-cell activating factor (BAFF). Belimumab can be used for systemic lupus erythematosus (SLE) research.
|
-
- HY-17471A
-
1,1-Dimethylbiguanide hydrochloride
|
AMPK
Autophagy
Mitophagy
|
Metabolic Disease
Cardiovascular Disease
|
Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.
|
-
- HY-P1430
-
-
- HY-17376S
-
-
- HY-12074
-
|
GSK-3
|
Metabolic Disease
|
Cazpaullone is a glycogen synthase kinase-3 (GSK-3) inhibitor. Cazpaullone can activate pancreatic beta cell protection and replication. Cazpaullone can be used for the research of diabetes.
|
-
- HY-W001174
-
|
ERK
NF-κB
|
Inflammation/Immunology
|
2,5-Dihydroxyacetophenone, isolated from Rehmannia glutinosa, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.
|
-
- HY-N10865
-
|
NO Synthase
|
Inflammation/Immunology
|
Chloranthalactone E (compound 6), a labdane diterpene, can be isolated from the aerial parts of Chloranthus serratus. Chloranthalactone E inhibits NO production in LPS-activated RAW 264.7 macrophages.
|
-
- HY-153225
-
|
HIV
|
Infection
|
PYR01 is a potent HIV-1 nonnucleoside reverse transcriptase inhibitor. PYR01 is an also targeted activator of cell kill molecules eliminate cells expressing HIV-1.
|
-
- HY-13520
-
Oncodazole; R17934
|
Microtubule/Tubulin
Bcr-Abl
CRISPR/Cas9
Autophagy
Apoptosis
|
Cancer
|
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
|
-
- HY-100164
-
MKS 492
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
|
-
- HY-N0447
-
-
- HY-10219
-
Sirolimus; AY-22989
|
mTOR
FKBP
Fungal
Autophagy
Endogenous Metabolite
Antibiotic
Bacterial
|
Cancer
|
Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
|
-
- HY-145849
-
|
VEGFR
|
Cancer
|
VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition.
|
-
- HY-138683
-
|
STING
|
Inflammation/Immunology
|
STING-IN-3 is an inhibitor of stimulator of interferon genes (STING). STING-IN-3 efficiently inhibits both hsSTING and mmSTING through covalently target the predicted transmembrane cysteine residue 91 and thereby block the activation-induced palmitoylation of STING.
|
-
- HY-100016
-
|
ATM/ATR
Apoptosis
|
Cancer
|
AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
|
-
- HY-N2006
-
|
HIV Protease
|
Infection
Inflammation/Immunology
|
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC50: 170 μM).
|
-
- HY-N0112
-
Ampelopsin; Ampeloptin
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Cancer
Infection
|
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
|
-
- HY-W018723
-
p-Aminobenzamidine dihydrochloride
|
Ser/Thr Protease
|
Cancer
|
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice.
|
-
- HY-155974
-
|
MDM-2/p53
|
Cancer
|
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction.
|
-
- HY-102011
-
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-102011A
-
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-148368
-
|
Bcl-2 Family
Apoptosis
|
Cancer
|
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis.
|
-
- HY-124697
-
|
TGF-β Receptor
|
Cancer
|
BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
|
-
- HY-137638
-
|
PKA
|
Metabolic Disease
|
Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U46619-induced activation of Rho, Gq and G12/G13 in platelets.
|
-
- HY-N1970
-
|
Keap1-Nrf2
Arenavirus
Caspase
PARP
|
Neurological Disease
|
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
|
-
- HY-B1218
-
|
Bacterial
|
Infection
|
Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
|
-
- HY-114330A
-
|
PAI-1
Ser/Thr Protease
|
Inflammation/Immunology
|
ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
|
-
- HY-N11548
-
|
NO Synthase
|
Inflammation/Immunology
|
Inflexuside A, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO production (NO Synthase) in RAW264.7 macrophages.
|
-
- HY-146334
-
|
Chloride Channel
|
Inflammation/Immunology
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
|
-
- HY-12357S2
-
ETC-1002-d4; ESP-55016-d4
|
ATP Citrate Lyase
AMPK
|
Others
|
Bempedoic acid-d4 is the deuterium labeled Bempedoic acid. Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK[1][2].
|
-
- HY-78131BS
-
(R)-Ibuprofen-d3
|
NF-κB
|
Inflammation/Immunology
Cancer
|
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
|
-
- HY-N0139
-
-
- HY-126361
-
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
|
-
- HY-123963
-
C-178
4 Publications Verification
|
STING
|
Inflammation/Immunology
|
C-178 is a potent and selective covalent inhibitor of STING. C-178 binds to Cys91 and suppresses the STING responses elicited by distinct bona fide activators in mouse but not human.
|
-
- HY-114330
-
|
PAI-1
Ser/Thr Protease
|
Inflammation/Immunology
|
ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
|
-
- HY-16031
-
NSC710464 free base
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
|
-
- HY-B0649S
-
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
Propofol-d17 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties[1].
|
-
- HY-148973
-
|
ATP Synthase
|
Metabolic Disease
|
ZW290 is a compound to activate brown adipose tissue (BAT) thermogenic function. ZW290 increases the expression of uncoupling Protein 1 (UCP1) protein and inhibits ATP synthesis in BAT.
|
-
- HY-N11544
-
|
NO Synthase
|
Inflammation/Immunology
|
Inflexuside B, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO Synthase in RAW264.7 macrophages.
|
-
- HY-U00441
-
DPBQ
1 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
|
-
- HY-N4053
-
-
- HY-126361A
-
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
ZK824190 hydrochloride is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
|
-
- HY-14256
-
-
- HY-50733A
-
|
Apoptosis
Ras
Casein Kinase
|
Cancer
|
CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death.
|
-
- HY-155954
-
|
Autophagy
Apoptosis
|
Cancer
|
UCM-1336 is a potent ICMT inhibitor, with an IC50 of 2 μM. UCM-1336 induces mislocalization of endogenous Ras, decreases Ras activation and induces cell death by autophagy and apoptosis.
|
-
- HY-18711A
-
Metatinib anhydrous; c-Met inhibitor 2
|
c-Met/HGFR
VEGFR
|
Cancer
|
SCR-1481B1 (Metatinib anhydrous) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
|
-
- HY-78869
-
Osimertinib analog
|
EGFR
|
Cancer
|
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
|
-
- HY-P1288
-
PKC fragment (530-558)
|
PKC
|
Others
|
Protein Kinase C (530-558), a peptide fragment of protein kinase C (PKC), is a potent PKC activator. Protein Kinase C (530-558) significantly inhibits osteoclastic bone resorption.
|
-
- HY-13694S
-
-
- HY-123632
-
|
Cytochrome P450
|
Others
|
(3S,5S)-Atorvastatin sodium salt is a pregnane X receptor (PXR) activator and the inactive enantiomer of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor with lipid-lowering capabilities.
|
-
- HY-126420
-
-
- HY-13694S1
-
MRX-1024-d4; D-Methionine-d4
|
GABA Receptor
Endogenous Metabolite
|
|
Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
|
-
- HY-13757A
-
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
|
-
- HY-12041
-
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
|
-
- HY-N10358
-
|
NF-κB
|
Others
|
3-(2-Hydroxyethyl) thio withaferin A is a Withaferin A derivative. Withaferin A, a steroidal lactone, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-151970
-
|
STING
|
Inflammation/Immunology
|
STING-IN-4 (Compound 1) is a STING inhibitor that inhibits STING expression and hence reducing activation of STING and nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis.
