Search Result
Results for "Activators" in MCE Product Catalog:
1202
Inhibitors & Agonists
Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-P1328
-
TAT-14
|
Keap1-Nrf2
|
Others
|
TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-P1328A
-
TAT-14 TFA
|
Keap1-Nrf2
|
Others
|
TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-133987
-
AP-1/NF-κB activation inhibitor 1
|
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-P0078
-
TRAP-6
PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6
|
Protease-Activated Receptor (PAR)
|
Inflammation/Immunology
|
TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
|
-
- HY-117958
-
HJC0197
|
Others
|
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-102011
-
BMS-1166
|
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-113313
-
Aldosterone
|
Endogenous Metabolite
|
Cardiovascular Disease
|
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
|
-
- HY-103349
-
PETCM
|
Caspase
Apoptosis
|
Cancer
|
PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
|
-
- HY-13856
-
(R)-PS210
|
PDK-1
|
Cancer
|
(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
|
-
- HY-15870
-
SR 11302
|
Others
|
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-19121A
-
TCV-309 chloride
|
Others
|
Cancer
|
TCV-309 chloride is a potent and specific platelet activating factor (PAF) antagonist. TCV-309 chloride specifically inhibits PAF-induced aggregation of rabbit and human platelets, and [3H]PAF binding to rabbit platelet microsomes with IC50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock.
|
-
- HY-115537
-
NAE-IN-M22
|
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-101923B
-
-
- HY-12545
-
Brevetoxin-3
PbTx-3
|
Sodium Channel
|
Inflammation/Immunology
|
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
|
-
- HY-101042
-
AG-494
Tyrphostin AG 494
|
EGFR
CDK
|
Cancer
|
AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
|
-
- HY-10595
-
-
- HY-15394
-
-
- HY-P2230
-
Angstrom6
A6 Peptide
|
PAI-1
|
Cancer
|
Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
|
-
- HY-14165
-
-
- HY-112257
-
S-23
|
Androgen Receptor
|
Metabolic Disease
|
S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
|
-
- HY-124858
-
SC99
|
STAT
JAK
Apoptosis
|
Cancer
Cardiovascular Disease
|
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.
|
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- HY-12496
-
-
- HY-N0336
-
3-Butylidenephthalide
Butylidenephthalide
|
Parasite
|
Infection
|
3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae).
|
-
- HY-78263
-
MNS
NSC 170724; 5-(2-Nitrovinyl)benzodioxole
|
Src
Syk
|
Cancer
|
MNS (NSC 170724), the beta-nitrostyrene derivative, is a potent tyrosine kinase inhibitor and a broad-spectrum antiplatelet agent. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC50 values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively.
|
-
- HY-12884
-
OAC2
|
Oct3/4
|
Others
|
OAC2 is an Oct4-activating compound which activates expression through the Oct4 gene promoter.
|
-
- HY-19734
-
NK-252
|
Keap1-Nrf2
|
Cancer
|
NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
|
-
- HY-12831
-
-
- HY-107301
-
-
- HY-19339
-
-
- HY-134477
-
NF-κΒ activator 2
|
NF-κB
|
Neurological Disease
|
NF-κΒ activator 2 is a potent and orally active NF-ҡB activator, with an EC50 of 1.58 μM. NF-κΒ activator 2 induces SOD2 through increasing NF-ҡB expression and activation. NF-κΒ activator 2 can be used for the research of amyotrophic lateral sclerosis (ALS).
|
-
- HY-100508
-
ITSA-1
|
HDAC
|
Cancer
|
ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
|
-
- HY-13103
-
NS 11021
|
Potassium Channel
|
Others
|
NS 11021 is a potent and specific Ca 2-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
|
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- HY-15122
-
-
- HY-P1308
-
-
- HY-P0283
-
-
- HY-15122A
-
-
- HY-12689
-
-
- HY-P1308A
-
-
- HY-131334
-
AMPK activator 4
|
AMPK
|
Metabolic Disease
|
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
|
-
- HY-13971
-
-
- HY-135825
-
TFEB activator 1
|
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-114304
-
COH000
|
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.
|
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- HY-134476
-
-
- HY-P0297
-
-
- HY-107988
-
-
- HY-N6631
-
-
- HY-117656
-
ESI-05
NSC 116966
|
Others
|
Others
|
ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.
|
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- HY-N0277
-
-
- HY-N1446B
-
-
- HY-104038
-
-
- HY-100548
-
GSK621
|
AMPK
Autophagy
Apoptosis
|
Cancer
|
GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
|
-
- HY-100221
-
-
- HY-N0625A
-
-
- HY-12070
-
DPH
|
Bcr-Abl
|
Cancer
|
DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.
|
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- HY-19635A
-
-
- HY-100381
-
-
- HY-B0493
-
-
- HY-110153
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NS19504
|
Potassium Channel
|
Neurological Disease
|
NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
|
-
- HY-N1446
-
-
- HY-108330
-
AG126
Tyrphostin AG126
|
ERK
|
Inflammation/Immunology
|
AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
|
-
- HY-70002
-
-
- HY-102052
-
DCEBIO
|
Potassium Channel
|
Inflammation/Immunology
|
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl - secretion in T84 colonic cells. DCEBIO stimulates Cl - secretion via the activation of hIK1 K + channels and the activation of an apical membrane Cl - conductance.
|
-
- HY-101047
-
D-erythro-Sphingosine
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-15336
-
AG 555
Tyrphostin AG 555
|
EGFR
Reverse Transcriptase
|
Cancer
|
AG 555 (Tyrphostin AG 555), a potent antiretroviral drug, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
|
-
- HY-N2312
-
Mogrol
|
ERK
STAT
|
Cancer
|
Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
|
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- HY-10484
-
-
- HY-108593
-
-
- HY-70062
-
-
- HY-12303
-
OAC1
|
Oct3/4
|
Others
|
OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.
|
-
- HY-14714
-
-
- HY-N2632
-
Uvarigrin
|
Apoptosis
|
Cancer
|
Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
|
-
- HY-100489
-
TBHQ
tert-Butylhydroquinone
|
Keap1-Nrf2
ERK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
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-
- HY-14754
-
Salirasib
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.
|
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- HY-131018
-
-
- HY-12647
-
-
- HY-P2519
-
-
- HY-B0167
-
-
- HY-103368
-
Eact
|
Chloride Channel
|
Neurological Disease
|
Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity.
|
-
- HY-15542A
-
FRAX597
|
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-17538
-
-
- HY-104047
-
-
- HY-14290A
-
-
- HY-75342
-
-
- HY-U00292
-
-
- HY-N0509
-
-
- HY-15027
-
-
- HY-133615
-
8(14)-Abietenic acid
|
Others
|
Others
|
8(14)-Abietenic acid is an abietane diterpenoid. Abietenic acid is racemic of 8(14)-Abietenic acid. Abietenic acid acts as a PPARα/γ dual activator.
|
-
- HY-15542B
-
FRAX486
|
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
-
-
- HY-19635
-
G-5555
|
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-101069
-
-
- HY-N2432
-
Paederoside
|
HBV
|
Cancer
Infection
|
Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virus activation.
|
-
- HY-108391
-
C8-Ceramide
N-Octanoyl-D-erythro-sphingosine
|
Others
|
Cancer
Inflammation/Immunology
|
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a synthetic cell-permeable analog of endogenous ceramides, interfered with cell proliferation, and was cytotoxic to papilloma virus-containing human cervix carcinoma cells. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections.
|
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- HY-14233
-
-
- HY-15723A
-
-
- HY-P0240
-
-
- HY-101594
-
-
- HY-101675
-
-
- HY-135516
-
Wnt pathway activator 1
|
Wnt
|
Cancer
|
Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an IC50s of 28-29 nM.
|
-
- HY-133614
-
Dihydroisopimaric acid
|
Potassium Channel
|
Others
|
Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.
|
-
- HY-B0289
-
-
- HY-12005
-
-
- HY-N1380
-
-
- HY-P2518
-
-
- HY-13764
-
-
- HY-N6892
-
3'-O-Acetylhamaudol
|
Others
|
Cancer
|
3'-O-Acetylhamaudol, isolated from Angelica japonica roots, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.
|
-
- HY-N6065
-
Praeruptorin A
|
NF-κB
|
Inflammation/Immunology
|
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
|
-
- HY-123879
-
BAA473
|
Others
|
Inflammation/Immunology
|
BAA473 is a bile acid analog and is a potent activator of the pyrin inflammasome that induces the secretion of interleukin 18 (IL-18) through activation of the inflammasome in both myeloid and intestinal epithelial cells.
|
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- HY-111363
-
-
- HY-112483
-
-
- HY-N0019
-
-
- HY-15964
-
-
- HY-N0865
-
Ingenol
(-)-Ingenol
|
PKC
|
Cancer
|
Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
|
-
- HY-N0831
-
Jaceosidin
|
Bcl-2 Family
COX
Apoptosis
|
Cancer
Inflammation/Immunology
|
Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
|
-
- HY-100783A
-
(-)-Bicuculline methochloride
l-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
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-
- HY-15416
-
-
- HY-18749
-
-
- HY-100783
-
(-)-Bicuculline methobromide
l-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-18633
-
MDK83190
|
Apoptosis
|
Cancer
|
MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner.
|
-
- HY-17397
-
Strontium Ranelate
Distrontium renelate; S12911
|
CaSR
|
Metabolic Disease
|
Strontium Ranelate (S12911) is an antiosteoporotic agent that acts by reducing bone resorption and promoting bone formation, thereby inducing a positive bone balance. Strontium Ranelate also can activate the calcium-sensing receptor (CaSR) in non skeletal cells, resulting in the activation of inositol 1, 4, 5-triphosphate production and mitogen-activated protein kinase signaling.
|
-
- HY-14452
-
Fatostatin
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-12695
-
Guanosine 5'-triphosphate trisodium salt
5'-GTP trisodium salt
|
Endogenous Metabolite
|
Others
|
Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins which are involved in various cellular processes including proliferation, differentiation, and activation of several intracellular kinase cascades.
|
-
- HY-N0052A
-
Sanguinarine chloride
Sanguinarin chloride; Sanguinarium chloride; Pseudochelerythrine chloride
|
Apoptosis
Autophagy
Bacterial
Parasite
|
Cancer
|
Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
|
-
- HY-N0052
-
Sanguinarine
Sanguinarin; Sanguinarium; Pseudochelerythrine
|
Apoptosis
Autophagy
|
Cancer
|
Sanguinarine (Sanguinarin), a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
|
-
- HY-14255
-
-
- HY-112060
-
-
- HY-12376
-
-
- HY-13529
-
-
- HY-P1536
-
-
- HY-100472
-
ZYZ-488
|
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
-
NSC-70220
|
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-136173
-
TNO155
|
Phosphatase
|
Cancer
|
TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
|
-
- HY-100234A
-
-
- HY-W018781
-
Benzamidine hydrochloride
|
Ser/Thr Protease
|
Cancer
|
Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively.
|
-
- HY-18772
-
O4I2
|
Oct3/4
|
Others
|
O4I2 is a potent Oct3/4 inducer. O4I2 induces the expression of pluripotent-associated genes Lin28, Sox2 and Nanog, and suppresses Rex1.
|
-
- HY-135303
-
GLPG1205
|
GPR84
|
Inflammation/Immunology
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
|
-
- HY-100234
-
-
- HY-123962
-
-
- HY-P0256
-
-
- HY-N6258
-
Kahweol
|
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-N0608
-
Myrislignan
|
NF-κB
|
Inflammation/Immunology
|
Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
|
-
- HY-12754
-
ML228
CID-46742353
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
|
-
- HY-10162
-
Olaparib
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-B1197
-
-
- HY-14909
-
-
- HY-59047
-
-
- HY-P0136
-
-
- HY-115685
-
-
- HY-14256
-
-
- HY-10164
-
-
- HY-100295
-
-
- HY-U00040
-
-
- HY-10249
-
GSK-690693
|
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-14452A
-
Fatostatin hydrobromide
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-N0699
-
Daphnoretin
Dephnoretin; Thymelol
|
PKC
Influenza Virus
|
Infection
|
Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst.
