Search Result
| Targets Recommended: |
PAI-1
|
Results for "
activator
" in MCE Product Catalog:
1945
Inhibitors & Agonists
1
Biochemical Assay Reagents
177
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-144287
-
-
- HY-125996
-
|
NR1H4 activator 1
|
FXR
|
Inflammation/Immunology
|
|
NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
|
-
- HY-139791
-
|
KCNQ2/3 activator-1
|
Potassium Channel
|
Cancer
|
|
KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A).
|
-
- HY-145390
-
|
Nrf2 activator-1
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the treatment of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1).
|
-
- 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-101788
-
-
- HY-146109
-
|
RyRs activator 1
|
Parasite
|
Infection
|
|
RyRs activator 1 (compound 7f) is a potent activator of ryanodine receptors (RyRs). RyRs activator 1 at 0.5 mg/L displays 100% larvicidal activity. The larvicidal activity of RyRs activator 1 is 90% at 0.01 mg/L.
|
-
- 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-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-146110
-
|
RyRs activator 2
|
Parasite
|
Infection
|
|
RyRs activator 2 (compound 7o) is a potent activator of ryanodine receptors (RyRs). RyRs activator 2 is 30% larvicidal activity, comparable to chlorantraniliprole (30%) and better than cyantraniliprole (10%).
|
-
- HY-139674
-
-
- 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-104038
-
-
- HY-135884
-
-
- HY-13971
-
-
- HY-134476
-
-
- HY-111317
-
|
SIRT1 activator 3
|
Sirtuin
|
Metabolic Disease
|
|
SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches.
|
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- HY-135883
-
-
- HY-U00292
-
-
- HY-139692
-
|
EAAT2 activator 1
|
EAAT2
|
Neurological Disease
|
|
EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently.
|
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- HY-124873
-
|
SERCA2a activator 1
|
Calcium Channel
|
Cardiovascular Disease
|
|
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
|
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- HY-12647
-
-
- HY-143316
-
|
NPR-C activator 1
|
Others
|
Neurological Disease
|
|
NPR-C activator 1 (Compound 1) is a potent activator of natriuretic peptide receptor C (NPR-C). C-type natriuretic peptide (CNP) is involved in the regulation of vascular homeostasis. NPR-C activator 1 is identified as a potent agonist (EC50 ∼ 1 μM) with promising in vivo pharmacokinetic properties.
|
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- HY-128574
-
-
- HY-136073
-
-
- 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 EC50s of 28-29 nM.
|
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- HY-111671
-
|
SOS1 activator 1
|
Ras
|
Cancer
|
|
SOS1 activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS.
|
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- HY-146095
-
|
p53 Activator 2
|
MDM-2/p53
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models.
|
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- HY-122760
-
-
- HY-145992
-
-
- HY-146086
-
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Nrf2 activator-4
|
Keap1-Nrf2
ROS
|
Inflammation/Immunology
Neurological Disease
|
|
Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC50 of 0.63 µM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model.
|
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- HY-145879
-
|
Nrf2 activator-2
|
Keap1-Nrf2
|
Cancer
|
|
Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells.
|
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- HY-144231
-
|
SIK1 activator 1
|
Others
|
Metabolic Disease
|
|
SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis by enhancing the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice.
|
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- 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.
|
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- HY-144828
-
-
- 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.
|
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- 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.
|
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- HY-123962
-
|
G6PD activator AG1
|
Others
|
Metabolic Disease
|
|
G6PD activator AG1 is a potent and selective glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ. G6PD activator AG1 reduces hemolysis of human erythrocytes.
|
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- 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.
|
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- HY-106199
-
-
- HY-P1536
-
-
- 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.
|
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- HY-115627
-
|
PKUMDL-LC-101-D04
GPX4-activator-1d4
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
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PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a potent ferroptosis regulator glutathione peroxidase 4 (GPX4) allosteric activator (pEC50=4.7). PKUMDL-LC-101-D04 increases GPX4 activity to 150% at 20 μM in the cell-free assay and 61 μM in cell extracts.
|
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- 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.
|
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- 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.
|
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- HY-145983
-
|
Suc-Gly-Pro-AMC
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Others
|
Cancer
|
|
Suc-Gly-Pro-AMC is a fibroblast activation protein (FAP)-specific substrate. Suc-Gly-Pro-AMC can be used to study the activity of FAP.
|
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- HY-112472
-
|
S3969
|
Sodium Channel
|
Metabolic Disease
|
|
S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC50 for S3969 activation of hENaC is 1.2 μm.
|
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- HY-121320
-
|
Raptinal
|
Caspase
|
Cancer
|
|
Raptinal, a agent that directly activates caspase-3, initiates intrinsic pathway caspase-dependent apoptosis. Raptinal is able to rapidly induce cancer cell death by directly activating the effector caspase-3, bypassing the activation of initiator caspase-8 and caspase-9.
|
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- HY-106029
-
|
4α-TPA
α-TPA
|
Others
|
Cancer
|
|
4α-TPA is an inactive form of TPA, and is used as a negative control for TPA-activated events.
|
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- HY-N1033
-
-
- HY-122098
-
-
- HY-A0144
-
-
- HY-139553
-
|
Zunsemetinib
ATI-450; CDD-450
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.
|
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- HY-19345
-
|
Vacquinol-1
NSC13316
|
Others
|
Cancer
|
|
Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways. Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model. Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell.
|
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- HY-10255AS
-
|
Sunitinib-d10
SU 11248-d10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
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- HY-107753
-
|
XRP44X
|
Ras
|
Cancer
Inflammation/Immunology
|
|
XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules.
|
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- HY-117958
-
|
HJC0197
|
Ras
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
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- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
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- HY-N8218
-
-
- 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.
|
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- 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-139303
-
|
LUF5771
|
Others
|
Endocrinology
|
|
LUF5771 is a potent allosteric recombinant luteinizing hormone (recLH) and Org 43553 inhibitor. LUF5771 is able to partially activate the LH receptor with low efficacy.
|
-
- HY-111516
-
-
- HY-114981
-
|
SRTCX1002
|
Sirtuin
|
Inflammation/Immunology
|
|
SRTCX1002 is a potent activator of SIRT1 (STAC), suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB Activity. SRTCX1002 suppresses stimuli-induced NF-κB transcriptional activation and LPS-induced TNFα secretion with IC50s of 0.71 and 7.58 µM, respectively.
|
-
- 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-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).
|
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- HY-N9615
-
-
- HY-117917
-
-
- HY-16785
-
|
Veledimex
INXN-1001; RG-115932
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.
|
-
- 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-124702
-
|
ICA-105574
|
Potassium Channel
|
Cardiovascular Disease
|
|
ICA-105574 is a potent and efficacious hERG channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC50 value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2.