|
-
- HY-17376S1
-
SCH 58235-d4-1
|
Keap1-Nrf2
Autophagy
|
Cardiovascular Disease
Cancer
|
Ezetimibe-d4-1 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-32735S
-
PG490-d3
|
NF-κB
Apoptosis
|
Cancer
|
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].
|
-
- HY-10508
-
|
MEK
|
Cancer
|
(R)-PD 0325901CL is an isomer of PD 0325901CL. PD 0325901CL is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) involved in cancer research. PD 0325901CL inhibits the growth of cancer cells in vitro and in vivo.
|
-
- HY-122052
-
|
Others
|
Metabolic Disease
|
UK‑396082 is a potent thrombin activated fibrinolytic inhibitor (TAFI) inhibitor. UK‑396082 increases plasmin activity and induces a parallel decrease in ECM levels. UK‑396082 can be used in research of chronic kidney disease (CKD).
|
-
- HY-144366
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
|
-
- HY-10256
-
SB 203580; RWJ 64809
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator.
|
-
- HY-B1739
-
3β-Hydroxy-5-pregnen-20-one monosulfate
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
|
-
- HY-10201S2
-
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
|
-
- HY-18980
-
Mallotoxin; NSC 56346; NSC 94525
|
PKC
Autophagy
Apoptosis
HIV
RABV
|
Infection
Cancer
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
|
-
- HY-110189
-
3β-Hydroxy-5-pregnen-20-one monosulfate sodium
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
|
-
- HY-P3444
-
PECAM-1
|
SHP2
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation -.
|
-
- HY-112671
-
RTA dh404
|
Keap1-Nrf2
NF-κB
|
Inflammation/Immunology
|
CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats.
|
-
- HY-151343
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NLRP3-IN-10 is a potent NLRP3 inhibitor, inhibits IL-1β release with an IC50 value of 251.1 nM. NLRP3-IN-10 suppresses NLRP3 inflammasome activation by attenuating ASC speck formation.
|
-
- HY-149710
-
|
ERK
ICMT
|
Cancer
|
POP-3MB (compound 1b) is an ICMT inhibitor (IC50: 2.5 μM). POP-3MB changes the subcellular localization of K-Ras and inhibits Ras activation. POP-3MB also inhibits Erk phosphorylation.
|
-
- HY-N6681
-
|
Caspase
Bacterial
Apoptosis
Antibiotic
|
Infection
|
15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3.
|
-
- HY-156595
-
|
BCL6
|
Neurological Disease
|
BCL6 ligand-1 (compound I-94) is a ligand for TCIP 1 (HY-156531). TCIP 1 is a BCL6 inhibitor that activates apoptosis and is used in cancer research.
|
-
- HY-117393
-
|
PKC
|
Cancer
|
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases.
|
-
- HY-N6261
-
|
Others
|
Inflammation/Immunology
|
Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects.
|
-
- HY-69359
-
(±)-β-Homoproline; Hexahydronicotinic acid; 3-Carboxypiperidine
|
GABA Receptor
|
Neurological Disease
|
Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM.
|
-
- HY-135145
-
CB-103
|
Notch
|
Cancer
|
Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity.
|
-
- HY-N1380S1
-
2-Methoxyphenol-d3
|
COX
NF-κB
|
Inflammation/Immunology
|
Guaiacol-d3 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity[1].
|
-
- HY-18937
-
|
RIP kinase
|
Cancer
|
WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
|
-
- HY-P1430A
-
-
- HY-N10083
-
|
Sirtuin
Reactive Oxygen Species
|
Cancer
|
Selaginellin is an inhibitor of Reactive Oxygen Species and an activator of SIRT1. Selaginellin protects endothelial cells against homocysteine-induced senescence by inhibitng reactive oxygen species and upregulating SIRT1 gene expression.
|
-
- HY-N8129
-
|
Others
|
Others
|
Rhaponticin 6′′-O-gallate is a stilbene glucoside gallate that can be found in rhizome of Rheum undulatum L. Rhaponticin 6′′-O-gallate inhibits nitric oxide production in lipopolysaccharide-activated macrophages.
|
-
- HY-16785B
-
INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
|
Interleukin Related
|
Cancer
|
Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
|
-
- HY-112125
-
-
- HY-13812
-
-
- HY-137552
-
MASTL Kinase Inhibitor-1
|
Others
|
Cancer
|
MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.
|
-
- HY-150073
-
|
Others
|
Cancer
|
DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer.
|
-
- HY-14530
-
AG 2037
|
Antifolate
|
Cancer
|
Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice.
|
-
- HY-18982
-
Flagecidin; Wuningmeisu C
|
DNA/RNA Synthesis
JNK
Bacterial
Apoptosis
Antibiotic
Parasite
|
Cancer
Infection
|
Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic.
|
-
- HY-139576
-
DUR-928
|
Endogenous Metabolite
|
Metabolic Disease
|
Larsucosterol (DUR-928), a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol as a potent endogenous regulator decreases lipogenesis. Larsucosterol inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
|
-
- HY-139576A
-
DUR-928 sodium
|
Endogenous Metabolite
|
Metabolic Disease
|
Larsucosterol (DUR-928) sodium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol sodium as a potent endogenous regulator decreases lipogenesis. Larsucosterol sodium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
|
-
- HY-111249
-
|
FLT3
|
Cancer
|
TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research.
|
-
- HY-122700
-
|
Complement System
|
Inflammation/Immunology
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
|
-
- HY-100431
-
IMR-1
4 Publications Verification
|
Notch
|
Cancer
|
IMR-1 is a novel class of Notch inhibitor targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth.
|
-
- HY-147214
-
|
YAP
|
Cancer
|
GNE-7883 is a pan-TEAD inhibitor with anti-cell proliferation activity. GNE-7883 overcomes resistance to KRAS G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation. GNE-7883 may be used in the study of YAP/TAZ-dependent cancers.
|
-
- HY-17376R
-
SCH 58235 (Standard)
|
Keap1-Nrf2
Autophagy
|
Cardiovascular Disease
Cancer
|
Ezetimibe (Standard) is the analytical standard of Ezetimibe. This product is intended for research and analytical applications. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-10999S
-
|
MEK
Autophagy
Apoptosis
|
Cancer
|
Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
|
-
- HY-150761
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity.
|
-
- HY-P3785
-
|
PKA
|
Neurological Disease
|
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors.
|
-
- HY-N6033
-
(+)-Ferruginol
|
HSV
Apoptosis
|
Cancer
Infection
Neurological Disease
Cardiovascular Disease
|
Ferruginol ((+)-Ferruginol), a natural diterpenoid, is an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). Ferruginol inhibits the growth of thyroid cancer cells through the induction of mitochondrial apoptosis. Ferruginol has antitumor, cardioprotective, antioxidant, gastroprotective, and neuroprotective activities.
|
-
- HY-112108
-
COS
|
AMPK
Endogenous Metabolite
|
Cancer
Metabolic Disease
|
Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
|
-
- HY-N4202
-
|
Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway.
|
-
- HY-15272
-
WAY-600
5 Publications Verification
|
mTOR
|
Cancer
Inflammation/Immunology
|
WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
|
-
- HY-136641
-
|
FAP
|
Cancer
|
NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI can be used as a probe for FAP-targeted tumour imaging. NOTA-FAPI has good tumour detection efficacy and excellent imaging quality.
|
-
- HY-P0318
-
-
- HY-B0190A
-
FUT-175
|
Ser/Thr Protease
Apoptosis
SARS-CoV
|
Cardiovascular Disease
Cancer
|
Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat mesylate supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat mesylate blocks activation of SARS-CoV-2..
|
-
- HY-B0190
-
-
- HY-N0220
-
|
NF-κB
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Dauricine, a bisbenzylisoquinoline alkaloid in Menispermum dauricum, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.