|
-
- HY-128591
-
DIPQUO
|
Others
|
Metabolic Disease
|
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
|
-
- HY-110105
-
NS8593 hydrochloride
|
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-107406
-
Antimycin A1
|
Mitochondrial Metabolism
|
Cancer
|
Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
|
-
- HY-N6688
-
Verruculogen
|
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-P0256A
-
-
- HY-P1847A
-
-
- HY-100602
-
-
- HY-U00434
-
-
- HY-14181
-
-
- HY-N3463
-
-
- HY-N0553
-
-
- HY-N0441
-
-
- HY-101214
-
-
- HY-N0933
-
-
- HY-100153
-
-
- HY-14181A
-
-
- HY-101918
-
DS-1040 Tosylate
|
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-N0608A
-
(Rac)-Myrislignan
|
NF-κB
|
Inflammation/Immunology
|
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
|
-
- HY-18739
-
-
- HY-N2433
-
Paederosidic acid methyl ester
|
Potassium Channel
|
Neurological Disease
|
Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
|
-
- HY-123054
-
BTSA1
|
Bcl-2 Family
Apoptosis
|
Cancer
|
BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
|
-
- HY-135388
-
ent-Ezetimibe
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-18377
-
Bioymifi
DR5 Activator
|
TNF Receptor
Apoptosis
|
Cancer
|
Bioymifi (DR5 Activator), a potent TRAIL receptor DR5 activator, binds to the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM. Bioymifi can act as a single agent to induce DR5 clustering and aggregation, leading to apoptosis.
|
-
- HY-136268
-
-
- HY-19706
-
ARS-853
|
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
-
-
- HY-P1376
-
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
|
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-B0167S
-
-
- HY-N6577
-
-
- HY-76847
-
-
- HY-100242
-
-
- HY-50662
-
-
- HY-15341
-
-
- HY-15300
-
-
- HY-104005
-
-
- HY-16397A
-
-
- HY-101804
-
-
- HY-100415
-
UKI-1
UKI-1C
|
Others
|
Infection
|
UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system.
|
-
- HY-19739
-
JW74
|
Wnt
|
Cancer
|
JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
|
-
- HY-108573
-
P-1075
|
Potassium Channel
|
Cardiovascular Disease
|
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
|
-
- HY-101180
-
C2 Ceramide
Ceramide 2
|
Phosphatase
Mitochondrial Metabolism
Apoptosis
|
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 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-117727
-
Leriglitazone
Hydroxypioglitazone
|
PPAR
|
Metabolic Disease
|
Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.
Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.
Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50
of 680 nM.
|
-
- HY-109121
-
Reldesemtiv
CK-2127107
|
Others
|
Cardiovascular Disease
|
Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model.
|
-
- HY-108638
-
NSC 146109 hydrochloride
|
MDM-2/p53
|
Cancer
|
NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and could be of value in treating breast cancer.
NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes[1].
|
-
- HY-103666
-
CY-09
|
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-131265
-
-
- HY-12316
-
20(S)-Hydroxycholesterol
20α-Hydroxycholesterol
|
Smo
Endogenous Metabolite
|
Cancer
|
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
|
-
- HY-W017212
-
Methyl cinnamate
Methyl 3-phenylpropenoate
|
Tyrosinase
Bacterial
AMPK
|
Infection
Metabolic Disease
|
Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
|
-
- HY-P1376A
-
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-100581
-
CORM-3
|
NF-κB
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
CORM-3, a carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels. CORM-3 reduces NLRP3 inflammasome activation.
|
-
- HY-P0190
-
Iberiotoxin
|
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-W006230
-
Anthraflavic acid
|
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-103000
-
-
- HY-100447
-
-
- HY-B1140
-
-
- HY-B0162A
-
-
- HY-B0809
-
-
- HY-16271
-
Kevetrin hydrochloride
4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
|
MDM-2/p53
|
Cancer
|
Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
|
-
- HY-101625
-
Recilisib
Ex-RAD; ON 01210
|
Akt
PI3K
|
Cancer
|
Recilisib is a radioprotectant, which can activate AKT, PI3K activities in cells.
|
-
- HY-128642
-
FAPI-2
|
Others
|
Cancer
|
FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
|
-
- HY-12359
-
-
- HY-114363A
-
SRI 31215 TFA
|
c-Met/HGFR
|
Cancer
|
SRI 31215 (TFA), a triplex inhibitor of matriptase, hepsin and hepatocyte growth factor activator (HGFA) with IC50s of 0.69 μM, 0.65 μM, 0.3 μM, blocks pro-HGF activation and thus mimics the activity of HAI-1/2.
|
-
- HY-108635
-
-
- HY-N3807
-
Enniatin B1
|
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-15477A
-
YS-49 monohydrate
|
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
-
YS-49
|
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-N0279
-
-
- HY-P1740
-
RGD peptide (GRGDNP)
|
Integrin
Apoptosis
|
Inflammation/Immunology
|
RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
|
-
- HY-116330A
-
Hyperforin dicyclohexylammonium salt
Hyperforin DCHA
|
TRP Channel
Calcium Channel
|
Neurological Disease
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
|
-
- HY-14266
-
Dapivirine
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-112558
-
-
- HY-P1260
-
-
- HY-124960
-
-
- HY-17517
-
Tiadinil
|
Bacterial
|
Infection
|
Tiadinil is a plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles; fungicide.
|
-
- HY-112473
-
-
- HY-12639
-
Bephenium
|
Parasite
|
Infection
|
Bephenium is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
|
-
- HY-B1058
-
-
- HY-101371
-
Hesperin
|
Keap1-Nrf2
|
Cancer
|
Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
|
-
- HY-32348
-
-
- HY-111441
-
-
- HY-B0131
-
-
- HY-12885A
-
-
- HY-128643
-
FAPI-4
|
Others
|
Cancer
|
FAPI-4 is a fibroblast activation protein (FAP) inhibitor used in cancer research.
|
-
- HY-P0249A
-
-
- HY-107854
-
-
- HY-15840
-
YLF-466D
C24
|
AMPK
|
Cancer
|
YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
|
-
- HY-106199
-
-
- HY-N1990
-
Gypenoside XLIX
|
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-136427
-
KRM-III
|
Others
|
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-10255A
-
Sunitinib
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-N2485
-
4'-Methoxyresveratrol
4'-O-Methylresveratrol
|
Others
|
Inflammation/Immunology
|
4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
|
-
- HY-114398
-
BAY-293
|
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
-
Gardiquimod diTFA
|
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-12519
-
Oltipraz
RP 35972; NSC 347901
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
|
Cancer
|
Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
|
-
- HY-B0167A
-
-
- HY-P1740A
-
RGD peptide (GRGDNP) (TFA)
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
|
-
- HY-10119
-
Vorapaxar
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-P0316
-
TP508
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-12639A
-
-
- HY-U00458
-
K-80003
TX-803
|
Akt
|
Cancer
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-W040055
-
-
- HY-P1260A
-
-
- HY-B1897A
-
Menadione bisulfite sodium
Menadione sodium bisulfite; Vitamin K3 sodium bisulfite
|
Others
|
Infection
|
Menadione bisulfite (sodium) is used as an agent to induce acute oxidative stress, and to function as a plant-defense activator against several pathogens.
|
-
- HY-18965
-
-
- HY-N0486
-
-
- HY-18723
-
-
- HY-137477
-
-
- HY-15252
-
-
- HY-117793
-
-
- HY-N0492
-
-
- HY-10255
-
Sunitinib Malate
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-N0896
-
Inulicin
1-O-Acetylbritannilactone
|
NF-κB
COX
|
Cancer
Inflammation/Immunology
|
Inulicin (1-O-Acetylbritannilactone) is an active compound isolated from Inula Britannica L. Inulicin (1-O-Acetylbritannilactone) 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-P1375
-
[D-Trp7,9,10]-Substance P
|
mAChR
|
|
[D-Trp7,9,10]-Substance P is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-124822
-
COH-SR4
|
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, and can be used for the research of obesity and related metabolic disorders.
|
-
- HY-W015445
-
SD-169
|
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-136477
-
Pentagamavunon-1
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-124748A
-
-
- HY-19800
-
ML-098
CID-7345532
|
Ras
|
Cancer
|
ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM.
|
-
- HY-N0897
-
Corylifol A
Corylifol-A; Corylinin
|
STAT
|
Others
|
Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
|
-
- HY-108599
-
-
- HY-13523
-
-
- HY-N8418
-
-
- HY-108599A
-
DCPLA-ME
DCPLA methyl ester
|
PKC
|
Neurological Disease
|
DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.
|
-
- HY-N1913
-
-
- HY-111498
-
-
- HY-N6971
-
-
- HY-15530
-
-
- HY-B1399
-
-
- HY-N2318
-
-
- HY-50703
-
MK-2461
|
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-N0290
-
-
- HY-13757A
-
Tamoxifen
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.
|
-
- HY-16561
-
Resveratrol
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.
|
-
- HY-P1375A
-
[D-Trp7,9,10]-Substance P TFA
|
mAChR
|
|
[D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-129390
-
Orelabrutinib
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-B1816
-
-
- HY-124037
-
SRT 1460
|
Sirtuin
|
Cancer
|
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
|
-
- HY-P0316A
-
TP508 TFA
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-N7526
-
Naphthazarin
DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone
|
Apoptosis
|
Cancer
Neurological Disease
|
Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
|
-
- HY-108586
-
NS3623
|
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-50694
-
Senicapoc
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-117433
-
-
- HY-N0516
-
Casticin
Vitexicarpin
|
STAT
|
Inflammation/Immunology
|
Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
|
-
- HY-17613
-
Evocalcet
KHK7580
|
CaSR
|
Metabolic Disease
|
Evocalcet has an activating effect on calcium sensing receptor (CaSR) extracted from patent WO 2017061621 A1, compound A.
|
-
- HY-101396
-
-
- HY-13719
-
Oleandrin
|
Na+/K+ ATPase
Apoptosis
|
Cancer
|
Oleandrin inhibits the Na +, K +-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.
|
-
- HY-101346
-
-
- HY-N0628
-
-
- HY-15577
-
GSK3787
|
PPAR
|
Cancer
|
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
|
-
- HY-10590
-
-
- HY-19793
-
-
- HY-N1411
-
-
- HY-B0887
-
Permethrin
NRDC-143
|
Parasite
|
Infection
|
Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
|
-
- HY-18985
-
-
- HY-14645A
-
(+)-DHMEQ
(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-17363
-
-
- HY-103638
-
-
- HY-112125A
-
-
- HY-19097
-
-
- HY-101580
-
Paliroden
SR 57667
|
Others
|
Neurological Disease
|
Paliroden is an orally bioactive neurotrophic, non-peptidic compound that activates synthesis of endogenous neurotrophines, used for treatment of Alzheimer's Disease and Parkinson's.
|
-
- HY-P0195
-
-
- HY-111202
-
-
- HY-133596
-
12,14-Dichlorodehydroabietic acid
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
|
-
- HY-77251
-
TAK1/MAP4K2 inhibitor 1
|
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-114372
-
Lycopodine
|
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-117102
-
ANI-7
|
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-13757
-
Tamoxifen Citrate
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.
|
-
- HY-14994
-
SCH79797 dihydrochloride
|
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-128586A
-
-
- HY-107004A
-
-
- HY-19330
-
-
- HY-B0686
-
-
- HY-100941
-
-
- HY-P1534
-
-
- HY-Y1683
-
DL-Menthol
Racementhol
|
GABA Receptor
|
Others
|
DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol induces surgical anesthesia for fish that relates to the activation of GABAA receptor.
