Search Result
Results for "Activated Integrinalpha 2 beta 1 Inhibitors" in MCE Product Catalog:
9177
Inhibitors & Agonists
21
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-P2294
-
|
pm26TGF-β1 peptide
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
|
-
- HY-P2294A
-
|
pm26TGF-β1 peptide TFA
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
|
-
- HY-P1868
-
|
α2β1 Integrin Ligand Peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-P1868A
-
|
α2β1 Integrin Ligand Peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-A0070
-
-
- HY-A0070A
-
-
- HY-A0275
-
-
- HY-B1154
-
-
- HY-129453
-
|
BOP sodium
|
Integrin
|
Inflammation/Immunology
|
|
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.
|
-
- HY-N2468
-
|
Xylobiose
1,4-β-D-Xylobiose; 1,4-D-Xylobiose
|
Others
|
Others
|
|
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is a disaccharide of xylose monomers with a β-1, 4 bond between monomers.
|
-
- HY-B0381A
-
-
- HY-B0381
-
-
- HY-100607A
-
-
- HY-N6712
-
|
Thiolutin
Acetopyrrothin
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
|
Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36. Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation.
|
-
- HY-108013
-
-
- HY-100445A
-
-
- 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-P1787
-
-
- HY-N3514
-
|
Kuwanon E
|
Others
|
Cancer
|
|
Kuwanon E is a flavonoid isolated from Morus alba, cytotoxic to human monocytic leukemic cell lines, and reduces the level of IL-1β.
|
-
- HY-101860
-
-
- HY-134130
-
|
Integrin modulator 1
|
Integrin
|
Inflammation/Immunology
|
|
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
|
-
- HY-117432
-
-
- HY-17497A
-
-
- HY-14823
-
-
- HY-103683
-
-
- HY-15770
-
|
TR-14035
|
Integrin
|
Inflammation/Immunology
|
|
TR-14035 is a dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune disease.
|
-
- HY-111413A
-
-
- HY-B0203A
-
-
- HY-B0203
-
-
- HY-U00066
-
-
- HY-15746
-
-
- 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-14126
-
-
- 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-10336
-
|
Brivanib (alaninate)
BMS-582664
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.
|
-
- HY-P0118
-
|
Disitertide
P144
|
TGF-beta/Smad
PI3K
Apoptosis
|
Cancer
|
Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer.
|
-
- HY-75385
-
-
- HY-19676
-
|
Pralnacasan
VX-740; HMR 3480
|
Caspase
|
Inflammation/Immunology
|
|
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
|
-
- HY-B0076
-
-
- HY-17503B
-
-
- HY-P0118A
-
|
Disitertide TFA
P144 TFA
|
TGF-beta/Smad
PI3K
Apoptosis
|
Cancer
|
Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.
|
-
- HY-75385A
-
-
- HY-126114
-
|
Lupeol acetate
|
Others
|
Inflammation/Immunology
|
|
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
|
-
- HY-17498
-
|
Atenolol
(RS)-Atenolol
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.
|
-
- HY-14951
-
|
Firategrast
SB 683699
|
Integrin
|
Neurological Disease
|
|
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
|
-
- HY-12043
-
|
SB 525334
|
TGF-β Receptor
|
Cancer
|
|
SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
|
-
- HY-N0074
-
|
Byakangelicol
|
COX
|
Inflammation/Immunology
|
|
Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.
|
-
- HY-N7697B
-
-
- HY-128591
-
|
DIPQUO
|
Others
|
Metabolic Disease
|
|
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
|
-
- HY-131166
-
|
Curdlan
|
Others
|
Others
|
|
Curdlan is a polysaccharide produced by bacteria and a homopolymer of glucose with β-1,3-glucosidic linkage.
|
-
- HY-112813
-
|
TUG-1375
|
Others
|
Metabolic Disease
|
|
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
|
-
- HY-117388
-
|
THI0019
|
Integrin
|
Inflammation/Immunology
|
|
THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
|
-
- HY-N1499
-
|
Nystose
|
Others
|
Metabolic Disease
|
|
Nystose is a tetrasaccharide with two fructose molecules linked via beta (1→2) bonds to the fructosyl moiety of sucrose.
|
-
- HY-13535A
-
-
- HY-N0722
-
-
- HY-N0847
-
|
Micheliolide
|
Others
|
Others
|
|
Micheliolide could effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs).
|
-
- HY-100506
-
|
GLPG0187
|
Integrin
|
Cancer
|
|
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
|
-
- HY-17503
-
-
- HY-113960
-
|
ERRα antagonist-1
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
|
-
- HY-U00183
-
-
- HY-12743A
-
-
- HY-12743
-
|
K-7174
|
Others
|
Inflammation/Immunology
|
|
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
|
-
- HY-15102
-
|
MK-0429
L-000845704
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.
|
-
- HY-N0633
-
-
- HY-15726
-
-
- HY-13715
-
-
- HY-13715A
-
-
- HY-107589A
-
|
BIO5192 hydrate
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-103214
-
-
- HY-17503A
-
-
- HY-N2587
-
|
Irigenin
|
Integrin
|
Cancer
|
|
Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells.
|
-
- HY-N0042
-
-
- HY-13954
-
|
A 839977
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
|
-
- HY-13713
-
-
- HY-N0569
-
-
- HY-13951
-
-
- HY-18644
-
|
CWHM-12
|
Integrin
|
Cancer
|
|
CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
|
-
- HY-13715B
-
-
- HY-124748A
-
-
- HY-100608
-
|
BMS453
BMS-189453
|
RAR/RXR
|
Cancer
|
|
BMS453 (BMS-189453), a synthetic retinoid, is an RARβ agonist and an RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
|
-
- HY-N7176
-
|
Kaempferol 3-O-β-D-glucuronide
Kaempferol-3-glucuronide; Kaempferol-3-O-glucuronide
|
Interleukin Related
|
Inflammation/Immunology
|
|
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10.
|
-
- HY-119802
-
-
- HY-17462
-
|
Adrenosterone
(+)-Adrenosterone
|
Androgen Receptor
Endogenous Metabolite
|
Endocrinology
|
|
Adrenosterone ((+)-Adrenosterone) is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone also is a selective and competitive inhibitor of hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1).
|
-
- HY-15483
-
-
- HY-119109
-
|
Laminaran
|
Others
|
Cancer
|
|
Laminaran is a neutral water-soluble β-1-3-glucan and a typical ligand for Dectin-1 isolated from the brown alga D. dichotoma, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
|
-
- HY-13013
-
|
(E)-SIS3
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
(E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
|
-
- HY-108831
-
|
Natalizumab
|
Integrin
|
Inflammation/Immunology
|
|
Natalizumab is a recombinant, humanized monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses.
|
-
- HY-13671
-
|
LW6
HIF-1α inhibitor; LW8
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
|
LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
|
-
- HY-17497S
-
-
- HY-P1060
-
|
LPYFD-NH2
|
Amyloid-β
|
Neurological Disease
|
|
LPYFD-NH2, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 can be used for the research of Alzheimer’s disease.
|
-
- HY-N0604
-
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-131945
-
-
- HY-10337
-
|
Brivanib
BMS-540215
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
|
-
- HY-P1189
-
|
Echistatin
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-P1420
-
|
TAT-cyclo-CLLFVY
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
|
-
- HY-P1060A
-
-
- HY-130778
-
|
N,N'-Diacetylchitobiose
|
Others
|
Others
|
|
N,N'-Diacetylchitobiose is a dimer of β(1,4) linked N-acetyl-D glucosamine. N,N'-Diacetylchitobiose is the hydrolysate of chitin and can be used as alternative carbon source by E. coli.
|
-
- HY-B1264
-
|
Celiprolol hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity.
|
-
- HY-13715C
-
-
- HY-P1189A
-
|
Echistatin TFA
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-103200
-
-
- HY-100672
-
-
- 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-B0240
-
|
Disulfiram
Tetraethylthiuram disulfide; TETD
|
Aldehyde Dehydrogenase (ALDH)
Interleukin Related
Pyroptosis
|
Metabolic Disease
Cancer
|
|
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
|
-
- HY-N1431A
-
|
Tabersonine hydrochloride
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Tabersonine hydrochloride is an indole alkaloid mainly isolated from Catharanthus roseus. Tabersonine disrupts Aβ(1-42) aggregation and ameliorates Aβ aggregate-induced cytotoxicity. Tabersonine has anti-inflammatory activities and is a potential therapeutic candidate for the treatment of ALI/ARDS.
|
-
- HY-P0299A
-
|
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
|
-
- HY-N1431
-
|
Tabersonine
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Tabersonine is an indole alkaloid mainly isolated from Catharanthus roseus. Tabersonine disrupts Aβ(1-42) aggregation and ameliorates Aβ aggregate-induced cytotoxicity. Tabersonine has anti-inflammatory activities and acts as a potential therapeutic candidate for the treatment of ALI/ARDS.
|
-
- HY-101355B
-
-
- HY-12560A
-
|
PNU-282987
|
nAChR
|
Neurological Disease
|
|
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
|
-
- HY-N0619
-
|
Mulberroside A
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- HY-10985
-
|
Marizomib
Salinosporamide A; NPI-0052
|
Proteasome
|
Cancer
|
|
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
|
-
- HY-N7142
-
-
- HY-19717
-
|
DCVC
S-[(1E)-1,2-dichloroethenyl]--L-cysteine
|
TNF Receptor
|
Inflammation/Immunology
|
|
DCVC (S-[(1E)-1,2-dichloroethenyl]--L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures.
|
-
- HY-N0506
-
|
Rosarin
|
Others
|
Neurological Disease
|
|
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice .
