Search Result
Results for "A new oral cox 2 specitic Inhibitors" in MCE Product Catalog:
9176
Inhibitors & Agonists
14
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-14445
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- HY-U00275
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- HY-101655
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COX-2-IN-2
|
COX
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Inflammation/Immunology
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COX-2-IN-2 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX-2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.
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- HY-14670
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Firocoxib
ML 1785713
|
COX
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Inflammation/Immunology
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Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
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- HY-B1888A
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Bromfenac sodium
|
COX
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Inflammation/Immunology
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Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME).
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- HY-B1888B
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Bromfenac sodium hydrate
Bromfenac monosodium salt sesquihydrate
|
COX
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Inflammation/Immunology
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Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium hydrate is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME).
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- HY-B0367
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- HY-B0619
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Zaltoprofen
CN100
|
COX
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Inflammation/Immunology
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Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
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- HY-B0360
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- HY-129113
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α-Chaconine
|
COX
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Inflammation/Immunology
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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.
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- HY-15036
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Diclofenac
|
COX
Apoptosis
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Inflammation/Immunology
|
Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
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- HY-15038
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Diclofenac potassium
|
COX
Apoptosis
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Inflammation/Immunology
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Diclofenac potassium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
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- HY-B0360S
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- HY-15036A
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Diclofenac diethylamine
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COX
Apoptosis
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Inflammation/Immunology
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Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
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- HY-15037
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Diclofenac Sodium
GP 45840
|
COX
Apoptosis
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Inflammation/Immunology
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Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
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- HY-N7688
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- HY-10439
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HPGDS inhibitor 1
|
PGE synthase
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Inflammation/Immunology
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HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
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- HY-15321
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Etoricoxib
MK-0663; L-791456
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COX
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Inflammation/Immunology
Cancer
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Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
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- HY-N2252
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- HY-17372
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Rofecoxib
MK 966
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COX
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Inflammation/Immunology
Cancer
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Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
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- HY-78131A
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(S)-(+)-Ibuprofen
(S)-Ibuprofen
|
COX
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Inflammation/Immunology
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(S)-(+)-Ibuprofen ((S)-Ibuprofen), a S(+)-enantiomer of Ibuprofen, is a potent COX-1 and COX-2 inhibitor with IC50s of 2.1 μM and 1.6 μM, respectively. (S)-(+)-Ibuprofen has analgesic, anti-inflammatory, anticancer and antipyretic effects.
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- HY-U00022
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- HY-B0363S
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Nimesulide D5
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COX
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Inflammation/Immunology
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Nimesulide D5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
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- HY-B0008
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- HY-15321S
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Etoricoxib D4
MK-0663 D4; L-791456 D4
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COX
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Others
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Etoricoxib D4 (MK-0663 D4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
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- HY-W015007
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Metyrosine
|
COX
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Cardiovascular Disease
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Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.
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- HY-126114
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Lupeol acetate
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Others
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Inflammation/Immunology
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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.
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- HY-17479A
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- HY-78131AS
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(S)-(+)-Ibuprofen D3
(S)-Ibuprofen D3
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COX
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Inflammation/Immunology
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(S)-(+)-Ibuprofen D3 ((S)-Ibuprofen D3) is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects.
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- HY-B0559
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Nabumetone
BRL14777
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COX
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Inflammation/Immunology
Cancer
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Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.
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- HY-17474A
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Parecoxib Sodium
SC 69124A
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COX
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Inflammation/Immunology
Cancer
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Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
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- HY-100580
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Asaraldehyde
Asaronaldehyde; Asaraldehyde; 2,4,5-trimethoxy-Benzaldehyde
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COX
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Inflammation/Immunology
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Asarylaldehyde is a natural COX-2 inhibitor, which isolated from carrot (Daucus carota L.) seeds significantly inhibits cyclooxygenase II (COX-2) activity at IC50 value 100 μg/mL.
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- HY-15762
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Valdecoxib
SC 65872
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COX
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Inflammation/Immunology
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Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.
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- HY-N3848
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- HY-N0929
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Hexahydrocurcumin
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COX
Reactive Oxygen Species
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Cancer
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Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities.
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- HY-W013164
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SC-58125
|
COX
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Cancer
Inflammation/Immunology
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SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo. SC-58125 also can inhibit edema at the inflammatory site and has analgesic effect.
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- HY-N2429
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Sphondin
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COX
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Inflammation/Immunology
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Sphondin, isolated from Heracleum laciniatum, possesses an inhibitory effect on IL-1β-induced increase in the level of COX-2 protein and PGE2 release in A549 cells.
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- HY-U00239
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- HY-103387
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DuP-697
|
COX
Apoptosis
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Cancer
Inflammation/Immunology
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DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.
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- HY-B0808
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Oxaprozin
Oxaprozinum; Wy21743
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COX
NF-κB
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Inflammation/Immunology
Cancer
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Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
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- HY-N0613
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Sauchinone
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NF-κB
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Inflammation/Immunology
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Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
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- HY-19212
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S-2474
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COX
Lipoxygenase
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Inflammation/Immunology
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S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
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- HY-B1799
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Tolmetin
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COX
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Cancer
Inflammation/Immunology
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Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID).
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- HY-N0767
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- HY-U00083
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- HY-14654
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- HY-B1489
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- HY-B0335
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Tolfenamic Acid
GEA 6414
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COX
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Inflammation/Immunology
Cancer
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Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
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- HY-N0356
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(-)-Catechin gallate
(-)-Catechin 3-gallate; (-)-Catechin 3-O-gallate
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COX
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Cancer
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(-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
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- HY-B2137
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- HY-15030A
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- HY-15030
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- HY-17357
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- HY-U00146
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- HY-N0147
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- HY-B0580
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Ketorolac
RS37619
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COX
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Inflammation/Immunology
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Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
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- HY-N0256
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Hederagenin
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Others
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Cancer
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Hederagenin is a triterpenoid saponin. It can inhibit LPS-stimulated expression of iNOS, COX-2, and NF-κB.
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- HY-14397A
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Indomethacin sodium hydrate
Indometacin sodium hydrate
|
COX
Autophagy
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Cancer
Inflammation/Immunology
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Indomethacin sodium hydrate (Indometacin sodium hydrate) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin sodium hydrate disrupts autophagic flux by disturbing the normal functioning of lysosomes.
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- HY-14397
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Indomethacin
Indometacin
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COX
Autophagy
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Cancer
Inflammation/Immunology
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Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
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- HY-N0396
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- HY-14398
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- HY-B0261
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- HY-N0481
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Roburic acid
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COX
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Inflammation/Immunology
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Roburic acid, a tetracyclic triterpenoid found in Gentiana macrophylla, acts as an inhibitor of COX, with IC50s of 5 and 9 μM for COX-1 and COX-2, respectively.
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- HY-N0389
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Columbin
|
COX
Parasite
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Inflammation/Immunology
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Columbin is an orally active diterpenoid furanolactone from Calumbae radix, has anti-inflammatory and anti-trypanosomal effects. Columbin selectively inhibits COX-2 (EC50=53.1 μM) over COX-1 (EC50=327 μM).
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- HY-N0447
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- HY-B0138
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Ketorolac tromethamine salt
Ketorolac Tromethamine; Ketorolac tris salt; RS37619 tromethamine salt
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COX
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Inflammation/Immunology
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Ketorolac tromethamine salt (RS37619 tromethamine salt) is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
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- HY-78131S
-
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- HY-U00197
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Tilmacoxib
JTE522; JTP19605; RWJ57504
|
COX
|
Inflammation/Immunology
|
Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
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- HY-17357S
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Nepafenac D5
AHR-9434 D5; AL-6515 D5
|
COX
|
Others
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Nepafenac D5 (AHR-9434 D5) is the deuterium labeled Nepafenac, which is a selective COX-2 inhibitor.
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- HY-N0774
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Isofraxidin
|
COX
MMP
Toll-like Receptor (TLR)
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Inflammation/Immunology
|
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
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- HY-B0253
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Piroxicam
CP-16171
|
COX
|
Inflammation/Immunology
Cancer
|
Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.
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- HY-N0232
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Psoralidin
|
COX
Lipoxygenase
Notch
Reactive Oxygen Species
Bacterial
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Cancer
|
Psoralidin, isolated from the seed of Psoralea corylifolia, is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties. Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation.
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- HY-126121
-
-
- HY-119447
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Mavacoxib
|
COX
|
Inflammation/Immunology
|
Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.
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- HY-122591
-
-
- HY-U00129
-
-
- HY-N5015
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Rosmanol
|
Others
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Inflammation/Immunology
Cancer
|
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
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- HY-14397S
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Indomethacin-D4
Indometacin-D4
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COX
Autophagy
|
Cancer
Inflammation/Immunology
|
Indomethacin-D4 (Indometacin-D4) is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
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- HY-131259
-
-
- HY-N2599
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Taraxerol acetate
|
COX
Apoptosis
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Cancer
|
Taraxerol acetate is a COX-1 and COX-2 inhibitor with IC50 values of 116.3 μM and 94.7 μM, respectively. Taraxerol acetate the has the anticancer potential and induces cell apoptosis.
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- HY-131258
-
-
- HY-131260
-
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- HY-W012399
-
-
- HY-B0227
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Ketoprofen
RP-19583
|
COX
Apoptosis
|
Inflammation/Immunology
|
Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively.
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- HY-78131
-
-
- HY-N7630
-
-
- HY-108259
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HQL-79
|
PGE synthase
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Inflammation/Immunology
|
HQL-79, a potent, selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, highly selectively inhibits the synthesis of PGD2, and acts as an anti-allergic agent, with a Kd of 0.8 μM and an IC50 of 6 μM. Shows no obvious effect on COX-1, COX-2, m-PGES, or L-PGDS.
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- HY-17009
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Iguratimod
T614
|
COX
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Inflammation/Immunology
|
Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.
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- HY-B1227
-
-
- HY-15123
-
-
- HY-B0167
-
-
- HY-N0074
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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.
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- HY-B0261S
-
-
- HY-B0578
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Loxoprofen
|
COX
|
Inflammation/Immunology
|
Loxoprofen is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
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- HY-B0578A
-
Loxoprofen sodium
|
COX
|
Inflammation/Immunology
|
Loxoprofen sodium is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
|
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- HY-111950
-
(-)-Ibuprofenamide
(R)-Ibuprofenamide
|
Others
|
Inflammation/Immunology
|
(-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
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- HY-B0336
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Pranoprofen
|
COX
Apoptosis
PGE synthase
|
Cancer
Inflammation/Immunology
|
Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis.
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- HY-N2266
-
-
- HY-14617
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Paradol
[6]-Gingerone; [6]-Paradol
|
COX
|
Cancer
|
Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.
|
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- HY-N1380
-
-
- HY-B0363
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Nimesulide
R805
|
COX
|
Inflammation/Immunology
|
Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
|
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- HY-19675
-
Naproxen etemesil
LT-NS 001; MX 1094
|
COX
|
Inflammation/Immunology
|
Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
|
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- HY-B0253S
-
Piroxicam D3
CP-16171 D3
|
COX
|
Cancer
Inflammation/Immunology
|
Piroxicam D3 (CP-16171 D3) is deuterium labeled Piroxicam. Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively .
|
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- HY-119304
-
-
- HY-105028
-
Tenidap
CP-66248
|
COX
|
Inflammation/Immunology
|
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor.
|
-
- HY-114200
-
Imrecoxib
BAP-909
|
COX
|
Inflammation/Immunology
|
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.
|
-
- 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-121537
-
CAY10404
|
COX
Akt
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.
|
-
- HY-B1026
-
-
- HY-121899
-
1-Oxo Ibuprofen
Ibuprofen EP impurity J
|
Others
|
Others
|
1-Oxo Ibuprofen (Ibuprofen EP impurity J) is a degradation product and a potential impurity in preparations of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
|
-
- HY-13913
-
NS-398
|
COX
|
Inflammation/Immunology
Cancer
|
NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.
|
-
- HY-17474
-
Parecoxib
SC 69124
|
COX
|
Cancer
Inflammation/Immunology
|
Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
|
-
- 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-66004
-
4-Acetamidophenyl acetate
|
Others
|
Inflammation/Immunology
|
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-N7067
-
Revaprazan hydrochloride
|
Bacterial
COX
|
Infection
|
Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection.
|
-
- HY-W012126
-
2,6-Dichlorodiphenylamine
2,6-Dichloro-N-phenylaniline
|
Bacterial
|
Cancer
Infection
|
2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
|
-
- HY-118139
-
Desmethyl Celecoxib
|
COX
|
Inflammation/Immunology
|
Desmethyl Celecoxib (compound 3b) is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50=32 nM) with anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib and with the optimal yield of 75%.
|
-
- HY-N6968
-
α-Humulene
Humulene; α-Caryophyllene
|
NO Synthase
COX
|
Inflammation/Immunology
|
α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
|
-
- HY-135325
-
-
- HY-N0346A
-
-
- HY-66005
-
-
- HY-B0580A
-
-
- HY-N0635
-
-
- HY-B1138
-
Fenbufen
CL-82204
|
COX
Caspase
|
Inflammation/Immunology
|
Fenbufen is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.