|
-
- HY-N2506
-
-
- HY-P0249
-
-
- HY-B0686A
-
-
- HY-B0923
-
Danthron
Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone
|
AMPK
Autophagy
Bacterial
Virus Protease
|
Cancer
|
Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
|
-
- HY-15869
-
-
- HY-128586
-
-
- HY-14831
-
Arhalofenate
MBX 102; JNJ 39659100
|
PPAR
|
Metabolic Disease
|
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
|
-
- HY-13519
-
-
- HY-78131B
-
-
- HY-100407
-
JNJ16259685
|
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-130354
-
Dibutyryl-cGMP sodium
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-112769
-
EX229
|
AMPK
|
Metabolic Disease
|
EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
|
-
- HY-B1546
-
Benzamil
Benzylamiloride
|
Sodium Channel
Na+/Ca2+ Exchanger
|
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-116084
-
-
- HY-18307
-
SYN1143
|
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-B1546A
-
Benzamil hydrochloride
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-126429
-
Nav1.1 activator 1
|
Sodium Channel
|
Neurological Disease
|
Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant τ of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
|
-
- HY-100410
-
FCCP
Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone
|
Mitochondrial Metabolism
|
Cancer
|
FCCP is an uncoupler of oxidative phosphorylation (OXPHOS) in mitochondria. FCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
|
-
- HY-108594
-
-
- HY-W011641
-
-
- HY-19354
-
Aglafoline
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-16785
-
-
- HY-B0513
-
-
- HY-15251
-
-
- HY-N6630
-
-
- HY-103683
-
-
- HY-15285
-
-
- HY-N2283
-
-
- HY-N0593
-
-
- HY-32735
-
Triptolide
PG490
|
NF-κB
Apoptosis
|
Cancer
|
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.
|
-
- HY-111789
-
-
- HY-12213
-
CDDO-EA
CDDO ethyl amide; TP319; RTA 405
|
Keap1-Nrf2
|
Cancer
|
CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
|
-
- HY-127018
-
Maltoheptaose
|
Others
|
Metabolic Disease
|
Maltoheptaose is an activator of phosphorylase B to prepare heptulose-2-phosphate. Maltoheptaose is a maltooligosaccharide contanins seven glucose units.
|
-
- HY-N2084
-
-
- HY-N0593A
-
-
- HY-136352
-
Adenosine 5'-succinate
|
Others
|
Others
|
Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
|
-
- HY-131281
-
Ivabradine impurity 1
|
Others
|
Others
|
Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-50910
-
Temsirolimus
CCI-779
|
mTOR
Autophagy
Apoptosis
|
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-109128
-
Danicamtiv
|
Myosin
|
Cancer
|
Danicamtiv, an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
|
-
- HY-101833
-
YM-264
|
Others
|
Inflammation/Immunology
|
YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
|
-
- HY-101746
-
GSK376501A
|
PPAR
|
Metabolic Disease
|
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
|
-
- HY-W007355
-
-
- HY-127018A
-
-
- HY-12524
-
Bikinin
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-131282
-
Ivabradine impurity 2
|
Others
|
Others
|
Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-N6946
-
Mitraphylline
|
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
-
-
- HY-112920
-
TM-25659
|
Others
|
Metabolic Disease
|
TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
|
-
- HY-N7018
-
20-Hydroxyganoderic Acid G
|
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 drug discovery of nerve inflammation diseases associated with microglia activated by LPS.
|
-
- HY-B1221
-
Flufenamic acid
|
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-16592
-
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
|
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-14600
-
-
- HY-103370
-
Talniflumate
BA 7602-06
|
Chloride Channel
|
Inflammation/Immunology
|
Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.
|
-
- HY-107818
-
4-Hydroxychalcone
|
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
-
RSVA405
|
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 also can be used for the research of obesity.
|
-
- HY-131035
-
Lys-CoA TFA
|
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-12323
-
ISX-9
Isoxazole 9
|
Others
|
Neurological Disease
|
ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+ influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).
|
-
- HY-16312
-
MDL-29951
|
iGluR
|
Neurological Disease
|
MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [ 3H]glycine binding in vitro and in vivo.
|
-
- HY-111098
-
-
- HY-111634
-
Epsilon-momfluorothrin
|
Others
|
Cancer
|
Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats.
|
-
- HY-111928
-
-
- HY-N2209
-
Angeloylgomisin H
|
PPAR
|
Metabolic Disease
|
Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating PPAR-γ.
|
-
- HY-15707
-
-
- HY-12885
-
ADU-S100
MIW815; ML RR-S2 CDA
|
STING
|
Inflammation/Immunology
|
ADU-S100 (MIW815), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.
|
-
- HY-12357
-
-
- HY-15253
-
-
- HY-13694
-
-
- HY-131283
-
-
- HY-Y0152
-
Cinchonine
(8R,9S)-Cinchonine; LA40221
|
Apoptosis
Parasite
|
Cancer
|
Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
|
-
- HY-N0708
-
-
- HY-N0606
-
-
- HY-N0892
-
-
- HY-N6913
-
3α-Hydroxymogrol
|
AMPK
|
Metabolic Disease
|
3α-Hydroxymogrol is a triterpenoid isolated from Siraitia grosvenorii Swingle, acts as a potent AMPK activator, and enhances AMPK phosphorylation.
|
-
- HY-N7452
-
-
- HY-B0099
-
-
- HY-13259
-
MG-132
Z-Leu-Leu-Leu-al; MG132
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
|
-
- HY-100487
-
TAK-243
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-137862
-
1-Oleoyl lysophosphatidic acid
1-Oleoyl-sn-glycero-3-phosphate; 1-Oleoyl-LPA
|
LPL Receptor
|
Neurological Disease
|
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant LPA species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation. 1-Oleoyl lysophosphatidic acid increases SRE-drivenβ-galactosidase activity.
|
-
- HY-12695B
-
-
- HY-15002
-
AST 487
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-119240
-
-
- HY-N3196
-
-
- HY-10535
-
Evofosfamide
TH-302
|
Apoptosis
|
Cancer
|
Evofosfamide (TH-302) is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
|
-
- HY-15718A
-
-
- HY-B1378
-
-
- HY-P0004
-
Lysipressin
Lysine vasopressin; [Lys8]-Vasopressin
|
Others
|
Others
|
Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families. Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase.
|
-
- HY-A0070
-
-
- HY-137207
-
MK-28
|
PERK
|
Neurological Disease
|
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
|
-
- HY-115453
-
UBCS039
|
Sirtuin
Autophagy
|
Cancer
|
UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
|
-
- HY-19205A
-
-
- HY-101929
-
-
- HY-108634
-
Apafant
WEB 2086
|
Others
|
Inflammation/Immunology
|
Apafant (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
|
-
- HY-A0070A
-
-
- HY-125465
-
SLLN-15
|
Autophagy
|
Cancer
|
SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
|
-
- HY-13108
-
Bz 423
BZ48
|
Bcl-2 Family
|
Inflammation/Immunology
|
Bz 423 is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
|
-
- HY-N2530
-
-
- HY-12306
-
8-Bromo-cAMP sodium salt
8-Br-Camp sodium salt
|
PKA
|
Cancer
|
8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
|
-
- HY-13294
-
-
- HY-100611
-
-
- HY-15145
-
-
- HY-75992
-
trans-Doxercalciferol
|
Others
|
Others
|
trans-Doxercalciferol is an isomer of Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
|
-
- HY-N2025
-
Oroxin A
|
PARP
Glucosidase
|
Metabolic Disease
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE), activates peroxisome proliferator-activated receptor γ (PPARγ) by docking into the PPARγ protein ligand-binding domain. Oroxin A exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
|
-
- HY-16915
-
RPR-260243
|
Potassium Channel
|
Cardiovascular Disease
|
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel.
|
-
- HY-124151
-
Adenosine-2'-monophosphate
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-P1061A
-
Colivelin TFA
|
STAT
Amyloid-β
|
Neurological Disease
|
Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
|
-
- HY-131296
-
5-A-RU-PABC-Val-Cit-Fmoc
|
Others
|
Inflammation/Immunology
|
5-A-RU-PABC-Val-Cit-Fmoc is the prodrug of 5-A-RU. 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
|
-
- HY-110247
-
TRAF-STOP inhibitor 6877002
|
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-134205A
-
CBR-470-1
|
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-19356
-
Rocaglamide
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-108596
-
BL-1249
|
Potassium Channel
|
Inflammation/Immunology
|
BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
|
-
- HY-P1314
-
-
- HY-N0377
-
-
- HY-16511
-
Upamostat
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-W011303
-
Phytosphingosine
|
Apoptosis
|
Cancer
|
Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells.
|
-
- HY-15098
-
Apoptozole
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-112675
-
-
- HY-75041
-
Calcitriol Impurities A
|
VD/VDR
|
Metabolic Disease
|
Calcitriol Impurities A is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-50714
-
Quiflapon sodium
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-15725
-
-
- HY-110192
-
-
- HY-109030
-
-
- HY-16642A
-
-
- HY-100965
-
-
- HY-112929
-
DT-061
|
Phosphatase
|
Cancer
|
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
|
-
- HY-12343
-
-
- HY-N2370
-
-
- HY-19700
-
-
- HY-N0436
-
Engeletin
|
NF-κB
|
Infection
Inflammation/Immunology
|
Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-103640
-
WR-1065 dihydrochloride
|
MDM-2/p53
|
Cancer
|
WR-1065 dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.
|
-
- HY-13296
-
PYR-41
|
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
-
Ro-24-0238
|
Others
|
Inflammation/Immunology
|
Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
|
-
- HY-107780
-
Cyclic-di-GMP
c-di-GMP; cyclic diguanylate; 5GP-5GP
|
STING
Endogenous Metabolite
|
Cancer
|
Cyclic-di-GMP (c-di-GMP) is a STING activator and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.
|
-
- HY-N0629
-
-
- HY-12885B
-
ADU-S100 ammonium salt
MIW815 ammonium salt; ML RR-S2 CDA ammonium salt
|
STING
|
Inflammation/Immunology
|
ADU-S100 ammonium salt (MIW815 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.
|
-
- HY-124697
-
BMP signaling agonist sb4
|
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-N1970
-
5,7-Dihydroxychromone
|
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-17394
-
-
- HY-118266
-
BTdCPU
|
Phosphatase
Apoptosis
|
Cancer
|
BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator. BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.
|
-
- HY-N6781
-
Ophiobolin A
|
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-N0177
-
Diosgenin
|
STAT
|
Metabolic Disease
|
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
|
-
- HY-13772
-
Valrubicin
AD-32
|
PKC
|
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
-
Eupalinolide A
|
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-N4322
-
-
- HY-77274
-
Calcitriol Impurities D
|
VD/VDR
|
Metabolic Disease
|
Calcitriol Impurities D is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-N0474
-
-
- HY-112331
-
SJ000291942
|
TGF-β Receptor
|
Cancer
|
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
|
-
- HY-A0084
-
Procainamide hydrochloride
|
Autophagy
|
Cancer
|
Procainamide hydrochloride is an anti-arrhythmic agent and is used to treat cardiac arrhythmia; induces rapid block of the batrachotoxin(BTX)-activated sodium channels of the heart muscle and acts as antagonist to long gating closures.
|
-
- HY-103087
-
FIN56
|
Ferroptosis
|
Others
|
FIN56 is a specific inducer of ferroptosis. FIN56 induces ferroptosis by inducing degradation of GPX4. FIN56 also binds to and activates squalene synthase.
|
-
- HY-120261
-
-
- HY-B0649
-
-
- HY-N2337
-
-
- HY-B0021
-
-
- HY-N6046
-
-
- HY-P1314A
-
-
- HY-B0795
-
MHY1485
|
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-N2149A
-
-
- HY-135013
-
Umbellulone
|
TRP Channel
|
Neurological Disease
|
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.
|
-
- HY-N2149
-
-
- HY-111498A
-
-
- HY-N0050
-
Allomatrine
(+)-Allomatrine
|
Others
|
Neurological Disease
|
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
|
-
- HY-B1560
-
Bismuth subgallate
|
Others
|
Others
|
Bismuth subgallate, a hemostatic agent, acts on coagulation factor XII (Hageman factor), leading to the activation of the coagulation cascade and improving early formation of a fibrin clot.
|
-
- HY-18936
-
-
- HY-100671
-
L002
|
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-112671
-
CDDO-dhTFEA
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-10201
-
Sorafenib
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-16708A
-
ZLN024 hydrochloride
|
AMPK
|
Metabolic Disease
|
ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-N0822
-
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
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-15371
-
Forskolin
Coleonol; Colforsin
|
Adenylate Cyclase
FXR
Autophagy
|
Cancer
Endocrinology
Metabolic Disease
Inflammation/Immunology
|
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
|
-
- HY-18980
-
Rottlerin
Mallotoxin; NSC 56346; NSC 94525
|
PKC
Autophagy
Apoptosis
|
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.