|
-
- HY-A0295
-
-
- HY-13335
-
|
PKCβ inhibitor 1
|
PKC
Apoptosis
|
Cancer
|
|
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
|
-
- HY-129029
-
|
Bisoprolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-121186
-
-
- HY-B0449
-
|
Methacycline hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
|
Methacycline hydrochloride is a tetracycline antibiotic and can inhibits bacterial protein synthesis. Methacycline hydrochloride is a potent epithelial-mesenchymal transition (EMT) inhibitor. Methacycline hydrochloride blocks EMT in vitro and fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline hydrochloride is an antimicrobial and has the potential for pulmonary fibrosis.
|
-
- HY-123268
-
|
Ro 363
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
|
-
- HY-U00439
-
-
- HY-130252
-
|
YQ128
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
|
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.
|
-
- HY-18754
-
|
FR 167653 free base
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
|
-
- HY-N4285
-
-
- HY-14190
-
|
Valategrast
R-411 free base
|
Integrin
|
Inflammation/Immunology
|
|
Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.
|
-
- HY-10232
-
|
THIP
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
|
THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.
|
-
- HY-N2337
-
-
- HY-B0573A
-
|
(S)-(-)-Propranolol hydrochloride
|
Adrenergic Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
(S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-N0619A
-
|
cis-Mulberroside A
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- HY-N7652
-
|
Terminolic acid
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Terminolic acid is a pentacyclic triterpenoid glucoside isolated from Combretum racemosum. Terminolic acid can inhibit the pro-inflammatory cytokines by binding to receptor active site of IL-1β and IL-6, and enhance anti-inflammatory cytokines by binding to IL-4 receptor binding sites. Terminolic acid also exhibits moderate antibacterial activity.
|
-
- HY-18754A
-
|
FR 167653
FR 167653 sulfate
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
|
-
- HY-P0297
-
-
- HY-129113
-
|
α-Chaconine
|
COX
|
Inflammation/Immunology
|
|
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
|
-
- HY-15509A
-
|
Semapimod tetrahydrochloride
CNI-1493; CPSI-2364 tetrahydrochloride
|
TNF Receptor
Interleukin Related
p38 MAPK
|
Inflammation/Immunology
|
|
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
|
-
- HY-12308
-
-
- HY-N6927
-
|
Isoforskolin
Coleonol B
|
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis.
|
-
- HY-14300A
-
-
- HY-110266
-
|
GN44028
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
|
-
- HY-100935S
-
|
Cimaterol-D7
|
Adrenergic Receptor
|
|
|
Cimaterol-D7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
|
-
- HY-P0283
-
-
- HY-14300
-
-
- HY-10426
-
|
XCT790
|
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
|
-
- HY-15507
-
-
- HY-B0573
-
|
Propranolol hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-B0573B
-
|
Propranolol
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
Endocrinology
|
|
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-126236
-
-
- HY-133987
-
|
AP-1/NF-κB activation inhibitor 1
|
NF-κB
|
Inflammation/Immunology
|
|
AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
|
-
- HY-114170
-
|
ML604440
|
Proteasome
|
Inflammation/Immunology
|
|
ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
|
-
- HY-N6896
-
|
Isoviolanthin
|
Others
|
Cancer
|
|
Isoviolanthin is a flavonoid glycoside extracted from the leaves of Dendrobium officinale. Isoviolanthin reduces the migratory and invasive capacities of TGF-β1-treated HCC cells but exhibits no cytotoxic effects on normal live cells, and has potential as a therapeutic agent for the treatment of advanced-stage metastatic HCC.
|
-
- HY-19975
-
|
RN-1734
|
TRP Channel
|
Neurological Disease
|
|
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.
|
-
- HY-100634
-
|
4-Hydroxypropranolol hydrochloride
(±)-4-hydroxy Propranolol hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-13306
-
|
Pyrintegrin
|
Integrin
|
Metabolic Disease
|
|
Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
|
-
- HY-13205
-
|
Belnacasan
VX-765
|
Caspase
|
Inflammation/Immunology
|
|
Belnacasan (VX-765) is an orally bioactive prodrug of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM.
|
-
- HY-117937
-
|
BC-1215
|
Ligand for E3 Ligase
|
Inflammation/Immunology
|
|
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCF Fbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.
|
-
- HY-B0573S
-
|
Propranolol D7 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Propranolol D7 hydrochloride is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-N6018
-
-
- HY-124745
-
|
KY-05009
|
MAP4K
Wnt
Apoptosis
|
Cancer
|
|
KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
|
-
- HY-113402A
-
|
Gamma-glutamylcysteine TFA
γ-glutamylcysteine TFA
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Gamma-glutamylcysteine (TFA) ((γ-glutamylcysteine (TFA)), an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine (TFA) also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β) and attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes.
|
-
- HY-16702
-
-
- HY-N2056
-
|
11-Keto-beta-boswellic acid
11-Keto-β-boswellic acid
|
Lipoxygenase
Leukotriene Receptor
NF-κB
|
Cancer
|
|
11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.
|
-
- HY-100634S
-
|
4-Hydroxypropranolol D7 hydrochloride
(±)-4-hydroxy Propranolol D7 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-P2518
-
-
- HY-B1803A
-
|
Tracazolate hydrochloride
ICI 136753 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
|
-
- HY-P1308
-
-
- HY-13453
-
|
BAY 11-7082
BAY 11-7821
|
IKK
Deubiquitinase
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
|
-
- HY-19744
-
|
T6167923
|
MyD88
|
Inflammation/Immunology
|
|
T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an 50 of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
|
-
- HY-16702A
-
-
- HY-N2187
-
|
Deoxyshikonin
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Infection
Cardiovascular Disease
|
|
Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA.
|
-
- HY-N0550
-
|
β-Pinene
(-)-β-Pinene
|
Bacterial
|
Infection
|
|
β-Pinene ((-)-β-Pinene), a major component of turpentine, inhibit infectious bronchitis virus (IBV) with an IC50 of 1.32 mM. β-Pinene presents antimicrobial activity.
|
-
- HY-123489
-
|
3α,21-Dihydroxy-5α-pregnan-20-one
THDOC
|
GABA Receptor
|
|
|
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
|
-
- HY-P2519
-
-
- 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-125586
-
|
β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-P1328
-
|
TAT-14
|
Keap1-Nrf2
|
Others
|
|
TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-P1308A
-
-
- HY-N0892
-
-
- HY-D0886
-
-
- HY-B1837A
-
|
β-Cyfluthrin
beta-Cyfluthrin
|
Calcium Channel
|
Infection
|
|
β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca 2+ ATPase involved in calcium transport.
|
-
- HY-107324
-
|
β-Elemene
(-)-β-Elemene; Levo-β-elemene
|
Apoptosis
|
Cancer
|
|
β-Elemene ((-)-β-Elemene; Levo-β-elemene) is isolated from natural plant Curcuma wenyujin with an antitumor activity. β-Elemene can induce cell apoptosis.
|
-
- HY-135386
-
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-Y1750
-
-
- HY-N5112A
-
-
- HY-P1286
-
-
- HY-113953
-
|
Z-Asp-CH2-DCB
|
Caspase
|
Inflammation/Immunology
|
|
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
|
-
- HY-N2454
-
-
- HY-133680
-
|
β-Tocopherol
|
Tyrosinase
|
Metabolic Disease
|
|
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
|
-
- HY-N2513
-
|
β-Boswellic acid
|
Lipoxygenase
DNA/RNA Synthesis
|
Cancer
|
|
β-Boswellic acid is isolated from the gum resin of Boswellia serrate.
β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells.
|
-
- HY-126144
-
-
- HY-135670A
-
-
- HY-124957
-
|
β-NETA
|
AChE
Apoptosis
|
Cancer
|
|
β-NETA is a potent and noncompetitive choline acetyltransferase (ChA; IC50=76 μM) and cholinesterase (ChE; IC50=40 µM) inhibitor. β-NETA weakly inhibits acetylcholinesterase (AChE; IC50=1 mM).
|
-
- HY-N1940
-
|
β-Anhydroicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
|
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
|
-
- HY-131005
-
-
- HY-N7606
-
-
- HY-N2920
-
|
β-Amyrenonol
11-Oxo-β-amyrin
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids.
|
-
- HY-107373
-
|
β-Chloro-L-alanine
L-β-Chloroalanine
|
Bacterial
|
Infection
|
|
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
|
-
- HY-136234
-
|
9-cis-β-Carotene
|
Others
|
Others
|
|
9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal. 9-cis-β-Carotene inhibits photoreceptor degeneration and restores retinal function in vivo. 9-cis-β-Carotene has the potential for the study of congenital stationary night blindness and fundus albipunctatus.
|
-
- HY-P1084
-
-
- HY-108059
-
-
- HY-P1286A
-
-
- HY-114464
-
|
11-Beta-hydroxyandrostenedione
4-Androsten-11β-ol-3,17-dione
|
Endogenous Metabolite
|
Endocrinology
|
|
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.
|
-
- HY-U00272
-
|
Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)-
Androst-4-ene-3β,17β-diol, dipropionate
|
Androgen Receptor
|
Metabolic Disease
Neurological Disease
|
|
Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- is the dipropanoate of 4-Androstenediol, a metabolite of testosterone.
|
-
- HY-P1328A
-
|
TAT-14 TFA
|
Keap1-Nrf2
|
Others
|
|
TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-N2922
-
|
β-Amyrin
|
Others
|
Neurological Disease
|
|
β-Amyrin, an ingredient of the surface wax of tomato fruit and dandelion coffee, blocks amyloid β (Aβ)-induced long-term potentiation (LTP) impairment. β-amyrin is a promising candidate of treatment for AD.
|
-
- HY-N5112B
-
|
β,β-Dimethylacrylshikonin
|
Others
|
Cancer
|
|
β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. Arnebin 1 has anti-tumor activity.
|
-
- HY-10590
-
-
- HY-136464
-
|
β-catenin-IN-2
|
β-catenin
|
Cancer
|
|
β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.
|
-
- HY-N0941
-
|
beta-Mangostin
β-Mangostin
|
Others
|
Others
|
|
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).
|
-
- HY-12452
-
|
DPN
Diarylpropionitrile
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC50 of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.