|
-
- HY-N10227
-
-
- 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-109897
-
|
CV-6209
|
Others
|
Cardiovascular Disease
|
|
CV-6209 is a potent antagonist of platelet activating factor (PAF). CV-6209 inhibits the PAF-induced aggregation of rabbit and human platelets, with IC50s of 75 nM and 170 nM, respectively. CV-6209 can inhibit PAF-induced hypotension in rats.
|
-
- 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-101923A
-
-
- HY-101923
-
-
- HY-113492
-
-
- HY-115768
-
|
Compound 48/80
Poly-p-methoxyphenethylmethylamine
|
Others
|
Cancer
Neurological Disease
|
|
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways.
|
-
- HY-111447
-
-
- 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-137331
-
|
FAPI-46
|
Others
|
Cancer
|
|
FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI-46 can be used for tumor imaging of a multitude of different cancers.
|
-
- HY-10595
-
-
- 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-P9952
-
|
Belimumab
LymphoStat B
|
TNF Receptor
|
Inflammation/Immunology
|
|
Belimumab (LymphoStat B) is a human IgG1λ monoclonal antibody that inhibits B-cell activating factor (BAFF). Belimumab can be used for systemic lupus erythematosus (SLE) research.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
|
-
- HY-136501
-
|
MRS2395
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6.
|
-
- HY-114842
-
|
TDRL-551
|
Others
|
Cancer
|
|
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50=18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the efficacy of Platinum (Pt)-based chemotherapy in lung and ovarian cancer. RPA plays essential roles in both nucleotide excision repair (NER) and homologous recombination (HR), along with its role in DNA replication and DNA damage checkpoint activation.
|
-
- HY-N10322
-
|
2-Hydroxyemodin
|
Drug Metabolite
|
Others
|
|
2-Hydroxyemodin is an active metabolite of emodin in the hepatic microsomes. Emodin is an anthraquinone present in fungal metabolites and constituent of rhubarb. 2-Hydroxyemodin proves to be mutagenic to Salmonella typhimurium TA1537 in the absence of activation system.
|
-
- 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-15394
-
-
- HY-14165
-
-
- HY-100164
-
|
SDZ-MKS 492
MKS 492
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
|
-
- HY-B1456A
-
|
Fenoprofen
LILLY-53858
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation.
|
-
- 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-108391
-
|
C8-Ceramide
N-Octanoyl-D-erythro-sphingosine
|
Apoptosis
PKC
Autophagy
|
Cancer
Inflammation/Immunology
|
|
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
|
-
- HY-117724
-
|
AZ3976
|
PAI-1
|
Cardiovascular Disease
|
|
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay.
|
-
- HY-145239
-
|
PD-1/PD-L1-IN-13
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 + T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model.
|
-
- HY-P1375A
-
-
- 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.
|
-
- HY-121035
-
|
7BIO
7-Bromoindirubin-3-Oxime
|
CDK
GSK-3
|
Neurological Disease
|
|
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice[1].
|
-
- HY-137446
-
-
- 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-19339
-
-
- HY-N2164
-
-
- 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.
|
-
- HY-15122
-
-
- HY-15416
-
-
- HY-P1308
-
-
- HY-P0283
-
-
- HY-131012
-
-
- HY-15122A
-
-
- HY-P1308A
-
-
- 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.
|
-
- HY-122974
-
-
- 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-P0297
-
-
- HY-132247A
-
|
(±)-ErSO
|
Others
|
Cancer
|
|
(±)-ErSO is the racemate of ErSO. ErSO is a selective anticipatory unfolded protein response (a-UPR) activator.
|
-
- 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.
|
-
- HY-P3414A
-
|
Proteasome-activating peptide 1 TFA
|
Others
Proteasome
|
Neurological Disease
|
|
Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis.
|
-
- HY-N0277
-
-
- HY-N3425
-
|
Kazinol U
|
AMPK
|
Others
|
|
Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation.
|
-
- HY-142163
-
|
S62798
|
Others
|
Cardiovascular Disease
|
|
S62798 is a selective and potent inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) with an IC50 value of 6 mM.
|
-
- HY-N1446B
-
-
- HY-108356
-
|
NS3694
|
Apoptosis
|
Cancer
|
|
NS3694, a diarylurea compound, is an apoptosome inhibitor. NS3694 inhibits apoptosome formation and caspase activation.
|
-
- HY-111364
-
|
Roy-Bz
|
PKC
|
Cancer
|
|
Roy-Bz is a selecive PKCδ activator. Roy-Bz potently inhibits the proliferation of colon cancer cells by inducing a PKCδ-dependent mitochondrial apoptotic pathway involving caspase-3 activation.
|
-
- 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-N0509
-
-
- HY-139214
-
|
IXA4
|
IRE1
|
Neurological Disease
|
|
IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation.
|
-
- HY-110273
-
-
- 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.
|
-
- HY-19635A
-
-
- HY-100381
-
-
- HY-B0493
-
-
- HY-110153
-
|
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-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-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-B0172A
-
-
- HY-P3410
-
|
Trichomide A
|
Phosphatase
|
Inflammation/Immunology
|
|
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases.
|
-
- HY-N4231
-
-
- 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.
|
-
- HY-10484
-
-
- HY-103239
-
-
- HY-108593
-
-
- HY-70062
-
-
- HY-122203
-
|
PCS1055 dihydrochloride
|
mAChR
AChE
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
|
-
- 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.
|
-
- 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-131018
-
-
- HY-134975
-
|
NY2267
|
c-Myc
|
Cancer
|
|
NY2267 is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM. NY2267 inhibits Myc- and Jun-induced transcriptional activation.
|
-
- HY-14714
-
-
- HY-N1380
-
-
- 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-134964
-
-
- 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.
|
-
- 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-136172
-
|
ESI-08
|
Ras
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
|
-
- HY-75342
-
-
- HY-107586
-
|
Demethylasterriquinone B1
DAQ B1; L-783281; Dimethylasterriquinone
|
Insulin Receptor
Akt
|
Endocrinology
|
|
Demethylasterriquinone B1 is a selective insulin receptor activator. Demethylasterriquinone B1 stimulates tyrosine phosphorylation of the IR β subunit, and the activation of PIK3 and AKT.
|
-
- HY-P2519A
-
-
- 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-18739
-
|
Phorbol 12-myristate 13-acetate
PMA; TPA; Phorbol myristate acetate
|
PKC
SphK
NF-κB
|
Inflammation/Immunology
|
|
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells.
|
-
- HY-122550
-
|
Artemisitene
|
Keap1-Nrf2
Topoisomerase
Apoptosis
|
Cancer
|
|
Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
|
-
- 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-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-15723A
-
-
- HY-P0240
-
-
- HY-101594
-
-
- HY-101675
-
-
- 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.
|
-
- HY-N0878
-
|
Bufotalin
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation.
|
-
- HY-N5101
-
-
- 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-P2518
-
-
- HY-136251
-
|
BRD0539
|
CRISPR/Cas9
|
Infection
|
|
BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.
|
-
- HY-117103
-
|
AMG131
INT131
|
PPAR
|
Metabolic Disease
|
|
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM).