|
-
- HY-B0190B
-
|
Ser/Thr Protease
Apoptosis
SARS-CoV
|
Cardiovascular Disease
|
Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat hydrochloride supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat hydrochloride blocks activation of SARS-CoV-2..
|
-
- HY-P9958
-
Immunoglobulin G2; Ranmark
|
NF-κB
|
Cancer
|
Denosumab is a human monoclonal antibody binding to, and inhibiting, the receptor activator of RANKL (TNFSF11). Denosumab can reduce the risk of vertebral, nonvertebral and hip fractures, also has anti-cancer activity.
|
-
- HY-N0250
-
-
- HY-14759
-
PAZ-417
|
PAI-1
Amyloid-β
|
Neurological Disease
|
Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research.
|
-
- HY-19151
-
IS-741
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
Fuzapladib (IS-741), an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.
|
-
- HY-N3255
-
|
STAT
CXCR
|
Cancer
Inflammation/Immunology
|
Minecoside is a CXCR4/STAT3 inhibitor with anticancer and anti-inflammatory activity. Minecoside decreases CXCR4 expression and suppresses STAT3 activation, thus to inhibit CXCL 12-induced invasion. Minecoside potently inhibits cancer metastasis and promotes apoptotic progression.
|
-
- HY-111549
-
|
Others
|
Cancer
|
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
|
-
- HY-19151A
-
IS-741 sodium
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
Fuzapladib (IS-741) sodium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.
|
-
- HY-108900
-
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Cancer
Infection
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
|
-
- HY-100415
-
WX-UK1; UKI-1C
|
PAI-1
Ser/Thr Protease
|
Cancer
|
UKI-1 (WX-UK1) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
|
-
- HY-B0151S1
-
3β-Hydroxy-5-pregnen-20-one-13C2,d2
|
Isotope-Labeled Compounds
TRP Channel
Endogenous Metabolite
Cannabinoid Receptor
Autophagy
|
Neurological Disease
|
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[1][2][3][4].
|
-
- HY-B0151S
-
3β-Hydroxy-5-pregnen-20-one-d4
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- HY-117693
-
|
ATM/ATR
|
Cancer
|
Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells.
|
-
- HY-B0151S2
-
3β-Hydroxy-5-pregnen-20-one-d4-1
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- HY-17537
-
|
IRE1
|
Cancer
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
|
-
- HY-N0592A
-
|
NF-κB
AMPK
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
Demethyleneberberine chloride is a natural mitochondria-targeted antioxidant. Demethyleneberberine chloride alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine chloride could serve as a AMPK activator for researching non-alcoholic fatty liver disease (NAFLD).
|
-
- HY-155785
-
|
Reactive Oxygen Species
Autophagy
Apoptosis
JAK
|
Cancer
|
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma.
|
-
- HY-13418
-
Compound C dihydrochloride; BML-275 dihydrochloride
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-145358
-
|
PI3K
|
Cancer
|
FAP-PI3KI1 is a fibroblast-activated protein (FAP)-targeted PI3K inhibitor that selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells and effectively inhibits collagen synthesis and reduces collagen deposition.
|
-
- HY-135815
-
TAK-788; AP32788
|
EGFR
|
Cancer
|
Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research.
|
-
- HY-B0466A
-
|
Antibiotic
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
Cloxacillin is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.
|
-
- HY-13297
-
|
E1/E2/E3 Enzyme
|
Cancer
|
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
|
-
- HY-109897
-
-
- HY-B0466
-
|
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium monohydrate can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.
|
-
- HY-135815B
-
TAK-788 mesylate; AP32788 mesylate
|
EGFR
|
Cancer
|
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research.
|
-
- HY-B0466B
-
|
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
Cloxacillin sodium is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.
|
-
- HY-N0592
-
|
NF-κB
AMPK
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD).
|
-
- HY-152265
-
|
Mitophagy
|
Neurological Disease
|
PARL-IN-1 is a potent PARL inhibitor with an IC50 value of 28 nM. PARL-IN-1 inhibits PARL and leads to a robust activation of the PINK1/Parkin pathway. PARL-IN-1 promotes PINK1/Parkin-dependent mitophagy.
|
-
- HY-P3204
-
AL-78898A
|
Complement System
|
Metabolic Disease
|
POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research
|
-
- HY-N0109
-
Rhodioloside
|
mTOR
Apoptosis
Prolyl Endopeptidase (PREP)
|
Cancer
|
Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
|
-
- HY-13255A
-
|
APC
|
Cancer
|
TAME hydrochloride is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest. TAME hydrochloride is not cell permeable.
|
-
- HY-116120
-
-
- HY-N0802
-
Senegenin
|
NF-κB
Bacterial
|
Infection
Inflammation/Immunology
|
Tenuigenin is a major active component isolated from the root of the Chinese herb Polygala tenuifolia. Tenuigenin protects against S.aureus-induced pneumonia by inhibiting NF-κB activation. Tenuigenin has anti-inflammatory effect.
|
-
- HY-13255
-
|
APC
|
Cancer
|
TAME is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest. TAME is not cell permeable.
|
-
- 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-N0020
-
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche deserticola, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
|
-
- HY-15880
-
|
Phosphatase
Apoptosis
Autophagy
|
Cancer
|
CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy.
|
-
- HY-124956
-
|
Others
|
Others
|
GIV3727 is a bitter taste receptor hTAS2R antagonist, which can inhibit the activation of hTAS2R31 by saccharin and acesulfame potassium, and can effectively reduce the bitter quality of food, beverage and medicine.
|
-
- HY-126675A
-
|
CDK
STAT
|
Inflammation/Immunology
|
AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
|
-
- HY-147082
-
|
YAP
|
Cancer
|
GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids.
|
-
- HY-120026
-
KB015
|
Thyroid Hormone Receptor
|
Neurological Disease
|
KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle.
|
-
- HY-P3444A
-
PECAM-1 TFA
|
SHP2
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation -.
|
-
- HY-B0689A
-
MK-639; L735524
|
HIV
HIV Protease
SARS-CoV
Apoptosis
MMP
|
Infection
Cancer
|
Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CL pro inhibitor.
|
-
- HY-B0689
-
MK-639 free base; L-735524 free base
|
HIV
HIV Protease
Apoptosis
MMP
SARS-CoV
|
Inflammation/Immunology
Cancer
|
Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL pro inhibitor.
|
-
- HY-13757
-
ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.
|
-
- HY-13757AS1
-
ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
|
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
|
Cancer
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
|
-
- HY-141645
-
WS070117
|
AMPK
TGF-β Receptor
NF-κB
JNK
AP-1
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
|
-
- HY-13757AR
-
ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
Tamoxifen (Standard) is the analytical standard of Tamoxifen. This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
|
-
- HY-136179
-
|
Tyrosinase
|
Inflammation/Immunology
|
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
|
-
- HY-10219S
-
Sirolimus-d3; AY-22989-d3
|
mTOR
FKBP
Autophagy
|
Cancer
|
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
|
-
- HY-N0177
-
|
STAT
MicroRNA
|
Metabolic Disease
|
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57. Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression.
|
-
- HY-149604
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly.
|
-
- HY-139576B
-
DUR-928 (trimethylamine)
|
LXR
Endogenous Metabolite
|
Metabolic Disease
|
Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
|
-
- HY-10999S1
-
|
MEK
Autophagy
Apoptosis
|
Cancer
|
Trametinib- 13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
|
-
- HY-118628
-
ACA
|
Phospholipase
TRP Channel
|
Cardiovascular Disease
|
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia.
|
-
- HY-N0191
-
-
- HY-149816
-
-
- HY-111926
-
|
Others
|
Metabolic Disease
|
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor.