|
-
- HY-N7012
-
|
7,3',4'-Tri-O-methylluteolin
5-Hydroxy-3',4',7-trimethoxyflavone
|
TNF Receptor
Interleukin Related
COX
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid from the herb Lippia nodiflora L. (Verbenaceae) which has been documented to exhibit anti-inflammatory, antipyretic, antitussive, antidiabetic, anticancer, and antimelanogenesis properties. 7,3',4'-Tri-O-methylluteolin obviously reduces the prodn of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β in a concentration-dependent manner. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2, representing that inhibition occurs at the transcriptional level.
|
-
- HY-131096
-
-
- HY-15310
-
|
Ivermectin
MK-933
|
Parasite
HIV
Mitophagy
HSV
SARS-CoV
Antibiotic
Autophagy
|
Infection
Cancer
|
|
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
|
-
- HY-117958
-
|
HJC0197
|
Others
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
|
-
- HY-W010231
-
|
β-Cyclocitral
|
Others
|
Others
|
|
β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis. β-Cyclocitral, one of the predominant volatile terpenoid compounds, can upregulate the expression of defence genes to enhance excess light (EL) acclimation. β-Cyclocitral is a powerful repellent.
|
-
- HY-15870
-
|
SR 11302
|
Others
|
Cancer
Inflammation/Immunology
|
|
SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).
|
-
- HY-113351
-
-
- HY-114392
-
|
Gly-β-MCA
|
FXR
Autophagy
|
Metabolic Disease
|
|
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.
|
-
- HY-F0004
-
|
β-Nicotinamide mononucleotide
β-NM; NMN
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD(+) intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.
|
-
- HY-135594
-
|
4'-Raloxifene-β-D-glucopyranoside
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.
|
-
- HY-135595
-
|
6-Raloxifene-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Drug Metabolite
|
Metabolic Disease
|
|
6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.
|
-
- HY-108693
-
-
- HY-16673
-
|
PSN632408
|
GPR119
|
Metabolic Disease
|
|
PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.
|
-
- HY-P1084A
-
-
- HY-P1522
-
-
- HY-P1051
-
|
β-amyloid (12-28)
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-N7682
-
|
β-Tomatine
|
Others
|
Others
|
|
β-Tomatine is a breakdown product of α-tomatine and a less fungitoxic compound. β-Tomatine can suppress plant defense responses.
|
-
- HY-15679
-
-
- HY-P1521
-
-
- HY-B0141
-
-
- HY-P0128
-
|
β-Amyloid (25-35)
Amyloid beta-peptide (25-35); Aβ25-35; β-Amyloid peptide (25-35)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (25-35) (Amyloid beta-peptide (25-35)) is the fragment Aβ(25-35) of the Alzheimer's amyloid β-peptide, has shown neurotoxic activities in cultured cells.
|
-
- HY-N6741
-
|
β-Zearalenol
|
Others
|
Infection
Endocrinology
|
|
β-Zearalenol is a non-steroidal estrogenic mycotoxin synthesized by Fusarium species. β-Zearalenol potentially influences transcription and effects gene expression on translational level.
|
-
- HY-136552
-
|
β-Bisabolene
|
Others
|
Cancer
|
|
β-Bisabolene is a sesquiterpene isolated from opoponax (Commiphora guidotti). β-Bisabolene, an anti-cancer agent, can be used for the study of breast cancer.
|
-
- HY-P1046
-
|
β-Amyloid 1-15
Amyloid β-Protein (1-15)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-P0179
-
-
- HY-50900
-
-
- HY-N1484
-
-
- 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-102011
-
|
BMS-1166
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
|
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-P1772
-
-
- HY-N5053
-
-
- HY-113418
-
-
- HY-107201
-
|
β-Cyclodextrin
|
Influenza Virus
|
Infection
|
|
β-Cyclodextrin is a cyclic polysaccharide composed of seven units of glucose (α-D-glucopyranose) linked by α-(1,4) type bonds. β-Cyclodextrin has often been used to enhance the solubility of drugs. β-Cyclodextrin has anti-influenza virus H1N1 activities.
|
-
- HY-P1481A
-
-
- HY-P1468
-
|
β-Amyloid (1-28)
Amyloid β-Protein (1-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-28) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-P1466
-
|
β-Amyloid 1-16
Amyloid β-Protein (1-16)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-16) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- 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-N4201
-
|
β-Hydroxyisovalerylshikonin
|
EGFR
Src
|
Cancer
|
|
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
|
-
- HY-125849
-
-
- HY-P1474
-
|
β-Amyloid (22-35)
Amyloid β-Protein (22-35)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-N1968
-
-
- HY-128976
-
-
- HY-N2274
-
|
23-Hydroxylongispinogenin
12-Oleanene-3β,16β,23,28-tetrol; 3β,16β-12-Oleanene-3, 16,23,28-tetrol
|
Others
|
Cancer
|
|
23-Hydroxylongispinogenin (12-Oleanene-3β,16β,23,28-tetrol) is extracted from Lysimachia heterogenea Klatt. Lysimachia heterogenea Klatt is a perennial herb, which is used as a folk medicine in subduing swelling and detoxicating in China. The effective fraction LH-1 of L. heterogene has antitumor activity.
|
-
- HY-12780S
-
-
- HY-22306
-
-
- HY-P1880
-
-
- HY-P1879
-
-
- HY-113478
-
|
3β-Ursodeoxycholic acid
Isoursodeoxycholic acid
|
Others
|
Metabolic Disease
|
|
3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) is a bile acid. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) shows good tolerance and well intestinal absorption by oral adminstation. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) can be isomerized by intestinal and hepatic enzymes to yield UDCA.
|
-
- HY-N6652
-
|
1-beta-D-Arabinofuranosyluracil
Uracil 1-β-D-arabinofuranoside
|
Others
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties. 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells.
|
-
- HY-136344
-
-
- HY-P1051A
-
|
β-amyloid (12-28) (TFA)
Amyloid β-Protein (12-28) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) TFA is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-N1501
-
|
Beta-asarone
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties of
immunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease.
|
-
- HY-N6740
-
|
Beta-Zearalanol
|
Apoptosis
|
Metabolic Disease
|
|
Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid.
|
-
- HY-N7683
-
|
Prunetin 5-O-β-D-glucopyranoside
|
Glucosidase
|
Metabolic Disease
|
|
Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC50 of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes.
|
-
- HY-N2182
-
-
- HY-P1895
-
-
- HY-P1903
-
-
- HY-125773
-
|
β-cyano-L-Alanine
beta-cyano-l-alanine
|
Others
|
Neurological Disease
|
|
β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.
|
-
- HY-P1510
-
-
- HY-P1517
-
-
- HY-121879
-
-
- HY-N0520
-
-
- HY-N0411
-
-
- HY-P1850
-
-
- HY-B1449
-
|
Uridine
β-Uridine
|
Endogenous Metabolite
|
Others
|
|
Uridine (β-Uridine) is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond.
|
-
- HY-N0087
-
|
Gambogic Acid
beta-Guttiferrin
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
|
-
- HY-N2188
-
-
- HY-131108
-
-
- HY-P1362
-
|
β-Amyloid (42-1), human
Amyloid β Peptide (42-1)(human)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (42-1), human is the inactive form of Amyloid β Peptide (1-42). Amyloid β Peptide (1-42) is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
|
-
- HY-N1415
-
-
- HY-N7635
-
-
- HY-P0179A
-
-
- HY-P1474A
-
|
β-Amyloid (22-35) (TFA)
Amyloid β-Protein (22-35) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-N7489
-
|
β-Hederin
|
Parasite
|
Infection
Inflammation/Immunology
|
|
β-Hederin, a saponin isolated from Hedera helix L.(Araliaceae), possesses antileishmanial activity. β-Hederin exhibits IC50 values of 1.5 μM, 68 nM and 4.57 μM in L. Mexicana promastigotes, L. mexicana amastigotes and THP1 cells, respectively.
|
-
- HY-N4034
-
-
- HY-N0181A
-
|
Lumisterol
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
|
-
- HY-N0338
-
-
- HY-N6824
-
-
- 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-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-N7401
-
-
- HY-100740C
-
|
(1α,1'S,4β)-Lanabecestat
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a Beta site APP Cleaving Enzymel (BACE1) inhibitor extracted from patent WO2012087237A1, compound 20a, has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.
|
-
- HY-P1854
-
|
β-Amyloid (1-9)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism [1].
|
-
- 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-N0180
-
-
- HY-P1502
-
|
β-Endorphin, human
|
Opioid Receptor
|
Neurological Disease
|
|
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
|
-
- HY-141379
-
|
N-Bromoacetyl-β-alanine
|
PROTAC Linker
ADC Linker
|
Cancer
|
|
N-Bromoacetyl-β-alanine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. N-Bromoacetyl-β-alanine is also a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-P1053
-
-
- HY-136537A
-
-
- HY-N6851
-
|
Glycyrrhetic acid 3-O-β-D-glucuronide
|
Others
|
Inflammation/Immunology
|
|
Glycyrrhetic acid 3-O-β-D-glucuronide, isolated from glycyrrhiza, is an important derivative of glycyrrhizin (GL) with an anti -allergic activity. Glycyrrhetic acid 3-O-β-D-glucuronide (GAMG) shows that β‐glucuronidases (β‐GUS) are key GAMG-producing enzymes, displaying a high potential to convert GL directly into GAMG.Glycyrrhetic acid 3-O-β-D-glucuronide is valuable as a sweetener.
|
-
- HY-14165
-
-
- HY-N2168
-
|
Pinoresinol 4-O-β-D-glucopyranoside
(+)-Pinoresinol 4-O-β-D-glucopyranoside
|
Others
|
Cardiovascular Disease
|
|
Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is the major active furofuran type lignans in Fructus Forsythiae. Pinoresinol 4-O-β-D-glucopyranoside shows antioxidant, blood pressure reducing, and cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitory effects.