|
-
- HY-119874
-
|
Alkannin
|
Ras
|
Cancer
Inflammation/Immunology
|
|
Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent.
|
-
- HY-N4323
-
-
- 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.
|
-
- 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-P2518A
-
-
- 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 can also 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-111363
-
-
- HY-112878
-
-
- 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-13626
-
|
Spisulosine
ES-285
|
PKC
|
Cancer
|
|
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation.
|
-
- HY-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-124306
-
|
ML-099
CID-888706
|
Ras
|
Cancer
|
|
ML-099 (CID-888706) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, Rab7, and Rab-2A.
|
-
- HY-B0172AS
-
|
Isoallolithocholic acid-d2
3β-Hydroxy-5α-cholanic acid-d2
|
Potassium Channel
|
Neurological Disease
|
|
Isoallolithocholic acid-d2 is the deuterium labeled Isoallolithocholic acid. Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes.
|
-
- 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-B0493S
-
-
- 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-101047S
-
|
D-erythro-Sphingosine-d7
Erythrosphingosine-d7; erythro-C18-Sphingosine-d7; trans-4-Sphingenine-d7
|
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
|
D-erythro-Sphingosine-d7 (Erythrosphingosine-d7) is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
|
-
- HY-12364
-
|
C75
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator.
|
-
- HY-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-132247
-
|
ErSO
|
Others
|
Cancer
|
|
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.
|
-
- HY-N8498
-
|
GKK1032B
|
Apoptosis
|
Cancer
|
|
GKK1032B is an alkaloid compound that can be found in endophytic fungus Penicillium sp. GKK1032B can induce the apoptosis of human osteosarcoma MG63 cells through caspase pathway activation.
|
-
- HY-14255
-
-
- HY-112060
-
-
- HY-12376
-
-
- HY-13529
-
-
- HY-14290A
-
-
- HY-P0256
-
-
- HY-117962
-
|
(Rac)-BI 703704
|
Guanylate Cyclase
|
Metabolic Disease
|
|
(Rac)-BI 703704 is a potent soluble guanylyl cyclase (sGC) activator. (Rac)-BI 703704 reduces progression of renal damage in the ZSF1 rat, and highlight the potential of sGC activation as an effective therapy for diabetic nephropathy.
|
-
- 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-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-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-N0279
-
-
- HY-P1847
-
|
IKKγ NBD Inhibitory Peptide
|
NF-κB
|
Cancer
|
|
IKKγ NBD Inhibitory Peptide is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
|
-
- HY-B0099S
-
|
Edaravone-d5
MCI-186-d5
|
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone D5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
|
-
- 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
|
Phosphatase
|
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-N1446S4
-
-
- HY-14233
-
-
- HY-B1197
-
-
- HY-14909
-
-
- HY-59047
-
-
- HY-P0136
-
-
- HY-14256
-
-
- HY-10164
-
-
- HY-100295
-
-
- HY-U00040
-
-
- 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-128920
-
|
Phortress free base
|
Cytochrome P450
|
Cancer
|
|
Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
|
-
- HY-P1847A
-
-
- 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-N8041
-
|
Mogroside III A2
|
HSV
|
Infection
|
|
Mogroside III A2 is a cucurbitane glycoside. Mogroside III A2 can inhibit Epstein-Barr virus early antigen (EBV-EA) activation. Mogroside III A2 shows weak inhibitory effects on activation of NOR 1.
|
-
- HY-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-N0896
-
|
Inulicin
1-O-Acetylbritannilactone
|
NF-κB
COX
|
Cancer
Inflammation/Immunology
|
|
Inulicin (1-O-Acetylbritannilactone) is an active compound that inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
|
-
- HY-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-17538S
-
-
- HY-100602
-
-
- HY-U00434
-
-
- HY-N3989
-
-
- HY-14181
-
-
- HY-N3463
-
-
- HY-N0553
-
-
- HY-N0441
-
-
- HY-101214
-
-
- HY-101738A
-
-
- HY-100934
-
-
- HY-100153
-
-
- HY-14181A
-
-
- 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-138936
-
|
SSK1
|
p38 MAPK
Apoptosis
|
Inflammation/Immunology
|
|
SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted prodrug attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of 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-B0887S
-
|
Permethrin-d5
|
Parasite
|
Infection
|
|
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
|
-
- 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-B0167S
-
-
- 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
Autophagy
|
Endocrinology
Metabolic Disease
|
|
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation, autophagy and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
|
-
- HY-117727A
-
|
Leriglitazone hydrochloride
Hydroxypioglitazone hydrochloride
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone (Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) hydrochloride 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) hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM.
|
-
- 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 a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an 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
Apoptosis
|
Cancer
|
|
NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and can be used for breast cancer research. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes.
|
-
- HY-17500
-
|
Ataciguat
HMR-1766
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects.
|
-
- HY-N0219
-
|
Bicuculline
(+)-Bicuculline; d-Bicuculline
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) .
|
-
- 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-N1446S1
-
-
- HY-131265
-
-
- HY-N1446S3
-
-
- 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-N6577
-
-
- HY-N10125
-
-
- HY-76847
-
-
- HY-100242
-
-
- HY-50662
-
-
- HY-U00411
-
-
- HY-15341
-
-
- HY-15300
-
-
- HY-N8418
-
-
- HY-136094
-
-
- HY-104005
-
-
- HY-16397A
-
-
- HY-101804
-
-
- HY-19739
-
|
JW74
|
Wnt
|
Cancer
|
|
JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
|
-
- HY-17376S2
-
-
- 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-139667
-
|
PKM2-IN-3
|
Pyruvate Kinase
|
Neurological Disease
|
|
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
|
-
- HY-N3796
-
|
Echinulin
Echinuline
|
NF-κB
|
Inflammation/Immunology
|
|
Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of T cell subsets, which leads to NF-κB activation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent.
|
-
- HY-N2025
-
|
Oroxin A
|
PPAR
Glucosidase
|
Metabolic Disease
|
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also 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-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-113673
-
|
A-935142
|
Potassium Channel
|
Cardiovascular Disease
|
|
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.
|
-
- HY-B0069
-
|
Fludarabine
F-ara-A; NSC 118218
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
STAT
Apoptosis
|
Cancer
|
|
Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.
|
-
- HY-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-N3552
-
|
Catalposide
|
NF-κB
|
Inflammation/Immunology
|
|
Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages.
|
-
- HY-103697
-
|
Gardiquimod
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
|
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-100447
-
-
- HY-B1140
-
-
- HY-144289
-
-
- HY-139858
-
-
- HY-N9404
-
-
- 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-128642
-
|
FAPI-2
|
Others
|
Cancer
|
|
FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
|
-
- HY-12359
-
-
- 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-N1446S
-
-
- 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-10162S1
-
|
Olaparib-d8
AZD2281-d8; KU0059436-d8
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib D8 (AZD2281 D8) is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
|
-
- 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-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-110302
-
|
6'-GNTI dihydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
|
-
- 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-12512
-
|
cGAMP
Cyclic GMP-AMP; 3',3'-cGAMP
|
STING
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-15027S
-
-
- HY-117727S
-
|
Leriglitazone-d4
Hydroxypioglitazone-d4
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone-d4 is deuterium labeled Leriglitazone. 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-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-Y1683
-
|
DL-Menthol
Racementhol
|
GABA Receptor
|
Others
|
|
DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor.