|
-
- HY-10999A
-
GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
|
MEK
Apoptosis
|
Cancer
|
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
|
-
- HY-115537
-
|
Apoptosis
|
Cancer
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
|
-
- HY-155978
-
|
Others
|
Inflammation/Immunology
|
RDN2150 (Compound 25) is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 covalently binds to the C346 residue of ZAP-70. RDN2150 inhibits the expression of CD25 and CD69, and inhibits CD4 + T cell activation. RDN2150 can be used for research of psoriasis.
|
-
- HY-15271
-
WYE-687
3 Publications Verification
|
mTOR
PI3K
|
Cancer
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-N3828
-
|
Apoptosis
ERK
JNK
|
Cancer
|
epi-Eriocalyxin A (Epieriocalyxin A), a diterpenoid isolated from Isodon eriocalyx, induces colon cancer apoptosis. epi-Eriocalyxin A also inhibits ERK1/2 and JNK activation, which suppresses Bcl-2 expression.
|
-
- HY-15874A
-
GSK2190915 sodium salt; AM-803 sodium
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
|
-
- HY-109011
-
AQX-1125
|
Phosphatase
|
Cancer
|
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
|
-
- HY-110228
-
1,1-Dimethylbiguanide-d6 (hydrochloride)
|
AMPK
Autophagy
Mitophagy
|
Metabolic Disease
Cardiovascular Disease
|
Metformin-d6 (hydrochloride)e is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy[1].
|
-
- HY-B0627
-
1,1-Dimethylbiguanide
|
AMPK
Autophagy
Mitophagy
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggers autophagy.
|
-
- HY-151626
-
|
Bacterial
|
Infection
|
MRV03-037 is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-037 prevents gut bacterial genotoxin production.
|
-
- HY-18952A
-
|
FLT3
Apoptosis
|
Cancer
|
(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3.
|
-
- HY-109011A
-
AQX-1125 acetate
|
Phosphatase
|
Cancer
|
Rosiptor (AQX-1125) acetate is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor acetate (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
|
-
- HY-N12283
-
|
NF-κB
|
Inflammation/Immunology
|
NF-κB-IN-13 (compound 12) can significantly inhibit LPS-induced NF-κB activation and NO production in RAW264.7 macrophages. NF-κB-IN-13 has anti-inflammatory effects.
|
-
- HY-N0375
-
-
- HY-15251A
-
(Rac)-Repertaxin; (Rac)-DF 1681Y
|
Others
|
Cancer
Endocrinology
Inflammation/Immunology
|
(Rac)-Reparixin is the inactive isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
|
-
- HY-16696
-
SN 2
3 Publications Verification
|
TRP Channel
Flavivirus
|
Infection
|
SN 2 is a potent activator of TRPML3 ion channel with an EC50 of 1.8 μM.
SN 2 also acts as a potent inhibitor of Dengue virus 2 (DENV2) and Zika virus (ZIKV).
|
-
- HY-19700S
-
|
MEK
ERK
Endogenous Metabolite
|
Others
|
trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
|
-
- HY-111447
-
|
NADPH Oxidase
Apoptosis
|
Cancer
Cardiovascular Disease
|
VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins.
|
-
- HY-P99462
-
CDX 0159
|
c-Kit
|
Inflammation/Immunology
|
Barzolvolimab (CDX 0159) is a humanized anti-KIT IgG1 monoclonal antibody. Barzolvolimab specificity and potently inhibits KIT activation by SCF. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria.
|
-
- HY-15874
-
GSK2190915; AM-803
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
|
-
- HY-P99196
-
|
c-Met/HGFR
|
Cancer
|
Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). Ficlatuzumab blocks the activation of the HGF/c-Met signaling pathway, and inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion.
|
-
- HY-135808
-
|
NF-κB
|
Inflammation/Immunology
|
BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases.
|
-
- HY-12762
-
QS11
1 Publications Verification
|
Others
|
Cancer
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-100345
-
|
TRP Channel
|
Cancer
Neurological Disease
|
AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC50 of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (NaV).
|
-
- HY-148591
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
GSK761 is a selective inhibitor of speckled 140 kDa (SP140) with an IC50 value of 77.79 nM. GSK761 reduces monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. GSK761 induces the production of CD206 + regulatory macrophages by inhibiting SP140.
|
-
- HY-101246
-
|
RET
|
Cancer
|
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
|
-
- HY-130369
-
|
HSV
Necroptosis
Bacterial
|
Cancer
Infection
|
NSC10010 hydrochloride inhibits gammaherpesvirus associated B-lymphomas growth through activation of NF-kB and c-Myc-mediated signaling pathways. NSC10010 hydrochloride induces necrotic cell death in gammaherpesvirus infected B-cells. NSC10010 hydrochloride is also an inhibitor of Mtb ClpC1 ATPase.
|
-
- HY-103639A
-
|
Toll-like Receptor (TLR)
|
Infection
|
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis.
|
-
- HY-B2145
-
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-B2145A
-
IY-81149 sodium hydrate
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor. Ilaprazole sodium hydrate irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium hydrate is used for the research of gastric ulcers. Ilaprazole sodium hydrate is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-110189S1
-
3β-Hydroxy-5-pregnen-20-one monosulfate-d4 (sodium)
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
|
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- HY-N11009
-
|
EBV
|
Infection
|
11-Oxomogroside II A1 (compound 7) is an oxidized cucurbitin. It can be isolated from the ethanol extract of Rohanberry fruit. 11-Oxomogroside II A1 inhibits the activation of Epstein-Barr virus (EBV) early antigen (EBV-EA) induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). 11-Oxomogroside II A1 also weakly inhibits the activation of (±)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor.
|
-
- HY-109041
-
AKB-9778
|
Phosphatase
Tie
|
Inflammation/Immunology
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM).
|
-
- HY-P5762
-
PNX-14
|
GnRH Receptor
|
Neurological Disease
|
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia.
|
-
- HY-134885
-
RM-023
|
SHP2
Ras
|
Cancer
|
RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction.
|
-
- HY-137813
-
|
PERK
|
Cancer
Metabolic Disease
Neurological Disease
|
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
|
-
- HY-P3065
-
|
Calcium Channel
|
Neurological Disease
|
Calcicludine is a protein toxin from the venom of the green mamba Dendroaspis angusticeps that inhibits high-voltage-activated calcium channel, especially L-type calcium channel with the IC50 of 88 nM. Calcicludine has role in excitatory synaptic transmission.
|
-
- HY-P1396A
-
|
G Protein-coupled Receptor Kinase (GRK)
|
Others
|
GRK2i TFA is a GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. GRK2i TFA corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.
|
-
- HY-155765
-
|
NF-κB
|
Inflammation/Immunology
|
Anti-inflammatory agent 51 (compound 11d) is an amide/sulfonamide derivative with anti-inflammatory activities. Anti-inflammatory agent 51 inhibits NF-κB activation, has the potential for acute lung injury and ulcerative colitis research.
|
-
- HY-N0589
-
|
NF-κB
COX
Bacterial
|
Infection
Inflammation/Immunology
|
Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions. Dehydrodiisoeugenol inhibits LPS- stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages.
|
-
- HY-125354
-
|
Caspase
|
Cancer
|
Limonin glucoside can be isolated from seeds of Citrus reticulata. Limonin glucoside induces activation of caspase-3. Limonin glucoside inhibits the proliferation of human colon adenocarcinoma (SW480) cells (IC50: 37.39 μM).