|
-
- HY-N0171B
-
|
Beta-Sitosterol (purity>75%)
β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)
|
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-107670
-
|
Dihydro-β-erythroidine hydrobromide
DHβE hydrobromide
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities.
|
-
- HY-13555
-
|
β-Lapachone
ARQ-501; NSC-26326
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
|
-
- HY-N0171
-
|
Beta-Sitosterol (purity>80%)
β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)
|
Endogenous Metabolite
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-130269
-
|
β-Naphthoflavone-CH2-OH
β-NF-CH2-OH
|
Ligand for E3 Ligase
|
Cancer
|
|
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins [1].
|
-
- HY-128737
-
-
- HY-N3517
-
-
- HY-N3516
-
-
- HY-W015084
-
|
β-Ionone
|
Apoptosis
|
Cancer
|
|
β-Ionone, isolated from plant oils, is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity.
|
-
- HY-116284
-
-
- HY-112044
-
-
- 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-P1567
-
-
- HY-N2075
-
-
- HY-W012875
-
-
- HY-N4099
-
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-N2100
-
-
- HY-19373
-
-
- HY-N0406
-
|
2"-O-beta-L-galactopyranosylorientin
|
Others
|
Metabolic Disease
|
|
2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).
|
-
- HY-101953
-
-
- HY-P2283
-
-
- HY-B0708
-
-
- HY-N5111
-
-
- HY-129993
-
-
- HY-N2212
-
-
- HY-P1548
-
-
- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-N6904
-
-
- 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-N2394
-
-
- HY-N0192
-
|
Arbutin
β-Arbutin
|
Tyrosinase
|
Cancer
|
|
Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-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-P2290
-
|
Beta-defensin 1, pig
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Beta-defensin 1, pig is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig is active against bacteria such as Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis and Candida albicans.
|
-
- HY-N7598
-
-
- HY-100084
-
-
- 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-N3523
-
|
3-O-Beta-D-Glucopyranosylplatycodigenin
|
Others
|
Cancer
|
|
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM.
|
-
- HY-P0265
-
-
- HY-113949A
-
-
- 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-P1378
-
-
- HY-100260
-
|
beta-L-D4A
2'3'-didehydro-2'3'-dideoxyadenosine
|
HIV
|
Infection
|
|
beta-L-D4A is a nucleoside HIV-1 reverse transcriptase inhibitor.
|
-
- HY-N6677
-
|
β-Apo-8'-carotenal
Apocarotenal
|
Cytochrome P450
|
Cancer
|
|
β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of CYPlA1 and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables.
|
-
- HY-P1548B
-
-
- HY-N2142
-
-
- HY-P1363
-
-
- 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-N5091
-
-
- HY-N0171A
-
-
- HY-N7422
-
|
Kauran-16,17-diol
ent-Kauran-16β,17-diol
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages.
|
-
- HY-N6630
-
-
- HY-N6986
-
-
- HY-P1866
-
-
- HY-W015546
-
|
β-N-methylamino-L-alanine hydrochloride
BMAA hydrochloride
|
Others
|
Neurological Disease
|
|
β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride could cause amyotrophic lateral sclerosis (ALS) and possibly other neurodegenerative diseases.
|
-
- HY-11012
-
|
TDZD-8
GSK-3β Inhibitor I; NP 01139
|
GSK-3
|
Cancer
|
|
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
|
-
- HY-P2290A
-
|
Beta-defensin 1, pig TFA
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Beta-defensin 1, pig TFA is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig TFA is active against bacteria such as Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis and Candida albicans.
|
-
- HY-43470
-
-
- 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-P1378A
-
-
- HY-N6938
-
-
- HY-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-N6885
-
|
Puerarin-4'-O-β-D-glucopyranoside
|
Others
|
Cancer
|
|
Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells.
|
-
- HY-N2451
-
-
- HY-N6911
-
-
- HY-103238
-
|
RSVA405
|
AMPK
STAT
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.
|
-
- HY-N6879
-
-
- HY-N6260
-
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid a sulfur-containing flavor component produced by Asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-101804
-
-
- HY-101953S
-
|
β-Apo-13-carotenone D3
D'Orenone D3
|
Others
|
Cancer
|
|
β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
|
-
- HY-16561
-
|
Resveratrol
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model.
|
-
- HY-P2313
-
|
Human β-defensin-2
HβD-2
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-2 (HβD-2) is a small cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by a number of epithelial cells.Human β-defensin-2 has antimicrobial activity against gram-negative bacteria and Candida, but not gram-positive Staphylococcus aureus. Human β-defensin-2 can be used for the study of colitis.
|
-
- HY-113320
-
|
Etiocholanolone
5β-Androsterone
|
GABA Receptor
|
Neurological Disease
|
|
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
|
-
- HY-P1548A
-
-
- HY-10256A
-
|
SB 203580 hydrochloride
RWJ 64809 hydrochloride
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
|
-
- HY-N6006
-
-
- HY-135103
-
|
Tauro-β-muricholic acid sodium
T-βMCA sodium
|
FXR
|
Cancer
|
|
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
|
-
- HY-W010452
-
-
- HY-113378
-
-
- HY-101923B
-
-
- HY-112023
-
|
Lumisterol 3 (>90%)
9β,10α-Cholesta-5,7-dien-3β-ol; Cholecalciferol EP Impurity A
|
Endogenous Metabolite
|
Others
|
|
Lumisterol 3 (>90%) (9β,10α-Cholesta-5,7-dien-3β-ol) is a normal human secosterooid metabolite from the class of vitamin D3 photoisomer derivatives. Lumisterol 3 (>90%) is used in the preparation of vitamin D.
|
-
- HY-126047B
-
|
(R)-(+)-Anatabine
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-P0265A
-
-
- HY-N4088
-
-
- HY-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-B0406
-
|
Bethanechol
Carbamyl-β-methylcholine
|
mAChR
|
Neurological Disease
|
|
Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
|
-
- HY-B0406A
-
|
Bethanechol chloride
Carbamyl-β-methylcholine chloride
|
mAChR
|
Neurological Disease
|
|
Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
|
-
- HY-N0377
-
-
- HY-P1388
-
-
- HY-125801
-
|
3-Oxo-5β-cholanoic acid
Dehydrolithocholic acid; 3-oxoLCA
|
ROR
|
Inflammation/Immunology
|
|
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
|
-
- HY-N2107
-
-
- HY-136329
-
-
- HY-128974
-
|
N-Dodecyl-β-D-maltoside
Lauryl Maltoside
|
Others
|
Others
|
|
N-Dodecyl-β-D-maltoside (Lauryl Maltoside) is a derivatives of pyrene (Py), and it is a alkyl maltopyranoside detergent, especially in transporters and respiratory complexes. N-Dodecyl-β-D-maltoside has also been employed in applications such as in the purification and stabilization of RNA polymerase and detection of protein-lipid interactions.
|
-
- HY-75342
-
-
- HY-N0230
-
-
- HY-111642
-
-
- HY-141131
-
-
- HY-141132
-
-
- HY-140012
-
-
- HY-P2291
-
-
- 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-10256
-
|
SB 203580
RWJ 64809
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
|
-
- HY-129492
-
|
GNF4877
|
DYRK
GSK-3
|
Metabolic Disease
|
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
|
-
- HY-N7715
-
|
Ferulic acid acyl-β-D-glucoside
Ferulic acid glucoside
|
Drug Metabolite
|
Others
|
|
Ferulic acid acyl-β-D-glucoside is a metabolite of Ferulic Acid (HY-N0060). Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
|
-
- HY-P1866A
-
-
- HY-19773
-
|
beta-lactamase-IN-1
|
Bacterial
|
Cancer
|
|
beta-lactamase-IN-1 targets Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.
|
-
- HY-A0058
-
-
- HY-B1192
-
|
Estradiol benzoate
β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
|
-
- HY-N2601
-
-
- HY-P2312
-
|
Human β-defensin-3
HβD-3
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml.
|
-
- HY-77591A
-
-
- HY-103687
-
|
Abiraterone metabolite 1
3β-OH-5α-Abi
|
Drug Metabolite
|
Cancer
|
|
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
|
-
- HY-10512
-
-
- HY-N0713
-
-
- HY-19918A
-
|
Anatabine dicitrate
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-P2315
-
|
Human β-defensin-1
HβD-1
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-1 (HβD-1) is a cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by all epithelial surfaces, but also by circulatory cells and cells of the reproductive tract. Human β-defensin-1 has antimicrobial activities against a broad-sperm bacteria.
|
-
- HY-13027
-
|
DAPT
GSI-IX
|
γ-secretase
Amyloid-β
Autophagy
Notch
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
|
-
- HY-108652
-
-
- HY-P1504
-
-
- HY-135813
-
|
LtaS-IN-1
|
Bacterial
|
Infection
|
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- 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-P2291A
-
-
- HY-10595
-
-
- HY-P1388A
-
-
- HY-N4180
-
|
Pennogenin 3-O-beta-chacotrioside
|
Autophagy
|
Cancer
|
|
Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.
|
-
- HY-B1209
-
|
Etofylline
7-(β-Hydroxyethyl)theophylline
|
Others
|
Cardiovascular Disease
|
|
Etofylline (7-(β-Hydroxyethyl)theophylline) is a N-7-substituted derivative of Theophylline. Etofylline is a bronchodilator which can be used for the research of asthma. Etofylline is also an anticholesteremic and reduces total cholesterol level in the blood.
|
-
- HY-109564
-
-
- HY-77591
-
-
- HY-15394
-
-
- HY-N7604
-
-
- HY-N0627
-
-
- 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-P2285
-
|
AC 253
|
Amyloid-β
|
|
|
AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
|
-
- HY-B0672
-
-
- HY-B0151
-
|
Pregnenolone
3β-Hydroxy-5-pregnen-20-one
|
Cannabinoid Receptor
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.