|
-
- HY-111441
-
-
- HY-105198
-
|
Lexipafant
BB-882
|
Others
|
Inflammation/Immunology
|
|
Lexipafant is a platelet-activating factor (PAF) antagonist that inhibits the inflammatory response and is used in the treatment of acute pancreatitis.
|
-
- HY-12885A
-
-
- HY-128643
-
|
FAPI-4
|
Others
|
Cancer
|
|
FAPI-4 is a fibroblast activation protein (FAP) inhibitor used in cancer research.
|
-
- HY-P0195
-
-
- HY-P0249A
-
-
- HY-107854
-
-
- HY-15840
-
|
YLF-466D
C24
|
AMPK
|
Cancer
|
|
YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
|
-
- 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-115685
-
|
3-Methyl-GABA
|
GABA Receptor
|
Neurological Disease
|
|
3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABAA receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity.
|
-
- 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-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-N0492
-
-
- HY-116626
-
|
SM-7368
|
NF-κB
p38 MAPK
MMP
|
Cancer
|
|
SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
|
-
- HY-110385
-
|
cGAMP disodium
Cyclic GMP-AMP disodium; 3',3'-cGAMP disodium
|
STING
Endogenous Metabolite
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) disodium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- 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-110385A
-
|
cGAMP diammonium
Cyclic GMP-AMP diammonium; 3',3'-cGAMP diammonium
|
STING
Endogenous Metabolite
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-17363
-
-
- 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-10119A
-
|
Vorapaxar sulfate
SCH 530348 sulfate
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-N1446S2
-
-
- HY-124748A
-
-
- HY-12639A
-
-
- HY-N1260
-
|
Scutebarbatine A
(-)-Scutebarbatine A
|
Others
|
Cancer
|
|
Scutebarbatine A inhibits the proliferation of HCC cells and triggers their apoptosis via the activation of MAPK and ER stress.
|
-
- 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
|
Others
|
|
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-143510
-
|
RMC-4627
|
mTOR
|
Cancer
|
|
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
|
-
- HY-138652
-
-
- HY-18965
-
-
- HY-N0486
-
-
- HY-18723
-
-
- HY-145938
-
|
OncoFAP
|
Others
|
Cancer
|
|
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
|
-
- HY-137477
-
-
- HY-15252
-
-
- HY-117793
-
-
- HY-N0019S
-
-
- HY-107543
-
|
8-CPT-2Me-cAMP sodium
|
Ras
|
Others
|
|
8-CPT-2Me-cAMP sodium is a selective activator of exchange proteins activated by cAMP (Epac), the cAMP sensitive guanine nucleotide exchange factors (GEFs) for the small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50> 10 μM). 8-CPT-2Me-cAMP sodium stimulates Epac-mediated Ca 2+ release in pancreatic β-cells in vitro.
|
-
- HY-111673
-
|
8-CPT-Cyclic AMP sodium
8-CPT-cAMP sodium; 8-(p-Chlorophenylthio)-cAMP sodium
|
PKA
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator.
|
-
- HY-139308
-
|
T0467
|
Mitochondrial Metabolism
|
Neurological Disease
|
|
T0467 activates parkin mitochondrial translocation in a PINK1-dependent manner in vitro. T0467 do not induce mitochondrial accumulation of PINK1in dopaminergic neurons. T0467 is a potential compound for PINK1-Parkin signaling activation, and can be used for parkinson's disease and related disorders research.
|
-
- HY-B0289S
-
-
- 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-113313S1
-
|
Aldosterone-d7
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone-d7 is the deuterium labeled Aldosterone. 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-128468
-
-
- 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-101790
-
-
- 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-100181
-
-
- 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-101625
-
|
Recilisib
ON 01210
|
Akt
PI3K
|
Cancer
|
|
Recilisib (ON 01210) is a radioprotectant, which can activate AKT, PI3K activities in cells.
|
-
- 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-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-14993
-
|
SCH79797
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-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-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-139504
-
|
CC-99677
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). CC-99677 is extracted from patent WO2020236636, compound 1.
|
-
- HY-10162S3
-
|
Olaparib-d4-1
AZD2281-d4-1; KU0059436-d4-1
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
|
-
- 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-132173
-
|
GL0388
|
Bcl-2 Family
|
Cancer
|
|
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
|
-
- 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-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. COH-SR4 can be used for the research of obesity and related metabolic disorders.
|
-
- 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-101346
-
-
- HY-N0628
-
-
- HY-N10196
-
-
- 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-145882
-
|
BOD-NH-NP
|
Others
|
Others
|
|
BOD-NH-NP is an activatable fluorescent probe for imaging endogenous nitric oxide via the eNOS enzymatic pathway.
|
-
- 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-114745
-
|
MoTP
|
Others
|
Cancer
|
|
MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.
|
-
- 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-139401
-
|
FAPI-34
|
Others
|
Cancer
|
|
FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).
|
-
- HY-111202
-
-
- HY-N0411
-
|
β-Carotene
Provitamin A; beta-Carotene
|
Endogenous Metabolite
ROS
Apoptosis
|
Cancer
Metabolic Disease
|
|
β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities.
|
-
- 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-12496
-
|
NS-1619
|
Potassium Channel
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
NS-1619 is an opener of large conductance Ca 2+-activated K + (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.
|
-
- HY-130354
-
|
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-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. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-137455
-
-
- HY-128586A
-
-
- HY-16785A
-
-
- HY-14351
-
-
- HY-107004A
-
-
- HY-19330
-
-
- HY-N10114
-
-
- HY-B0686
-
-
- HY-N1533
-
-
- HY-100941
-
-
- HY-143477
-
-
- HY-P1534
-
-
- HY-N2506
-
-
- HY-113221
-
-
- HY-P0249
-
-
- HY-B0686A
-
-
- HY-N6617
-
-
- 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-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-144634
-
|
DDO-7263
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2 activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory 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 can also 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
|
Calcium Channel
|
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-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-B0513
-
-
- HY-15251
-
-
- HY-N6630
-
-
- HY-103683
-
-
- HY-15285
-
-
- HY-N2283
-
-
- HY-139742
-
|
ADTL-SA1215
|
Sirtuin
|
Cancer
|
|
ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
|
-
- HY-N0593
-
-
- 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-110274
-
-
- 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-N9481
-
-
- 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-P1562
-
|
PUMA BH3
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- HY-101239
-
-
- 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-126421
-
-
- 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-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. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
|
-
- HY-12005
-
|
Fingolimod hydrochloride
FTY720
|
LPL Receptor
PAK
|
Inflammation/Immunology
Cancer
|
|
Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
|
-
- HY-P1061
-
|
Colivelin
|
STAT
Amyloid-β
|
Neurological Disease
|
|
Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
|
-
- HY-P3412
-
|
MMI-0100
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease.