|
-
- HY-N0589
-
-
- HY-N2434
-
[10]-Shogaol
|
COX
|
Cancer
|
[10]-Shogaol is an antioxidant from Zingiber officinale for human skin cell growth and a migration enhancer. [10]-Shogaol inhibits COX-2 with an IC50 of 7.5 μM and has antiproliferation activity.
|
-
- HY-N1067
-
Xanthohumol
|
COX
Acyltransferase
Apoptosis
HSV
CMV
Influenza Virus
|
Cancer
Infection
|
Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol also has antiviral activity against bovine viral diarrhea virus (BVDV), rhinovirus, HSV-1, HSV-2 and cytomegalovirus (CMV).
|
-
- HY-N6891
-
Hamaudol
|
COX
|
Inflammation/Immunology
|
Hamaudol is a chromone isolated from Saposhnikovia divaricata. Hamaudol shows significant inhibitory activity on cyclooxygenase (COX)-1 and COX-2 activities with IC50 values of 0.30, 0.57 mM, respectively, and has potent analgesia and anti-inflammary effects.
|
-
- HY-19217
-
-
- HY-N2410
-
N-trans-Feruloyltyramine
N-feruloyltyramine; Moupinamide
|
COX
|
Inflammation/Immunology
|
N-trans-Feruloyltyramine (N-feruloyltyramine), an alkaloid from Piper nigru, is an inhibitor of COX1 and COX2, with potential antioxidant properties. N-trans-Feruloyltyramine possesses anti-inflammatory activity.
|
-
- HY-B0167S
-
-
- HY-N0493
-
-
- HY-B0760
-
Fenofibric acid
FNF acid
|
PPAR
COX
|
Metabolic Disease
|
Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
|
-
- HY-B0167A
-
-
- HY-U00046
-
Apyramide
|
COX
|
Inflammation/Immunology
|
Apyramide is an anti-inflammatory agent (NSAID) and behaves as a prodrug of indomethacin (HY-14397). Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2.
|
-
- HY-136592
-
-
- HY-N0908
-
-
- HY-N2454
-
-
- HY-N0722
-
-
- HY-N1390
-
Syringaldehyde
|
COX
|
Metabolic Disease
Inflammation/Immunology
|
Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL. Anti-hyperglycemic and anti-inflammatory activities.
|
-
- HY-W010983
-
-
- 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-N0710
-
alpha-Cyperone
α-Cyperone; (+)-α-Cyperone
|
Endogenous Metabolite
|
Inflammation/Immunology
|
alpha-Cyperone (α-Cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1, resulting in reduction of inflammation, which would be highly beneficial for treatment of inflammatory diseases such as AD.
|
-
- HY-B0075S
-
-
- HY-N0041
-
Ginsenoside Rb3
Gypenoside IV
|
NF-κB
COX
NO Synthase
|
Cancer
Inflammation/Immunology
|
Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
|
-
- HY-N2435
-
[8]-Shogaol
|
COX
Apoptosis
|
Cancer
|
[8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC50=5 μM) and inhibits COX-2 (IC50=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells.
|
-
- HY-N2008
-
-
- HY-B1130
-
Isoxicam
|
COX
|
Inflammation/Immunology
|
Isoxicam is an orally active, long-acting, non-steroidal anti-inflammatory agent for the research of arthritis. Isoxicam is a nonselective inhibitor of COX-1 and COX-2.
|
-
- HY-N2106
-
Dehydroevodiamine
|
NF-κB
COX
PGE synthase
NO Synthase
|
Inflammation/Immunology
|
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
|
-
- HY-N6663
-
3-Carene
|
Others
|
Inflammation/Immunology
|
3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation.
|
-
- HY-N2007
-
Veratric acid
3,4-Dimethoxybenzoic acid
|
COX
Reactive Oxygen Species
|
Inflammation/Immunology
Cardiovascular Disease
|
Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
|
-
- HY-N0569
-
-
- HY-N6966
-
-
- HY-N0603
-
-
- HY-N2459
-
Peonidin chloride
YGM-6 chloride
|
COX
|
Cancer
|
Peonidin chloride is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. Peonidin chloride exhibits chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.
|
-
- HY-N0831
-
Jaceosidin
|
Bcl-2 Family
COX
Apoptosis
|
Cancer
Inflammation/Immunology
|
Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
|
-
- HY-N0904
-
Ginsenoside C-K
Ginsenoside compound K; Ginsenoside K
|
COX
NO Synthase
Cytochrome P450
|
Inflammation/Immunology
|
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
|
-
- HY-W018643
-
Ferulic acid methyl ester
Methyl ferulate
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Neurological Disease
Cancer
|
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders. Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages.
|
-
- HY-13425
-
Deguelin
(-)-Deguelin; (-)-cis-Deguelin
|
Akt
Autophagy
Apoptosis
|
Cancer
|
Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
|
-
- HY-B0075
-
-
- HY-N1942
-
5-O-Demethylnobiletin
5-Demethylnobiletin
|
Lipoxygenase
Leukotriene Receptor
|
Inflammation/Immunology
Neurological Disease
Cancer
|
5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Sideritis tragoriganum, is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
|
-
- HY-N2176
-
-
- HY-N6257
-
Cafestol
|
ERK
PGE synthase
COX
NF-κB
|
Cancer
Inflammation/Immunology
|
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects.
|
-
- HY-N0811
-
Anemarsaponin B
|
NO Synthase
COX
NF-κB
|
Inflammation/Immunology
|
Anemarsaponin B is a steroidal saponin isolated from the rhizomes of A. asphodeloides (Liliaceae). Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
|
-
- HY-N1435
-
Oroxin B
|
Apoptosis
PI3K
PTEN
Autophagy
|
Cancer
|
Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent.
Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT.
Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.
|
-
- HY-B0580S
-
Ketorolac D5
|
COX
|
Inflammation/Immunology
|
Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
|
-
- HY-N0043
-
-
- HY-128463
-
-
- HY-17485
-
Alminoprofen
EB-382
|
Phospholipase
COX
|
Inflammation/Immunology
|
Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2.
|
-
- HY-N0698
-
-
- HY-N0523
-
-
- HY-N0523A
-
-
- HY-N0632
-
Esculentoside A
|
COX
NF-κB
|
Inflammation/Immunology
|
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta.
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models, has selective inhibitory activity towards cyclooxygenase-2 (COX-2).
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways.
|
-
- HY-U00347
-
-
- HY-U00439
-
-
- HY-W009248
-
-
- 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-N0222
-
Avicularin
|
Others
|
Cancer
Inflammation/Immunology
|
Avicularin is a bio-active flavonoid from plants, anti-inflammatory, anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. Avicularin ameliorates human hepatocellular carcinoma via the regulation of NF κB (p65), COX 2 and PPAR γ activities.
|
-
- HY-U00041
-
-
- HY-100125
-
Timegadine
SR1368
|
COX
|
Inflammation/Immunology
|
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
|
-
- 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-W010144
-
Phenidone
|
COX
Lipoxygenase
|
Inflammation/Immunology
Cardiovascular Disease
|
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone is used as a photographic developer.
|
-
- HY-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-105024
-
FPL 62064
|
Lipoxygenase
COX
|
Inflammation/Immunology
|
FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC50 values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity.
|
-
- HY-B0368
-
Captopril
SQ 14225
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
|
-
- HY-131973
-
-
- HY-10004
-
-
- HY-B2158
-
-
- HY-106080A
-
Furegrelate sodium
U-63557A
|
Others
|
Cardiovascular Disease
|
Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
|
-
- HY-15028
-
ATB-346
|
COX
Apoptosis
|
Inflammation/Immunology
|
ATB-346 an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2) ATB-346 possesses antiinflammatory and antinociceptive activities.
|
-
- HY-131005
-
-
- HY-101873S
-
-
- HY-101726
-
DuP 105
|
Bacterial
|
Infection
|
DuP 105 is an orally active oxazolidinone, a new class of synthetic antimicrobial agent with activity against gram-positive bacteria.
|
-
- HY-N2109
-
Macranthoidin A
|
Others
|
Metabolic Disease
|
Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil.
|
-
- HY-U00122
-
-
- HY-N0923
-
Corydaline
(+)-Corydaline; Corydalin
|
AChE
Enterovirus
Opioid Receptor
|
Neurological Disease
|
Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 µM. Corydaline is a μ-opioid receptor (Ki of 1.23 µM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 µM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities.
|
-
- HY-100501
-
M2698
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
|
-
- HY-19741
-
-
- HY-133541
-
Glucopiericidin A
|
GLUT
ADC Cytotoxin
Apoptosis
|
Cancer
|
Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts.
|
-
- HY-59105
-
SC-560
|
COX
|
Cancer
|
SC-560 is a potent and selective COX-1 inhibitor with an IC50 of 9 nM.
|
-
- HY-B1279
-
-
- HY-N0355
-
-
- HY-12507
-
-
- HY-112731
-
-
- HY-N0898
-
-
- HY-D0713
-
7ACC2
|
Monocarboxylate Transporter
|
Cancer
|
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.
|
-
- HY-121879
-
-
- HY-10038
-
A 922500
DGAT-1 Inhibitor 4a
|
Acyltransferase
|
Metabolic Disease
|
A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
|
-
- HY-N0002
-
-
- HY-B1279A
-
-
- HY-N0149
-
-
- HY-50709
-
-
- HY-U00434
-
-
- HY-106579
-
Tiaprofenic acid
|
COX
|
Inflammation/Immunology
|
Tiaprofenic acid is an orally active nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic potency. Tiaprofenic acid inhibits prostaglandin synthesis by suppressing cyclo-oxygenase (COX). Tiaprofenic acid can be used in the treatment of rheumatic diseases.
|
-
- HY-10252
-
NVP-ADW742
ADW742; GSK 552602A; ADW
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
|
-
- HY-10846
-
-
- HY-11011
-
A-770041
|
Src
|
Inflammation/Immunology
|
A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
|
-
- HY-U00175
-
-
- 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-14336A
-
SB 271046 Hydrochloride
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
|
-
- HY-19373
-
-
- HY-12422B
-
-
- HY-B0999
-
-
- HY-100226
-
A-205804
|
Integrin
|
Inflammation/Immunology
|
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.
|
-
- HY-131705
-
-
- HY-101479
-
Iclaprim
AR-100
|
Bacterial
|
Infection
|
Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
|
-
- HY-N0001
-
-
- HY-15531
-
Venetoclax
ABT-199; GDC-0199
|
Bcl-2 Family
Autophagy
|
Cancer
|
Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy.
|
-
- HY-N4019
-
Maohuoside A
|
Others
|
Metabolic Disease
|
Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
|
-
- 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-16735
-
Avoralstat
BCX4161
|
Others
|
Others
|
Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.
|
-
- HY-12428
-
-
- HY-13553
-
-
- HY-19663
-
-
- HY-B1461
-
Deoxyarbutin
|
Tyrosinase
|
Others
|
Deoxyarbutin is a new effective lighten ingredient, can effectively inhibit tyrosinase activity and melanin synthesis to get significant and lasting lightening effect.
|
-
- HY-13728A
-
(R)-Plevitrexed
(R)-ZD 9331; (R)-BGC9331
|
Others
|
Cancer
|
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.
|
-
- 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-100411
-
MLi-2
|
LRRK2
|
Neurological Disease
|
MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.
|
-
- HY-B0422
-
Nateglinide
A4166; Senaglinide
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-13728B
-
(Rac)-Plevitrexed
(Rac)-ZD 9331; (Rac)-BGC9331
|
Thymidylate Synthase
|
Cancer
|
(Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331) is a racemate of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.
|
-
- HY-15891A
-
-
- HY-U00258
-
-
- HY-U00092
-
-
- HY-14543
-
-
- HY-19713
-
-
- HY-N1996
-
-
- HY-B0386
-
-
- HY-112543
-
S119-8
|
Influenza Virus
|
Infection
|
S119-8 is a broad spectrum inhibitor of influenza A and B viruses, showing activity against multiple influenza B viruses and an oseltamivir-resistant influenza A virus, but does not inhibit a non-influenza virus, vesicular stomatitis nirus (VSV).
|
-
- HY-131182
-
DS-1971a
|
Sodium Channel
|
Neurological Disease
|
DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.
|
-
- HY-B0162AS1
-
-
- HY-B0162AS
-
-
- HY-N0898A
-
(-)-Catechin
(-)-Cianidanol; (-)-Catechuic acid
|
COX
|
Cancer
|
(-)-Catechin, isolated from green tea, is an isomer of Catechin having a trans 2S,3R configuration at the chiral center. Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
|
-
- HY-B0476
-
Phenacetin
Acetophenetidin
|
COX
|
Inflammation/Immunology
|
Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats.