|
-
- HY-128358
-
MR-L2
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.
|
-
- HY-127019
-
Nigericin
|
Sodium Channel
NOD-like Receptor (NLR)
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrial membranes.Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis.
|
-
- HY-10201A
-
Sorafenib Tosylate
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-N1469
-
-
- HY-B0926A
-
Sodium diatrizoate
Diatrizoic acid sodium salt; Sodium amidotrizoate
|
Others
|
Inflammation/Immunology
|
Sodium diatrizoate (Diatrizoic acid sodium salt) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Sodium diatrizoate induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium.
|
-
- HY-N0014
-
-
- HY-N0233
-
Bavachin
Corylifolin
|
Estrogen Receptor/ERR
|
Cancer
|
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
|
-
- HY-101255
-
ODQ
|
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
-
VII-31
|
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
-
-
- HY-N6018
-
-
- HY-16677A
-
-
- HY-W011890
-
-
- HY-19770
-
GSK2981278
|
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-15004
-
AUZ 454
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-13595
-
Chrysophanol
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
-
-
- HY-104073
-
-
- HY-10003
-
Alfacalcidol
1-hydroxycholecalciferol; 1.alpha.-Hydroxyvitamin D3
|
VD/VDR
|
Metabolic Disease
|
Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.
|
-
- HY-15332
-
Alfacalcidol-D6
|
VD/VDR
|
Metabolic Disease
|
Alfacalcidol-D6, a deuterated Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3), is a non-selective VDR activator medication.
|
-
- HY-134001
-
-
- HY-10257
-
-
- HY-13008
-
-
- HY-100316
-
-
- HY-P0233
-
-
- HY-B0926
-
Diatrizoic acid
Diatrizoate; Amidotrizoic acid
|
Others
|
Inflammation/Immunology
|
Diatrizoic acid (Diatrizoate) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Diatrizoic acid induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium.
|
-
- HY-P1333
-
Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-103667
-
2-HBA
|
Caspase
|
Cancer
|
2-HBA is a potent inducer of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1) which can also activate caspase-3 and caspase-10.
|
-
- HY-N6673
-
-
- HY-14739
-
Choline Fenofibrate
ABT-335
|
PPAR
COX
|
Cardiovascular Disease
|
Choline Fenofibrate (ABT-335) is the choline salt of Fenofibric acid (HY-B0760), which releases free fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
|
-
- HY-19987
-
BML-284
|
Wnt
|
Cancer
|
BML-284 is a potent and cell-permeable Wnt signaling activator. BML-284 induces TCF-dependent transcriptional activity with an EC50 of 700 nM.
|
-
- HY-101860
-
-
- HY-N1713
-
-
- HY-131096
-
-
- HY-B0329
-
Isoniazid
INH; Isonicotinic acid hydrazide; Isonicotinic hydrazide
|
Bacterial
Autophagy
Mitophagy
|
Infection
|
Isoniazid (INH) is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity.
|
-
- HY-P2228
-
Chlamydocin
|
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-N0518
-
Toddalolactone
|
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-101106
-
AR7
|
RAR/RXR
|
Cancer
Neurological Disease
|
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
|
-
- HY-P1313A
-
-
- HY-114481
-
Imidazole ketone erastin
IKE
|
Ferroptosis
|
Cancer
|
Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc - and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.
|
-
- HY-125567
-
Antileukinate
|
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-101455
-
CDN1163
|
Calcium Channel
|
Metabolic Disease
|
CDN1163 is an allosteric sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) activator that improves Ca 2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders.
|
-
- HY-B0260
-
-
- HY-107780A
-
Cyclic-di-GMP sodium
c-di-GMP sodium; cyclic diguanylate sodium; 5GP-5GP sodium
|
STING
Endogenous Metabolite
|
Cancer
|
Cyclic di-GMP sodium (c-di-GMP sodium) is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species.
|
-
- HY-112606
-
ML-290
|
Others
|
Others
|
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM.
|
-
- HY-W015026
-
Isobutylparaben
Isobutyl 4-hydroxybenzoate
|
Bacterial
|
Inflammation/Immunology
|
Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.
|
-
- HY-113204
-
-
- HY-P0233A
-
Melittin TFA
|
Phospholipase
|
Cancer
Infection
|
Melittin TFA is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2.
|
-
- HY-18657
-
TEPP-46
ML-265
|
Pyruvate Kinase
|
Cancer
|
TEPP-46 is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR.
|
-
- HY-N1912
-
Andropanolide
|
NF-κB
|
Inflammation/Immunology
|
Andrographolide (Andro) is a small antagonist for NF-κB activation by covalent modifying reduced cysteine 62 of p50. Andrographolide is a bicyclic diterpenoid lactone mainly produced from the plant Andrographis (Andrographis paniculate).
Andrographolide suppresses the activation of NF-κB in stimulated endothelial cells, which reduces the expression of cell adhesion molecule E-selectin and prevents E-selectin-mediated leukocyte adhesion, but has no effect on IκBα degradation, p50 and p65 nuclear translocation.
|
-
- HY-126675A
-
AS2863619
|
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-128892
-
EN6
|
Autophagy
Proton Pump
|
Neurological Disease
|
EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H + ATPase (v-ATPase). EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner.
|
-
- HY-16591
-
Birinapant
TL32711
|
IAP
Apoptosis
HIV
|
Cancer
|
Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
|
-
- HY-105118A
-
Zaldaride maleate
CGS-9343B; KW 5617
|
nAChR
|
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-15124
-
-
- HY-B1505
-
-
- HY-12885C
-
ADU-S100 enantiomer ammonium salt
MIW815 enantiomer ammonium salt; ML RR-S2 CDA enantiomer ammonium salt
|
Others
|
Inflammation/Immunology
|
ADU-S100 enantiomer ammonium salt (MIW815 enantiomer ammonium salt) is the less active enantiomer of ADU-S100. ADU-S100 is an activator of stimulator of interferon genes (STING).
|
-
- HY-13417A
-
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
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-13324
-
Bardoxolone methyl
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-13255A
-
TAME hydrochloride
|
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.
|
-
- HY-105170B
-
ABT-418 hydrochloride
|
nAChR
|
Neurological Disease
|
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.
|
-
- HY-131443
-
TRC-766
|
Others
|
Others
|
TRC-766 is a negative control of RTC-5 (TRC-382). TRC-766 binds protein phosphatase 2A (PP2A) and does not activate the phosphatase.
|
-
- HY-N6651
-
Isocryptotanshinone
|
STAT
Phosphatase
|
Cancer
|
Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.
|
-
- HY-126382
-
Hesperidin methylchalcone
|
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-136447
-
ASP4132
|
AMPK
|
Cancer
|
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
|
-
- HY-13735B
-
Quinacrine hydrochloride hydrate
Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Cancer
Infection
|
Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis.
|
-
- HY-N2310
-
Domoic acid
(-)-Domoic acid; L-Domoic acid
|
iGluR
|
Neurological Disease
|
Domoic acid ((-)-Domoic acid; L-Domoic acid) is an excitatory neurotransmitter isolated from a form of marine vegetation, Nitzschia pungens. Domoic acid produces neurotoxic effect through activating kainate receptor.
|
-
- HY-N0341
-
Scopolin
|
Sirtuin
|
Metabolic Disease
|
Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades.
|
-
- HY-N7439
-
Mogroside VI B
|
PGC-1α
|
Metabolic Disease
|
Mogroside VI B, a cucurbitane glucoside, separated from the crude extract of Siraitia grosvenorii. Mogroside VI B shows effect on activating PGC-1α transcription.
|
-
- HY-13255
-
TAME
|
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.
|
-
- HY-17376
-
-
- HY-128400
-
4'-Methoxychalcone
|
PARP
|
Metabolic Disease
Cancer
|
4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
|
-
- HY-17471A
-
-
- HY-N2065
-
Withaferin A
|
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-14608
-
-
- HY-108036
-
Pro-xylane
Hydroxypropyl tetrahydropyrantriol
|
Others
|
Metabolic Disease
|
Pro-xylane (Hydroxypropyl tetrahydropyrantriol) is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis. Pro-xylane is the first example of 'Green' chemical used in cosmetic.
|
-
- HY-122816
-
HLY78
|
Wnt
|
Cancer
Neurological Disease
|
HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
|
-
- HY-19937
-
Saroglitazar
|
PPAR
|
Metabolic Disease
|
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-18935A
-
CBL0137 hydrochloride
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-13417
-
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
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-103097
-
ST271
|
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-B0711
-
Carglumic Acid
N-Carbamyl-L-glutamic acid
|
Others
|
Cancer
|
Carglumic acid (N-Carbamyl-L-glutamic acid), a functional analogue of N-acetylglutamate (NAG) and a carbamoyl phosphate synthetase 1 (CPS1) activator, is used to treat acute and chronic hyperammonemia associated with NAG synthase (NAGS) deficiency.
|
-
- HY-N1490
-
-
- HY-B1218
-
Sulfaphenazole
|
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-10167A
-
Tecalcet Hydrochloride
R-568 hydrochloride
|
CaSR
|
Others
|
Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
|
-
- HY-114330A
-
-
- HY-104049
-
Lanifibranor
IVA337
|
PPAR
|
Metabolic Disease
Cancer
|
Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
|
-
- HY-N0139
-
-
- HY-N0773
-
Isovitexin
Saponaretin; Homovitexin
|
JNK
NF-κB
|
Inflammation/Immunology
|
Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
|
-
- HY-123963
-
C-178
|
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-33350
-
-
- HY-19937A
-
Saroglitazar Magnesium
|
PPAR
|
Metabolic Disease
|
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-P1333A
-
Dynorphin A TFA
|
Opioid Receptor
|
Neurological Disease
|
Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-N7697
-
Chitotetraose tetrahydrochloride
|
Others
|
Others
|
Chitotetraose tetrahydrochloride is an arbuscular mycorrhizal (AM) fungal short-chain chitin oligomer. Chitotetraose tetrahydrochloride activates the AM fungal-dependent conserved symbiosis signaling pathway (CSSP) in actinorhizal plant species.
|
-
- HY-108908
-
-
- HY-U00441
-
DPBQ
|
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-P1955A
-
Etelcalcetide hydrochloride
AMG 416 hydrochloride; KAI-4169 hydrochloride
|
CaSR
|
Endocrinology
|
Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide hydrochloride is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis.
|
-
- HY-N0048
-
Polyphyllin II
|
Apoptosis
|
Cancer
|
Polyphyllin II is one of the most significant saponins in Rhizoma Paridis and has toxic effects on kinds of cancer cells. Polyphyllin II induces apoptosis through caspases activation and cell-cycle arrest.
|
-
- HY-12809
-
Optovin
|
TRP Channel
|
Neurological Disease
|
Optovin is a reversible photoactivated TRPA1 ligand that enables light-mediated neuronal excitation. Optovin activates TRPA1 via structure-dependent photochemical reactions with redox-sensitive cysteine residues.
|
-
- HY-P1594
-
-
- HY-78869
-
Mutated EGFR-IN-1
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-101572
-
MHP
Methyl caprooyl tyrosinate
|
SPHK
|
Inflammation/Immunology
|
MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production. MHP (Methyl caprooyl tyrosinate) enhances antimicrobial defense and innate immunity.
|
-
- HY-W001174
-
-
- HY-14608A
-
-
- HY-N0815
-
Resibufogenin
Bufogenin; Recibufogenin
|
Others
|
Cancer
|
Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.
|
-
- HY-111617
-
BTR-1
|
Apoptosis
|
Cancer
|
BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death.
|
-
- HY-P0172A
-
ATI-2341 TFA
|
CXCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
|
-
- HY-N6257
-
Cafestol
|
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
-
AS2863619 free base
|
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-117163
-
FzM1.8
|
Wnt
β-catenin
|
Cancer
|
FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
|
-
- HY-N6681
-
-
- HY-U00201
-
-
- HY-13735A
-
Quinacrine dihydrochloride
Mepacrine dihydrochloride; SN-390 dihydrochloride
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Cancer
Infection
|
Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
|
-
- HY-N4225
-
-
- HY-110228
-
-
- HY-108908A
-
Modipafant
UK-80067
|
Others
|
Inflammation/Immunology
|
Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505.