|
-
- HY-113013
-
|
Hydroxypyruvic acid
β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-N2094
-
|
Genipin 1-β-D-gentiobioside
Genipin 1-gentiobioside; Genipin 1-β-gentiobioside; Genipin gentiobioside
|
Others
|
Inflammation/Immunology
|
|
Genipin 1-β-D-gentiobioside (Genipin 1-gentiobioside) is one of the most abundant and bioactive iridoid glycosides in Gardenia jasminoides Ellis, which possesses hepatoprotective, anti-inflammatory, antioxidant, and antithrombotic activities.
|
-
- HY-135588
-
-
- HY-13520
-
|
Nocodazole
Oncodazole; R17934
|
Microtubule/Tubulin
Bcr-Abl
CRISPR/Cas9
Autophagy
Apoptosis
|
Cancer
|
|
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
|
-
- HY-P0318
-
-
- HY-N0250
-
-
- HY-136614
-
|
H-Val-βNA
L-Valine β-naphthylamide
|
Others
|
Others
|
|
H-Val-βNA (L-Valine β-naphthylamide) can be used as an aminopeptidase and a Valine arylamidase substrate.
|
-
- HY-A0083
-
|
Methacholine chloride
Acetyl-β-methylcholine chloride
|
mAChR
|
Others
|
|
Methacholine (Acetyl-β-methylcholine) chloride acts a muscarinic M3 receptor agonist in the parasympathetic nervous system. Methacholine chloride acts directly on acetylcholine receptors on smooth muscle causing contraction and airway narrowing. Methacholine challenges are widely used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
|
-
- HY-W007648
-
|
Methyl 3-aminopropanoate hydrochloride
β-Alanine methyl ester hydrochloride
|
Others
|
Others
|
|
Methyl 3-aminopropanoate hydrochloride is prepared by esterification of Β-Alanine (I). Methyl 3-aminopropanoate hydrochloride can be used in the synthesis of bidentate pyridine-acid ligand.
|
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-P1504A
-
-
- HY-100538A
-
|
DTP3 TFA
|
DNA/RNA Synthesis
JNK
|
Cancer
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
|
-
- HY-135955
-
-
- HY-18728
-
-
- HY-14602
-
|
Tramiprosate
Homotaurine; 3-Amino-1-propanesulfonic acid
|
Amyloid-β
|
Cancer
|
|
Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent deposition
target: Aβ
In vitro: Tramiprosate provides neuroprotection against Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors.
|
-
- HY-111974
-
|
β-D-Glucopyranosyl abscisate
ABA-GE; (S)-cis,trans-Abscisic acid glucosyl ester
|
Others
|
Endocrinology
|
|
β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable abscisic acid (ABA) conjugate that accumulates in the vacuole and presumably also in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate allows the rapid formation of free ABA in response to abiotic stress conditions such as dehydration and salt stress. β-D-Glucopyranosyl abscisate contributes to the maintenance of ABA homeostasis.
|
-
- HY-N0020
-
|
Echinacoside
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
|
-
- HY-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-N7024
-
-
- HY-N2190
-
-
- HY-N7035
-
-
- HY-141133
-
-
- HY-N4179
-
-
- HY-141135
-
-
- HY-141127
-
-
- HY-P2558
-
-
- HY-125033
-
|
EIDD-1931
β-D-N4-hydroxycytidine; NHC
|
SARS-CoV
Enterovirus
HCV
Topoisomerase
|
Infection
|
|
EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV).
|
-
- HY-125957
-
|
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-N3811
-
-
- HY-B0770
-
|
Artemotil
β-Arteether; (+)-Arteether; Arteether
|
Parasite
|
Infection
Cancer
|
|
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.
|
-
- HY-14649
-
|
Retinoic acid
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-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-113949
-
-
- HY-N5039
-
-
- HY-N7681
-
|
Taxifolin 7-O-β-D-glucoside
Taxifolin 7-O-glucoside
|
Others
|
Others
|
|
Taxifolin 7-O-β-D-glucoside (Taxifolin 7-O-glucoside) is one of the main metabolites at the seed germination stage in Scutellaria baicalensis. Taxifolin 7-O-β-D-glucoside, a flavonoid, mainly exists in the episperm and participates in defending against pathogens and UV-damage.
|
-
- HY-115365
-
-
- HY-N7003
-
|
28-Demethyl-β-amyrone
28-Norolean-12-en-3-one
|
Bacterial
|
Infection
|
|
28-Demethyl-β-amyrone (28-Norolean-12-en-3-one) is one of the main triterpenes from Pistacia lentiscus var. Chia. 28-Demethyl-β-amyrone is an antitoxin and can effectively for the toxic effects of Staphylococcal enterotoxins (SEs).
|
-
- HY-133407
-
-
- HY-111638
-
-
- HY-131447
-
|
KY19382
A3051
|
GSK-3
|
Metabolic Disease
|
|
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
|
-
- HY-131086
-
-
- HY-N4008
-
-
- HY-N6679A
-
|
10,11-Dehydrocurvularin
|
HSP
TGF-beta/Smad
|
Cancer
Infection
|
|
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
|
-
- HY-136318
-
-
- HY-10456
-
|
TAK-715
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.
|
-
- HY-N6082
-
|
Rhein 8-Glucoside
Rhein 8-O-β-D-Glucopyranoside
|
Others
|
Metabolic Disease
|
|
Rhein 8-Glucoside (Rhein 8-O-β-D-Glucopyranoside) is an anthraquinone glycoside that has been found in rhubarb. Purgative activity.
|
-
- 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-130929
-
-
- 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-12383
-
|
Pelubiprofen
|
COX
|
Inflammation/Immunology
Neurological Disease
|
|
Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects.
|
-
- HY-50937
-
|
ST 2825
|
MyD88
|
Inflammation/Immunology
|
|
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
|
-
- HY-B1739
-
|
Pregnenolone monosulfate
3β-Hydroxy-5-pregnen-20-one monosulfate
|
Cannabinoid Receptor
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.
|
-
- HY-110189
-
|
Pregnenolone monosulfate sodium salt
3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt
|
Cannabinoid Receptor
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication.
|
-
- HY-12762
-
|
QS11
|
Others
|
Cancer
|
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-N7628
-
|
Cassiaside C
Toralactone 9-O-β-D-gentiobioside
|
Others
|
Metabolic Disease
|
|
Cassiaside C (Toralactone 9-O-β-D-gentiobioside) is a naphthopyrone isolated from the seed of Cassia tora and has inhibitory activity on advanced glycation end products (AGE) formation in vitro.
|
-
- 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-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-15583
-
-
- HY-109030
-
-
- HY-N0651
-
|
Spinosin
|
Others
|
Neurological Disease
|
|
Spinosyn a C-glycoside flavonoid isolated from the seeds of Zizyphus jujube, with neuroprotective effects. Spinosin inhibits Aβ1-42 production and aggregation via activating Nrf2/HO-1 pathway.
|
-
- HY-N5128
-
-
- HY-P0178A
-
|
LXW7 TFA
|
Integrin
|
Inflammation/Immunology
|
|
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
|
-
- HY-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-107661
-
|
Arundic Acid
ONO-2506; (R)-2-Propyloctanoic acid
|
Others
|
Neurological Disease
|
|
Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid has the potential for stroke and Alzheimer’s disease research.
|
-
- HY-103254
-
|
ML221
|
Others
|
Neurological Disease
|
|
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
|
-
- HY-N3893
-
-
- HY-P9911
-
|
Vedolizumab
Anti-Human lymphocyte α4β7 integrin, Humanized Antibody
|
Integrin
|
Inflammation/Immunology
|
|
Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
|
-
- 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-W011890
-
-
- HY-131087
-
-
- HY-117541
-
|
Glycyl-glutamine
Glycyl-L-glutamine
|
Others
|
Neurological Disease
|
|
Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems. Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln).
|
-
- HY-107829
-
|
3-Aminopropionitrile fumarate (2:1)
Di-β-aminopropionitrile fumarate; β-Aminopropionitrile fumarate; β-Ammoniumpropionitrile hemifumarate
|
Others
|
Others
|
|
3-Aminopropionitrile fumarate (2:1) is a lathyrogen which inhibits crosslinking of collagen.
|
-
- HY-112700
-
|
SHIP2-IN-1
|
Phosphatase
|
Neurological Disease
|
|
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease.
|
-
- HY-135591
-
-
- HY-N6958
-
-
- HY-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM [1].
|
-
- HY-113013A
-
|
Hydroxypyruvic acid lithium hydrate
β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-N5084
-
-
- 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-18980
-
|
Rottlerin
Mallotoxin; NSC 56346; NSC 94525
|
PKC
Autophagy
Apoptosis
|
Infection
Cancer
|
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.
|
-
- HY-10009
-
-
- 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-10277
-
|
Odiparcil
SB-424323
|
Thrombin
|
Cardiovascular Disease
|
|
Odiparcil (SB-424323) is an orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) [1].
|
-
- HY-W018512
-
-
- HY-B0252
-
|
Hydrochlorothiazide
HCTZ
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
|
-
- HY-B0116
-
-
- HY-B0116A
-
-
- HY-19805
-
|
STO-609
|
CaMK
AMPK
Autophagy
|
Metabolic Disease
|
|
STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
|
-
- HY-107436
-
|
LE135
|
RAR/RXR
TRP Channel
|
Cancer
Neurological Disease
|
|
LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively.
|
-
- HY-N2174
-
-
- HY-10108
-
|
LY294002
|
PI3K
Casein Kinase
DNA-PK
Autophagy
Apoptosis
|
Cancer
Infection
|
|
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
|
-
- HY-107819
-
-
- 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-B1794A
-
-
- HY-17631A
-
-
- 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) [1].
|
-
- HY-N8441
-
|
Neriifolin
17β-Neriifolin
|
Na+/K+ ATPase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells[2.