|
-
- HY-B1045A
-
-
- HY-101422
-
-
- HY-107771
-
-
- HY-17553
-
-
- HY-B0255
-
-
- HY-10582
-
Flurbiprofen
dl-Flurbiprofen
|
COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer.
|
-
- HY-B0958
-
Mupirocin
BRL-4910A; Pseudomonic acid
|
Bacterial
Antibiotic
|
Infection
|
Mupirocin (BRL-4910A) is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin (BRL-4910A) apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.
|
-
- 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-106628
-
Sudoxicam
|
COX
|
Inflammation/Immunology
|
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity.
|
-
- HY-111388B
-
SEL120-34A HCl
|
CDK
|
Cancer
|
SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-18303
-
AMG-47a
|
Src
VEGFR
p38 MAPK
JAK
|
Inflammation/Immunology
|
AMG-47a is a potent and orally bioavailable lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2,p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
|
-
- HY-19732
-
-
- HY-100151
-
-
- HY-131003
-
Taletrectinib
DS-6051b; AB-106
|
ROS
|
Cancer
|
Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
|
-
- HY-B0580B
-
(R)-Ketorolac
(+)-Ketorolac
|
Others
|
Neurological Disease
|
(R)-Ketorolac is the R-enantiomer of Ketorolac, shows potent analgesic activity, reduces ulcerogenic potential. (R)-Ketorolac is inactive on COX.
|
-
- 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-B0317
-
Amlodipine
|
Calcium Channel
|
Cardiovascular Disease
|
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium.
|
-
- HY-U00169
-
-
- HY-101481
-
-
- HY-B0317B
-
Amlodipine besylate
Amlodipine benzenesulfonate
|
Calcium Channel
|
Cardiovascular Disease
|
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium.
|
-
- HY-19477
-
-
- HY-109099
-
Pemigatinib
INCB054828
|
FGFR
|
Cancer
|
Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
|
-
- 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-17525
-
Bethoxazin
|
Bacterial
|
Infection
|
Bethoxazin(Bethoguard) is a new broad spectrum industrial microbicide with applications in material and coating preservation.
|
-
- HY-19684
-
-
- HY-U00283
-
-
- HY-122856
-
AZ12601011
|
TGF-β Receptor
|
Cancer
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-12143
-
-
- HY-15898
-
-
- HY-B1558A
-
Bifemelane hydrochloride
MCI-2016
|
Monoamine Oxidase
|
Neurological Disease
|
Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease.
|
-
- 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-10524
-
GSK1904529A
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
|
-
- HY-18728
-
-
- HY-78131B
-
-
- HY-100436
-
-
- HY-B0079
-
-
- HY-N0543
-
-
- HY-101928
-
-
- HY-N2897
-
-
- HY-B0089
-
Acarbose
BAY g 5421
|
Glucosidase
|
Metabolic Disease
|
Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.
|
-
- HY-76251
-
-
- HY-U00013
-
Nitroflurbiprofen
HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen
|
COX
|
Cardiovascular Disease
|
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
|
-
- HY-114286A
-
PXS-5153A monohydrochloride
|
Monoamine Oxidase
|
Inflammation/Immunology
|
PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.
|
-
- HY-19264
-
264W94
|
Others
|
Metabolic Disease
|
264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action.
|
-
- HY-13959
-
MS436
|
Epigenetic Reader Domain
|
Cancer
|
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
|
-
- HY-13950
-
S186
|
Others
|
Others
|
S186 is a kind of sodium salts of calcium-acetylpropylamine phosphonate(APA); a new strontium-specific chelating agent.
|
-
- HY-U00039
-
-
- HY-101437
-
-
- HY-131448
-
A3334
|
Others
|
Metabolic Disease
|
A3051 is a potent and orally active inhibtor of CXXC5-DVL extracted from patent WO2020079569, has an IC50 of 63.06 nM. A3334 can be used for the research of high fat diet (HFD)-induced and methionine-choline deficient diet (MCD)-induced phenotypes such as obesity, diabetes, and NASH.
|
-
- HY-13512
-
Camostat mesylate
Camostat mesilate; FOY305; FOY-S980
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
|
-
- HY-101437A
-
-
- HY-77591
-
-
- HY-77591A
-
-
- HY-10443
-
Balapiravir
Ro 4588161; R1626
|
HCV
DNA/RNA Synthesis
|
Infection
|
Balapiravir (Ro 4588161; R1626) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity.
|
-
- HY-B0281A
-
-
- HY-B0693
-
-
- HY-B0592S
-
-
- HY-B2145
-
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-137892
-
GSK620
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
|
-
- HY-12054A
-
-
- HY-12054
-
-
- HY-12072
-
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-B1452
-
Licofelone
ML-3000
|
COX
Lipoxygenase
Apoptosis
|
Cancer
Inflammation/Immunology
|
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
|
-
- HY-103706
-
ROC-325
|
Autophagy
Apoptosis
|
Cancer
|
ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
|
-
- HY-P1290
-
PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-101664
-
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-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-P1290A
-
PKA Inhibitor Fragment (6-22) amide TFA
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-14904A
-
Umifenovir hydrochloride
|
Influenza Virus
SARS-CoV
|
Infection
|
Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity.
|
-
- HY-12281
-
FPH2
BRD-9424
|
Others
|
Metabolic Disease
Cancer
|
FPH2 induces of functional proliferation of primary human hepatocytes and may lead to the development of new therapeutics for liver diseases.
|
-
- HY-B0798
-
-
- HY-106571
-
-
- HY-136270
-
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-15583
-
-
- HY-B1355A
-
-
- HY-12661A
-
AMG PERK 44
|
PERK
Autophagy
|
Cancer
|
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy.
|
-
- HY-19672
-
Lirimilast
BAY 19-8004
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties.
|
-
- HY-16759
-
Verubecestat
MK-8931
|
Beta-secretase
|
Neurological Disease
|
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
|
-
- HY-A0213A
-
Tiludronate disodium
Tiludronic Acid disodium
|
Proton Pump
|
Inflammation/Immunology
|
Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- 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-W014815
-
BPBA
2-Bromopyridine-5-boronic acid
|
Others
|
Others
|
BPBA (2-Bromopyridine-5-boronic acid) is a new labeling reagent to derivatize brassinosteroids (BRs).
|
-
- HY-15781A
-
Morinidazole (R enantiomer)
R-Morinidazole
|
Bacterial
|
Infection
|
Morinidazole R enantiomer is the R-enantiomer of Morinidazole. Morinidazole is a new 5-nitroimidazole class antimicrobial agent. Morinidazole R enantiomer is the less active enantiomer.
|
-
- HY-N8420
-
Thalifoline
|
Fungal
|
Infection
|
Thalifoline is an alkaloid isolated from the New Caledonian plant Cryptocarya longifolia and displays antifungal activity.
|
-
- HY-12384
-
Tenosal
|
Others
|
Inflammation/Immunology
|
Tenosal is a new compound obtained by esterifying salicylic acid with 2-thiophene-carboxylic acid and displays anti-inflammatory, analgesic and antipyretic properties.
|
-
- HY-15961
-
Antitumor agent-3
|
Others
|
Cancer
|
Antitumor agent-3 is a potent compound which comprises a new imidazopyridine having excellent antitumor activity as an active ingredient.
|
-
- HY-120295
-
A-192621
|
Endothelin Receptor
Apoptosis
|
Endocrinology
Cardiovascular Disease
|
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
|
-
- HY-100888
-
Simurosertib
TAK-931
|
CDK
|
Cancer
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.
|
-
- HY-14691
-
Refametinib
BAY 869766; RDEA119
|
MEK
|
Cancer
|
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
|
-
- HY-18010
-
PCI 29732
|
Btk
BCRP
|
Inflammation/Immunology
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
|
-
- HY-10913
-
-
- HY-10913A
-
-
- HY-15295
-
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-N0693
-
-
- 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-B1526
-
Thiacetazone
Thioacetazone; Amithiozone
|
Bacterial
|
Infection
|
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL.
|
-
- HY-18233
-
E1210
APX001A
|
Fungal
|
Infection
|
E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.
|
-
- HY-13503
-
-
- HY-126052
-
Gnetol
|
COX
Tyrosinase
HDAC
|
Cancer
Metabolic Disease
|
Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.
|
-
- HY-A0213B
-
Tiludronate disodium hemihydrate
Tiludronic acid disodium hemihydrate
|
Proton Pump
|
Metabolic Disease
|
Tiludronate (Tiludronic Acid) disodium hemihydrate, an orally active bisphosphonate, can act an osteoregulator. Tiludronate disodium hemihydrate is used for the research of the metabolic bone disorders. Tiludronate disodium hemihydrate is a potent inhibitor of the osteoclast vacuolar H +-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- 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 (P-CAB), 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-10716A
-
PF-03463275
|
GlyT
|
Neurological Disease
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
|
-
- HY-14953
-
Imepitoin
AWD 131-138
|
GABA Receptor
|
Neurological Disease
|
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
|
-
- HY-15481
-
-
- HY-N7125
-
Cinnamyl acetate
|
Others
|
Others
|
Cinnamyl acetate has a wide application in the flavor and fragrance industry. Cinnamyl acetate is a new broad spectrum antibacterial agent.
|
-
- HY-137551
-
Tiafenacil
|
Others
|
Others
|
Tiafenacil is a new protoporphyrinogen IX oxidase (PPO)-inhibiting herbicide, with IC50 values of 22 to 28 nM for various plant species, including amaranth (Amaranthus tuberculatus), soybean (Glycine max), arabidopsis (Arabidopsis thaliana), and rapeseed (Brassica napus).
|
-
- HY-W011651
-
-
- HY-10309
-
Sibrafiban
RO 48-3657
|
Integrin
|
Cardiovascular Disease
|
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.
|
-
- HY-100399
-
Nevanimibe
PD-132301; ATR-101
|
Acyltransferase
Apoptosis
|
Cancer
|
Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
|
-
- HY-100399A
-
Nevanimibe hydrochloride
PD-132301 hydrochloride; ATR101 hydrochloride
|
Acyltransferase
Apoptosis
|
Cancer
|
Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
|
-
- HY-19631B
-
Ilginatinib hydrochloride
NS-018 hydrochloride
|
JAK
|
Cancer
|
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-19631A
-
Ilginatinib
NS-018
|
JAK
|
Cancer
|
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-19631
-
Ilginatinib maleate
NS-018 maleate
|
JAK
|
Cancer
|
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-138294
-
RAS/RAS-RAF-IN-1
|
Ras
Raf
|
Cancer
|
RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.
|
-
- HY-121450
-
Lavoltidine
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
|
-
- HY-107676
-
SIB-1553A
|
nAChR
|
Neurological Disease
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-107426
-
Verrucarin A
Muconomycin A
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53.
|
-
- HY-18763
-
Indobufen
Ibustrin
|
COX
|
Cardiovascular Disease
|
Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.
|
-
- HY-N2221
-
-
- HY-N3733
-
Deoxylapachol
|
Fungal
|
Cancer
Infection
|
Deoxylapachol is a major cytotoxic component of New Zealand brown alga, Landsburgia quercifolia. Deoxylapachol has antifungal and anti-cancer activity.
|
-
- HY-16637
-
-
- HY-B0187A
-
Doripenem monohydrate
S 4661 monohydrate
|
Bacterial
Antibiotic
|
Infection
|
Doripenem monohydrate is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.
|
-
- HY-B0187
-
Doripenem
S 4661
|
Bacterial
Antibiotic
|
Infection
|
Doripenem is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.
|
-
- 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-106697
-
Statil
Ponalrestat
|
Aldose Reductase
|
Metabolic Disease
|
Statil (Ponalrestat) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Statil selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Statil inhibits the conversion of glucose to sorbitol.
|
-
- HY-13271
-
Tubastatin A Hydrochloride
Tubastatin A HCl; TSA HCl
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
Tubastatin A (Hydrochloride) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
|
-
- HY-N0607
-
-
- HY-14165
-
-
- HY-18342
-
Diflunisal
MK-647
|
COX
|
Inflammation/Immunology
Cancer
|
Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
|
-
- HY-131914A
-
-
- 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 .
|
-
- HY-N1447
-
-
- HY-N6962
-
α-Spinasterol
|
TRP Channel
COX
|
Infection
Neurological Disease
|
α-Spinasterol, isolated from Spinacia oleracea, has antibacterial activity. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.
|
-
- HY-102064
-
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-16694
-
BAMB-4
ITPKA-IN-C14
|
Others
|
Cancer
|
BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay.
|
-
- HY-18983
-
Calyculin A
(-)-Calyculin A
|
Phosphatase
|
Cancer
|
Calyculin A ((-)-Calyculin A) is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM, respectively.