|
-
- HY-N6261
-
Epimagnolin B
|
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-U00442
-
CTX1
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system.
|
-
- HY-124293
-
AA147
|
Others
|
Metabolic Disease
|
AA147, a small molecule endoplasmic reticulum (ER) proteostasis regulator, selectively activates ATF6 arm of the unfolded protein response (UPR) extracted from patent WO2017117430A1, compound 147*.
|
-
- HY-11063
-
-
- HY-18937
-
WEHI-345
|
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-N5083
-
Saponarin
|
Others
|
Inflammation/Immunology
|
Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake.
|
-
- HY-115658
-
VU0420373
|
Bacterial
|
Infection
Metabolic Disease
|
VU0420373 is a potent heme sensor system (HssRS) activator with an EC50 of 10.7 μM and a pEC50 of 4.97. VU0420373 induces heme biosynthesis, and is toxic to fermenting S. aureus.
|
-
- HY-108036A
-
(S)-Pro-xylane
(S)-Hydroxypropyl tetrahydropyrantriol
|
Others
|
Others
|
(S)-Pro-xylane ((S)-Hydroxypropyl tetrahydropyrantriol) is the S-enantiomer of Pro-xylane (HY-108036). Pro-xylane is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis.
|
-
- HY-101731
-
-
- HY-16785B
-
Veledimex (S enantiomer)
INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
|
Interleukin Related
Cytochrome P450
|
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-N6826
-
Asatone
|
NF-κB
|
Inflammation/Immunology
|
Asatone is an active component isolated from Radix et Rhizoma Asari, with anti-inflammatory effect via activation of NF-κB and donwn regulation of p-MAPK (ERK, JNK and p38) pathways.
|
-
- HY-112125
-
KRN2
|
Others
|
Inflammation/Immunology
|
KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
|
-
- HY-N0826
-
-
- HY-W011241
-
Cinchonine hydrochloride
(8R,9S)-Cinchonine hydrochloride; LA40221 hydrochloride
|
Apoptosis
Parasite
|
Cancer
|
Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural compound present in Cinchona bark. Cinchonine hydrochloride activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
|
-
- HY-13812
-
-
- HY-137552
-
MKI-1
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-112108
-
Chitosan oligosaccharide
COS
|
AMPK
|
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-W010737
-
-
- HY-12290
-
Arg-Gly-Asp-Ser
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
|
-
- HY-N2585
-
Isodeoxyelephantopin
|
Reactive Oxygen Species
NF-κB
Autophagy
|
Cancer
|
Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
|
-
- HY-N4202
-
-
- HY-10999
-
Trametinib
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-N0614
-
Sucralose
E955; Trichlorosucrose
|
Endogenous Metabolite
|
Cancer
|
Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents.
|
-
- HY-N0109
-
Salidroside
Rhodioloside
|
mTOR
Apoptosis
|
Cancer
|
Salidroside 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-113134
-
-
- HY-13567
-
Bendamustine
SDX-105 free base
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-15272
-
WAY-600
|
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-N0605
-
Ginsenoside Rh2
20(S)-Ginsenoside Rh2; 20(S)-Rh2; Ginsenoside-Rh2
|
Caspase
Apoptosis
Endogenous Metabolite
|
Cancer
|
Ginsenoside Rh2 is isolated from the root of Ginseng. Ginsenoside Rh2 induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.
|
-
- HY-N0847
-
Micheliolide
|
Others
|
Others
|
Micheliolide could effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs).
|
-
- HY-P0318
-
-
- HY-N2247A
-
(+)-Guaiacin
|
Others
|
Metabolic Disease
|
(+)-Guaiacin is a compound extracted of the bark of Machilus wangchiana Chun. (Lauraceae). (+)-Guaiacin shows potent in vitro activities against the release of β-glucuronidase in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor (PAF) .
|
-
- HY-13293
-
Impurity C of Calcitriol
|
VD/VDR
|
Cancer
|
Impurity C of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-P2319
-
-
- HY-13292
-
Impurity B of Calcitriol
1β,25-Dihydroxyvitamin-D3; 1-Epicalcitriol
|
VD/VDR
|
Cancer
|
Impurity B of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-B0190A
-
-
- HY-N2119
-
Sciadopitysin
|
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-B0190
-
-
- HY-N7117
-
-
- HY-N4171
-
Dihydrocucurbitacin B
|
Others
|
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-B0190B
-
-
- HY-124108
-
Eicosatetraynoic acid
ETYA
|
COX
PPAR
|
Others
|
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.
|
-
- HY-N0250
-
-
- HY-P0082A
-
Glucagon hydrochloride
Porcine glucagon hydrochloride
|
Glucagon Receptor
|
Metabolic Disease
|
Glucagon hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone, produced by pancreatic α-cells. Glucagon hydrochloride stimulates gluconeogenesis. Glucagon hydrochloride activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-18711A
-
SCR-1481B1
c-Met inhibitor 2
|
c-Met/HGFR
VEGFR
|
Cancer
|
SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
|
-
- HY-N0141
-
Parthenolide
(-)-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-U00036
-
Naveglitazar racemate
LY519818 racemate
|
PPAR
|
Metabolic Disease
|
Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.
|
-
- HY-P0082
-
Glucagon
Porcine glucagon
|
Glucagon Receptor
|
Metabolic Disease
|
Glucagon (Porcine glucagon) is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-P1594A
-
-
- HY-N1485
-
Astramembrangenin
Cyclosieversigenin
|
Apoptosis
|
Inflammation/Immunology
Neurological Disease
|
Astramembrangenin (Cycloastragenol) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus (Fisch.) Bunge.
Astramembrangenin is orally safe and has broad Extensive pharmacological effects, including telomerase activation, telomere elongation, anti-inflammatory and anti-oxidative properties.
Astramembrangenin has antiaging properties, CAG stimulates telomerase activity in human neonatal keratinocytes and rat neuronal cells, and induces CREB activation followed by tert and bcl2 expression. Cycloastragenol (CAG) may have a novel therapeutic role in depression.
|
-
- HY-15340
-
LG100268
LG268
|
RAR/RXR
Autophagy
|
Metabolic Disease
|
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
|
-
- HY-10108
-
LY294002
|
PI3K
Casein Kinase
DNA-PK
Autophagy
Apoptosis
|
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 inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
|
-
- HY-N0674A
-
Dehydrocorydaline chloride
13-Methylpalmatine chloride
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-10256A
-
SB 203580 hydrochloride
RWJ 64809 hydrochloride
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
SB 203580 hydrochloride (RWJ 64809 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. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
|
-
- HY-110353
-
CU-T12-9
|
Toll-like Receptor (TLR)
|
Cancer
Infection
Inflammation/Immunology
|
CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
|
-
- HY-N0674
-
Dehydrocorydaline
13-Methylpalmatine
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-N3005
-
Britannin
|
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
|
Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities.
|
-
- HY-136651
-
BNTA
|
Others
|
Inflammation/Immunology
|
BNTA, a potent extracellular matrix (ECM) modulator, facilitates cartilage structural molecule synthesis on chondrocytes by activating superoxide dismutase 3 (SOD3). BNTA shows a promising potential for osteoarthritis alleviation by modulating cartilage generation.
|
-
- HY-107414
-
-
- HY-101843
-
-
- HY-12848
-
SAG
|
Smo
|
Cancer
|
SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-P2319A
-
-
- HY-108439
-
Neurodazine
|
Wnt
Hedgehog
|
Neurological Disease
|
Neurodazine is an imidazole-based small molecule, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways. Neurodazine selectively suppresses astrocyte differentiation of P19 cells.
|
-
- HY-120675
-
SSTC3
|
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-12848C
-
SAG dihydrochloride
|
Smo
|
Cancer
|
SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-N0802
-
Tenuigenin
Senegenin
|
NF-κB
|
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-12848B
-
SAG hydrochloride
|
Smo
|
Cancer
|
SAG hydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG hydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-17363S
-
Dimethyl fumarate D6
DMF D6
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Dimethyl fumarate D6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
|
-
- HY-122445
-
-
- HY-124867
-
D3-βArr
|
TSH Receptor
|
Endocrinology
|
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
|
-
- HY-108539
-
CE3F4
|
Others
|
Cardiovascular Disease
|
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
|
-
- HY-N0220
-
Dauricine
|
NF-κB
Apoptosis
|
Cancer
Inflammation/Immunology
|
Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, 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-N3026
-
Soyasaponin Ab
|
Others
|
Metabolic Disease
|
Soyasaponin Ab is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
|
-
- HY-N3027
-
Soyasaponin Aa
|
Others
|
Metabolic Disease
|
Soyasaponin Aa is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
|
-
- HY-N0020
-
Echinacoside
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
|
-
- HY-12764
-
6-OAU
GTPL5846
|
GPR84
|
Inflammation/Immunology
|
6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
|
-
- HY-15880
-
CCT007093
|
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-15874A
-
Fiboflapon sodium
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
-
Rosiptor
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-100164
-
SDZ-MKS 492
MKS 492
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
SDZ-MKS 492 (MKS 492) is a selective type III isozyme inhibitor of cyclic nucleotide phosphodiesterase, effective in allergic bronchoconstriction and platelet activating factor (PAF) or LTB4-induced inflammatory reactions in animals.
|
-
- HY-B0627
-
-
- HY-16696
-
SN 2
|
TRP Channel
|
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-103269
-
BAI1
|
Bcl-2 Family
|
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-15874
-
Fiboflapon
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-124729A
-
-
- HY-103490
-
Takinib
|
MAP3K
Apoptosis
|
Cancer
|
Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
|
-
- HY-135808
-
BIZ 114
|
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-B1371A
-
-
- HY-10256
-
SB 203580
RWJ 64809
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
|
-
- HY-N4238
-
Dehydrocorydaline nitrate
13-Methylpalmatine nitrate
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-115576
-
-
- HY-119931
-
-
- HY-N1419
-
Vaccarin
|
AMPK
|
Metabolic Disease
|
Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
|
-
- HY-N4097
-
Incensole
|
Others
|
Neurological Disease
|
Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.
|
-
- HY-100227
-
E 64c
|
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-N0589
-
-
- HY-N6748
-
-
- HY-134333
-
ICCB280
|
Apoptosis
|
Cancer
|
ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets.
|
-
- HY-102004
-
-
- HY-12825
-
BHPI
|
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-N0039
-
-
- HY-106916
-
Unoprostone
|
Potassium Channel
|
Neurological Disease
|
Unoprostone, a prostaglandin F2α analogs (PGAs), activates BK channels to reduce oxidative stress- and light-induced retinal cell death, and phagocytotic dysfunction. Unoprostone reduces intraocular pressure and is used topically for glaucoma or ocular hypertension.
|
-
- HY-76814
-
Calcitriol D6
|
VD/VDR
|
Metabolic Disease
|
Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-B0285
-
-
- HY-14854
-
Tecarfarin
ATI-5923
|
Others
|
Cardiovascular Disease
|
Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .
|
-
- HY-B0285A
-
-
- HY-N0499
-
Cyanidin Chloride
IdB 1027
|
Others
|
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-N0431
-
Astragaloside IV
|
MMP
ERK
JNK
|
Cancer
|
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
|
-
- HY-128900
-
11-cis-Vaccenyl acetate
|
Endogenous Metabolite
|
Others
|
11-cis-Vaccenyl acetate is male-specific lipid that mediates aggregation behavior in both male and female flies, which activates a few dozen olfactory neurons located in T1 sensilla on the antenna of both male and female flies.
|
-
- HY-136278
-
NOC 18
|
NO Synthase
|
Cardiovascular Disease
|
NOC 18 is a nitric oxide donor and activates an inward current in cultured rat cerebellar granules cells. NOC 18 increases cGMP production in cultured vascular smooth muscle cells. NOC 18 reduces contractility of cardiac muscle preparations in vitro.
|
-
- HY-105940
-
IQB-782
|
Others
|
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-112126
-
KRN5
|
Others
|
Inflammation/Immunology
|
KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.