|
-
- HY-141139
-
-
- 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-N0277
-
-
- HY-U00424
-
-
- HY-116084
-
-
- HY-B0381B
-
-
- HY-124867
-
|
D3-βArr
|
TSH Receptor
|
Endocrinology
|
|
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
|
-
- HY-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-124634
-
|
PZ-2891
|
Others
|
Neurological Disease
|
|
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
|
-
- HY-19383
-
|
Ertiprotafib
PTP 112
|
Phosphatase
IKK
PPAR
|
Metabolic Disease
|
|
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
|
-
- HY-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-12270
-
|
T-5224
|
MMP
|
Others
|
|
T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
|
-
- HY-19635A
-
-
- HY-14879A
-
|
Avibactam sodium
NXL-104
|
Bacterial
Antibiotic
|
Infection
|
|
Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
|
-
- HY-14879B
-
|
Avibactam sodium hydrate
NXL-104 hydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Avibactam sodium hydrate (NXL-104 hydrate) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
|
-
- HY-N4128
-
|
4''-methyloxy-Daidzin
Daidzein 7-O-Β-D-glucoside 4''-O-methylate
|
Others
|
Inflammation/Immunology
|
|
4''-methyloxy-Daidzin (Daidzein 7-O-Β-D-glucoside 4''-O-methylate), an isoflavone methyl-glycoside, is isolated from Cordyceps militaris grown on germinated soybeans. Isoflavones possess immunomodulating and antiallergic activities.
|
-
- HY-15723A
-
-
- HY-12292
-
|
IM-12
|
GSK-3
|
Cancer
|
|
IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
|
-
- HY-19050
-
-
- HY-137862
-
|
1-Oleoyl lysophosphatidic acid
1-Oleoyl-sn-glycero-3-phosphate; 1-Oleoyl-LPA
|
LPL Receptor
|
Neurological Disease
|
|
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant LPA species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation. 1-Oleoyl lysophosphatidic acid increases SRE-drivenβ-galactosidase activity.
|
-
- HY-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-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-18676
-
|
OSU-T315
|
Integrin
Autophagy
Apoptosis
|
Cancer
|
|
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
|
-
- HY-B1127
-
|
Betamipron
N-Benzoyl-β-alanine
|
Bacterial
Antibiotic
|
Others
|
|
Betamipron is a chemical compound which is used together with Panipenem to inhibit Panipenem uptake into the renal tubule and prevent nephrotoxicity.
|
-
- HY-14879
-
|
Avibactam free acid
NXL-104 free acid
|
Bacterial
Antibiotic
|
Infection
|
|
Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
|
-
- HY-10182B
-
|
CHIR-99021 trihydrochloride
CT99021 trihydrochloride
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 trihydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 trihydrochloride induces autophagy.
|
-
- HY-10182
-
|
CHIR-99021
CT99021
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 (CT99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces autophagy.
|
-
- HY-N7676
-
|
Marein
|
AMPK
HDAC
|
Metabolic Disease
Neurological Disease
Cardiovascular Disease
|
|
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
|
-
- HY-W008566
-
-
- 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-10484
-
-
- HY-70062
-
-
- HY-14872
-
|
Tideglusib
NP031112
|
GSK-3
|
Neurological Disease
|
|
Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3β WT (1 h preincubation) and GSK-3β C199A (1 h preincubation), respectively.
|
-
- HY-P1061A
-
|
Colivelin TFA
|
STAT
Amyloid-β
|
Neurological Disease
|
|
Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
|
-
- HY-N2481
-
|
Oroxylin A-7-O-glucuronide
Oroxyloside; Oroxylin A-7-O-β-D-glucuronide
|
Others
|
Neurological Disease
|
|
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitory activity.
|
-
- HY-U00426
-
-
- HY-18173
-
|
AZD8329
|
Others
|
Metabolic Disease
|
|
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
|
-
- 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-13783
-
|
BIBF0775
|
TGF-β Receptor
|
Cancer
|
|
BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
|
-
- HY-B1275A
-
-
- HY-14565
-
|
Pozanicline
ABT-089
|
nAChR
|
Neurological Disease
|
|
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM.
Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
|
-
- HY-B0167
-
-
- 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-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-B1418
-
|
Tazobactam
CL-298741; YTR-830H
|
Bacterial
Antibiotic
|
Infection
|
|
Tazobactam is a beta Lactamase Inhibitor with antibacterial activity
Target: Antibacterial
Tazobactam is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups.
|
-
- HY-59090
-
|
1-Azakenpaullone
1-Akp
|
GSK-3
|
Metabolic Disease
|
|
1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM.
|
-
- HY-128483
-
-
- HY-10403
-
-
- HY-16143
-
|
Cilengitide TFA
EMD 121974 TFA
|
Integrin
Autophagy
|
Cancer
|
|
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
|
-
- HY-B0320A
-
-
- HY-18748
-
|
BQR-695
NVP-BQR695
|
PI4K
Parasite
|
Infection
|
|
BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
|
-
- 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-15027
-
-
- HY-B1197
-
-
- 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-101275
-
-
- HY-18055
-
-
- HY-18053
-
-
- HY-P1260
-
-
- 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-119486A
-
|
(Rac)-Tavapadon
(Rac)-PF-06649751; (Rac)-CVL-751
|
Dopamine Receptor
|
Neurological Disease
|
|
(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.
|
-
- 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-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-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-112502
-
|
MethADP
Adenosine 5'-(α,β-methylene)diphosphate
|
CD73
|
Cancer
|
|
MethADP is a specific CD73 inhibitor.
|
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-116624
-
|
MAZ51
|
VEGFR
Apoptosis
|
Cancer
|
|
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
|
-
- HY-100602
-
-
- HY-U00434
-
-
- HY-N0441
-
-
- HY-101214
-
-
- HY-B0289
-
-
- HY-N1380
-
-
- HY-13764
-
-
- HY-P1260A
-
-
- HY-18965
-
-
- HY-N0373
-
|
Licochalcone B
|
Amyloid-β
|
Neurological Disease
|
|
Licochalcone B is an extract from the root of Glycyrrhiza inflate. Licochalcone B inhibits amyloid β (Aβ42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ions.
|
-
- HY-10182A
-
|
CHIR-99021 monohydrochloride
CT99021 monohydrochloride
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 monohydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 monohydrochloride induces autophagy.
|
-
- HY-19964
-
-
- HY-101091
-
-
- HY-50948
-
-
- HY-112045
-
|
PRI-724
|
Wnt
|
Cancer
|
|
PRI-724 is a selective inhibitor of the CBP/β-catenin interaction.
|
-
- HY-105661
-
-
- HY-16777
-
-
- HY-19306
-
|
SB-267268
|
Integrin
|
Cancer
|
|
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
|
-
- 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-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-N1280
-
|
Semilicoisoflavone B
|
Amyloid-β
|
Neurological Disease
|
|
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation.
|
-
- HY-B0445
-
|
NAD+
β-DPN; β-NAD; β-Nicotinamide Adenine Dinucleotide
|
Endogenous Metabolite
|
Metabolic Disease
|
|
NAD+ is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
|
-
- HY-15300
-
-
- HY-100415
-
|
UKI-1
UKI-1C
|
Others
|
Infection
|
|
UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system.
|
-
- 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-16752
-
|
Relebactam
MK-7655
|
Bacterial
|
Infection
|
|
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.
|
-
- HY-18749
-
-
- 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-B0167A
-
-
- 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-15721
-
-
- HY-103705
-
-
- HY-19930
-
-
- HY-119706
-
|
Barbadin
|
Others
|
Others
|
|
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors.
|
-
- HY-120697
-
|
MSAB
|
Wnt
β-catenin
|
Cancer
|
|
MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells.
|
-
- HY-103394
-
|
TC HSD 21
|
Others
|
Cancer
|
|
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
|
-
- HY-N0527
-
|
Pentagalloylglucose
Penta-O-galloyl-β-D-glucose; 1,2,3,4,6-Pentagalloyl glucose
|
Influenza Virus
|
Infection
|
|
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a gallotannin isolated from various plants. It suppressed interleukin (IL)-4 induced signal pathway in B cell, and inhibited IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors. Pentagalloylglucose possesses significant anti-rabies virus (RABV) activity.
|
-
- HY-100447
-
-
- HY-B0809
-
-
- HY-128642
-
|
FAPI-2
|
Others
|
Cancer
|
|
FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
|
-
- HY-W010907
-
|
Pamoic acid disodium
|
ERK
|
Neurological Disease
|
|
Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.
|
-
- HY-135581
-
|
Raloxifene 6-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
|
-
- HY-135582
-
|
Raloxifene 4'-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
|
-
- 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-15253
-
-
- HY-N6640
-
|
2-O-Acetyl-20-hydroxyecdysone
20-Hydroxyeedysone 2-acetate
|
Others
|
Neurological Disease
|
|
2-O-Acetyl-20-hydroxyecdysone, an ecdysterones in insects and terrestrial plants, inhibits amyloid-β42 (Aβ42)-induced cytotoxicity. 2-O-Acetyl-20-hydroxyecdysone could decrease Aβ oligomer formation through promotion of fibrogenesis, transforming Aβ oligomers to the low-toxicity fibrils.
|
-
- HY-15438
-
|
SB 415286
|
GSK-3
Apoptosis
|
Metabolic Disease
|
|
SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
|
-
- HY-13060
-
-
- HY-100944
-
-
- HY-107368
-
-
- HY-A0256A
-
-
- HY-12704
-
-
- HY-15374
-
-
- HY-P1481
-
-
- 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-103374
-
|
Phenserine
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
AChE
Amyloid-β
|
Neurological Disease
|
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
|
-
- HY-12012
-
-
- 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-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-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-112473
-
-
- HY-128643
-
|
FAPI-4
|
Others
|
Cancer
|
|
FAPI-4 is a fibroblast activation protein (FAP) inhibitor used in cancer research.
|
-
- HY-15840
-
|
YLF-466D
C24
|
AMPK
|
Cancer
|
|
YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
|
-
- 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-N4186
-
-
- 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-12496
-
-
- HY-101444A
-
-
- HY-100207
-
|
CP21R7
CP21
|
GSK-3
|
Cancer
|
|
CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
|
-
- HY-N1064
-
|
Xanthoplanine
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
|
-
- HY-N0249
-
|
Saikosaponin C
|
Amyloid-β
|
Neurological Disease
|
|
Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression.