|
-
- HY-15214
-
|
Histone Methyltransferase
|
Cancer
|
CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
|
-
- HY-15214A
-
|
Histone Methyltransferase
|
Cancer
|
CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
|
-
- HY-N6748
-
-
- HY-153967
-
|
PKA
|
Cancer
|
BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research.
|
-
- HY-102004
-
SB 659032
|
Phosphatase
|
Inflammation/Immunology
Neurological Disease
|
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist.
|
-
- HY-12825
-
|
Estrogen Receptor/ERR
|
Cancer
|
BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
|
-
- HY-N0003
-
NSC 293100
|
Akt
Autophagy
HCV
ERK
|
Cancer
|
Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
|
-
- HY-N3260
-
-
- HY-139486
-
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.
|
-
- HY-111789A
-
(S)-TAK-981
|
Others
|
Cancer
Inflammation/Immunology
|
(S)-Subasumstat is the inactive isomer of Subasumstat (HY-111789), and can be used as an experimental control. Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
|
-
- HY-B0285
-
-
- HY-B0285A
-
-
- HY-N0499
-
IdB 1027
|
RANKL/RANK
|
Cancer
|
Cyanidin Chloride (IdB 1027), a subclass of anthocyanin, displays antioxidant and anti-carcinogenesis properties. Cyanidin Chloride (IdB 1027) inhibits osteoclast formation, hydroxyapatite resorption, and receptor activator of NF-κB ligand (RANKL)-induced osteoclast marker gene expression.
|
-
- HY-105940
-
|
Amino Acid Derivatives
|
Cardiovascular Disease
|
IQB-782 is a cysteine derivative. IQB-782 has inhibition for thrombin activatable fibrinolysis inhibitor (TAFI), with an Ki(app) of 0.14 μM. IQB-782 shows a potent mucolytic-expectorant activity.
|
-
- HY-N0722
-
trans-5-O-Caffeoylquinic acid
|
NF-κB
Interleukin Related
TNF Receptor
COX
|
Inflammation/Immunology
Cancer
|
Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
|
-
- HY-126390
-
NSC 150117
|
Phosphatase
Apoptosis
|
Cancer
Inflammation/Immunology
|
(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-149700
-
|
ROCK
MMP
STAT
|
Others
|
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model.
|
-
- HY-W009724
-
2-APB
|
Calcium Channel
TRP Channel
|
Others
|
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
|
-
- HY-148606
-
|
STING
|
Cancer
|
STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an Ki value of 43.1 nM in scintillation proximity assay. STING modulator-3 has no effect on IRF-3 activation or TNF-β induction in THP-1 cells.
|
-
- HY-100612
-
|
Chloride Channel
|
Others
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-135815A
-
TAK-788 succinate; AP32788 succinate
|
EGFR
|
Cancer
|
Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.
|
-
- HY-136093B
-
IM156 free base; HL156A free base; HL271 free base
|
Mitochondrial Metabolism
|
Cancer
|
Lixumistat (IM156) is a novel biguanide mitochondrial protein complex 1 inhibitor of oxidative phosphorylation (OXPHOS) with anti-tumor activity. Lixumistat regulates OXPHOS to attenuate mitochondrial metabolic reprogramming and inhibit lung fibrosis. Lixumistat also suppresses B-cell activation to alleviate systemic lupus erythematosus.
|
-
- HY-120111
-
MW01-18-150SRM
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Neurological Disease
|
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
|
-
- HY-150751
-
ODN A151
|
Toll-like Receptor (TLR)
AIM2
|
Inflammation/Immunology
|
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.
|
-
- HY-101287
-
|
Microtubule/Tubulin
JNK
Apoptosis
Caspase
|
Cancer
|
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
|
-
- HY-N6257
-
|
ERK
PGE synthase
COX
NF-κB
|
Cancer
Inflammation/Immunology
|
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects.
|
-
- HY-126675
-
|
CDK
STAT
|
Inflammation/Immunology
|
AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
|
-
- HY-132304
-
|
PKC
|
Inflammation/Immunology
|
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by inhibiting IL-2 expression.
|
-
- HY-103347
-
|
Apoptosis
|
Inflammation/Immunology
|
M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia.
|
-
- HY-133015
-
|
Bcl-2 Family
|
Cancer
|
Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity..
|
-
- HY-138537
-
|
IKK
|
Cancer
|
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.
|
-
- HY-101664
-
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-B0689B
-
MK-639 ethanolate; L735524 ethanolate
|
Apoptosis
MMP
HIV
HIV Protease
SARS-CoV
|
Cancer
Infection
|
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CL pro inhibitor.
|
-
- HY-118618
-
Hiyodorilactone A; Schkuhrin I
|
STAT
|
Cancer
|
Eucannabinolide is a STAT3 inhibitor. Eucannabinolide suppresses STAT3 activation at tyrosine 705, inhibiteds its translocation to nucleus, and decreases its DNA binding capacity. Eucannabinolide can be used for triple negative breast cancer (TNBC) diseases research.
|
-
- HY-N0168AS
-
|
p38 MAPK
Apoptosis
Autophagy
|
Cancer
Neurological Disease
|
(Rac)-Hesperetin-d3 is the deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
|
-
- HY-19820
-
|
Akt
Ser/Thr Protease
|
Cancer
Neurological Disease
|
NSC45586 is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 can activate AKT in neurons.
|
-
- HY-149055
-
|
CXCR
|
Inflammation/Immunology
|
ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11.
|
-
- HY-P3204A
-
AL-78898A TFA
|
Complement System
|
Metabolic Disease
|
POT-4 TFA (AL-78898A TFA), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 TFA can be used for age-related macular degeneration research.
|
-
- HY-135042
-
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model.
|
-
- HY-N6679A
-
|
HSP
TGF-beta/Smad
|
Cancer
Infection
|
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
|
-
- HY-122881
-
JTP-0819958
|
IKK
|
Cancer
|
HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro.
|
-
- HY-W011102
-
NSC 83265; S-Tritylcysteine; 3-Tritylthio-L-alanine
|
Kinesin
Apoptosis
|
Cancer
|
S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities.
|
-
- HY-119339
-
SX-682
3 Publications Verification
|
CXCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
|
-
- HY-129087
-
|
Apoptosis
|
Cancer
|
BC-1258, an F-box/LRR-repeat protein 2 (FBXL2) activator, can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells, and profoundly inhibits tumor formation in mice.
|
-
- HY-126114
-
|
COX
Interleukin Related
|
Inflammation/Immunology
|
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
|
-
- HY-19820A
-
|
Akt
Ser/Thr Protease
|
Cancer
Neurological Disease
|
NSC45586 sodium is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 sodium targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 sodium can activate AKT in neurons.
|
-
- HY-151629
-
|
Others
|
Cancer
|
MRV03-069 (Compound 3) is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-069 can be used in colorectal cancer research.
|
-
- HY-151628
-
|
Others
|
Cancer
|
MRV03-068 (Compound 2) is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-068 can be used in colorectal cancer research.
|
-
- HY-N11058
-
|
Lipoxygenase
NO Synthase
|
Inflammation/Immunology
|
Damnacanthol is a natural product that can be isolated from Damnacanthus major. Damnacanthol has anti-15-lipoxygenase activity and can inhibit nitric oxide production in LPS-activated macrophages RAW 264.7 cells.
|
-
- HY-N2078
-
Neodiosgenin
|
LXR
|
Metabolic Disease
|
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
|
-
- HY-122727
-
|
DNA-PK
Apoptosis
|
Cancer
|
STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis.
|
-
- HY-101084
-
|
EGFR
Histone Acetyltransferase
Epigenetic Reader Domain
|
Cancer
|
NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
|
-
- HY-13423
-
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.