|
-
- HY-13520
-
Nocodazole
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-I1070
-
D-Isoleucine
(R)-Isoleucine
|
Others
|
Neurological Disease
|
D-Isoleucine ((R)-Isoleucine), an isoleucine stereoisomer, is a selective activator of Asc-1 antiporter, which enhances long-term potentiation at the hippocampal CA1-CA3 via release of endogenous D-serine.
|
-
- HY-N2237
-
-
- HY-N0447
-
-
- HY-N6679A
-
10,11-Dehydrocurvularin
|
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-18200
-
Atopaxar
E5555; ER-172594-00
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
|
-
- HY-N0791
-
Tectoridin
|
Estrogen Receptor/ERR
|
Cancer
|
Tectoridin is a isoflavone isolated from Maackia amurensis. Tectoridin is a phytoestrogen and activates estrogen and thyroid hormone receptors. Tectoridin exerts the estrogenic effects via ER-dependent genomic pathway and GPR30-dependent nongenomic pathway.
|
-
- HY-10219
-
Rapamycin
Sirolimus; AY-22989
|
mTOR
FKBP
Fungal
Autophagy
Endogenous Metabolite
Antibiotic
|
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-B0351
-
Taurine
2-Aminoethanesulfonic acid
|
Autophagy
Endogenous Metabolite
|
Metabolic Disease
|
Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
|
-
- HY-N7038
-
Phytohemagglutinin
PHA-M
|
Others
|
Inflammation/Immunology
|
Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, accumulates in the parenchyma cells of the cotyledons. Phytohemagglutinin is a T-cell activator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis.
|
-
- HY-119339
-
SX-682
|
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-U00280
-
Potassium Channel Activator 1
|
Others
|
Neurological Disease
|
Potassium Channel Activator 1 is an agent for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.
|
-
- HY-126114
-
Lupeol acetate
|
Others
|
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-N1504
-
Loureirin B
|
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-107608
-
-
- HY-100016
-
AZD0156
|
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-75161
-
(-)-Menthol
|
TRP Channel
Endogenous Metabolite
|
Cancer
|
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i. Antitumor activity.
|
-
- HY-N3376
-
Liriodenine
Spermatheridine; VLT045
|
Others
|
Cancer
|
Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant Mitrephora sirikitiae and has anti-cancer activities. Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9.
|
-
- HY-N2078
-
Yamogenin
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-107738
-
Guggulsterone
Z/E-Guggulsterone
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
|
Cancer
|
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
|
-
- HY-109041
-
Razuprotafib
AKB-9778
|
Phosphatase
|
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-B0963
-
Cloxiquine
5-Chloro-8-quinolinol
|
Bacterial
Fungal
Parasite
PPAR
|
Cancer
Infection
|
Cloxiquine (5-Chloro-8-quinolinol) is an antibacterial, antifungal and antiamoebic agent. Cloxiquine can be used for the research of tuberculosis and dermatoses. Cloxiquine suppresses the growth and metastasis of melanoma cells through activation of PPARγ.
|
-
- HY-13030
-
-
- HY-137864
-
Amifostine thiol
WR-1065
|
MDM-2/p53
|
Cancer
|
Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine (HY-B0639). Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway.
|
-
- HY-50937
-
ST 2825
|
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-N2941
-
Bisandrographolide C
|
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
Bisandrographolide C is an unusual dimer of ent-labdane diterpenoid isolated and identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels with Kd values of 289 and 341 μM respectively, and protects cardiomyocytes from hypoxia-reoxygenation injury.
|
-
- HY-B0764A
-
Bucladesine calcium
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
-
(E)-[6]-Dehydroparadol
|
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-N2006
-
Ganoderic acid B
|
HIV Protease
|
Infection
|
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.
|
-
- HY-115545
-
DBCO-NHS ester 3
|
ADC Linker
|
Cancer
|
DBCO-NHS ester 3 (Compound 12) is a cleavable linker that is used for making antibody-drug conjugate (ADC). DBCO-NHS ester 3 is a derivative of Dibenzylcyclooctyne (DBCO) obtained by activation of N-hydroxysuccinimide by the carboxylic acid moiety of both methyl-oxanorbornadiene (MeOND) and dibenzoazacyclooctyne (DIBAC).
|
-
- HY-N2374
-
Eupatorin
|
Others
|
Cancer
|
Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage.
|
-
- HY-N7015
-
Zerumbone
|
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-N5018
-
Nepodin
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-100738
-
-
- HY-P1179
-
-
- HY-W008956
-
Myoseverin
|
Microtubule/Tubulin
|
Inflammation/Immunology
|
Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration.
|
-
- HY-N0651
-
Spinosin
|
Others
|
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-N2344
-
Procyanidin A1
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-19843
-
MK-0941
|
Glucokinase
|
Metabolic Disease
|
MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes.
|
-
- HY-N2116
-
Ginkgolic acid C17:1
|
PTEN
Phosphatase
|
Cancer
|
Ginkgolic acid C17:1, extracted from Ginkgo biloba Leaves, suppresses constitutive and inducible STAT3 activation through induction of PTEN and SHP-1 tyrosine phosphatase. Ginkgolic acid C17:1 has anticancer effects.
|
-
- HY-10532
-
SRT 1720
|
Sirtuin
Autophagy
|
Metabolic Disease
|
SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
|
-
- HY-N6872
-
Actein
|
JNK
Akt
Apoptosis
Autophagy
|
Cancer
|
Actein is a triterpene glycoside isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in human bladder cancer. Actein has little toxicity in vivo.
|
-
- HY-N6807
-
Elemicin
|
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-101942
-
CM-4620
|
CRAC Channel
|
Neurological Disease
|
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-N6641
-
Monascin
|
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-N4053
-
Heraclenin
|
Others
|
Inflammation/Immunology
|
Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
|
-
- HY-B0285B
-
-
- HY-114335
-
Triphala
|
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-14612
-
CPPHA
|
mGluR
|
Neurological Disease
|
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.
|
-
- HY-B1899A
-
Taurodeoxycholic acid sodium hydrate
Sodium taurodeoxycholate monohydrate
|
Caspase
|
Metabolic Disease
Inflammation/Immunology
|
Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid sodium hydrate is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
|
-
- HY-N2497
-
Isoliquiritin apioside
|
NF-κB
MMP
p38 MAPK
|
Cancer
|
Isoliquiritin apioside, a component isolated from Glycyrrhizae radix rhizome, significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells.
|
-
- HY-110249
-
CINPA1
|
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-15262
-
SRT 2104
|
Sirtuin
|
Metabolic Disease
Neurological Disease
Cancer
|
SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD + dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease.
|
-
- HY-N6861
-
Lucidenic acid B
|
Apoptosis
|
Cancer
|
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells.
|
-
- HY-B0341
-
Nicorandil
SG-75
|
Potassium Channel
|
Cardiovascular Disease
|
Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
|
-
- HY-107661
-
Arundic Acid
ONO-2506; (R)-2-Propyloctanoic acid
|
Others
|
Neurological Disease
|
Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid has the potential for stroke and Alzheimer’s disease research.
|
-
- HY-126585
-
SAICAR
|
Endogenous Metabolite
|
Cancer
|
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions.
|
-
- HY-100530D
-
Rp-cAMPS sodium salt
|
PKA
|
Neurological Disease
|
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-P1149A
-
Epitalon TFA
Epithalon TFA; Epithalamin TFA
|
Telomerase
|
Cancer
Neurological Disease
|
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa.
|
-
- HY-133114
-
-
- HY-N0003
-
Honokiol
NSC 293100
|
Akt
ERK
Autophagy
HCV
|
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 and enhances the phosphorylation of ERK1/ERK2. Honokiol can readily cross the blood brain barrier.
|
-
- HY-121685A
-
Tipepidine hydrochloride
|
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-P1179A
-
-
- HY-N0496
-
Ruscogenin
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities.
|
-
- HY-13459
-
PF-5274857
|
Smo
|
Cancer
|
PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
|
-
- HY-118532
-
Tyrphostin AG30
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-100530A
-
Rp-cAMPS
|
PKA
|
Neurological Disease
|
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-101379A
-
8-Bromo-cGMP sodium
|
Calcium Channel
|
Neurological Disease
|
8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator and significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K +. 8-Bromo-cGMP sodium has antinociceptive effects.
|
-
- HY-18686
-
AS1949490
|
Phosphatase
|
Metabolic Disease
|
AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes.
|
-
- HY-103254
-
ML221
|
Others
|
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
-
Niraparib tosylate
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-17537
-
APY29
|
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-14590
-
-
- HY-103023
-
CLP290
|
Potassium Channel
|
Neurological Disease
|
CLP290 is an orally available activator of the neuron-specific K +-Cl − cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats.
|
-
- HY-13649
-
Indibulin
ZIO 301; D 24851
|
Microtubule/Tubulin
Apoptosis
|
Cancer
Neurological Disease
|
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.
|
-
- HY-112233
-
O-304
|
AMPK
|
Metabolic Disease
Cardiovascular Disease
|
O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a drug to treat type 2 diabetes (T2D) and associated cardiovascular complications .
|
-
- HY-112820
-
Chlorantraniliprole
|
Others
|
Others
|
Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ∼300-fold more potent than that in the mouse myoblast cell line, C2C12 (EC50, 14 μM).
|
-
- HY-13297
-
PYZD-4409
|
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-125827
-
13-Methylberberine chloride
13-Methylberberinium chloride
|
Others
|
Cancer
Metabolic Disease
|
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.
|
-
- HY-133168
-
Englerin A
|
TRP Channel
|
Cancer
|
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.
|
-
- HY-B0258
-
-
- HY-B0764
-
Bucladesine sodium
Dibutyryl cAMP sodium salt; DBcAMP sodium salt
|
PKA
Phosphodiesterase (PDE)
|
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.
|
-
- HY-15415
-
KB-R7943 mesylate
|
Na+/Ca2+ Exchanger
Autophagy
|
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.
|
-
- HY-125355
-
SEC
|
Apoptosis
|
Cancer
|
SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
|
-
- HY-N0592
-
Demethyleneberberine
|
NF-κB
AMPK
|
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-108434
-
Ceapin-A7
|
Others
|
Metabolic Disease
Neurological Disease
|
Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings.
|
-
- HY-N0112
-
Dihydromyricetin
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-11062
-
Icilin
AG-3-5
|
TRP Channel
|
Cancer
Neurological Disease
|
Icilin (AG-3-5) is an agonist of nonselective cation channel TRPM8, with antiproliferative activity. Icilin activated currents only in wild type TRPM8 and in the presence of Ca 2+. Icilin can induce G1 arrest in prostate cancer cells.
|
-
- HY-N0393
-
Glabridin
|
PPAR
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
|
-
- HY-10529
-
-
- HY-15615A
-
TIC10
ONC-201
|
TNF Receptor
Apoptosis
|
Cancer
|
TIC10 is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
|
-
- HY-120528A
-
-
- HY-12041
-
SP600125
|
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-10619
-
Niraparib
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.
|
-
- HY-136179
-
ZAP-180013
|
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-122727
-
STL127705
|
DNA-PK
|
Cancer
|
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
|
-
- HY-10619A
-
Niraparib hydrochloride
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-117541
-
Glycyl-glutamine
Glycyl-L-glutamine
|
Others
|
Neurological Disease
|
Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems. Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln).
|
-
- HY-16059
-
-
- HY-100530
-
Rp-cAMPS triethylammonium salt
|
PKA
|
Neurological Disease
|
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-15671
-
GKA50
|
Glucokinase
|
Metabolic Disease
|
GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats.
|
-
- HY-118628
-
-
- HY-N0191
-
-
- HY-N3806
-
-
- HY-19702
-
-
- HY-P2282
-
APTSTAT3-9R
|
STAT
|
Cancer
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
|
-
- HY-107212
-
Selamectin
|
Parasite
Chloride Channel
P-glycoprotein
|
Infection
|
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
|
-
- HY-10936
-
S 18986
|
iGluR
|
Neurological Disease
|
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
|
-
- HY-111926
-
-
- HY-N0479
-
Licarin B
(-)-Licarin B
|
PPAR
GLUT
|
Metabolic Disease
|
Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.
|
-
- HY-10999A
-
Trametinib (DMSO solvate)
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-12762
-
QS11
|
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-120272
-
SMAP-2
DT-1154
|
Phosphatase
|
Cancer
|
SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. SMAP-2 (DT-1154) inhibits the growth of KRAS-mutant lung cancers .