|
-
- HY-10262
-
-
- HY-U00238
-
-
- HY-14674
-
CP-724714
|
EGFR
Apoptosis
|
Cancer
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
|
-
- HY-131907
-
LpxC-IN-5
|
Bacterial
|
Infection
|
LpxC-IN-5 is a potent non-hydroxamate LpxC (UDP-3-O-acyl-N-acetylglucosamine deacetylase) inhibitor with an IC50 of 20 nM. LpxC-IN-5 shows antibacterial activity against E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883 and P. aeruginosa 5567 with MIC of 16, 4, 64, and 4 μg/mL, respectively.
|
-
- HY-B1050
-
Gemifloxacin mesylate
SB-265805S; LB-20304a
|
Bacterial
|
Infection
|
Gemifloxacin mesylate is an oral broad-spectrum quinolone antibacterial agent, used in the treatment of acute bacterial exacerbation of chronic bronchitis, and mild-to-moderate pneumonia.
|
-
- HY-B1682
-
-
- HY-B1682A
-
-
- HY-15658
-
GSK2801
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.
|
-
- HY-136185
-
Atorvastatin Epoxy Tetrahydrofuran Impurity
|
Others
|
Others
|
Atorvastatin Epoxy Tetrahydrofuran Impurity is an impurity isolated oxidative degradation products of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-14262
-
Vilazodone
EMD 68843; SB659746A
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
|
-
- 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-B0422S
-
Nateglinide D5
A4166 D5; Senaglinide D5
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-12085
-
-
- HY-17493
-
MI-773
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction.
|
-
- HY-N0071
-
Crotonoside
Isoguanosine
|
FLT3
HDAC
|
Cancer
|
Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML.
|
-
- HY-N2150
-
Psammaplin A
|
HDAC
DNA Methyltransferase
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
|
-
- HY-B0395C
-
Sitafloxacin hydrate
DU6859a hydrate
|
Bacterial
Antibiotic
|
Infection
|
Sitafloxacin (DU6859a) hydrate is a potent, orally active fluoroquinolone antibiotic with in vitro activity against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection.
|
-
- HY-B0395
-
Sitafloxacin
DU6859a
|
Bacterial
Antibiotic
|
Infection
|
Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic with in vitro activity against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection.
|
-
- HY-129388B
-
LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
LSD1-IN-7 benzenesulfonate is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity extracted from patent WO2017079670A1, compound 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile.
|
-
- HY-108486
-
Herbimycin A
|
Bacterial
Antibiotic
|
Infection
|
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
|
-
- HY-10999A
-
Trametinib (DMSO solvate)
GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
|
MEK
Apoptosis
|
Cancer
|
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
|
-
- HY-14383
-
-
- HY-15681
-
-
- HY-10322
-
Falnidamol
BIBX 1382
|
EGFR
|
Cancer
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
|
-
- HY-136194
-
TL13-22
|
ALK
|
Cancer
|
TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
|
-
- HY-112852
-
TL02-59
|
Src
Apoptosis
|
Cancer
|
TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.
|
-
- 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-15670
-
BMS-906024
|
γ-secretase
Notch
|
Cancer
|
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
|
-
- HY-137742
-
SBP-7455
|
ULK
Autophagy
|
Cancer
|
SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research.
|
-
- HY-135299
-
CH6953755
|
Src
|
Cancer
|
CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.
|
-
- HY-16670
-
Dafadine-A
|
Cytochrome P450
|
Others
|
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
|
-
- HY-B1800
-
-
- HY-N0505
-
Rosiridin
|
Monoamine Oxidase
|
Neurological Disease
|
Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC50=5.38).
|
-
- HY-12501A
-
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-100014
-
KDM5A-IN-1
|
Histone Demethylase
|
Cancer
|
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
|
-
- HY-B1617A
-
-
- HY-13236
-
-
- HY-15178
-
Oglemilast
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
|
-
- HY-125916
-
Pseurotin A
|
Others
|
Cancer
|
Pseurotin A, a secondary metabolite of Aspergillus and other fungi, is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50=3.6 μM). Antitumor activity.
|
-
- HY-109019
-
Vorolanib
CM082; X-82
|
VEGFR
PDGFR
|
Cancer
Cardiovascular Disease
|
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
|
-
- HY-16929
-
Latrunculin A
LAT-A
|
Arp2/3 Complex
|
Others
|
Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively.
|
-
- HY-100560
-
Abscisic acid
(S)-(+)-Abscisic acid; ABA
|
Endogenous Metabolite
Proton Pump
|
Metabolic Disease
|
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome.
|
-
- HY-116090
-
Conoidin A
|
Parasite
|
Infection
Neurological Disease
Cardiovascular Disease
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII). Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
|
-
- HY-13254A
-
-
- HY-124330
-
Tripolin A
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
|
-
- HY-130841
-
Apcin-A
|
APC
Ligand for Target Protein for PROTAC
|
Cancer
|
Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor. Apcin-A interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V (HY-130257).
|
-
- HY-13331
-
Clascoterone
Cortexolone 17 alpha-propionate; Cortexolone 17α-propionate; CB-03-01
|
Androgen Receptor
|
Endocrinology
|
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
|
-
- HY-134463
-
NHWD-870
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
|
-
- HY-B0467S
-
Amoxicillin D4
Amoxycillin D4
|
Bacterial
|
Infection
|
Amoxicillin D4 (Amoxycillin D4) is a deuterium labeled Amoxicillin. Amoxicillin is an antibiotic with good oral absorption and broad spectrum antimicrobial activity.
|
-
- HY-N7225
-
Yuanhuacine
Gnidilatidin
|
Others
|
Cancer
|
Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active.
|
-
- HY-13271A
-
Tubastatin A
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
|
-
- HY-N2498
-
-
- HY-107531
-
A 1070722
|
GSK-3
|
Cancer
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
|
-
- HY-N0694
-
Schisantherin A
Gomisin-C; Schizantherin-A; Wuweizi ester-A
|
NF-κB
|
Inflammation/Immunology
|
Schisantherin A is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
|
-
- HY-100748
-
CXD101
|
HDAC
|
Cancer
|
CXD101 is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. CXD101 has no activity against HDAC class II. CXD101 has antitumor activity.
|
-
- HY-135401
-
VU6015929
|
Discoidin Domain Receptor
|
Inflammation/Immunology
|
VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.
|
-
- HY-126290
-
PF-06826647
|
JAK
|
Inflammation/Immunology
|
PF-06826647 is an orally active and selective TYK2 inhibitor (IC50=17 nM), which binds to TYK2 catalytically active JH1 domain. PF-06826647 displays selectivity for TYK2 over JAK1 (IC50=383 nM) and JAK2 (74 nM). PF-06826647 can be used for the research of psoriasis, ulcerative colitis, and hidradenitis suppurativa.
|
-
- HY-N6796
-
Manumycin A
|
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
|
Cancer
Infection
|
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity [2]. Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A is a nSMase inhibitor (EC50=0.25 μM).
|
-
- HY-N0466
-
-
- HY-13261
-
A66
|
PI3K
|
Cancer
|
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
|
-
- HY-129337
-
Reveromycin A
|
Antibiotic
Fungal
Apoptosis
|
Cancer
Infection
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
|
-
- HY-B1651
-
Iron(II) fumarate
Ferrous fumarate
|
Others
|
Metabolic Disease
|
Iron(II) fumarate (Ferrous fumarate) is the iron(II) salt of fumaric acid. Iron(II) fumarate is an orally active dietary supplement and has the potential for iron deficiency anemia treatment.
|
-
- HY-19947
-
PF-06291874
Glucagon receptor antagonists-4
|
Glucagon Receptor
|
Metabolic Disease
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM).
|
-
- HY-113974
-
trans-AUCB
t-AUCB
|
Epoxide Hydrolase
|
Cancer
|
trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.
|
-
- HY-114153A
-
PLX5622 hemifumarate
|
c-Fms
|
Neurological Disease
|
PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
|
-
- HY-12501
-
ITI-214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-N6773
-
Cytochalasin A
|
HIV Protease
Fungal
|
Infection
|
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives.
|
-
- HY-16699
-
Nexturastat A
|
HDAC
|
Cancer
|
Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.
|
-
- HY-N3417
-
Kongensin A
|
HSP
RIP kinase
Apoptosis
|
Cancer
Inflammation/Immunology
|
Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.
|
-
- HY-17387
-
(-)-Huperzine A
Huperzine A
|
AChE
Apoptosis
iGluR
|
Neurological Disease
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
|
-
- HY-10358
-
MK-2206 dihydrochloride
MK-2206 (2HCl)
|
Akt
Autophagy
Apoptosis
|
Cancer
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
|
-
- HY-110155A
-
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-122643
-
NITD-916
|
Bacterial
|
Infection
|
NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active and highly lipophilic mycobacterial enoyl reductase InhA inhibitor with an IC50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 has potent anti-tuberculosis effects.
|
-
- HY-14806
-
Teneligliptin
MP-513
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
|
-
- HY-17463
-
Prednisolone
|
Glucocorticoid Receptor
Endogenous Metabolite
|
Endocrinology
|
Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
|
-
- HY-100176
-
-
- HY-19376
-
NAMI-A
|
FAK
|
Cancer
|
NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.
|
-
- HY-N1505
-
-
- HY-114315
-
NQO1 substrate
|
Others
|
Cancer
|
NQO1 substrate acts as an efficient NQO1 substrate and may be a new option for the treatment of NQO1-overexpresssing drug-resistant NSCLC.
|
-
- HY-17452A
-
Cefditoren (Pivoxil)
Cefditoren pivoxyl; Cefditoren pivaloyloxymethyl ester; ME 1207
|
Bacterial
Antibiotic
|
Infection
|
Cefditoren pivoxil is a new-third generation cephalosporin antibiotic that has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including common respiratory and skin pathogens.
|
-
- HY-101903A
-
BMS-309403 sodium
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-101903
-
BMS-309403
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-111828
-
TTA-A2
|
Calcium Channel
|
Neurological Disease
|
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
|
-
- HY-103129
-
SB-200646A
|
5-HT Receptor
|
Neurological Disease
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
|
-
- HY-128849
-
Eprodisate
|
Others
|
Inflammation/Immunology
|
Eprodisate is a new compound designed to interfere with interactions between amyloidogenic proteins and glycosaminoglycans and thereby inhibit polymerization of amyloid fibrils and deposition of the fibrils in tissues.
Eprodisate slow the progression of AA amyloidosis-related renal disease and has possible applicability to other types of amyloidosis.
|
-
- HY-10529
-
-
- HY-103397
-
Nanaomycin A
|
DNA Methyltransferase
Parasite
|
Cancer
Infection
|
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
|
-
- HY-123823
-
Nitroaspirin
NCX 4016
|
COX
Apoptosis
|
Cancer
|
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
|
-
- HY-110096
-
-
- HY-126406
-
-
- HY-12047
-
Ponatinib
AP24534
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
|
-
- HY-15595A
-
360A iodide
360 A iodide
|
G-quadruplex
Telomerase
|
Cancer
|
360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
|
-
- HY-19725
-
-
- HY-N6584
-
-
- HY-12458
-
Pyrindamycin A
|
DNA/RNA Synthesis
|
Cancer
Infection
|
Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
|
-
- HY-N7557
-
-
- 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-N2392
-
-
- HY-N6687
-
Calcimycin
A-23187; Antibiotic A-23187
|
Bacterial
Fungal
Apoptosis
Autophagy
Antibiotic
|
Cancer
Infection
|
Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis.
|
-
- HY-B0856
-
Validamycin A
|
Fungal
Tyrosinase
|
Infection
|
Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A shows potent inhibitory activity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
|
-
- HY-17600S
-
Acalabrutinib D4
ACP-196 D4
|
Btk
|
Cancer
|
Acalabrutinib D4 (ACP-196 D4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor.
|
-
- HY-14454
-
TPh A
Triphenyl Compound A
|
Others
|
Cancer
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
|
-
- HY-15595
-
360A
|
G-quadruplex
Telomerase
|
Cancer
|
360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
|
-
- HY-16014
-
A-385358
|
Bcl-2 Family
|
Cancer
|
A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.
|
-
- HY-A0042
-
Rufinamide
CGP 33101; E 2080; RUF 331
|
Others
|
Neurological Disease
|
Rufinamide(E 2080; CGP 33101; RUF 331) is a new antiepileptic agent that differs structurally from other antiepileptic drugs and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS).
|
-
- HY-N6793
-
Phomopsin A
|
Microtubule/Tubulin
|
Cancer
|
Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis. Phomopsin A is a noncompetitive inhibitor of the binding of radiolabeled vincristine to tubulin.
|
-
- HY-A0122
-
-
- HY-12222
-
Obeticholic acid
INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid
|
FXR
Autophagy
|
Others
|
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
|
-
- HY-B1390B
-
-
- HY-N0465
-
Olaquindox
|
Antibiotic
Bacterial
|
Infection
|
Olaquindox, a quinoxalin derivative, is an orally active antibiotic. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets.
|
-
- HY-Y0272
-
-
- HY-136657
-
SC-43
|
Phosphatase
STAT
Apoptosis
|
Cancer
|
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
|
-
- HY-10619B
-
Niraparib tosylate
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-131343
-
HBV-IN-4
|
HBV
DNA/RNA Synthesis
|
Infection
|
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.
|
-
- HY-10614
-
A-966492
|
PARP
|
Cancer
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
|
-
- HY-N2300
-
-
- HY-123797
-
KGA-2727
|
SGLT
|
Metabolic Disease
|
KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy.
|
-
- HY-136195
-
TL13-110
|
ALK
|
Cancer
|
TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
|
-
- HY-100201
-
A-196
|
Histone Methyltransferase
|
Cancer
|
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.
|
-
- HY-118773
-
MreB Perturbing Compound A22 hydrochloride
A22 hydrochloride
|
Bacterial
|
Inflammation/Immunology
|
MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
|
-
- HY-N3389
-
-
- HY-107433
-
-
- HY-N7452
-
-
- HY-125824
-
-
- HY-B0561
-
-
- HY-111558A
-
Bobcat339 hydrochloride
|
DNA Methyltransferase
|
Cancer
|
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
-
- HY-121765
-
Dacisteine
N,S-Diacetyl-L-cysteine
|
Endogenous Metabolite
|
Metabolic Disease
|
Dacisteine (N,S-Diacetyl-L-cysteine) is a cysteine derivative and displays a less New Delhi metallo-beta-lactamase-1 (NDM-1) inhibitor with an IC50 value of 1000 μM. Dacisteine can be used for the treatment of cardiovascular and cerebrovascular diseases caused by platelet aggregation.
|
-
- HY-10450
-
Dapagliflozin
BMS-512148
|
SGLT
|
Metabolic Disease
Cancer
|
Dapagliflozin (BMS-512148), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine.