|
-
- HY-16677A
-
MDL72974A
|
Monoamine Oxidase
|
Neurological Disease
|
Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO).
|
-
- HY-113592
-
|
ERK
|
Cancer
|
ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2.
|
-
- HY-129239
-
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
|
-
- HY-13965
-
ML161
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
|
-
- HY-131649
-
|
Others
|
Cancer
|
Compound C108 is a G3BP2 inhibitor. Compound C108 also targeted stress granule-associated proteins and Gtpase-activating protein (SH3 domain) binding protein 2. Compound C108 potently inhibits esophageal squamous cell carcinoma (ESCC) cell metastasis.
|
-
- HY-N2892
-
Aristololactam A IIIa; Sch 546909
|
DYRK
|
Cancer
Cardiovascular Disease
|
Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells.
|
-
- HY-117656
-
ESI-05
3 Publications Verification
NSC 116966
|
Acyltransferase
|
Metabolic Disease
Neurological Disease
|
ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
|
-
- HY-12467
-
|
TOPK
CDK
Apoptosis
|
Cancer
|
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
|
-
- HY-P5182
-
|
Potassium Channel
|
Inflammation/Immunology
|
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity.
|
-
- HY-10999S2
-
GSK1120212-13C,d3; JTP-74057-13C,d3
|
Isotope-Labeled Compounds
MEK
Autophagy
Apoptosis
|
Cancer
|
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
|
-
- HY-135231
-
|
Mitochondrial Metabolism
Autophagy
|
Cancer
|
NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway.
|
-
- HY-12810
-
|
Ras
|
Cancer
|
EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor. EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration.
|
-
- HY-N3548
-
|
NF-κB
|
Inflammation/Immunology
|
Catalpalactone has anti-inflammatory effect. Catalpalactone inhibits LPS-induced NO production and iNOS expression in RAW264.7 cells, and also inhibits IRF3, NF-κB, and IFN-β/STAT-1 activation. Catalpalactone also inhibits dopamine biosynthesis by reducing tyrosine hydroxylase (TH) and aromatic-l-amino acid decarboxylase (AADC) activities.
|
-
- HY-14654
-
-
- HY-N3711
-
|
JNK
ERK
Apoptosis
|
Neurological Disease
|
Dehydrocrenatidine, a β-carboline alkaloid that can be isolated from Picrasma quassioides. Dehydrocrenatidine induces cell apoptosis by activates ERK and JNK. Dehydrocrenatidine inhibits invasion and migration of cancer cells, it also suppresses neuronal excitability to exert analgesic effects.
|
-
- HY-107867
-
|
Others
|
Cardiovascular Disease
|
Clopidogrel sulfate is an antiplatelet agent. Specifically, Clopidogrel sulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. Clopidogrel sulfate can be used for research of heart disease and stroke.
|
-
- HY-13030
-
-
- HY-111036
-
|
TRP Channel
|
Others
|
AMG0347 is a transient receptor potential type V1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC50 = 0.2 nm), protons (IC50= 0.8 nm), or capsaicin (IC50 = 0.7 nm).
|
-
- HY-141550
-
|
Others
|
Inflammation/Immunology
|
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
|
-
- HY-124156A
-
|
Wnt
|
Metabolic Disease
|
KY-02327 acetate, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 acetate shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation.
|
-
- HY-50937
-
|
MyD88
|
Inflammation/Immunology
|
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
|
-
- HY-B0764A
-
Dibutyryl cAMP calcium salt; DBcAMP calcium salt
|
PKA
Phosphodiesterase (PDE)
Apoptosis
|
Others
|
Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
|
-
- HY-77293
-
|
Apoptosis
Keap1-Nrf2
|
Cancer
|
(E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol (HY-14616), is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells.
|
-
- HY-139361
-
PIN1-3
|
Others
|
Cancer
|
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors.
|
-
- HY-120294
-
|
CGRP Receptor
TRP Channel
|
Neurological Disease
|
Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research.
|
-
- HY-N7015
-
|
HSV
|
Infection
|
Zerumbone is a monocyclic sesquiterpene compound isolated from the rhizomes of Zingiber zerumbet Smith. Zerumbone potently inhibits the activation of Epstein-Barr virus with an IC50 of 0.14 mM. Zerumbone has anti-cancer, antioxidant, anti-inflammatory and anti-proliferative activity.
|
-
- HY-127002
-
|
Src
|
Cancer
|
Squarunkin A is a potent and selective UNC119-cargo interaction inhibitor, interrupting the UNC119A-myristoylated Src N-terminal peptide interaction (IC50=10 nM). Squarunkin A interferes with the activation of Src kinase in cells.
|
-
- HY-N5018
-
Musizin
|
Parasite
AMPK
|
Infection
|
Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus.Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasma membrane by activation of AMPK.Nepodin (Musizin) has antidiabetic and antimalarial activities.
|
-
- HY-N8218
-
-
- HY-100738
-
NSC144303
|
Apoptosis
|
Cancer
|
Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
|
-
- HY-P99904
-
MEDI-507
|
CD2
|
Inflammation/Immunology
|
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes T cells, decreases T cell activation, inhibites T cell proliferation and enriches naïve and bona fide regulatory T cells.
|
-
- HY-124156
-
|
Wnt
|
Metabolic Disease
|
KY-02327, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation.
|
-
- HY-101837
-
|
Others
|
Inflammation/Immunology
|
CGP 53716 is a potent protein tyrosine kinase inhibitor. CGP 53716 has selective activity of platelet-derived growth factor (PDGF) receptor. CGP 53716 can be used in the study of disease induced by abnormal cell proliferation induced by PDGF receptor activation .
|
-
- HY-152089
-
-
- HY-W395779
-
|
Filovirus
|
Infection
|
EBOV-IN-1 (com 3.47) is an adamantane dipeptide piperazine and an inhibitor of Ebola virus (EBOV). EBOV-IN-1 targets Niemann-Pick C1 (NPC1) and inhibits its binding to the EBOV glycoprotein (GP) that activates and mediates viral penetration into host cells, thereby inhibiting EBOV infection. EBOV-IN-1 inhibits pseudotyped EBOV infection with an IC50 of 13 nM.
|
-
- HY-N0492
-
Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
|
α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
|
-
- HY-144634
-
|
Keap1-Nrf2
|
Inflammation/Immunology
Neurological Disease
|
DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD).
|
-
- HY-120920
-
|
Dopamine Receptor
|
Inflammation/Immunology
|
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions.
|
-
- HY-N0492A
-
Thioctic acid sodium; (±)-α-Lipoic acid sodium; DL-α-Lipoic acid sodium
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
|
α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
|
-
- HY-149391
-
|
Btk
PROTACs
|
Inflammation/Immunology
|
PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6).
|
-
- HY-102073
-
|
Glutaminase
Integrin
FAK
Src
|
Cancer
|
TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research.
|
-
- HY-155864
-
|
Others
|
Inflammation/Immunology
|
AJ2-30 is a SLCl5A4 inhibitor. AJ2-30 inhibits TLR9-mediated B cell activation. AJ2-30 block endogenous NOD signaling in human and mouse macrophages. AJ2-30 can be used for research of inflammation.
|
-
- HY-122936
-
|
Histone Methyltransferase
Keap1-Nrf2
Sirtuin
|
Cancer
Cardiovascular Disease
|
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research.
|
-
- HY-152949
-
|
Myosin
|
Neurological Disease
|
Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex.
|
-
- HY-124514
-
|
Ras
ERK
|
Cancer
|
UC-857993 is a selective SOS1-Ras inhibitor (Kd=14.7 μM, His6-SOS1cat), suppressing catalytic activity. UC-857993 also inhibits ERK and Ras activation, suppresses the growth of mouse embryonic fibroblasts (MEFs).