|
-
- HY-114739
-
MA-0204
|
PPAR
|
Metabolic Disease
|
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
|
-
- HY-W011434
-
Triglycidyl isocyanurate
TGIC; Teroxirone
|
MDM-2/p53
Apoptosis
|
Cancer
Inflammation/Immunology
|
Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.
|
-
- HY-N0577
-
Apiin
|
Others
|
Inflammation/Immunology
|
Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitory activity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells.
|
-
- HY-18982
-
Anisomycin
Flagecidin; Wuningmeisu C
|
DNA/RNA Synthesis
JNK
Bacterial
Apoptosis
Antibiotic
|
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 isolated from Streptomyces griseolus.
|
-
- HY-112929B
-
(1S,2S,3R)-DT-061
|
Others
|
Cancer
|
(1S,2S,3R)-DT-061 is an enantiomer of DT-061. DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
|
-
- HY-119917
-
Gossypetin
|
p38 MAPK
Bacterial
|
Cancer
Infection
|
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
|
-
- HY-N0316
-
Mollugin
|
Others
|
Cancer
|
Mollugin is a major bioactive component isolated from Rubia cordifolia L.. Mollugin has an anti-cancer therapeutic effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 via the p38-Smad signaling pathway .
|
-
- HY-13757AS
-
Tamoxifen-d5
ICI 47699-d5; (Z)-Tamoxifen-d5; trans-Tamoxifen-d5
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
|
-
- HY-19759
-
SRT 2183
|
Sirtuin
Apoptosis
|
Cancer
|
SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
|
-
- HY-108741
-
Plecanatide
|
Guanylate Cyclase
|
Inflammation/Immunology
|
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.
|
-
- HY-13434
-
Ionomycin
SQ23377
|
Calcium Channel
PKC
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC).
|
-
- HY-19638A
-
Cangrelor tetrasodium
|
P2Y Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist.
|
-
- HY-121538
-
CUDA
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
|
-
- HY-W009884
-
Acetosyringone
|
Others
|
Others
|
Acetosyringone is a phenolic compound from wounded plant cells, enables virA gene which encodes a membrane-bound kinase to phosphorylate itself and activate the virG gene product, which stimulates the transcription of other vir genes and itself. Acetosyringone enhances efficient Dunaliella transformation of Agrobacterium strains.
|
-
- HY-B2099
-
Buformin
1-Butylbiguanide
|
AMPK
|
Cancer
Metabolic Disease
|
Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
|
-
- HY-10277
-
Odiparcil
SB-424323
|
Thrombin
|
Cardiovascular Disease
|
Odiparcil (SB-424323) is an orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) .
|
-
- HY-N0722
-
-
- HY-16926
-
CK-666
|
Arp2/3 Complex
|
Others
|
CK-666 is a cell-permeable inhibitor of actin-related protein Arp2/3 complex, and binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation.
|
-
- HY-N0789
-
Delsoline
|
Others
|
Metabolic Disease
Neurological Disease
|
Delsoline, a major alkaloid of Delphinium anthriscifolium Hance, has both a curare-like effect and a ganglion-blocking effect and is used to relieve muscle tension or hyperkinesia. D. anthriscifolium Hance has effects of dispelling wind and dampness, activating collaterals, and relieving pains and is used to treat rheumatism, hemiplegia, indigestion, and cough.
|
-
- HY-126390
-
(E/Z)-BCI
NSC 150117
|
Phosphatase
|
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-B2099A
-
Buformin hydrochloride
1-Butylbiguanide hydrochloride
|
AMPK
|
Cancer
|
Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).
|
-
- HY-W063968
-
RO8191
RO4948191
|
IFNAR
JAK
STAT
HCV
|
Infection
|
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon.
|
-
- HY-W009724
-
-
- HY-135401
-
VU6015929
|
Discoidin Domain Receptor
|
Inflammation/Immunology
|
VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.
|
-
- HY-100530B
-
Sp-cAMPS
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
|
Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
|
-
- HY-100612
-
T16Ainh-A01
|
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-100973A
-
-
- HY-N0569
-
-
- HY-B0589C
-
(3S,5S)-Atorvastatin
|
Cytochrome P450
|
Metabolic Disease
|
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-100530C
-
Sp-cAMPS sodium salt
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
|
Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
|
-
- HY-18366A
-
RU-SKI 43 hydrochloride
|
Hedgehog
|
Cancer
|
RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity.
|
-
- HY-120111
-
-
- HY-B1521
-
Aluminum Hydroxide
|
Others
|
Inflammation/Immunology
|
Aluminum Hydroxide is an orally active main form of aluminum used as adjuvant. Aluminum hydroxide-based adjuvant researches including the repository effect, pro-phagocytic effect, and activation of the pro-inflammatory NLRP3 pathway. Aluminum Hydroxide also acts as adjuvant to compensate low inherent immunogenicity of subunit vaccines.
|
-
- HY-137977
-
DMU-212
|
ERK
Apoptosis
|
Cancer
|
DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active.
|
-
- HY-12150
-
CCMI
|
nAChR
|
Neurological Disease
|
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
|
-
- HY-10219S
-
Rapamycin-d3
Sirolimus-d3; AY-22989-d3
|
mTOR
FKBP
Autophagy
|
Cancer
|
Rapamycin-d3 (Sirolimus-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. Rapamycin is an autophagy activator, an immunosuppressant.
|
-
- HY-B0075S
-
-
- HY-124729
-
BL-918
|
ULK
Autophagy
|
Neurological Disease
|
BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
|
-
- HY-P1098
-
Ac2-26
|
NF-κB
|
Inflammation/Immunology
|
Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-N7043
-
Isosilybin A
|
Apoptosis
|
Cancer
|
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
|
-
- HY-W010907
-
Pamoic acid disodium
|
ERK
|
Neurological Disease
|
Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.
|
-
- HY-P2285
-
AC 253
|
Amyloid-β
|
|
AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
|
-
- HY-14417
-
VU0155041
|
mGluR
|
Neurological Disease
|
VU0155041 is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site.
|
-
- HY-101084
-
NSC 228155
|
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
-
-
- HY-111549
-
Bragsin1
|
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-B0252
-
Hydrochlorothiazide
HCTZ
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
|
-
- HY-127106
-
VU0810464
|
Potassium Channel
|
Neurological Disease
|
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration.
|
-
- HY-W058849
-
MT 63-78
|
AMPK
mTOR
Apoptosis
|
Cancer
|
MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
|
-
- HY-N1381
-
Periplocin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.
|
-
- HY-P2544
-
-
- HY-13965
-
Parmodulin 2
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-108588
-
NS5806
|
Potassium Channel
|
Cardiovascular Disease
|
NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
|
-
- HY-N0633
-
-
- HY-110084
-
BTZO-1
|
Apoptosis
|
Cardiovascular Disease
|
BTZO-1 binds to Macrophage migration inhibitory factor (MIF) with a Kd value of 68.6 nM, and its binding requires the N-terminal Pro1. BTZO-1 can activate antioxidant response element (ARE)-mediated gene expression and suppress oxidative stress-induced cardiomyocyte apoptosis in vitro.
|
-
- HY-108900
-
Leu-AMS
|
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-N4113
-
Glycycoumarin
|
Autophagy
|
Cancer
|
Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase .
|
-
- HY-109854A
-
(R)-Lisofylline
(R)-Lisophylline
|
STAT
|
Metabolic Disease
Inflammation/Immunology
|
(R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
|
-
- HY-18981
-
Decursin
(+)-Decursin
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
Decursin ((+)-Decursin) is a cytotoxic agent and a potent protein kinase C activator from the Root of Angelica gigas. Decursin inhibits tumor growth, migration, and invasion in gastric cancer by down-regulating CXCR7 expression. Decursin inhibits the growth of HepG2 cells via Hippo/YAP signaling pathway.
|
-
- HY-117066
-
CL075
3M002
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
|
-
- HY-N0817
-
Polyphyllin G
|
Apoptosis
Autophagy
Bacterial
|
Cancer
Inflammation/Immunology
|
Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs).
Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy.
|
-
- HY-12467
-
OTS964 hydrochloride
|
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-B0808
-
Oxaprozin
Oxaprozinum; Wy21743
|
COX
NF-κB
|
Inflammation/Immunology
Cancer
|
Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
|
-
- HY-108328
-
PF-04937319
|
Glucokinase
|
Metabolic Disease
|
PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4 μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus.
PF-04937319 is designed to maintain glucose-lowering efficacy while mitigating the risk of hypoglycaemia observed with many other GKAs.
|
-
- HY-N6966
-
-
- HY-103319
-
Calmidazolium chloride
R 24571
|
CaMK
Autophagy
|
Cancer
Neurological Disease
|
Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM.
|
-
- HY-N0643
-
Carnosol
|
Ribosomal S6 Kinase (RSK)
Keap1-Nrf2
|
Cancer
|
Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
|
-
- HY-P2343
-
BH3 hydrochloride
|
Apoptosis
|
Cancer
|
BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian.
|
-
- HY-129522
-
Sulfo-ara-F-NMN
CZ-48
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.
|
-
- HY-135231
-
NL-1
|
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-16531A
-
YF-2 hydrochloride
|
Histone Acetyltransferase
|
Cancer
Neurological Disease
|
YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
|
-
- HY-103355
-
YM022
|
CCR
|
Metabolic Disease
|
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
|
-
- HY-100549
-
(S)-Crizotinib
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models.
|
-
- HY-111550
-
Bragsin2
|
Others
|
Cancer
|
Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells.
|
-
- HY-P1832A
-
PTD-p65-P1 Peptide TFA
|
NF-κB
|
Cancer
Inflammation/Immunology
|
PTD-p65-P1 Peptide TFA is a nuclear transcription factor NF-kappaB inhibitor, composed of a membrane-translocating peptide sequence generated from antennapedia (PTD) conjugated with p65-P1, which selectively inhibits activation induced by various inflammatory stimuli.
|
-
- HY-P1382
-
Rac1 Inhibitor W56
|
Ras
|
|
Rac1 Inhibitor W56 is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.
|
-
- HY-122534
-
Mensacarcin
|
Mitochondrial Metabolism
ADC Cytotoxin
Apoptosis
|
Cancer
|
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-120994A
-
Rp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.
|
-
- HY-133073
-
CCR7 Ligand 1
CCR7-Cmp2105
|
CCR
Ligand for Target Protein for PROTAC
|
Cancer
|
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
|
-
- HY-N0179
-
Ecdysone
α-Ecdysone
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
|
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
|
-
- HY-135897
-
-
- HY-114268
-
BRD-K98645985
|
HIV
|
Infection
|
BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity.
|
-
- HY-100538A
-
DTP3 TFA
|
DNA/RNA Synthesis
JNK
|
Cancer
|
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
|
-
- HY-16531
-
YF-2
|
Histone Acetyltransferase
|
Cancer
Neurological Disease
|
YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
|
-
- HY-P1098A
-
Ac2-26 TFA
|
NF-κB
|
Inflammation/Immunology
|
Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-129239
-
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
|
-
- HY-P0175
-
740 Y-P
740YPDGFR; PDGFR 740Y-P
|
PI3K
Autophagy
|
Cancer
|
740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
|
-
- HY-118482
-
Sauristolactam
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-B0557
-
Bisacodyl
|
Others
|
Metabolic Disease
|
Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
|
-
- HY-P2048A
-
MOTS-c(human) acetate
|
AMPK
GLUT
|
Metabolic Disease
|
MOTS-c(human) acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.
|
-
- HY-112700
-
SHIP2-IN-1
|
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-10585A
-
Valproic acid sodium salt
Sodium Valproate
|
HDAC
Autophagy
Mitophagy
HIV
Notch
|
Cancer
|
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.