Dapagliflozin induces HIF1 expression and attenuates renal IR injury.
|
-
- HY-107833
-
A40926
|
Bacterial
|
Infection
|
A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae.
|
-
- HY-N6862
-
Lucideric acid A
|
MMP
|
Cancer
|
Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-135747
-
Gut restricted-7
GR-7
|
Bacterial
|
Infection
|
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice.
|
-
- HY-19544
-
JAK3-IN-1
|
JAK
|
Cancer
|
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
|
-
- HY-103258
-
TC ASK 10
|
MAP3K
Apoptosis
|
Cancer
|
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM).
|
-
- HY-110195
-
Smurf1-IN-A01
A01
|
Others
|
Others
|
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
|
-
- HY-113957
-
MPI_5a
|
HDAC
|
Cancer
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
|
-
- HY-110238
-
MK6-83
|
TRP Channel
|
Metabolic Disease
|
MK6-83 is a new candidate agonist of TRPML1 with an improved efficacy and potency. MK6-83 has the potential for Mucolipidosis type IV study.
|
-
- 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-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-N6702
-
-
- HY-130247
-
JAK2/FLT3-IN-1
|
JAK
FLT3
Apoptosis
|
Cancer
|
JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.
|
-
- HY-14682
-
GSK319347A
|
IKK
|
Inflammation/Immunology
|
GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
|
-
- HY-10619
-
Niraparib
MK-4827
|
PARP
Apoptosis
|
Cancer
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-10619A
-
Niraparib hydrochloride
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-125817
-
BI-3406
|
Ras
p38 MAPK
|
Cancer
|
BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.
|
-
- HY-13020
-
-
- HY-B1856
-
Haloxyfop
|
Others
|
Metabolic Disease
|
Haloxyfop is an aryloxyphenoxypropionic acid herbicide and is widely used in grass weeds in broad-leaf crops. Haloxyfop inhibits the acetyl coenzyme A carboxylase (EC 6.4.1.2) from corn seedling chloroplasts with an IC50 of 0.5 μM, but has no effect on this enzyme in pea.
|
-
- HY-137473
-
Methyl pyropheophorbide-a
Pyropheophorbide-a methyl ester
|
Apoptosis
|
Cancer
|
Methyl pyropheophorbide-a (Pyropheophorbide-a methyl ester), a chlorophyll-a derivative, is a potent photosensitizer that can be used in photodynamic therapy (PDT) of cancer. Methyl pyropheophorbide-a has photodynamic activity and can induce apoptosis and inhibit tumor growth.
|
-
- HY-17388
-
(±)-Huperzine A
|
AChE
|
Neurological Disease
|
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
|
-
- HY-N4185
-
-
- HY-10425
-
A-443654
|
Akt
|
Cancer
|
A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
|
-
- HY-101835
-
-
- HY-10847A
-
SB-277011 dihydrochloride
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-100599
-
-
- HY-N6017
-
Bakkenolide A
|
Others
|
Cancer
|
Bakkenolide A is a natural product extracted from Petasites tricholobus. Bakkenolide A inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways.
|
-
- HY-N0365
-
Sennoside A
|
HIV
|
Infection
|
Sennoside A is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside A is a HIV-1 inhibitor effective on HIV-1 replication.
|
-
- HY-122122
-
ML-60218
|
DNA/RNA Synthesis
|
Cancer
Infection
|
ML-60218 is a broad-spectrum RNA pol III inhibitor, with IC50s of 32 and 27 μM for Saccharomyces cerevisiae and human. ML-60218 disrupts already assembled viroplasms and to hamper the formation of new ones without the need for de novo transcription of cellular RNAs.
|
-
- HY-107427
-
PF-3644022
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
|
-
- HY-130208
-
Thiodigalactoside
TDG
|
Galectin
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats.
|
-
- HY-A0060
-
Malotilate
NKK 105
|
Lipoxygenase
|
Cancer
|
Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes.
|
-
- HY-119104
-
AZD1940
|
Cannabinoid Receptor
|
Neurological Disease
|
AZD1940 is an orally active, high affinity cannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action.
|
-
- HY-105755
-
Antimycin A3
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
Infection
|
Antimycin A3, an antibiotic isolated from a number of Streptomyces species, shows antifungal activities. Antimycin A3 is a potent inhibitor of respiration. Antimycin A3 inhibits the electron transfer activity of ubiquinol-cytochrome c oxidoreductase. Antimycin A3 inhibits ATP-citrate lyase with a Ki value of 60.1 µM.
|
-
- HY-100459
-
GSK3179106
|
RET
|
Metabolic Disease
Inflammation/Immunology
|
GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.
|
-
- HY-17361
-
Etofenamate
|
Others
|
Inflammation/Immunology
|
Etofenamate, a non-steroid anti-inflammatory drug (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases.
|
-
- HY-N4096
-
Tsugaric acid A
|
Others
|
Inflammation/Immunology
|
Tsugaric acid A can significantly inhibit superoxide anion formation. Tsugaric acid A also protects human keratinocytes against damage induced by ultraviolet B (UV B) light. Tsugaric acid A can protect keratinocytes from photodamage.
|
-
- HY-N3925
-
-
- HY-W013172
-
Norgestimate
|
Progesterone Receptor
|
Endocrinology
|
Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive.
|
-
- HY-136527
-
BMS-986251
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
|
-
- HY-16346
-
-
- HY-W040129
-
Chromomycin A3
|
Bacterial
Fungal
Antibiotic
|
Cancer
Infection
|
Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
|
-
- HY-114305
-
A1874
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
|
-
- HY-N2575
-
Hypocrellin A
|
PKC
|
Cancer
Infection
|
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT).
|
-
- HY-101945
-
A-69412
|
Lipoxygenase
|
Inflammation/Immunology
|
A-69412 is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
|
-
- HY-B2087
-
-
- HY-15405
-
Teriflunomide
A77 1726
|
Others
|
Inflammation/Immunology
|
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
|
-
- HY-B0698A
-
Ceftibuten dihydrate
Sch-39720 dihydrate
|
Bacterial
Antibiotic
|
Infection
|
Ceftibuten (Sch39720) dihydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens.
|
-
- HY-19642A
-
Glesatinib hydrochloride
MGCD265 hydrochloride
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
|
-
- HY-110155
-
LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-N2998
-
Ganoderenic acid A
|
Others
|
Metabolic Disease
|
Ganoderenic acid A is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid A is a potent inhibitor of β-glucuronidase. Ganoderenic acid A has a potent hepatoprotective effect against CCl4-induced liver injury.
|
-
- HY-13672
-
-
- HY-N2344
-
Procyanidin A1
Proanthocyanidin A1
|
PKC
|
Inflammation/Immunology
|
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
|
-
- HY-100558
-
Bafilomycin A1
|
Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
|
Cancer
Infection
|
Bafilomycin A1 is a specific inhibitor of vacuolar H +-ATPase (V-ATPase) with I50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.
|
-
- HY-11000
-
-
- HY-N5012
-
Eurycomanone
Pasakbumin A
|
Others
|
Endocrinology
|
Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
|
-
- HY-18944
-
FIT-039
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-P1687
-
Siomycin A
|
Bacterial
Apoptosis
|
Cancer
|
Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis.
|
-
- HY-116830
-
BRD0705
|
GSK-3
|
Cancer
|
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.
|
-
- HY-136447
-
ASP4132
|
AMPK
|
Cancer
|
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
|
-
- HY-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-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-107455
-
-
- HY-100433
-
PACMA 31
|
Others
|
Cancer
|
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues.
|
-
- HY-N6744
-
Chaetoglobosin A
|
Apoptosis
|
Cancer
Infection
|
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration.
|
-
- HY-101512
-
A-395
|
Histone Methyltransferase
|
Cancer
|
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
|
-
- HY-N6936
-
Sennidin A
|
HCV
Akt
GLUT
|
Infection
|
Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
|
-
- HY-10181A
-
Dasatinib hydrochloride
BMS-354825 hydrochloride
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
Dasatinib hydrochloride (BMS-354825 hydrochloride) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor, with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride has potent antitumor activity.
|
-
- HY-122610
-
VUT-MK142
|
Others
|
Cardiovascular Disease
|
VUT-MK142 is a potent new cardiomyogenic synthetic agent promoting the differentiation of pre-cardiac mesoderm into cardiomyocytes, which may be useful to differentiate stem cells into cardiomyocytes for cardiac repair.
|
-
- HY-N6073
-
Soyasapogenol A
|
Apoptosis
|
Inflammation/Immunology
|
Soyasapogenol A, a triterpene compound, isolated from the roots of Abrus cantoniensis. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
|
-
- HY-N7560
-
Safranal
|
Others
|
Inflammation/Immunology
Neurological Disease
|
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research.
|
-
- HY-105124A
-
-
- HY-105040C
-
Pomaglumetad methionil hydrochloride
LY2140023 hydrochloride
|
mGluR
|
Neurological Disease
|
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.
|
-
- HY-15779
-
K145
|
SPHK
Apoptosis
|
Cancer
|
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
|
-
- HY-15779A
-
K145 hydrochloride
|
SPHK
Apoptosis
|
Cancer
|
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
|
-
- HY-50880
-
-
- HY-18990
-
GSK180736A
|
ROCK
|
Cardiovascular Disease
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-10171
-
NPS-2143 hydrochloride
SB-262470A hydrochloride
|
CaSR
|
Metabolic Disease
|
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-10007
-
NPS-2143
SB-262470A
|
CaSR
|
Metabolic Disease
|
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-117832
-
-
- HY-12468
-
A-1210477
|
Bcl-2 Family
Apoptosis
|
Cancer
|
A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.
|
-
- HY-121750
-
CCG-222740
|
Ras
ROCK
|
Cancer
|
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
|
-
- HY-N6795
-
Leptomycin A
|
CRM1
HIV
|
Infection
|
Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
|
-
- HY-100540
-
Golgicide A
|
Enterovirus
|
Cancer
Infection
|
Golgicide A is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF), GBF1. Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
|
-
- HY-107416
-
RHC 80267
U-57908
|
Acyltransferase
mAChR
COX
Phospholipase
|
Metabolic Disease
Neurological Disease
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
|
-
- HY-104066
-
Theliatinib
HMPL-309
|
EGFR
|
Cancer
|
Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
|
-
- HY-100017
-
BAY-876
|
GLUT
|
Cancer
|
BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
|
-
- HY-15652
-
Freselestat
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
|
-
- HY-N1483
-
Guanfu base A
|
Potassium Channel
|
Cardiovascular Disease
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.
|
-
- HY-13001
-
Quizartinib
AC220
|
FLT3
Ligand for Target Protein for PROTAC
Apoptosis
Autophagy
|
Cancer
|
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
|
-
- HY-137563
-
A2793
|
Potassium Channel
|
Neurological Disease
|
A2793 is an efficient dual TWIK-related acid-sensitive K + channel (TASK)-1/TRESK inhibitor, with an IC50 of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1.
|
-
- HY-15764A
-
A 419259 trihydrochloride
RK 20449 trihydrochloride
|
Src
|
Cancer
|
A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.