|
-
- HY-118482
-
Saurolactam
|
Others
|
Neurological Disease
|
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
|
-
- HY-112700
-
|
Phosphatase
|
Neurological Disease
|
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease.
|
-
- HY-13418A
-
Compound C; BML-275
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-154960
-
|
Microtubule/Tubulin
Apoptosis
Akt
|
Cancer
|
Tubulin/AKT1-IN-1 (Compound D1-1) is an inhibitor of tubulin polymerization and AKT pathway activation. Tubulin/AKT1-IN-1 significantly inhibits the proliferation and metastasis of H1975 cells and slightly induced their apoptosis and can be used for non-small-cell lung cancer (NSCLC) research .
|
-
- HY-114038
-
|
p38 MAPK
|
Inflammation/Immunology
|
SB-747651A is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A can be used for inflammation research.
|
-
- HY-110313
-
|
p38 MAPK
|
Inflammation/Immunology
|
SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research.
|
-
- HY-143235
-
|
Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
|
Cancer
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research.
|
-
- HY-N2344
-
Proanthocyanidin A1
|
PKC
|
Inflammation/Immunology
|
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
|
-
- HY-155786
-
|
TGF-beta/Smad
|
Others
|
3,7-DMF is an orally active inhibitor of TGF-β1-induced activation of HSCs. 3,7-DMF induces antioxidant genes and quenches ROS away, which can be used to study liver fibrosis.
|
-
- HY-103639
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis.
|
-
- HY-P5133
-
SSTN92-119
|
Integrin
|
Cancer
|
Synstatin (92-119) is an anti-tumor agent that inhibits angiogenesis and cancer cell invasion. Synstatin (92-119) down-regulates integrin α?β3 and reduces the activation of angiogenic growth factors VEGF and FGF-2.
|
-
- HY-147557
-
|
Others
|
Neurological Disease
|
PAC1R antagonist 1 (compound 3d) is a potent and orally active antagonist of PAC1 receptor. PAC1R antagonist 1 can inhibit pituitary adenylate cyclase-activating polypeptide (PACAP)- and nerve injury-induced allodynia.
|
-
- HY-122311
-
SMTP-7
|
Reactive Oxygen Species
|
Inflammation/Immunology
Neurological Disease
|
Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS.
|
-
- HY-N6807
-
|
Stearoyl-CoA Desaturase (SCD)
Influenza Virus
|
Cancer
Infection
|
Elemicin is a alkenylbenzene widely distributed in many herbs and spices. Elemicin inhibits Stearoyl-CoA Desaturase 1 (SCD1) by metabolic activation. Elemicin is one of the main components in aromatic food and has antimicrobial, antioxidant, and antiviral activities. Elemicin possesses genotoxicity and carcinogenicity.
|
-
- HY-N8812
-
|
NO Synthase
|
Inflammation/Immunology
|
19-[(β-D-Glucopyranosyl)oxy]-19-oxo-ent-labda-8(17),13-dien-16,15-olide, the metabolite of Neoandrographolide, inhibits nitric oxide (NO) production in lipopolysaccharide-activated macrophages.
|
-
- HY-N6641
-
|
Others
|
Cancer
Inflammation/Immunology
|
Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor).
|
-
- HY-114174
-
|
Amyloid-β
|
Neurological Disease
|
Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing.
|
-
- HY-B0285B
-
MK-870 hydrochloride dihydrate
|
Sodium Channel
Apoptosis
TRP Channel
|
Metabolic Disease
Cardiovascular Disease
|
Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel.
|
-
- HY-114335
-
|
NF-κB
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
Triphala, an Ayurvedic polyherbal formulation comprising of equiproportional fruit parts of Terminalia chebula, Terminalia bellerica, and Phyllanthus emblica. Triphala inhibits NF-κB activation. Triphala exerts antifungal action. Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities.
|
-
- HY-153343A
-
|
ERK
DGK
|
Cancer
|
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501 (HY-153343). BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer.
|
-
- HY-136741
-
|
IKK
|
Inflammation/Immunology
|
BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription.
|
-
- HY-110249
-
CINPA1
1 Publications Verification
|
Others
|
Metabolic Disease
|
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
|
-
- HY-145996
-
|
Bacterial
|
Infection
|
STC314 is a small polyanion that interact electrostatically with histones. STC314 blocks disruption of lipid-bilayers by histones that inhibits the cytotoxic, platelet-activating and erythrocyte-damaging effects of histones. STC314 has anti-infective effects and can be uesd for sepsis research.
|
-
- HY-147769
-
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 23 (Compound 4m) is an anti-inflammatory agent. Anti-inflammatory agent 23 inhibits the production of NO activated by LPS with an IC50 of 0.449 μM. Anti-inflammatory agent 23 has a good affinity for p65 protein.
|
-
- HY-103344
-
|
Aminopeptidase
mGluR
|
Inflammation/Immunology
Neurological Disease
|
ZJ43 is a potent NAAG peptidase inhibitor, with an IC50 of 2.4 nM and a Ki of 0.8 nM. ZJ43 sufficiently activates group II mGluR and reduces some of the behavioral effects of PCP. ZJ43 shows an analgesic effect in neuropathic and inflammatory and pain models.
|
-
- HY-124958
-
|
NF-κB
Dipeptidyl Peptidase
|
Metabolic Disease
Inflammation/Immunology
|
NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
|
-
- HY-114511
-
|
Others
|
Cardiovascular Disease
|
BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT).
|
-
- HY-N8884
-
|
PTEN
Akt
NF-κB
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein.
|
-
- HY-107613A
-
DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride
|
PKC
5-HT Receptor
|
Cancer
Infection
Inflammation/Immunology
|
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-15271A
-
|
mTOR
PI3K
|
Cancer
|
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-107613
-
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-151252
-
|
Proteasome
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.
|
-
- HY-146765
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
Neurological Disease
|
AMS-17 is a potent NLRP3 inhibitor, inhibiting microglia activation in vitro and in vivo. AMS-17 also inhibits cytokines such as caspase-1, TNF-α, IL-1β and inducible nitric oxide synthase (iNOS) in N9 cells. AMS-17 can be used for researching inflammation-associated neurological disorders.
|
-
- HY-101761
-
TM5441
5 Publications Verification
|
PAI-1
Apoptosis
|
Cancer
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.
|
-
- HY-110189S
-
3β-Hydroxy-5-pregnen-20-one monosulfate (sodium)-13C2,d2
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- 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-100112
-
|
RIP kinase
|
Others
|
WEHI-345 analog is the analog of WEHI-345. WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
|
-
- HY-N0651
-
|
Amyloid-β
|
Neurological Disease
|
Spinosyn a C-glycoside flavonoid isolated from the seeds of Zizyphus jujube, with neuroprotective effects. Spinosin inhibits Aβ1-42 production and aggregation via activating Nrf2/HO-1 pathway.
|
-
- HY-121685
-
|
Potassium Channel
|
Neurological Disease
|
Tipepidine reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine subsequently activates VTA dopamine neuron. Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect.
|
-
- HY-P5117
-
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice.
|
-
- HY-P9947
-
|
Integrin
|
Others
|
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research.
|
-
- HY-101942
-
CM-4620
|
CRAC Channel
|
Neurological Disease
|
Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
|
-
- HY-142972
-
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels.