|
-
- HY-B1193
-
-
- HY-N6693
-
Valinomycin
NSC 122023
|
Bacterial
Apoptosis
Antibiotic
|
Infection
|
Valinomycin (NSC 122023) is a cyclic depsipeptide antibiotic first isolated from Streptomyces fulvissimus, act as a potassium selective ionophore. Valinomycin (NSC 122023) inhibits lymphocyte proliferation by its effects on the cell membrane, and induces apoptosis in CHO cells. Valinomycin induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
|
-
- HY-N0047
-
Polyphyllin I
|
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
|
-
- HY-131039
-
MDNI-caged-L-glutamate
MDNI-glu
|
Others
|
|
MDNI-caged-L-glutamate (MDNI-glu) rapidly and efficiently releases glutamate when photolysed (350-365 nm excitation). MDNI-caged-L-glutamate is inactive at neuronal glutamate receptors (up to 200 μM) and stable at neutral pH. MDNI-caged-L-glutamate is activated by laser to evoke a rapid increase in intracellular ca 2+ concentration in astrocytes.
|
-
- HY-111759
-
Jaspamycin
7-CN-7-C-Ino
|
PKA
Parasite
|
Infection
|
Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity.
|
-
- HY-125858
-
MI-1061
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.
|
-
- HY-113596
-
Acetyl Coenzyme A trisodium
Acetyl-CoA trisodium
|
Endogenous Metabolite
|
Metabolic Disease
|
Acetyl Coenzyme A trisodium (Acetyl-CoA trisodium) is a central metabolic intermediate. Acetyl Coenzyme A trisodium is the actual molecule through which glycolytic pyruvate enters the tricarboxylic acid (TCA) cycle, is a key precursor of lipid synthesis, and is the sole donor of the acetyl groups for acetylation. Acetyl Coenzyme A trisodium acts as a potent allosteric activator of pyruvate carboxylase (PC).
|
-
- HY-128694
-
Foropafant
SR27417
|
Others
|
Cardiovascular Disease
|
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets.
|
-
- HY-P1858
-
-
- HY-N0510
-
Aristolochic acid A
Aristolochic acid I; TR 1736
|
NF-κB
|
Cancer
|
Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines.
|
-
- HY-120994
-
-
- HY-133910
-
Lu AE98134
|
Sodium Channel
|
Neurological Disease
|
Lu AE98134 is a potent and selective positive modulator of NaV1.1 channels and also activates NaV1.6 channels.Lu AE98134 normalizes the altered firing properties of fast spiking interneurons (FSINs) in Dlx5/6 +/- mice and can be used for the research of cognitive restoring in schizophrenia.
|
-
- HY-101364A
-
CHPG sodium salt
|
mGluR
NF-κB
ERK
Akt
|
Inflammation/Immunology
Neurological Disease
|
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
|
-
- HY-120934
-
C25-140
|
TNF Receptor
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.
|
-
- HY-13755
-
Sulforaphane
|
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-W017316
-
Terpinen-4-ol
4-Carvomenthenol
|
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
Terpinen-4-ol (4-Carvomenthenol), a naturally occurring monoterpene, is the main bioactive component of tea-tree oil. Terpinen-4-ol suppresses inflammatory mediator production by activated human monocytes. Terpinen-4-ol significantly enhances the effect of several chemotherapeutic and biological agents.
|
-
- HY-108741A
-
Plecanatide acetate
|
Guanylate Cyclase
|
Inflammation/Immunology
|
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis.
|
-
- HY-N0636
-
Eriocitrin
|
Apoptosis
|
Cancer
|
Eriocitrin is a flavonoid isolated from lemon, which is a strong antioxidant agent. Eriocitrin could inhibit the proliferation of hepatocellular carcinoma cell lines by arresting cell cycle in S phase through up-regulation of p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating mitochondria-involved intrinsic signaling pathway.
|
-
- HY-12741
-
LDN-212320
LDN-0212320; OSU-0212320
|
EAAT2
|
Neurological Disease
|
LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1]
|
-
- HY-100431
-
IMR-1
|
Notch
|
Cancer
|
IMR-1 is a novel class of Notch inhibitors 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 in a patient-derived tumor xenograft model.
|
-
- HY-116364
-
AZT triphosphate
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-107613
-
R 59-022
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR 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-B1794A
-
-
- HY-114180
-
RU.521
RU320521
|
Cyclic GMP-AMP Synthase
|
Metabolic Disease
|
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 700 nM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
|
-
- HY-P1858A
-
-
- HY-19694
-
BRD7552
|
Others
|
Endocrinology
|
BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.
|
-
- HY-128588
-
STAT3-IN-3
|
STAT
|
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-101364
-
CHPG
|
mGluR
NF-κB
ERK
Akt
|
Inflammation/Immunology
Cardiovascular Disease
|
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.
|
-
- HY-108355
-
R59949
|
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-122114
-
ICA-27243
|
Potassium Channel
|
Neurological Disease
|
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects.
|
-
- HY-N6843
-
Arnicolide D
|
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-108361
-
CCG-203971
|
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-129492
-
GNF4877
|
DYRK
GSK-3
|
Metabolic Disease
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
|
-
- HY-P1382A
-
Rac1 Inhibitor W56 TFA
|
Ras
|
|
Rac1 Inhibitor W56 TFA is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 TFA selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.
|
-
- HY-110258
-
ML334
LH601A
|
Keap1-Nrf2
|
Cancer
|
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
|
-
- HY-15959
-
Savolitinib
Volitinib; HMPL-504; AZD-6094
|
c-Met/HGFR
|
Cancer
|
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.
|
-
- HY-14649
-
Retinoic acid
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-120994B
-
Sp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.
|
-
- HY-12810
-
EHop-016
|
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-13434A
-
Ionomycin calcium
SQ23377 calcium
|
Calcium Channel
PKC
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC).
|
-
- HY-N7056
-
4'-Hydroxychalcone
|
Proteasome
|
Cancer
Inflammation/Immunology
|
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.
|
-
- HY-B2145
-
Ilaprazole sodium
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-B0413S
-
Fenbendazole-d3
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Antibiotic
|
Infection
|
Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole is a benzimidazole anthelmintic. Fenbendazole is active against Giardia in vitro (IC50 = 0.3 μM). Fenbendazole (20 mg/kg) prevents infiltration of parasites into the brain in a rabbit model of E. cuniculi infection. Fenbendazole also activates HIF-1α and prevents oxidative stress-induced death in primary neurons in vitro.
|
-
- HY-B0116
-
-
- HY-B0116A
-
-
- HY-131945
-
-
- HY-N6009
-
8-Deoxygartanin
|
Parasite
NF-κB
|
Infection
|
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE). 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum. 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM.
|
-
- HY-124952
-
iKIX1
|
Fungal
|
Infection
|
iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.
|
-
- HY-19805
-
STO-609
|
CaMK
AMPK
Autophagy
|
Metabolic Disease
|
STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
|
-
- HY-120111A
-
MW-150 hydrochloride
MW01-18-150SRM hydrochloride
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Neurological Disease
|
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
|
-
- HY-123033A
-
Nicotinamide riboside chloride
|
Sirtuin
|
Metabolic Disease
Neurological Disease
|
Nicotinamide riboside Chloride, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
|
-
- HY-N6743
-
Cercosporin
|
PKC
|
Cancer
|
Cercosporin is produced by a plant pathogen, Cercosporakikuchii, and the elsinochromes, pigments of the elsinoe family of fungi. Cercosporin is a potent photosensitizer with a short activation wavelength, mostly suitable for superficial photodynamic therapy (PDT) treatments, especially when it is necessary to avoid perforations.
Cercosporin contains the perylenequinone structural features necessary to PKC activity with an IC50 of 0.6-1.3 μM.
|
-
- HY-P1309A
-
-
- HY-N7110
-
6-Hydroxyflavone
|
Others
|
Inflammation/Immunology
|
6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .
|
-
- HY-10585
-
Valproic acid
VPA; 2-Propylpentanoic Acid
|
HDAC
Autophagy
Mitophagy
HIV
Notch
|
Cancer
|
Valproic acid (VPA; 2-Propylpentanoic Acid) 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 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.
|
-
- HY-P1446
-
Cholera toxin
Choleragen
|
Adenylate Cyclase
|
Inflammation/Immunology
|
Cholera toxin (Choleragen), an AB(5)-subunit toxin, enters host cells by binding the ganglioside GM1 at the plasma membrane (PM) and travels retrograde through the trans-Golgi Network into the endoplasmic reticulum (ER). Choleragen activates adenylate cyclase by catalyzing ADP-ribosylation of Gs alpha, the stimulatory guanine nucleotide-binding protein.
|
-
- HY-136093A
-
IM156
HL156A; HL271 acetate
|
AMPK
|
Cancer
Neurological Disease
|
IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
|
-
- HY-N6246
-
Asperulosidic Acid
|
NF-κB
ERK
|
Cancer
Inflammation/Immunology
|
Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities.
ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
|
-
- HY-115452
-
G5-7
|
JAK
Apoptosis
|
Cancer
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
|
-
- HY-117857
-
-
- HY-N4237
-
Saikogenin D
|
Prostaglandin Receptor
Potassium Channel
|
Inflammation/Immunology
|
Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca 2+]i due to Ca 2+ release from intracellular stores.
|
-
- HY-N5097
-
-
- HY-123033
-
Nicotinamide riboside
|
Sirtuin
|
Metabolic Disease
Neurological Disease
|
Nicotinamide riboside, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
|
-
- HY-101597
-
NVX-207
|
Apoptosis
|
Cancer
|
NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP.
|
-
- HY-16576
-
TCS-PIM-1-4a
SMI-4a
|
Pim
Apoptosis
|
Cancer
|
TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).
|
-
- HY-G0021
-
N-Desmethylclozapine
Norclozapine; Desmethylclozapine; Normethylclozapine
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
|
-
- HY-104027
-
-
- HY-A0072S
-
Zilpaterol-d7
|
Adrenergic Receptor
|
Endocrinology
|
Zilpaterol-d7 is a deuterium labeled Zilpaterol. Zilpaterol is a β-adrenergic receptor agonist that putatively, through activation of protein kinase A, increases protein synthesis in skeletal muscle fibers as well as reduces lipogenesis and increases lipolysis in adipose tissues. Formulations containing Zilpaterol have been used to increase lean body weight and improve feed efficiency in commercial beef cattle.
|
-
- HY-13634A
-
Ezatiostat
TER199(free base); TLK199
|
Gutathione S-transferase
Apoptosis
|
Cancer
|
Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.
|
-
- HY-120348
-
-
- HY-100233
-
IQ-1S free acid
|
JNK
|
Cancer
Inflammation/Immunology
|
IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
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- HY-100822
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(R)-(+)-HA-966
(+)-HA-966
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iGluR
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Neurological Disease
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(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.
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- HY-101664
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Ilaprazole
IY-81149
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Proton Pump
TOPK
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Cancer
Inflammation/Immunology
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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.
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- HY-15271A
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WYE-687 dihydrochloride
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mTOR
PI3K
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Cancer
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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.
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- HY-14602
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Tramiprosate
Homotaurine; 3-Amino-1-propanesulfonic acid
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Amyloid-β
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Cancer
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Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent deposition
target: Aβ
In vitro: Tramiprosate provides neuroprotection against Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors.
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- HY-103193
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NKH477
Colforsin dapropate hydrochloride
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Adenylate Cyclase
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Cardiovascular Disease
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NKH477 (Colforsin dapropate hydrochloride) is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.
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- HY-113756A
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Latanoprost acid
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Prostaglandin Receptor
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Inflammation/Immunology
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Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
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- HY-P1076
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CALP2
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Calcium Channel
Phosphodiesterase (PDE)
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Inflammation/Immunology
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CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
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- HY-116364A
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AZT triphosphate TEA
3'-Azido-3'-deoxythymidine-5'-triphosphate TEA
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HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
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Infection
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AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.
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- HY-13716
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Noscapine
(S,R)-Noscapine
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Opioid Receptor
Apoptosis
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Cancer
Inflammation/Immunology
Neurological Disease
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Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.
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- HY-12383
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Pelubiprofen
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COX
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Inflammation/Immunology
Neurological Disease
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Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects.
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- HY-W014502
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D-Kynurenine
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Aryl Hydrocarbon Receptor
Endogenous Metabolite
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Cancer
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D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).
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- HY-102070
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NS13001
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Potassium Channel
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Neurological Disease
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NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.
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- HY-101761
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TM5441
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PAI-1
Apoptosis
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Cancer
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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.
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- HY-126047B
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