|
-
- HY-120160
-
Darglitazone
CP-86325
|
PPAR
|
Metabolic Disease
Neurological Disease
|
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
|
-
- HY-14554
-
-
- HY-B1271
-
Sulfinpyrazone
G-28315
|
Others
|
Inflammation/Immunology
|
Sulfinpyrazone (G-28315) is an orally active and potent uricosuric agent for chronic and intermittent gouty arthritis. Sulfinpyrazone has antithrombotic and platelet inhibitory effects.
|
-
- HY-131059
-
CBS1117
|
Influenza Virus
|
Infection
|
CBS1117 is a virus entry inhibitor with an IC50 of 70 nM for influenza A virus, A/Puerto Rico/8/34 (H1N1). CBS1117 interferes with the hemagglutinin (HA)-mediated fusion process.
|
-
- HY-119257
-
ABT-100
|
Farnesyl Transferase
Apoptosis
|
Cancer
|
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity.
|
-
- HY-P0018
-
Pepstatin
Pepstatin A
|
Proteasome
HIV Protease
Autophagy
|
Infection
Cancer
|
Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-136532
-
ZT-1a
|
Others
|
Neurological Disease
|
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.
|
-
- HY-P0018A
-
Pepstatin Trifluoroacetate
Pepstatin A Trifluoroacetate
|
Proteasome
HIV Protease
|
Infection
|
Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-N2112
-
Glaucocalyxin A
|
PI3K
Akt
Apoptosis
|
Cancer
|
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
|
-
- HY-12583
-
A-366
|
Histone Methyltransferase
Epigenetic Reader Domain
|
Cancer
|
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
|
-
- HY-111458
-
-
- HY-100368A
-
-
- HY-100522
-
FMK 9a
|
Autophagy
|
Cancer
|
FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
|
-
- HY-N2638
-
Ilexsaponin A
|
Others
|
Cardiovascular Disease
|
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes.
|
-
- HY-N2306A
-
Aclacinomycin A hydrochloride
Aclarubicin hydrochloride
|
Proteasome
Topoisomerase
|
Cancer
|
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.
|
-
- HY-14164
-
-
- HY-N3029
-
Noreugenin
|
Others
|
Others
|
Noreugenin, 5,7-dihydroxy-2-methyl-4H-chromen-4-one, is a new chromone from Hymenocallis littoralis Salisb. (Amaryllidaceae).
|
-
- HY-N7043
-
Isosilybin A
|
Apoptosis
|
Cancer
|
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
|
-
- HY-N2298
-
Camellianin A
|
Apoptosis
|
Cancer
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population.
|
-
- HY-15614A
-
SC144 hydrochloride
|
Interleukin Related
Apoptosis
|
Cancer
|
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
|
-
- HY-15614
-
SC144
|
Interleukin Related
Apoptosis
|
Cancer
|
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
|
-
- HY-16992A
-
W-54011
|
Complement System
Reactive Oxygen Species
|
Inflammation/Immunology
|
W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
|
-
- HY-101143
-
-
- HY-136895
-
AZ12672857
|
Prostaglandin Receptor
|
Cancer
|
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).
|
-
- HY-18009
-
LFM-A13
|
Btk
Polo-like Kinase (PLK)
JAK
|
Cancer
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
|
-
- HY-B0976A
-
Fenoterol hydrobromide
Th-1165a; Phenoterol hydrobromide
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.
|
-
- HY-135891
-
AZD2423
|
CCR
|
Neurological Disease
|
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux [1].
|
-
- HY-15144
-
Trichostatin A
TSA
|
HDAC
|
Cancer
|
Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
|
-
- HY-101870B
-
INCB053914 phosphate
|
Pim
|
Cancer
|
INCB053914 phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. INCB053914 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
|
-
- HY-101402
-
Cyclo(his-pro)
Cyclo(histidyl-proline); Histidylproline diketopiperazine
|
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
|
-
- HY-136360
-
MI-3454
|
Epigenetic Reader Domain
|
Cancer
|
MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis.
|
-
- HY-14164A
-
-
- HY-N5025
-
Bullatine A
|
P2X Receptor
Apoptosis
|
Cancer
Inflammation/Immunology
|
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
|
-
- HY-B0024
-
Prulifloxacin
NM441
|
Bacterial
Antibiotic
|
Infection
|
Prulifloxacin (NM441) is an orally active fluoroquinolone antibiotic with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is a prodrug of a thiazeto-quinoline carboxylic acid derivative Ulifloxacin (NM394). Prulifloxacin has the potential for lower urinary tract infections and exacerbations of chronic bronchitis.
|
-
- HY-100681
-
-
- HY-13775
-
XL019
|
JAK
Apoptosis
|
Cancer
|
XL019 is a potent,orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
|
-
- HY-W027951
-
N,N'-Dimethylthiourea
DMTU
|
Others
|
Inflammation/Immunology
|
N,N'-Dimethylthiourea (DMTU), isolated from Allii Sativi Bulbus, is an orally active scavenger of hydroxyl radical (•OH) and blocks •OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including •OH scavenging and anti-inflammatory action.
|
-
- HY-120118
-
Metarrestin
ML246
|
DNA/RNA Synthesis
|
Cancer
|
Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
|
-
- HY-15196
-
TAK-285
|
EGFR
|
Cancer
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
|
-
- HY-15652A
-
Freselestat quarterhydrate
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.
|
-
- HY-128553
-
-
- HY-118189
-
Misoprostol acid
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers. Misoprostol is an oral agent used to induce labor.
|
-
- HY-17507
-
Pantoprazole
BY1023; SKF96022
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-17507B
-
Pantoprazole sodium hydrate
BY1023 sodium hydrate; SKF96022 sodium hydrate
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-17507A
-
Pantoprazole sodium
BY1023 sodium; SKF96022 sodium
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-136789
-
BDTX-189
|
EGFR
|
Cancer
|
BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
|
-
- HY-116000
-
Glumetinib
SCC244
|
c-Met/HGFR
|
Cancer
|
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity.
|
-
- HY-100611
-
-
- HY-N7148
-
γ-Tocopherol
D-γ-Tocopherol; (+)-γ-Tocopherol
|
COX
|
Cancer
Inflammation/Immunology
|
γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity.
|
-
- HY-107725
-
BIBO3304 TFA
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively).
|
-
- HY-14347
-
EBE-A22
|
Others
|
Cancer
|
EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
|
-
- HY-15010
-
L-371,257
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
|
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
|
-
- HY-N2959
-
Brevilin A
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
|
-
- HY-10029
-
Nutlin-3a
|
MDM-2/p53
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
Nutlin-3a, an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
|
-
- HY-12324
-
SB269652
|
Dopamine Receptor
|
Neurological Disease
|
SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
|
-
- 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-17368
-
Rivastigmine
S-Rivastigmine
|
AChE
|
Neurological Disease
|
Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-B0758
-
Troxipide
|
Others
|
Inflammation/Immunology
|
Troxipide is an orally active defensive factor-enhancing therapeutic agent for gastritis and gastric ulcer (GU). Troxipide is a non-antisecretory gastro protective agent with antiulcer, anti-inflammatory and mucus-secreting properties.
|
-
- HY-15005C
-
Sofosbuvir impurity A
|
HCV
|
Infection
|
Sofosbuvir impurity A, an diastereoisomer of Sofosbuvir, is the impurity of Sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
|
-
- HY-78349
-
A 77-01
|
TGF-β Receptor
|
Cancer
|
A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
|
-
- HY-15613
-
Maritoclax
Marinopyrrole A
|
Bcl-2 Family
|
Cancer
|
Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
|
-
- HY-Y0189
-
Methyl Salicylate
Wintergreen oil
|
COX
|
Inflammation/Immunology
|
Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products. A systemic acquired resistance (SAR) signal in tobacco. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor.
|
-
- HY-12168
-
Tanomastat
BAY 12-9566
|
MMP
|
Cancer
|
Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.
|
-
- HY-133127A
-
-
- HY-100528
-
Nanchangmycin
Nanchangmycin A
|
Bacterial
Antibiotic
|
Infection
|
Nanchangmycin, a polyether antibiotic produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
|
-
- HY-13746B
-
-
- HY-123812
-
-
- HY-101402A
-
Cyclo(his-pro) TFA
Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA
|
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
|
-
- HY-14771A
-
-
- HY-137478A
-
KB-0742 dihydrochloride
|
CDK
|
Cancer
|
KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
|
-
- HY-13237
-
-
- HY-100183
-
-
- HY-14247
-
-
- HY-100118
-
-
- HY-120994B
-
Sp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.
|
-
- HY-120994A
-
Rp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.
|
-
- HY-120994
-
-
- HY-135809
-
A2764 dihydrochloride
|
Potassium Channel
|
Neurological Disease
|
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.
|
-
- HY-14362
-
GSK-25
|
ROCK
Ribosomal S6 Kinase (RSK)
|
Cardiovascular Disease
|
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).
|
-
- HY-108254
-
Bisindolylmaleimide IV
Arcyriarubin A
|
PKC
CMV
|
Infection
|
Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
|
-
- HY-112468
-
PNU112455A hydrochloride
|
CDK
|
Cancer
|
PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
|
-
- HY-12521
-
GSK-5498A
|
CRAC Channel
|
Inflammation/Immunology
|
GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
|
-
- HY-100641
-
-
- HY-114936
-
Piericidin A
AR-054
|
Bacterial
ADC Cytotoxin
Antibiotic
|
Cancer
Infection
Neurological Disease
|
Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity.
|
-
- HY-B1599
-
Chloramphenicol palmitate
|
Bacterial
|
Infection
|
Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes.
|
-
- HY-13302
-
CP-547632
|
VEGFR
FGFR
|
Cancer
|
CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
|
-
- HY-13302B
-
CP-547632 hydrochloride
|
VEGFR
FGFR
|
Cancer
|
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
|
-
- HY-N6601
-
Pomolic acid
Randialic acid A
|
Apoptosis
|
Cancer
|
Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
|
-
- HY-103565
-
AMN082
|
mGluR
|
Neurological Disease
|
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
|
-
- HY-12422
-
Voruciclib
|
CDK
|
Cancer
|
Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
|
-
- HY-12422A
-
Voruciclib hydrochloride
|
CDK
|
Cancer
|
Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
|
-
- HY-W020468
-
Linopirdine
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
|
-
- HY-133807
-
Benpyrine
|
TNF Receptor
|
Inflammation/Immunology
|
Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
|
-
- HY-108024A
-
Ganaplacide hydrochloride
KAF156 hydrochloride; GNF156 hydrochloride
|
Parasite
|
Infection
|
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
|
-
- HY-13036A
-
IBT6A
|
Btk
|
Cancer
|
IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
|
-
- HY-19794
-
MP-A08
|
SPHK
|
Cancer
|
MP-A08 is a highly selective ATP competitive sphingosine kinase (SPHK1) inhibitor that targets both SphK1 and SphK2 with Ki values of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.
|
-
- HY-13036B
-
IBT6A hydrochloride
|
Btk
|
Cancer
|
IBT6A hydrochloride is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
|
-
- HY-A0150
-
Alclometasone
7a-Chloro-16a-methyl prednisolone
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis.
|
-
- HY-100228A
-
-
- HY-N2059
-
Santalol
|
Others
|
Cancer
|
Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer.
|
-
- HY-N6687B
-
Calcimycin hemimagnesium
A-23187 hemimagnesium; Antibiotic A-23187 hemimagnesium
|
Bacterial
Fungal
Apoptosis
Autophagy
|
Cancer
Infection
|
Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemimagnesium induces apoptosis.
|
-
- HY-N6687A
-
Calcimycin hemicalcium salt
A-23187 hemicalcium salt; Antibiotic A-23187 hemicalcium salt
|
Bacterial
Fungal
Apoptosis
Autophagy
Antibiotic
|
Cancer
Infection
|
Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemicalcium salt induces apoptosis.
|
-
- HY-B1202A
-
-
- HY-13339
-
-
- HY-B0093A
-
-
- HY-104064
-
1A-116
|
Ras
|
Cancer
|
1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer. 1A-116 prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes [2].
|
-
- HY-15724A
-
Vercirnon sodium
GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium
|
CCR
|
Inflammation/Immunology
Endocrinology
|
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-15724
-
Vercirnon
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-107798
-
Potassium guaiacolsulfonate hemihydrate
|
Bacterial
|
Infection
|
Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other drugs.
|
-
- HY-U00235
-
SR121566A
|
Integrin
|
Inflammation/Immunology
|
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
|
-
- HY-A0279
-
Pristinamycin
Pristinamycine
|
Bacterial
|
Infection
|
Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA) and Enterococcus faecium (VREF).
|
-
- HY-N0931
-
Santacruzamate A
CAY-10683
|
HDAC
|
Cancer
|
Santacruzamate A (CAY-10683) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM.