|
-
- HY-121685A
-
|
Potassium Channel
|
Neurological Disease
|
Tipepidine hydrochloride reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine hydrochloride subsequently activates VTA dopamine neuron. Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
|
-
- HY-103254
-
ML221
5 Publications Verification
|
Apelin Receptor (APJ)
Arrestin
|
Neurological Disease
|
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
|
-
- HY-10619B
-
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-13755
-
|
HDAC
Keap1-Nrf2
Apoptosis
|
Cancer
Inflammation/Immunology
|
Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
|
-
- HY-P99161
-
BGB149
|
TAM Receptor
|
Cancer
|
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas.
|
-
- HY-116364
-
3'-Azido-3'-deoxythymidine-5'-triphosphate
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
|
Infection
|
AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.
|
-
- HY-B0004
-
|
Adenosine Receptor
Phosphodiesterase (PDE)
Reactive Oxygen Species
|
Inflammation/Immunology
|
Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm.
|
-
- HY-128588
-
|
STAT
Apoptosis
|
Cancer
|
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.
|
-
- HY-108355
-
|
PKC
|
Cancer
|
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
|
-
- HY-N6843
-
|
Caspase
PI3K
Akt
mTOR
STAT
|
Cancer
|
Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
|
-
- HY-146666
-
|
Apoptosis
STAT
|
Cancer
|
STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase.
|
-
- HY-108361
-
|
Ras
|
Inflammation/Immunology
Cancer
|
CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent.
|
-
- HY-W748591
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Amyloid-β
Apoptosis
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Cancer
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Cannflavin A can be isolated from Cannabis sativa L. Cannflavin A has anti-cancer, neuroprotective and anti-inflammatory activity. Cannflavin A inhibits Aβ1-42 aggregation. Cannflavin A also inhibits kynurenine-3-monooxygenase (KMO). Cannflavin A activates apoptosis via caspase-3 cleavage.
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- HY-15959
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Volitinib; HMPL-504; AZD-6094
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c-Met/HGFR
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Cancer
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Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity.
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- HY-P1111
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Src
Interleukin Related
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Inflammation/Immunology
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Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
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- HY-125542
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Apoptosis
PI3K
Akt
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Cancer
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DCZ3301 is a potent aryl-guanidino inhibitor. DCZ3301 inhibits cell proliferation, induces G2/M cell cycle arrest and apoptosis. DCZ3301 inhibits the activation of the PI3K/AKT pathway by downregulating the protein expression of PI3K and phosphorylation of AKT. DCZ3301 can be used in research of cancer.
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- HY-14654A
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- HY-10585AS1
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Sodium Valproate-d14 sodium
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Isotope-Labeled Compounds
HDAC
Autophagy
Mitophagy
HIV
Notch
Endogenous Metabolite
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Cancer
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Valproic acid-d14 (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
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- HY-149257
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JAK
STAT
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Cancer
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HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor with antitumor effects. HAT-SIL-TG-1&AT is the hypoxia-activated prodrug, witch inhibits JAK-STAT signaling in tumor tissue. And HAT-SIL-TG-1&AT inhibits HEL cells proliferation and downregulated phosphorylated STAT3/5 under hypoxic conditions.
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- HY-134901
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WM-3835
2 Publications Verification
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Histone Acetyltransferase
Apoptosis
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Cancer
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WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.
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- HY-156247
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NF-κB
MMP
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Cancer
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IVMT-Rx-3 is a inhibitor of SDCBP targeting of the PDZ1 and PDZ2 Domains of MDA-9/Syntenin. IVMT-Rx-3 blocks MDA-9/Syntenin interaction with Src, reduces NF-κB activation, and inhibits MMP-2/MMP-9 expression. IVMT-Rx-3 inhibits Melanoma Metastasis[1]
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- HY-116683
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MAL2-11B
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HSP
DNA/RNA Synthesis
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Cancer
Infection
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116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70.
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- HY-N3426
-
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NO Synthase
Akt
AMPK
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Metabolic Disease
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Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research.
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- HY-14590
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- HY-108565
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Prostaglandin Receptor
Adenylate Cyclase
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Cardiovascular Disease
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BMY 45778 is a non-prostanoid prostacyclin mimetic. BMY 45778 inhibits human (IC50 = 35 nM), rabbit (IC50: 136 nM) and rat (IC50 : 1.3 μM) platelet aggregation. BMY 45778 also activates adenylyl cyclase. BMY 45778 is a partial agonist at the prostacyclin receptor.
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- HY-17386B
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-
- HY-13649
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ZIO 301; D 24851
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Microtubule/Tubulin
Apoptosis
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Cancer
Neurological Disease
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Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.
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- HY-P99794
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BAY 1213790
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Factor Xa
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Cardiovascular Disease
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Osocimab (BAY 1213790), an anti-FXIa antibody (Ki=2.4 nM; EC50=0.2 nM). FXI inhibition may reduce the risk of thrombosis. Osocimab inhibits thrombin generation, and prolongs activated partial thromboplastin time. Osocimab exhibits anticoagulant effects.
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- HY-P0024
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DG3173; PTR-3173
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Somatostatin Receptor
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Cancer
Endocrinology
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Veldoreotide (DG3173) a somatostatin analogue, that can bind to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
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- HY-123422
-
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HIF/HIF Prolyl-Hydroxylase
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Cardiovascular Disease
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GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
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- HY-125827
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13-Methylberberinium chloride
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Interleukin Related
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Cancer
Metabolic Disease
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13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS.
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-
- HY-B0258
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-
- HY-17386
-
-
- HY-B0764
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Dibutyryl cAMP sodium salt; DBcAMP sodium salt
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PKA
Phosphodiesterase (PDE)
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Inflammation/Immunology
|
Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
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- HY-15415
-
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Na+/Ca2+ Exchanger
Autophagy
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Cancer
|
KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
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-
- HY-14460
-
|
FLAP
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Inflammation/Immunology
|
AM679 is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 2 nM in a human FLAP membrane binding assay. AM679 markedly reduces the respiratory syncytial virus-driven ocular pathology as well as the synthesis of cysteinyl leukotrienes (CysLTs) in the eye.
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-
- HY-139664
-
|
DNA Methyltransferase
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Cancer
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GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
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-
- HY-17386A
-
-
- HY-111053
-
|
Others
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Cancer
|
P11 is a selective inhibitor of platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3 that impairs cancer cell survival. P11 exhibits IC50 values of ~40 and 900 nM for PAFAH1b2 and 1b3, respectively.
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-
- HY-149913
-
|
Others
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Cancer
|
NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model.
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-
- HY-N2553
-
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LPL Receptor
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Metabolic Disease
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.
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-
- HY-10619E
-
MK-4827 tosylate hydrate
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PARP
Apoptosis
|
Cancer
|
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
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-
- HY-10619
-
MK-4827
|
PARP
Apoptosis
|
Cancer
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
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-
- HY-133859
-
|
Mitochondrial Metabolism
|
Metabolic Disease
|
M084 is a benzimidazole derivative. M084 inhibits the mitochondrial respiration, activate mitochondrial unfolded protein response and AMPK, recruites SIR-2.1 and SKN-1, and finally through the transcription factor DAF-16, delays the aging process of C. elegans.
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-
- HY-118266
-
BTdCPU
1 Publications Verification
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Phosphatase
Apoptosis
|
Cancer
|
BTdCPU is a potent heme regulated inhibitor kinase (HRI) activator that promotes eIF2α phosphorylation and induces apoptosis in Dexamethasone (HY-14648) (Dex)-resistant cancer cells. BTdCPU can be used in the study of cancers such as multiple myeloma and Dex-resistant multiple myeloma.
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-
- HY-153793
-
|
DGK
|
Cancer
|
DGKζ-IN-1 (compound 9) is an inhibitor of DGKζ. DGKζ-IN-1 can be used for research in cancer related to immunocyte activation or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody.
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-
- HY-10619A
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MK-4827 hydrochloride
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PARP
|