|
-
- HY-10255AS1
-
|
Sunitinib-d4
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d4 (SU 11248-d4) is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-125021
-
|
2BAct
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
|
2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB (HY-12495).
|
-
- 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-14266S
-
|
Dapivirine-d11
TMC120-d11; R147681-d11
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
|
Dapivirine-d11 (TMC120-d11) is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
|
-
- 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-133127
-
|
AR453588
|
Glucokinase
|
Metabolic Disease
|
|
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
|
-
- 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-111789
-
-
- HY-15707
-
-
- HY-133127A
-
-
- HY-N10359
-
-
- 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-117962A
-
-
- 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-B1140S
-
-
- 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-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-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-12519S
-
|
Oltipraz-d3
RP 35972-d3; NSC 347901-d3
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
|
Cancer
|
|
Oltipraz-d3 (RP 35972-d3) is the deuterium labeled Oltipraz. 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-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
Apoptosis
|
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-142694
-
-
- 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-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 lysophosphatidic acid (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-driven β-galactosidase activity.
|
-
- 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-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-132878
-
|
FgGpmk1-IN-1
|
Others
|
Infection
|
|
FgGpmk1-IN-1 is a novel fusarium graminearum mitogen-activated protein kinase (FgGpmk1) inhibitor with an EC50 value of 3.46 μg/mL.
|
-
- HY-132607
-
-
- HY-N8816
-
-
- HY-119240
-
-
- HY-N3196
-
-
- HY-120272
-
|
SMAP-2
DT-1154
|
Phosphatase
|
Cancer
|
|
SMAP-2 (DT-1154) is an orally active protein phosphatase 2A (PP2A) activator, with anti-cancer activity.
|
-
- 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
|
Adenylate Cyclase
|
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-U00123
-
-
- 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-139573
-
-
- 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-113505
-
|
Delta-12-Prostaglandin J2
Δ12-PGJ2
|
Endogenous Metabolite
Apoptosis
|
Cancer
|
|
Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation.
|
-
- 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. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats.
|
-
- HY-102011A
-
|
BMS-1166 hydrochloride
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
|
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-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-16561S
-
|
Resveratrol-d4
trans-Resveratrol-d4; SRT501-d4
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol-d4 (trans-Resveratrol-d4) is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-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
-
-
- HY-112675
-
-
- HY-U00123A
-
-
- 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-138558
-
-
- HY-115938
-
|
BEC2
|
Others
|
Metabolic Disease
|
|
BEC2 is an ester derivative of Baicalin, with good lipid-lowering activity. BEC2 can direct activate the carnitine palmitoyltransferase 1A (CPT1A).
|
-
- HY-N0605
-
-
- HY-N3055
-
|
Pinusolide
|
Apoptosis
|
Cancer
|
|
Pinusolide is a known platelet-activating factor (PAF) receptor binding antagonist. Pinusolide not only decreases the proliferation activity of tumor cells but specifically induces apoptosis.
|
-
- HY-N0197
-
-
- 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-W048510
-
|
Epiquinidine
|
Others
|
Others
|
|
Epiquinidine, a quinine analogue, can be used as the ggTas2r1 agonist. Epiquinidine activates ggTas2r1 at or beyond 10 µM.
|
-
- HY-133739
-
|
NBD-125
|
RAR/RXR
|
Cancer
|
|
NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC50 of 31.10 μM in KM12C cell.
|
-
- HY-143401
-
|
Hit 1
|
Others
|
Metabolic Disease
|
|
Hit 1 is an activator of ansulin degrading enzyme (IDE), with an EC50 of 5.5 μM. Hit 1 can decrease glucose-stimulating insulin secretion.
|
-
- HY-15725
-
-
- HY-145788
-
-
- HY-110192
-
-
- HY-109030
-
-
- HY-16642A
-
-
- HY-100965
-
-
- HY-111616
-
|
GSK1820795A
|
Others
|
Others
|
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides.
|
-
- 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-N10062
-
|
Amakusamine
|
Others
|
Others
|
|
Amakusamine inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinuclear osteoclasts with an IC50 value of 10.5 μM in RAW264 cells.
|
-
- 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-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-109128
-
|
Danicamtiv
MYK-491
|
Myosin
|
Cancer
|
|
Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
|
-
- HY-145127
-
|
ETZ
C3-CA-DTZ
|
Others
|
Neurological Disease
|
|
ETZ (C3-CA-DTZ) is a promising luciferase substrate (prosubstrate) activatable in vivo by nonspecific esterase to enhance the brain delivery of the luciferin.
|
-
- HY-131958
-
|
D942
|
AMPK
|
Cancer
|
|
D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth.
|
-
- HY-104026B
-
-
- 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
-
-
- HY-111498A
-
|
RGX-104
|
LXR
|
Cancer
Inflammation/Immunology
|
|
RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
|
-
- 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-116084S
-
-
- 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-P3316
-
|
OSK-1
|
Potassium Channel
|
Inflammation/Immunology
Neurological Disease
|
|
OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca 2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug.
|
-
- HY-117433S
-
-
- 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-15671A
-
|
GKA50 quarterhydrate
|
Glucokinase
|
Metabolic Disease
|
|
GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.
|
-
- 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-121629
-
|
PS210
|
PDK-1
|
Cancer
|
|
PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
|
-
- HY-N0492S
-
-
- 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 that 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-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-B1221S
-
|
Flufenamic acid-d4
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ 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-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-16708
-
|
ZLN024
|
AMPK
|
Metabolic Disease
|
|
ZLN024 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-N1490
-
-
- 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-122908
-
|
Atuliflapon
AZD5718
|
FLAP
|
Cardiovascular Disease
|
|
Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
|
-
- HY-N6781
-
|
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-112650
-
-
- HY-139621
-
-
- HY-115769
-
|
1,2-Didecanoylglycerol
|
PKC
|
Endocrinology
|
|
1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA10) and activates protein kinase C (PKC).
|
-
- HY-101360
-
-
- HY-120872
-
|
AJS1669 free acid
|
|
Metabolic Disease
|
|
AJS1669 free acid is a potent and orally available glycogen synthase (GS) activator. AJS1669 improves glucose metabolism and reduces body fat mass in mice.
|
-
- 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-B0649S1
-
-
- 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-136232
-
-
- 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-100534
-
|
IDE 2
|
TGF-beta/Smad
|
Others
|
|
IDE2 is a small molecule cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) by activating the TGF-βsignaling pathway.