|
-
- HY-100790
-
Ciliobrevin A
HPI-4
|
Hedgehog
|
Cancer
|
Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
|
-
- 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-10432A
-
A 83-01 sodium salt
|
TGF-β Receptor
ALK
|
Cancer
|
A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-11017
-
Rivastigmine tartrate
ENA 713; SDZ-ENA 713
|
AChE
|
Neurological Disease
|
Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-P1184
-
-
- HY-15790
-
Elobixibat
A 3309; AZD 7806
|
Others
|
Metabolic Disease
|
Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
|
-
- HY-100087
-
-
- HY-19617B
-
EGFR-IN-1 TFA
|
EGFR
|
Cancer
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-109083
-
Cilofexor
GS-9674
|
FXR
Autophagy
|
Inflammation/Immunology
|
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
|
-
- HY-118189S
-
Misoprostol acid D5
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
Misoprostol acid D5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers. Misoprostol is an oral agent used to induce labor.
|
-
- HY-10442
-
-
- HY-13302C
-
CP-547632 TFA
|
VEGFR
FGFR
|
Cancer
|
CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy.
|
-
- HY-100431A
-
IMR-1A
|
Notch
Drug Metabolite
|
Cancer
|
IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitors with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.
|
-
- HY-B0220E
-
Erythromycin A dihydrate
|
Bacterial
Antibiotic
|
Infection
|
Erythromycin dihyrate dihydrate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin dihyrate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid.
|
-
- HY-109785A
-
(R)-Gyramide A hydrochloride
|
|
Infection
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-12843
-
Bohemine
|
CDK
ERK
|
Cancer
|
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.
|
-
- HY-18299A
-
Purvalanol A
NG-60
|
CDK
Autophagy
Apoptosis
|
Cancer
|
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
|
-
- HY-16576
-
TCS-PIM-1-4a
SMI-4a
|
Pim
Apoptosis
|
Cancer
|
TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).
|
-
- HY-B1395
-
Mecamylamine hydrochloride
|
nAChR
|
Neurological Disease
|
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier.
|
-
- HY-N7613
-
-
- HY-117015
-
Purfalcamine
|
Parasite
|
Infection
|
Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage.
|
-
- HY-19838
-
JNJ-63533054
|
GPR139
|
Neurological Disease
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
|
-
- HY-B0597
-
-
- HY-10432
-
A 83-01
|
ALK
TGF-β Receptor
|
Cancer
|
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-109176
-
Giredestrant
GDC-9545
|
Estrogen Receptor/ERR
|
Cancer
|
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
|
-
- HY-B0723S
-
Ospemifene D4
FC-1271a D4
|
Estrogen Receptor/ERR
|
Cancer
|
Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
|
-
- HY-10409
-
Fedratinib
TG-101348; SAR 302503
|
JAK
Apoptosis
|
Cancer
|
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
|
-
- HY-10409A
-
Fedratinib hydrochloride hydrate
TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
|
JAK
Apoptosis
|
Cancer
|
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
|
-
- HY-N6704
-
Enniatin A1
|
ERK
Apoptosis
|
Cancer
|
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
|
-
- HY-13716
-
Noscapine
(S,R)-Noscapine
|
Opioid Receptor
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.
|
-
- HY-13716A
-
Noscapine hydrochloride
(S,R)-Noscapine hydrochloride
|
Opioid Receptor
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Noscapine hydrochloride ((S,R)-Noscapine hydrochloride) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
|
-
- HY-19896
-
COTI-2
|
MDM-2/p53
Apoptosis
|
Cancer
|
COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.
|
-
- HY-131909
-
CJ-2360
|
ALK
|
Cancer
|
CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated.
|
-
- HY-109592
-
-
- HY-14929A
-
Migalastat hydrochloride
GR181413A
|
Others
|
Others
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- 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-14595
-
Biochanin A
4-Methylgenistein; Olmelin
|
FAAH
Autophagy
|
Neurological Disease
Cancer
|
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
|
-
- HY-18662
-
RQ-00203078
|
TRP Channel
|
Cancer
Neurological Disease
|
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.
|
-
- HY-B0579
-
-
- HY-128553A
-
(Rac)-Antineoplaston A10
|
Ras
Apoptosis
|
Cancer
|
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
|
-
- HY-N0853
-
-
- 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-N3557
-
Cauloside A
Leontoside A
|
Fungal
|
Infection
|
Cauloside A (Leontoside A) is a saponin isolated from Dipsacus asper roots. Cauloside A has potent antifungal activity.
|
-
- HY-N0372
-
Licochalcone A
Licochalcone-A
|
Autophagy
|
Cancer
|
Licochalcone A, a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch, presents obvious anti-cancer effects.
|
-
- HY-N0873
-
Sagittatoside A
Icariin-A
|
Others
|
Others
|
Sagittatoside A is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii).
|
-
- HY-P0216
-
-
- HY-15488
-
-
- HY-N1924
-
Crassicauline A
Crassicaulin A
|
Others
|
Neurological Disease
|
Crassicauline A (Crassicaulin A) is a bioactive alkaloid found in roots of Aconitum carmichaeli. Crassicauline A (Crassicaulin A) possesses feeding deterrent activity against T. castaneum adults with an EC50 of 1134.5 ppm.
|
-
- HY-107633
-
A 1120
|
Others
|
Metabolic Disease
|
A 1120 is a high-affinity nonretinoid retinol-binding protein 4 (RBP4) antagonist with a Ki value of 8.3 nM. A 1120 disrupts the interaction between RBP4 and its binding partner transthyretin.
|
-
- HY-15488A
-
-
- HY-14604
-
Xaliproden hydrochloride
SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases.
|
-
- 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-10847B
-
SB-277011 hydrochloride
SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-111360
-
SPL-707
|
γ-secretase
|
Inflammation/Immunology
|
SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
|
-
- HY-10583
-
Y-27632 dihydrochloride
|
ROCK
Apoptosis
|
Cancer
|
Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
|
-
- HY-16677A
-
-
- HY-N0134
-
-
- HY-W002585
-
O6-Benzylguanine
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.
|
-
- 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-15858A
-
AP-III-a4 hydrochloride
ENOblock hydrochloride
|
Enolase
|
Cancer
|
AP-III-a4 hydrochloride (ENOblock hydrochloride) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
|
-
- HY-B2087S
-
-
- HY-19915
-
-
- HY-B2087S1
-
-
- HY-108411
-
Emedastine
|
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
|
-
- HY-N0304
-
L-DOPA
Levodopa; 3,4-Dihydroxyphenylalanine
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
|
-
- HY-14325A
-
L-745870 trihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
|
-
- HY-N2278
-
Kushenol A
Leachianone E
|
Tyrosinase
Glucosidase
|
Cancer
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
|
-
- HY-114245
-
Se-Methylselenocysteine
Methylselenocysteine; Se-Methylseleno-L-cysteine
|
Apoptosis
|
Cancer
|
Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis.
|
-
- HY-15550
-
-
- HY-106101
-
Echinomycin
Quinomycin A; NSC-13502
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
|
-
- 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-100115
-
-
- HY-129239
-
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
|
-
- HY-124729
-
BL-918
|
ULK
Autophagy
|
Neurological Disease
|
BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
|
-
- HY-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-135731
-
4-Methylamino antipyrine
|
COX
Drug Metabolite
|
Inflammation/Immunology
|
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.
|
-
- HY-135731A
-
4-Methylamino antipyrine hydrochloride
|
COX
Drug Metabolite
|
Inflammation/Immunology
|
4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties.
|
-
- HY-121149
-
Droloxifene
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats [1].
|
-
- HY-B2178
-
Emedastine difumarate
|
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
|
-
- HY-111174
-
-
- HY-10274
-
Dabigatran etexilate
BIBR 1048
|
Others
|
Cardiovascular Disease
|
Dabigatran etexilate (BIBR 1048) is an orally active prodrug of Dabigatran. Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
|
-
- HY-14137
-
-
- HY-111388A
-
SEL120-34A monohydrochloride
|
CDK
|
Cancer
|
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
|
-
- HY-103309
-
ML218
|
Calcium Channel
|
Neurological Disease
|
ML218 is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
|
-
- HY-17600
-
Acalabrutinib
ACP-196
|
Btk
|
Cancer
|
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
|
-
- HY-103128
-
-
- HY-P0018B
-
Pepstatin Ammonium
Pepstatin A Ammonium
|
Proteasome
HIV Protease
|
Cancer
Infection
|
Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-10181
-
Dasatinib
BMS-354825
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
Dasatinib (BMS-354825) is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC50s of 0.6 nM, 0.8 nM, respectively. Dasatinib also inhibits Abl, Src, Fyn, c-Kit and c-Kit D816V with IC50s of 2.8 nM, 79 nM and 37 nM, respectively. Dasatinib also induces apoptosis and autophagy. Dasatinib shows potently antitumor activity and has the potential for chronic myelogenous leukemia (CML) treatment.
|
-
- HY-19336
-
BAZ2-ICR
|
Epigenetic Reader Domain
|
Cancer
|
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
|
-
- HY-100612
-
T16Ainh-A01
|
Chloride Channel
|
Others
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-107623
-
TC-MCH 7c
|
MCHR1 (GPR24)
|
Metabolic Disease
|
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
|
-
- HY-130120
-
HWL-088
|
GPR40
PPAR
|
Metabolic Disease
|
HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
|
-
- HY-10274A
-
Dabigatran etexilate mesylate
BIBR 1048MS; Dabigatran etexilate methanesulfonate
|
Others
|
Cardiovascular Disease
|
Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
|
-
- HY-N7394A
-
(-)-Zuonin A
D-Epigalbacin
|
JNK
|
Cancer
|
(-)-Zuonin A (D-Epigalbacin), a naturally occurring lignin, is a potent, selective JNKs inhibitor, with IC50s of 1.7 μM, 2.9 μM and 1.74 μM for JNK1, JNK2 and JNK3, respectively.
|
-
- HY-80012
-
SJB3-019A
|
Deubiquitinase
|
Cancer
|
SJB3-019A is a potent and novel USP1 inhibitor, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.
|
-
- HY-136207
-
TC-2559 difumarate
|
nAChR
|
Neurological Disease
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
|
-
- HY-W008091
-
5-Methylcytosine
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Others
|
5-Methylcytosine is a well-characterized DNA modification, and is also predominantly in abundant non-coding RNAs in both prokaryotes and eukaryotes. 5-Methylcytosine in mRNA is a new epitranscriptome marker inArabidopsis, and that regulation of this modification is an integral part of gene regulatory networks underlying plant development.
|
-
- HY-112205A
-
RR-11a analog
|
Parasite
|
Infection
|
RR-11a analog is a potent and selective inhibitors of asparaginyl endopeptidases (AE) (Legumain), with IC50 values of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.
|
-
- HY-50877
-
-
- HY-18963
-
Lavendustin A
RG-14355
|
EGFR
|
Cancer
|
Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A.
|
-
- HY-13801
-
Fexinidazole
HOE 239
|
Parasite
|
Infection
|
Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal drug. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.
|
-
- HY-117391
-
-
- HY-129974
-
-
- HY-131061
-
BET bromodomain inhibitor 1
|
Epigenetic Reader Domain
|
Cancer
|
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
|
-
- HY-112569
-
-
- HY-13235
-
-
- HY-122909
-
-
- HY-13470
-
-
- HY-107018
-
AR-A 2
AR-A 000002
|
5-HT Receptor
|
Neurological Disease
|
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
|
-
- 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-13036
-
(Rac)-IBT6A
|
Btk
|
Cancer
|
(Rac)-IBT6A is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
|
-
- HY-106067A
-
-
- HY-U00387
-
-
- HY-14803
-
Tasimelteon
BMS-214778; VEC-162
|
Melatonin Receptor
|
Neurological Disease
Endocrinology
|
Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24).
|
-
- 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-106420
-
-
- HY-105189
-
Meclinertant
SR 48692
|
Neurotensin Receptor
|
Neurological Disease
|
Meclinertant (SR 48692) is a potent, selective, nonpeptide and orally active neurotensin receptor 1 (NTS1) antagonist. In human colon carcinoma (HT-29) cells, Meclinertant competitively antagonizes neurotensin-induced intracellular Ca 2+ mobilization with a pA2 values of 8.13. Meclinertant has anxiolytic, anti-addictive and memory-impairing effects.
|
-
- HY-N0204
-
Pulchinenoside A
Anemoside A3
|
Others
|
Others
|
Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.
|
-
- HY-N0476
-
Wilforlide A
Regelide; Abruslactone A
|
Others
|
Inflammation/Immunology
|
Wilforlide A is a bioactive triterpene isolated from Tripterygium wilfordii Hook f. Wilforlide A has anti-inflammatory and immune suppressive effects.
|
-
- HY-N0123
-
Aloin
Aloin-A; Barbaloin-A
|
Others
|
Cancer
|
Aloin(Aloin-A; Barbaloin-A) is a natural antitumor anthraquinone glycoside with iron chelating and non-atherogenic activities.