|
-
- HY-100563
-
-
- HY-100563A
-
-
- HY-B0788A
-
-
- HY-A0256B
-
-
- 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-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-N2566
-
|
Euscaphic acid
|
DNA/RNA Synthesis
PI3K
Apoptosis
|
Cancer
|
|
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
|
-
- HY-U00458
-
|
K-80003
TX-803
|
Akt
|
Cancer
|
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-15252
-
-
- HY-N0270
-
|
Ononin
Ononoside; Formononetin 7-O-β-D-glucopyranoside
|
Others
|
Others
|
|
Ononin is an isoflavonoid, is an additional growth inhibitor in soils associated with the weed, Pluchea lanceolata.
|
-
- HY-12357
-
-
- HY-N7452
-
-
- HY-N0896
-
|
Inulicin
1-O-Acetylbritannilactone
|
NF-κB
COX
|
Cancer
Inflammation/Immunology
|
|
Inulicin (1-O-Acetylbritannilactone) is an active compound isolated from Inula Britannica L. Inulicin (1-O-Acetylbritannilactone) inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
|
-
- HY-P1375
-
|
[D-Trp7,9,10]-Substance P
|
mAChR
|
|
|
[D-Trp7,9,10]-Substance P is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-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-19618
-
|
BRD3308
|
HDAC
HIV
|
Infection
Metabolic Disease
|
|
BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.
|
-
- HY-101090
-
-
- HY-19694
-
|
BRD7552
|
Others
|
Endocrinology
|
|
BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.
|
-
- HY-16294
-
|
LY2090314
|
GSK-3
|
Cancer
|
|
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
|
-
- HY-107790
-
|
5-Methoxyflavone
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
|
-
- 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-15530
-
-
- 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-12831
-
-
- 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-107301
-
-
- HY-P1375A
-
|
[D-Trp7,9,10]-Substance P TFA
|
mAChR
|
|
|
[D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-129390
-
|
Orelabrutinib
ICP-022
|
Btk
|
Cancer
|
|
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
|
-
- HY-B0167S
-
-
- HY-101930
-
|
BMS-816336
|
Others
|
Metabolic Disease
|
|
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
|
-
- HY-15761
-
|
AZD2858
|
GSK-3
|
Neurological Disease
|
|
AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
|
-
- HY-111931
-
-
- HY-14428
-
|
ICG-001
|
β-catenin
Apoptosis
|
Cancer
|
|
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.
|
-
- HY-16659
-
|
EHT 1864
|
Ras
|
Neurological Disease
Cancer
|
|
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo.
|
-
- HY-B1434
-
-
- HY-16321
-
-
- HY-103095
-
|
AAI101
|
Bacterial
|
Infection
|
|
AAI101 is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.
|
-
- HY-13019
-
|
BI605906
|
IKK
|
Others
|
|
BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.
|
-
- HY-10344
-
-
- HY-100337
-
-
- HY-14281
-
|
Trilostane
Win 24540
|
Others
|
Endocrinology
Cancer
|
|
Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
|
-
- HY-12014
-
-
- HY-76691
-
-
- HY-19339
-
-
- HY-134477
-
|
NF-κΒ activator 2
|
NF-κB
|
Neurological Disease
|
|
NF-κΒ activator 2 is a potent and orally active NF-ҡB activator, with an EC50 of 1.58 μM. NF-κΒ activator 2 induces SOD2 through increasing NF-ҡB expression and activation. NF-κΒ activator 2 can be used for the research of amyotrophic lateral sclerosis (ALS).
|
-
- HY-131265
-
-
- 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-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-100965
-
-
- 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-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-13719
-
|
Oleandrin
|
Na+/K+ ATPase
Apoptosis
|
Cancer
|
|
Oleandrin inhibits the Na +, K +-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.
|
-
- HY-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-112125A
-
-
- HY-W010041
-
|
Scyllo-Inositol
|
Amyloid-β
Endogenous Metabolite
|
Neurological Disease
|
|
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model.
|
-
- 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-103241
-
|
Ro 90-7501
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Cancer
Neurological Disease
|
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
|
-
- HY-A0072S
-
|
Zilpaterol-d7
|
Adrenergic Receptor
|
Endocrinology
|
|
Zilpaterol-d7 is a deuterium labeled Zilpaterol. Zilpaterol is a β-adrenergic receptor agonist that putatively, through activation of protein kinase A, increases protein synthesis in skeletal muscle fibers as well as reduces lipogenesis and increases lipolysis in adipose tissues. Formulations containing Zilpaterol have been used to increase lean body weight and improve feed efficiency in commercial beef cattle.
|
-
- HY-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-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-15122
-
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-124257
-
|
(R)-Citronellol
D-Citronellol; (R)-(+)-β-Citronellol
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
(R)-Citronellol (D-Citronellol) is an alcoholic monoterpene found in geranium essential oil. (R)-Citronellol inhibits degranulation of mast cells and does not affect caffeine bitterness perception. (R)-Citronellol can be used in decorative cosmetics, toiletries as well as in non-cosmetic products.
|
-
- HY-101853
-
-
- HY-U00206
-
-
- HY-B0974
-
-
- HY-B0703
-
-
- HY-135391
-
-
- HY-17453
-
-
- HY-15122A
-
-
- HY-128586A
-
-
- HY-N2506
-
-
- HY-15869
-
-
- HY-128586
-
-
- 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-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-12689
-
-
- HY-137315
-
|
TML-6
|
Amyloid-β
NF-κB
mTOR
Keap1-Nrf2
|
Neurological Disease
|
|
TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research.
|
-
- HY-10016
-
|
E 2012
|
γ-secretase
|
Neurological Disease
|
|
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
|
-
- HY-B0379A
-
|
Adiphenine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has narcotic and anticonvulsant effects.
|
-
- 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-10873
-
|
N-Desethyl Sunitinib
SU-12662
|
Others
|
Cancer
|
|
N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.
|
-
- HY-N7115
-
|
Sultamicillin
|
Bacterial
Antibiotic
|
Infection
|
|
Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with Ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant.
|
-
- 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-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-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-N0761
-
|
Isoferulic acid
3-Hydroxy-4-methoxycinnamic acid
|
Adrenergic Receptor
Influenza Virus
|
Infection
Endocrinology
Metabolic Disease
|
|
Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use. Isoferulic acid also has anti-influenza virus activities.
|
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- 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-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-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-13971
-
-
- HY-17006
-
-
- HY-B0555A
-
-
- HY-12662
-
-
- HY-12075
-
-
- HY-P1613A
-
-
- HY-13226
-
|
Galunisertib
LY2157299
|
TGF-β Receptor
|
Cancer
|
|
Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
|
-
- HY-N0283
-
-
- HY-13605
-
-
- HY-13605A
-
-
- HY-111055
-
|
BIP-135
|
GSK-3
|
Neurological Disease
|
|
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.
|
-
- HY-14176
-
|
Compound E
|
γ-secretase
|
Cancer
|
|
Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
|
-
- HY-B0927
-
|
Hydrastine
(-)-β-Hydrastine; (1R,9S)-β-Hydrastine
|
Others
|
Others
|
|
Hydrastine is a natural alkaloid which is present in Hydrastis canadensis and other plants of the ranunculaceae family.
|
-
- HY-N0410
-
-
- HY-19354
-
|
Aglafoline
Aglafolin; Rocaglamide U; (-)-Methyl rocaglate
|
Others
|
Cardiovascular Disease
|
|
Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor).
|
-
- HY-16785
-
-
- HY-15251
-
-
- HY-N2283
-
-
- HY-32735
-
|
Triptolide
PG490
|
NF-κB
Apoptosis
|
Cancer
|
|
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.
|
-
- HY-111789
-
-
- HY-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-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-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-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-A0009
-
|
Galanthamine hydrobromide
Galantamine hydrobromide
|
AChE
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
|
-
- HY-103442
-
|
CGP52411
DAPH
|
EGFR
Amyloid-β
|
Cancer
Neurological Disease
|
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
|
-
- HY-136065
-
|
bpV(phen)
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- 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-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-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-134476
-
-
- HY-B2230
-
-
- HY-N2147
-
|
Phorbol
4β-Phorbol
|
Others
|
Cancer
|
|
Phorbol is a highly toxic diterpene, whose esters have important biological properties.
|
-
- 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-112799
-
|
DK419
|
Wnt
β-catenin
|
Cancer
|
|
DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.
|
-
- HY-107988
-
-
- HY-N6631
-
-
- HY-101180
-
|
C2 Ceramide
Ceramide 2
|
Phosphatase
Mitochondrial Metabolism
Apoptosis
|
Endocrinology
Metabolic Disease
|
|
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
|
-
- HY-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-101130
-
-
- HY-12050
-
|
CP-673451
|
PDGFR
|
Cancer
|
|
CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-17579
-
-
- 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-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-108628
-
|
SU16f
|
PDGFR
|
Cancer
|
|
SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.
|
-
- HY-16910
-
|
WIKI4
|
PARP
β-catenin
|
Cancer
|
|
WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.
|
-
- HY-114454
-
|
INH14
|
IKK
|
Cancer
Inflammation/Immunology
|
|
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
|
-
- 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-15707
-
-
- HY-13694
-
-
- HY-N0708
-
-
- HY-B0099
-
-
- HY-N0702
-
|
Tenuifolin
|
Beta-secretase
AChE
|
Neurological Disease
|
|
Tenuifolin is a triterpene isolated from Polygala tenuifolia Willd, has neuroprotective effects. Tenuifolin reduces Aβ secretion by inhibiting β-secretase. Tenuifolin improves learning and memory in aged mice by decreasing AChE activity and has the potential for Alzheimer’s disease (AD) treatment.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-50845
-
|
Avagacestat
BMS-708163
|
γ-secretase
Notch
|
Cancer
|
|
Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.