|
-
- HY-103322
-
|
6-Bnz-cAMP sodium salt
|
PKA
|
|
|
6-Bnz-cAMP sodium salt is a cell-permeable cAMP analog. 6-Bnz-cAMP selectively activates cAMP-dependent PKA but not Epac signaling pathways.
|
-
- HY-120261
-
-
- HY-147005
-
-
- HY-B0649
-
-
- HY-N2337
-
-
- HY-15675
-
|
AZD1656
|
Glucokinase
|
Metabolic Disease
|
|
AZD1656 is a potent, selective and orally active glucokinase activator with an EC50 of 60 nM. AZD1656 has the potential for type 2 diabetes research.
|
-
- 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-N10393
-
|
Vibsanin A
|
PKC
HSP
|
Cancer
|
|
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor.
|
-
- HY-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-N0826
-
-
- 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-P1562A
-
|
PUMA BH3 TFA
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- 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-N0486S11
-
-
- HY-N1469
-
-
- HY-B0926A
-
|
Sodium diatrizoate
Diatrizoic acid sodium salt; Sodium amidotrizoate
|
Apoptosis
|
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-115767
-
|
(±)-1,2-Diolein
1,2-Dioleoyl-rac-glycerol
|
PKC
|
Others
|
|
(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) is a PKC activator. (±)-1,2-Diolein increases myotubes Ca 2+ influx.
|
-
- HY-144813
-
|
Gü2602
|
Cathepsin
|
Cancer
Inflammation/Immunology
|
|
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
|
-
- HY-B0887S1
-
|
Permethrin-d9
|
Parasite
|
Infection
|
|
Permethrin-d9 is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
|
-
- HY-14739
-
|
Choline Fenofibrate
ABT-335
|
PPAR
COX
|
Cardiovascular Disease
|
|
Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
|
-
- 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-76847S
-
-
- HY-N6018
-
-
- HY-N0486S4
-
-
- 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-N0486S
-
-
- 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-N0486S12
-
-
- 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-N0486S9
-
-
- HY-121134
-
-
- HY-76847S3
-
-
- 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-103640
-
|
Amifostine thiol dihydrochloride
WR-1065 dihydrochloride
|
MDM-2/p53
|
Cancer
|
|
Amifostine thiol (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-134001
-
-
- HY-110087
-
-
- HY-10257
-
-
- HY-13851
-
|
PS47
|
Others
|
Others
|
|
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48.
|
-
- HY-13008
-
-
- HY-100316
-
-
- HY-P0233
-
-
- HY-122808
-
|
(-)-Camphoric acid
|
mGluR
|
Metabolic Disease
|
|
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1.
|
-
- HY-135898
-
-
- HY-18286
-
|
NCGC00229600
|
TSH Receptor
|
Endocrinology
|
|
NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
|
-
- HY-B0926
-
|
Diatrizoic acid
Diatrizoate; Amidotrizoic acid
|
Apoptosis
|
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-18936
-
-
- 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-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. 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-147082
-
|
GA-017
|
YAP
|
Cancer
|
|
GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids.
|
-
- HY-144765
-
|
NF-κB-IN-4
|
NF-κB
Apoptosis
|
Inflammation/Immunology
Neurological Disease
|
|
NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research.
|
-
- HY-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-N0674
-
|
Dehydrocorydaline
13-Methylpalmatine
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
|
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that 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-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-122743
-
|
Iperoxo
|
mAChR
|
Neurological Disease
|
|
Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR). [ 3H]Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors.
|
-
- 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-19634
-
|
YK-3-237
|
Sirtuin
|
Cancer
|
|
YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells.
|
-
- 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-139701
-
|
NI-Pano
|
Others
|
Cancer
|
|
NI-Pano (CH-03) is a novel hypoxia-activated KDAC inhibitor. NI-Pano (CH-03) is reduced in an O2-dependent manner to release panobinostat.
|
-
- HY-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-108479
-
|
Nolpitantium
SR140333
|
Neurokinin Receptor
|
Neurological Disease
|
|
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation.
|
-
- 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-114164
-
|
Thrombin (MW 37kDa)
|
Thrombin
|
Neurological Disease
|
|
Thrombin (MW 37kDa) is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins.
|
-
- HY-19987A
-
|
BML-284 hydrochloride
|
Wnt
|
Cancer
|
|
BML-284 hydrochloride is a potent and cell-permeable Wnt signaling activator. BML-284 induces TCF-dependent transcriptional activity with an EC50 of 700 nM.
|
-
- HY-107780A
-
-
- 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-B2205
-
|
Magnesium silicate
Activated magnesium silicate
|
Fungal
|
Infection
Inflammation/Immunology
|
|
Magnesium silicate (Activated magnesium silicate) is a compound of magnesium oxide (MgO) and silicon dioxide (SiO2). Magnesium silicate is used in antiacid and antiulcer preparation, and as a deodorizer, decolorizer and antifungal.
|
-
- HY-15124
-
-
- HY-B1505
-
-
- HY-135715
-
|
(E)-UK122 TFA
|
Others
|
Others
|
|
(E)-UK122 TFA is the isomer of UK122 TFA. UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM.
|
-
- HY-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
Endogenous Metabolite
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-114384B
-
|
NV-5138 hydrochloride
|
mTOR
|
Neurological Disease
|
|
NV-5138 hydrochloride, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 hydrochloride is used for antidepressant studies.
|
-
- HY-114384
-
|
NV-5138
|
mTOR
|
Neurological Disease
|
|
NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 is used for antidepressant studies.
|
-
- HY-110382
-
-
- HY-144812
-
|
Gü1303
|
Cathepsin
|
Cancer
Inflammation/Immunology
|
|
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
|
-
- HY-117861
-
|
ML198
|
Glucosidase
|
Metabolic Disease
|
|
ML198 is a glucocerebrosidase (GCase) modulator with an EC50 of 0.4 μM. ML198 is an activator and non-inhibitory chaperone of glucocerebrosidase. ML198 can be used for the research of Gaucher disease.
|
-
- 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-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
|
Phosphatase
|
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-B0387A
-
|
Ibutilide
U70226E free base
|
Potassium Channel
|
Cardiovascular Disease
|
|
Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K + current (IKr) in AT-1 cells.
|
-
- 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-107780B
-
-
- 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-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-N9508
-
|
Perilla ketone
|
Others
|
Inflammation/Immunology
|
|
Perilla ketone is a naturally occurring xenobiotic compound. Perilla ketone is activated by pulmonary P450 cytochrome enzymes in the lung, resulting in severe pulmonary damage and development of diffuse pulmonary edema.
|
-
- 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
Endogenous Metabolite
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-14233S
-
-
- 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-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-P0172
-
|
ATI-2341
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
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-B0151
-
|
Pregnenolone
3β-Hydroxy-5-pregnen-20-one
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
|
-
- HY-101287
-
|
MPT0B392
|
Microtubule/Tubulin
JNK
Apoptosis
Caspase
|
Cancer
|
|
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
|
-
- HY-10256A
-
|
Adezmapimod hydrochloride
SB 203580 hydrochloride; RWJ 64809 hydrochloride
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator.
|
-
- HY-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-W009731
-
|
Dibenzoylmethane
|
Keap1-Nrf2
|
Cancer
Metabolic Disease
|
|
Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
|
-
- 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-B1121S
-
-
- HY-N0593S1
-
-
- HY-N0593S
-
-
- 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-P3279
-
|
EPQpYEEIPIYL
|
Src
|
Cancer
|
|
EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains.
|
-
- HY-141549
-
|
BPK-21
|
Others
|
Inflammation/Immunology
|
|
BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3.
|
-
- HY-146334
-
|
DFBTA
|
Chloride Channel
|
Inflammation/Immunology
|
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
|
-
- HY-P1955
-
|
Etelcalcetide
AMG 416; KAI-4169
|
CaSR
|
Endocrinology
|
|
Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis.
|
-
- 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-146288
-
|
LXR agonist 2
|
LXR
|
Metabolic Disease
|
|
LXR agonist 2 (compound 18rr) is a potent LXR (liver X receptor) agonist. LXR agonist 2 can stabilize NCOA1 (co-activator), leading to LXR agonism.
|
-
- 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-126361
-
|
ZK824190
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
|
ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
|
-
- HY-123963
-
|
C-178
|
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-32735
-
|
Triptolide
PG490
|
NF-κB
Apoptosis
|
Cancer
|
|
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.
|
-
- HY-114330
-
-
- HY-144776
-
|
NAT
|
Others
|
Neurological Disease
|
|
NAT is an initial hit of NAMPT activator. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases.
|
-
- HY-33350
-
-
- HY-16031
-
-
- HY-13715
-
-
- 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
-
-
- 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-136901
-
-
- 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-N4053
-
|
Heraclenin
|
Others
|
Inflammation/Immunology
|
|
Heraclenin, a natural furanocoumarin, 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-N0486S1
-
-
- 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-126361A
-
-
- HY-U00036A
-
|
Naveglitazar
LY519818
|
PPAR
|
Metabolic Disease
|
|
Naveglitazar (LY519818) is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.
|
-
- 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-110239
-
|
Perlapine
MP-11
|
mAChR
|
Neurological Disease
|
|
Perlapine is a potent muscarinic DREADD (Designer Receptors Exclusively Activated by Designer Drugs) agonist Perlapine exhibits >10000-fold selectivity for hM3Dq over hM3 receptors.
|
-
- HY-B0809S
-
-
- 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-13694S
-
|
Methionine-d3
MRX-1024-d3; D-Methionine-d3
|
GABA Receptor
Endogenous Metabolite
|
Cancer
|
|
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
|
-
- HY-13715A
-
-
- HY-P99040
-
|
Onvatilimab
JNJ-61610588
|
PD-1/PD-L1
|
Cancer
|
|
Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cell Activation) monoclonal antibody. Onvatilimab has an anti-tumor activity.
|
-
- 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-126420
-
-
- HY-13694S1
-
|
Methionine-d4
MRX-1024-d4; D-Methionine-d4
|
GABA Receptor
Endogenous Metabolite
|
|
|
Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
|
-
- HY-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-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-N0708S
-
-
- 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-69359
-
|
Nipecotic acid
(±)-β-Homoproline; Hexahydronicotinic acid; 3-Carboxypiperidine
|
GABA Receptor
|
Neurological Disease
|
|
Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM.
|
-
- HY-145263
-
|
VD2173
|
Ser/Thr Protease
|
Cancer
|
|
VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer.
|
-
- HY-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-13715B
-
-
- 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-130239
-
|
14(S)-HDHA
14(S)-HDoHE
|
Drug Metabolite
|
Neurological Disease
|
|
14(S)-HDHA (14(S)-HDoHE) is an oxygenation product of Docosahexaenoic acid (DHA). 14(S)-HDHA is a marker reflecting activation of a Docosahexaenoic acid carbon 14-lipoxygenation pathway.
|
-
- 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-N8129
-
|
Rhaponticin 6′′-O-gallate
|
Others
|
Others
|
|
Rhaponticin 6′′-O-gallate is a stilbene glucoside gallate that can be found in rhizome of Rheum undulatum L. Rhaponticin 6′′-O-gallate inhibits nitric oxide production in lipopolysaccharide-activated macrophages.
|
-
- HY-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, 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-N0486S5
-
-
- HY-N3001
-
|
Isolinderalactone
|
VEGFR
Bcl-2 Family
Survivin
IAP
|
Cancer
|
|
Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells. Isolinderalactone suppresses the expression of B-cell lymphoma 2 (Bcl-2), survi
|
-
- HY-76847S2
-
-
- 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-B1378S1
-
|
Ethosuximide-d5
|
Calcium Channel
|
Neurological Disease
|
|
Ethosuximide-d5 is deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
|
-
- HY-N0486S3
-
-
- HY-13812
-
-
- HY-18657
-
|
TEPP-46
ML-265
|
Pyruvate Kinase
|
Cancer
|
|
TEPP-46 (ML-265) 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-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-10256
-
|
Adezmapimod
SB 203580; RWJ 64809
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator.
|
-
- HY-B1739
-
|
Pregnenolone monosulfate
3β-Hydroxy-5-pregnen-20-one monosulfate
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
|
-
- HY-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
Apoptosis
Autophagy
|
Cancer
Infection
|
|
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator.
|
-
- HY-110353
-
|
CU-T12-9
|
Toll-like Receptor (TLR)
|
Cancer
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-10201S2
-
|
Sorafenib-13C,d3
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Sorafenib-13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
|
-
- HY-18980
-
|
Rottlerin
Mallotoxin; NSC 56346; NSC 94525
|
PKC
Autophagy
Apoptosis
HIV
|
Infection
Cancer
|
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
|
-
- HY-110189
-
|
Pregnenolone monosulfate sodium
3β-Hydroxy-5-pregnen-20-one monosulfate sodium
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
|
-
- HY-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-B0923S
-
|
Danthron-d6
Dantron-d6; Chrysazin-d6; 1,8-Dihydroxyanthraquinone-d6
|
AMPK
Autophagy
Bacterial
Virus Protease
|
Cancer
|
|
Danthron-d6 (Dantron-d6) is the deuterium labeled Danthron. Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
|
-
- 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-145700
-
-
- HY-107415
-
|
PLX7922
|
Raf
|
Cancer
|
|
PLX7922, a RAF inhibitor, can bind with BRAF V600E. PLX7922 inhibits pERK in BRAF V600E cell lines, and activates pERK in mutant NRAS cell lines.
|
-
- HY-N0847
-
|
Micheliolide
|
NF-κB
|
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-135145
-
|
CB-103
|
Notch
|
Cancer
|
|
CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
|
-
- 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-128344
-
|
BR102375
|
PARP
Apoptosis
|
Metabolic Disease
|
|
BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28 μM and Amax ratio of 98%.
|
-
- HY-129527
-
|
GNE-9278
|
iGluR
|
Neurological Disease
|
|
GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
|
-
- 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-N0486S10
-
-
- 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-P9958
-
|
Denosumab
Immunoglobulin G2; Ranmark
|
NF-κB
|
Cancer
|
|
Denosumab is a human monoclonal antibody binding to, and inhibiting, the receptor activator of RANKL (TNFSF11). Denosumab can reduce the risk of vertebral, nonvertebral and hip fractures, also has anti-cancer activity.
|
-
- HY-N0250
-
-
- HY-N10266
-
-
- HY-B1197S
-
-
- HY-13715C
-
-
- 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
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Naveglitazar racemate
LY519818 racemate
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PPAR
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Metabolic Disease
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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.