|
-
- HY-113914
-
|
9-ING-41
|
GSK-3
Apoptosis
|
Cancer
|
|
9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity.
|
-
- HY-B1367
-
|
Carbenoxolone disodium
|
Gap Junction Protein
|
Infection
Inflammation/Immunology
|
|
Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.
|
-
- HY-15785
-
|
TAS-116
|
HSP
|
Cancer
|
|
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
|
-
- 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-17376
-
-
- 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-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-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-11102
-
-
- HY-18988
-
|
ETC-159
ETC-1922159
|
Porcupine
Wnt
|
Cancer
|
|
ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
|
-
- HY-N0492
-
-
- HY-124822
-
|
COH-SR4
|
AMPK
|
Cancer
Metabolic Disease
|
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation, and can be used for the research of obesity and related metabolic disorders.
|
-
- HY-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-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-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-B0452
-
-
- HY-19468
-
-
- HY-120675
-
|
SSTC3
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-13076
-
|
CHIR-98014
|
GSK-3
|
Metabolic Disease
|
|
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
|
-
- HY-P0023
-
|
Cyclo(-RGDfK)
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-N1446B
-
-
- HY-104038
-
-
- HY-112619
-
|
TES-991
|
Others
|
Metabolic Disease
|
|
TES-991 is a potent and selective human α‑Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.
|
-
- HY-15837
-
|
SAR-260301
|
PI3K
|
Cancer
|
|
SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC50 of 23 nM.
|
-
- HY-N7111
-
|
Sultamicillin tosylate
|
Bacterial
|
Infection
|
|
Sultamicillin (tosylate) is a potent and orally active beta-lactamase inhibitor, an antibiotic with antibacterial activity. Sultamicillin (tosylate) is the tosylate salt of the double ester of sulbactam plus ampicillin.
|
-
- HY-100198
-
-
- HY-B0942
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-15718A
-
-
- HY-19205A
-
-
- 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-100611
-
-
- 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-112220
-
|
VIT-2763
|
Others
|
Metabolic Disease
|
|
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.
|
-
- HY-10230
-
|
Midostaurin
PKC412; CGP 41251
|
PKC
|
Cancer
|
|
Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
|
-
- 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-124607B
-
|
BRD3731
|
GSK-3
|
Neurological Disease
|
|
BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 can be used for the research of a mood disorder, post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorder.
|
-
- HY-125263
-
|
OP-1074
|
Estrogen Receptor/ERR
|
Cancer
|
|
OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
|
-
- HY-P0023A
-
|
Cyclo(-RGDfK) TFA
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-111267
-
-
- HY-108635
-
-
- HY-108742A
-
|
Abaloparatide TFA
BA 058 TFA; BIM 44058 TFA
|
Thyroid Hormone Receptor
|
Metabolic Disease
Endocrinology
|
|
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue selected to be a potent and selective activator of the PTHR1 signaling pathway. Abaloparatide TFA enhances Gs/cAMP signaling (EC50 of 0.3 nM) and β-arrestin recruitment (EC50 of 0.9 nM) in MC3T3-E1 osteoblast cells.
|
-
- 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-103490
-
|
Takinib
|
MAP3K
Apoptosis
|
Cancer
|
|
Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
|
-
- HY-B0158
-
-
- HY-109103
-
|
Tegatrabetan
BC2059
|
β-catenin
|
Cancer
|
|
Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).
|
-
- HY-100221
-
-
- HY-B1816
-
-
- 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-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-101085
-
|
SKL2001
|
Wnt
β-catenin
|
Cancer
|
|
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.
|
-
- HY-18959
-
|
CWP232228
|
β-catenin
Wnt
|
Cancer
|
|
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
|
-
- HY-137472
-
|
SAR502250
|
GSK-3
|
Neurological Disease
|
|
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-16276
-
-
- HY-101271
-
-
- HY-10453
-
|
Ixazomib
MLN2238
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
|
-
- HY-112182
-
|
UM-164
DAS-DFGO-II
|
Src
p38 MAPK
Autophagy
|
Cancer
|
|
UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
|
-
- HY-111507
-
|
PDGFRα kinase inhibitor 1
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-15098
-
|
Apoptozole
Apoptosis Activator VII
|
HSP
Apoptosis
|
Cancer
|
|
Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
|
-
- HY-16642A
-
-
- HY-19700
-
-
- HY-N0436
-
|
Engeletin
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-13296
-
|
PYR-41
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
|
-
- HY-19084
-
|
Ro-24-0238
|
Others
|
Inflammation/Immunology
|
|
Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF.
|
-
- HY-N0629
-
-
- HY-100227
-
|
E 64c
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-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-100381
-
-
- HY-B0493
-
-
- HY-15147
-
|
XAV-939
|
β-catenin
PARP
|
Cancer
|
|
XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
|
-
- HY-112613
-
|
UCB9608
|
PI4K
|
Inflammation/Immunology
|
|
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent.
|
-
- 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-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-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-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-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-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-N1446
-
-
- HY-70002
-
-
- HY-N2022
-
|
Castanospermine
|
Glucosidase
|
Cancer
|
|
Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
|
-
- HY-16665
-
|
iCRT 14
|
Wnt
|
Cancer
|
|
iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.
|
-
- HY-12325
-
|
GSK2194069
|
Others
|
Cancer
|
|
GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.
|
-
- HY-108313
-
|
T-00127_HEV1
|
PI4K
|
Infection
|
|
T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM.
|
-
- HY-B1643
-
-
- HY-16265
-
-
- HY-N2215
-
-
- HY-10407
-
|
SU 5402
|
VEGFR
FGFR
PDGFR
|
Cancer
|
|
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
|
-
- HY-14503
-
|
MDR-1339
DWK-1339
|
Amyloid-β
|
Neurological Disease
|
|
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
|
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker, with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- 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-N6781
-
|
Ophiobolin A
|
Phosphodiesterase (PDE)
|
Cancer
Infection
|
|
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
|
-
- HY-N0177
-
|
Diosgenin
|
STAT
|
Metabolic Disease
|
|
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
|
-
- HY-13772
-
|
Valrubicin
AD-32
|
PKC
|
Cancer
Inflammation/Immunology
|
|
Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
|
-
- HY-N0754
-
|
Eupalinolide A
|
HSP
|
Inflammation/Immunology
|
|
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
|
-
- HY-120261
-
-
- HY-B0649
-
-
- HY-N6046
-
-
- 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-50202
-
|
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-W009009
-
|
L-838417
|
GABA Receptor
|
Neurological Disease
|
|
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
|
-
- 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-108593
-
-
- HY-N2006
-
|
Ganoderic acid B
|
HIV Protease
|
Infection
|
|
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
|
-
- HY-13438
-
|
AZD3839 free base
|
Beta-secretase
|
Cancer
|
|
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
|
-
- HY-13862
-
|
AZD1080
|
GSK-3
|
Neurological Disease
|
|
AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
|
-
- HY-111930
-
|
5-Iodo-indirubin-3'-monoxime
|
GSK-3
CDK
|
Cancer
|
|
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
|
-
- HY-13289A
-
|
Nepicastat hydrochloride
SYN-117 hydrochloride; RS-25560-197 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-101930B
-
|
(R)-BMS-816336
|
Others
|
Metabolic Disease
|
|
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively [1].
|
-
- HY-W050031
-
|
(S)-3-Hydroxybutanoic acid
(S)-β-Hydroxybutanoic acid; L-(+)-3-Hydroxybutyric acid; L-β-Hydroxybutyric acid
|
Endogenous Metabolite
|
Others
|
|
(S)-3-Hydroxybutanoic acid is a normal human metabolite, that has been found elevated in geriatric patients remitting from depression. In humans, 3-Hydroxybutyric acid is synthesized in the liver from acetyl-CoA, and can be used as an energy source by the brain when blood glucose is low.
|
-
- HY-10431
-
-
- HY-10452
-
|
Ixazomib citrate
MLN9708
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
|
-
- HY-10114
-
|
TGX-221
|
PI3K
|
Cancer
|
|
TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.
|
-
- HY-50883
-
|
BMS 299897
|
γ-secretase
|
Neurological Disease
|
|
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
|
-
- HY-111365
-
|
TES-1025
|
Others
|
Metabolic Disease
|
|
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM.
|
-
- HY-W009168
-
|
Tazobactam sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Tazobactam sodium is an antibiotic of the beta-lactamase inhibitor class. Ceftolozane combines with Tazobactam, extends the activity of ceftolozane against many ESBL-producing Enterobacteriaceae and some Bacteroides spp..
|
-
- 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-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-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-N1469
-
-
- HY-N0014
-
-
- 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-16677A
-
-
- 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-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-10257
-
-
- HY-12303
-
|
OAC1
|
Oct3/4
|
Others
|
|
OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.
|
-
- HY-14714
-
-
- HY-N2632
-
|
Uvarigrin
|
Apoptosis
|
Cancer
|
|
Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
|
-
- HY-135674
-
|
SR-318
|
p38 MAPK
TNF Receptor
|
Cancer
Inflammation/Immunology
|
|
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
|
-
- HY-19807
-
|
Indirubin-3'-monoxime
Indirubin-3'-oxime
|
GSK-3
Lipoxygenase
|
Cancer
|
|
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
|
-
- HY-10580
-
|
GSK 3 Inhibitor IX
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-N0540
-
|
Cynaroside
Luteolin 7-glucoside; Luteolin 7-O-β-D-glucoside
|
Influenza Virus
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Cynaroside (Luteolin 7-glucoside) is a flavone, a flavonoid-like chemical compound. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM.
|
-
- 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-103269
-
|
BAI1
|
Bcl-2 Family
|
Cancer
|
|
BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
|
-
- HY-N4326
-
-
- HY-W010201
-
|
Citronellol
(±)-Citronellol; (±)-β-Citronellol
|
Reactive Oxygen Species
|
Cancer
|
|
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium capitatum. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation.
|
-
- 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. Ta |