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- HY-P1594A
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- HY-N2497
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Isoliquiritin apioside
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NF-κB
MMP
p38 MAPK
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Cancer
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Isoliquiritin apioside 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.
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- HY-123506
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Fenlean
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Src
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Inflammation/Immunology
Neurological Disease
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Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models.
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- HY-N0290
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Mangiferin
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NF-κB
Keap1-Nrf2
Apoptosis
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Cancer
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Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50. Mangiferin exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and antiinflammatory activities.
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- HY-P3204
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POT-4
AL-78898A
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Complement System
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Metabolic Disease
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POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research
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- HY-N3005
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Britannin
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Apoptosis
Autophagy
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Cancer
Inflammation/Immunology
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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.
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- HY-136651
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BNTA
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Others
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Inflammation/Immunology
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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.
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- HY-107414
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- HY-101843
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- HY-12848
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SAG
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Smo
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Cancer
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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.
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- HY-13255A
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TAME hydrochloride
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APC
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Cancer
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TAME hydrochloride is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest. TAME hydrochloride is not cell permeable.
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- HY-P2319A
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- HY-108439
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Neurodazine
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Wnt
Hedgehog
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Neurological Disease
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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.
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- HY-113473
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- HY-120675
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SSTC3
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Casein Kinase
Wnt
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Cancer
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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.
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- HY-12848C
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SAG dihydrochloride
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Smo
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Cancer
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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.
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- HY-N0802
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Tenuigenin
Senegenin
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NF-κB
Bacterial
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Infection
Inflammation/Immunology
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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.
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- HY-12848B
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SAG hydrochloride
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Smo
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Cancer
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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.
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- HY-N0474S
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- HY-17363S
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Dimethyl fumarate-d6
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Keap1-Nrf2
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Inflammation/Immunology
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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.
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- HY-P1313A
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- HY-13255
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TAME
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APC
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Cancer
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TAME is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest. TAME is not cell permeable.
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- HY-122445
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- HY-124867
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D3-βArr
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TSH Receptor
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Endocrinology
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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.
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- HY-108539
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CE3F4
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Others
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Cardiovascular Disease
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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.
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- HY-N0220
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Dauricine
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NF-κB
Apoptosis
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Cancer
Inflammation/Immunology
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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.
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- HY-N3026
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Soyasaponin Ab
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Others
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Metabolic Disease
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Soyasaponin Ab is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
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- HY-N3027
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Soyasaponin Aa
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Others
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Metabolic Disease
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Soyasaponin Aa is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
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- HY-N0020
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Echinacoside
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Wnt
Reactive Oxygen Species
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Neurological Disease
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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.
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- HY-12764
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6-OAU
GTPL5846
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GPR84
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Inflammation/Immunology
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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.
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- HY-129098
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DMHCA
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LXR
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Metabolic Disease
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DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects and can be used for the research of cholesterol homeostasis diabetes.
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- HY-15880
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CCT007093
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Phosphatase
Apoptosis
Autophagy
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Cancer
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CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy.
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- HY-14290
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Pinacidil
P-1134
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Potassium Channel
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Cardiovascular Disease
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Pinacidil is a potent activator of potassium channel. Pinacidil is an antihypertensive agent which hyperpolarises vascular smooth muscle by opening K +-channels. Pinacidil significantly improves the reperfusion function and cardiac compliance. Pinacidil has direct cardioprotective efficacy.
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- HY-B1371A
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- HY-N7041
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11-Oxomogroside IIa
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HSV
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Infection
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11-Oxomogroside IIa (11-oxomogroside II A1) is a cucurbitane glycoside extracted from the fruits of Siraitia grosVenorii.
11-Oxomogroside IIa has inhibitory effects against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), shows weak inhibitory effects on activation of (+/-)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor.
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- HY-117693
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Mirin
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ATM/ATR
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Cancer
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Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells.
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- HY-146073
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IRAK4-IN-12
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IRAK
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Cancer
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IRAK4-IN-12 (compound 37) is a potent IRAK4 inhibitor with an IC50 of 0.015 µM. IRAK4-IN-12 shows cell pIRAK4 potencies with an IC50 of 0.5 µM.
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- HY-146072
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IRAK4-IN-11
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IRAK
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Cancer
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IRAK4-IN-11 (compound 6) is a potent IRAK4 inhibitor with an IC50 of 0.008 µM. IRAK4-IN-11 shows cell pIRAK4 potencies with an IC50 of 0.19 µM.
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- HY-15874A
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Fiboflapon sodium
GSK2190915 sodium salt; AM-803 sodium
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FLAP
Leukotriene Receptor
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Inflammation/Immunology
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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.
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- HY-109011
-
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Rosiptor
AQX-1125
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Phosphatase
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Cancer
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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.
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- HY-108534
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PMX464
AW 464
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Others
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Cancer
Inflammation/Immunology
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PMX464 (AW 464), a thiol-reactive quinol, is the inhibitor of thioredoxin-thioredoxin reductase (Trx/TrxR) system. PMX464 can inhibit NF-κB-mediated proinflammatory activation of human type II alveolar epithelial cells.
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- HY-B0627
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- HY-139245
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MC-Ala-Ala-Asn-PAB
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Others
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Cancer
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MC-Ala-Ala-Asn-PAB is a linker extracted from patent CN104147612A, page 14. MC-Ala-Ala-Asn-PAB can be used to synthesis the tumor microenvironment specific activated micromolecular targeted conjugate.
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- HY-18952A
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(Z)-SU5614
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FLT3
Apoptosis
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Cancer
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(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3.
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- HY-B1378S
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Ethosuximide-d3
|
Calcium Channel
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Neurological Disease
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Ethosuximide-d3 is the deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
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- HY-N10106
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- HY-N0375
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- HY-16696
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SN 2
|
TRP Channel
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Infection
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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).
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- HY-19700S
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trans-Zeatin-d5
|
MEK
ERK
Endogenous Metabolite
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Others
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trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
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- HY-103269
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BAI1
|
Bcl-2 Family
Apoptosis
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Cancer
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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.
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- HY-15874
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Fiboflapon
GSK2190915; AM-803
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FLAP
Leukotriene Receptor
|
Inflammation/Immunology
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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.
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- HY-124729A
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