|
-
- HY-N2995
-
Poricoic acid A
Poricoic acid A(F)
|
Others
|
Cancer
|
Poricoic acid A, isolated from Poria cocos, possesses anti-tumor activity. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis.
|
-
- HY-78727
-
-
- HY-19828
-
Herboxidiene
GEX1A
|
DNA/RNA Synthesis
|
Cancer
|
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
|
-
- HY-P1184A
-
-
- HY-13863
-
Hydroxy-Dynasore
Dyngo-4a
|
Dynamin
|
Neurological Disease
|
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
|
-
- HY-15604
-
-
- HY-N0565
-
-
- HY-107986
-
-
- HY-N0565A
-
-
- HY-14184
-
-
- HY-15403
-
-
- HY-15403A
-
-
- HY-13646A
-
-
- HY-13646
-
-
- HY-19357
-
E3330
APX-3330
|
DNA/RNA Synthesis
|
Cancer
|
E3330 (APX-3330) is a direct, orally active and selective AP endonuclease 1 (APE1; REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration.
|
-
- HY-15701B
-
ADH-503
(Z)-Leukadherin-1 choline
|
Complement System
|
Cancer
|
ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-70044
-
GSK-1070916
GSK-1070916A
|
Aurora Kinase
Apoptosis
|
Cancer
|
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
|
-
- HY-101682
-
SCH 42495
|
Neprilysin
|
Cardiovascular Disease
|
SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
|
-
- HY-112131
-
-
- HY-120536
-
HPi1
|
Bacterial
|
Infection
|
HPi1 is a potent, selective and orally active antimicrobial against Helicobacter pylori with an IC50 of 0.24 μM and an MIC of 0.08-0.16 μg/mL. HPi1 is inactive against other bacteria, including the gut commensals Lactobacillus casei, Lactobacillus reuteri, and Bifidobacterium longum.
|
-
- HY-B0381B
-
-
- HY-130187
-
Sapienic acid
|
Bacterial
|
Infection
|
Sapienic acid is a fatty acid commonly found on the skin and in mucosa. Sapienic acid has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively.
|
-
- HY-16500
-
-
- HY-111485
-
-
- HY-15701A
-
(Z)-Leukadherin-1
ADH-503 free base
|
Complement System
|
Cancer
|
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-15881
-
TCS JNK 5a
JNK Inhibitor IX
|
JNK
Apoptosis
|
Cancer
|
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
|
-
- HY-18663B
-
CP-465022 hydrochloride
|
iGluR
|
Neurological Disease
|
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.
|
-
- HY-B0731A
-
Perospirone
SM-9018 free base
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
|
-
- HY-108260
-
Deferitrin
GT-56-252
|
Others
|
Cardiovascular Disease
|
Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major.
|
-
- HY-13580
-
Budesonide
|
Glucocorticoid Receptor
|
Cancer
Inflammation/Immunology
|
Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
|
-
- HY-100600
-
BGG463
K03859
|
CDK
|
Others
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-116594A
-
-
- HY-N0853A
-
-
- HY-120878
-
CXCR2-IN-2
|
CXCR
|
Inflammation/Immunology
|
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
|
-
- HY-100830
-
-
- HY-17630
-
-
- HY-B0492
-
-
- HY-B0492A
-
-
- HY-17448
-
-
- HY-N0875
-
-
- HY-U00185
-
-
- HY-N5120
-
Dihydrowithaferin A
2,3-Dihydrowithaferin A
|
AChE
|
Cancer
|
Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE).
|
-
- HY-N0567
-
-
- HY-136466
-
A2ti-2
|
Virus Protease
|
Infection
|
A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-136465
-
A2ti-1
|
Virus Protease
|
Infection
|
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-19620
-
Branaplam
LMI070; NVS-SM1
|
DNA/RNA Synthesis
Potassium Channel
|
Cancer
|
Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
|
-
- HY-100507
-
Avadomide
CC 122
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
Inflammation/Immunology
|
Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
|
-
- HY-N0565B
-
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
Antibiotic
MMP
Bacterial
|
Infection
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-14174
-
-
- HY-111493
-
-
- HY-130609A
-
Aβ42-IN-1 free base
|
γ-secretase
|
Neurological Disease
|
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
|
-
- HY-122218
-
JHU-083
|
Glutaminase
|
Neurological Disease
|
JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b + cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
|
-
- HY-130187A
-
Sapienic acid sodium
|
Bacterial
|
Infection
|
Sapienic acid sodium is a fatty acid commonly found on the skin and in mucosa. Sapienic acid sodium has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid sodium is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively.
|
-
- HY-P1333
-
Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-N2025
-
Oroxin A
|
PARP
Glucosidase
|
Metabolic Disease
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE), activates peroxisome proliferator-activated receptor γ (PPARγ) by docking into the PPARγ protein ligand-binding domain. Oroxin A exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
|
-
- HY-N2420
-
Flavokawain A
|
Apoptosis
|
Cancer
|
Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
|
-
- HY-N7496
-
Odoroside A
|
Apoptosis
|
Cancer
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-N0239
-
-
- HY-N3051
-
-
- HY-50697
-
-
- HY-130993
-
Isatropolone A
|
Parasite
|
Infection
|
Isatropolone A, a natural product containing a 1,5-diketone moiety, is reisolated from Streptomyces Gö66. Isatropolone A shows potent activity against Leishmania donovani with an IC50 of 0.5 μM.
|
-
- HY-N7621
-
Bryonamide A
|
Others
|
Others
|
Bryonamide A is a natural compound isolated from red algae Bostrychia radicans (Rhodomelaceae).
|
-
- HY-N2416
-
Taccalonolide A
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.
|
-
- HY-N7680
-
Neopuerarin A
|
Others
|
Metabolic Disease
|
Neopuerarin A is an isoflavones isolated from the water extraction of the dried roots of Pueraria lobata (Willd.). Neopuerarin A shows significant hepatoprotective effect.
|
-
- HY-N2606
-
-
- HY-N6065
-
Praeruptorin A
|
NF-κB
|
Inflammation/Immunology
|
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
|
-
- HY-N7028
-
Withanolide A
|
Others
|
Neurological Disease
|
Withanolide A, isolated from the indian herbal drug Ashwagandha (root of Withania somnifera), could regenerate neurites and reconstruct synapses in severely damaged neurons.
|
-
- HY-N0318
-
-
- HY-N0023
-
Cistanoside A
|
Others
|
Inflammation/Immunology
|
Cistanoside A is a phenylethanoid isolated from Cistanche deserticola, reduces NO accumulation, but shows no effect on iNOS mRNA, iNOS protein levels or iNOS activity. Anti-inflammatory effect.
|
-
- HY-131098
-
Enduracidin A
|
Antibiotic
|
Infection
|
Enduracidin A is a major component of Enduracidin. Enduracidin is a polypeptide antibiotic produced by Streptomyces fungicides.
|
-
- HY-N3201
-
-
- HY-N6820
-
-
- HY-N0581
-
-
- HY-N0257
-
-
- HY-11079
-
-
- HY-P1539
-
-
- HY-N7679
-
-
- HY-N0659
-
-
- HY-N5104
-
-
- HY-116941
-
A-381393
|
Dopamine Receptor
|
Neurological Disease
|
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM).
|
-
- HY-N6992
-
-
- HY-N1508
-
Ecliptasaponin A
|
Others
|
Inflammation/Immunology
|
Ecliptasaponin A , a pentacyclic triterpenoid saponin, is one of major compounds separated from Eclipta prostrate. Eclipta prostrate is considered as a nourishing herbal medicine with pleiotropic effects, including anti-inflammatory, hepatoprotective, antioxidant, and immunomodulatory.
|
-
- HY-N2175
-
-
- HY-N2440
-
-
- HY-N0081
-
(±)-Praeruptorin A
|
Calcium Channel
|
Infection
|
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker.
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-
- HY-P2324
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Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
Infection
|
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
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-
- HY-N2626
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Epimedoside A
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Others
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Infection
|
Epimedoside A is a flavonoid isolated from the roots of Epimedium wushanense. Epimedoside A exhibits significant antioxidant activity in vitro.
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-
- HY-N2281
-
-
- HY-N5057
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Przewalskinic acid A
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Others
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Cardiovascular Disease
|
Przewalskinic acid A is a rare, water-soluble phenolic acid thus far only found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion.
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-
- HY-N0237
-
-
- HY-N5087
-
-
- HY-12455
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Duocarmycin A
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ADC Cytotoxin
Apoptosis
Caspase
|
Cancer
|
Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.
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-
- HY-N1472
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Levistolide A
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Apoptosis
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Cancer
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Levistolide A (LA), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is used for treating cancer. Levistolide A can induce apoptosis via ROS-mediated ER stress pathway.
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-
- HY-N1371
-
-
- HY-N6930
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-
- HY-N0028
-
-
- HY-P1581
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Ceratotoxin A
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Bacterial
|
Infection
|
Ceratotoxin A, a 29-residue peptide isolated from the accessory gland secretion fluid, with strong anti-bacterial activity.
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-
- HY-N4210
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Yadanziolide A
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Others
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Cancer
Infection
|
Yadanziolide A, isolated from the cultivated dry seeds of Brucea javanica, has strong antiviral activities with IC50 of 5.5 μM against tobacco mosaic virus. Yadanziolide A shows significant antitumor effects.
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-
- HY-108463
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A-967079
|
TRP Channel
|
Inflammation/Immunology
|
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
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-
- HY-N2155
-
-
- HY-131058
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Muscotoxin A
|
ADC Cytotoxin
|
Cancer
|
Muscotoxin A is an ADC cytotoxin. Muscotoxin A is a cytotoxic lipopeptide that permeabilizes mammalian cell membranes and induces necrotic cell death.
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-
- HY-N2331
-
-
- HY-50662
-
-
- HY-N6776
-
Penitrem A
|
Potassium Channel
|
Cancer
Neurological Disease
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.
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-
- HY-N4084
-
Thonningianin A
|
Apoptosis
|
Cancer
|
Thonningianin A, an ellagitannin, is isolated from the methanolic extract of the African medicinal herb, Thonningia sanguinea. The antioxidant properties of Th A involve radical scavenging, anti-superoxide formation and metal chelation. Anti-cancer activities.
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-
- HY-15568A
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A-317491 sodium salt hydrate
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
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-
- HY-N2637
-
-
- HY-N4236
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Angelol A
|
Others
|
Others
|
Angelol A is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model.
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-
- HY-N2249
-
-
- HY-N2524
-
-
- HY-108421
-
Xinjiachalcone A
|
Bacterial
|
Infection
|
Xinjiachalcone A is an active principle of Glycyrrhiza inflata Batalin. Xinjiachalcone A shows both a low MIC and a strong bactericidal activity against H. pylori, with MIC values ranged from 12.5 to 50 µM for seventeen H. pylori strains.
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-
- HY-133168
-
Englerin A
|
TRP Channel
|
Cancer
|
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.
|
-
- HY-N0743
-
Senkyunolide A
|
Others
|
Cancer
|
Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity.
|
-
- HY-N7499
-
-
- HY-136293
-
Mechercharmycin A
|
Apoptosis
|
Cancer
|
Mechercharmycin A is a cytotoxic substance isolated from marine-derived Thermoactinomyces sp. YM3-251. Mechercharmycin A exhibits relatively strong antitumor activity.
|
-
- HY-N6076
-
Tenuifoliside A
|
ERK
|
Neurological Disease
|
Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
|
-
- HY-N4316
-
-
- HY-N4257
-
-
- HY-108013
-
-
- HY-125531
-
Dactylorhin A
|
Others
|
Others
|
Dactylorhin A, a succinate derivative ester, is isolated from rhizomes of Gymnadenia conopsea. Dactylorhin A exhibits moderate inhibitory effects on NO production effects in RAW 264.7 macrophage cells.
|
-
- HY-N2441
-
-
- HY-N2111
-
-
- HY-N2505
-
-
- HY-N0819
-
Raddeanin A
|
Apoptosis
|
Cancer
|
Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.
|
-
- HY-P2123
-
Colistin A
|
Bacterial
Antibiotic
|
Infection
|
Colistin A is a major component of Colistin. Colistin is a polymyxin antibiotic and can be used to combat infections caused by problematic gram-negative bacteria.
|
-
- HY-128851
-
Coenzyme A
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
Coenzyme A is is an obligatory cofactor in all living cells synthesised from pantothenate (Vitamin B5), adenosine triphosphate (ATP) and cysteine. Covalent binding of Coenzyme A to Peroxiredoxin 5 (Prdx5) results in complete inhibition of its peroxidase activity, which is reversed by reduction with DTT.Coenzyme A and its thioester derivatives are key players in major catabolic and anabolic pathways and the regulation of gene expression. Many human pathologies, including cancer, diabetes and neurodegeneration, have been associated with abnormal biosynthesis and homeostasis of CoA and its derivatives.
|
-
- HY-12761
-
-
- HY-N7644
-
Comanthoside A
|
Others
|
Others
|
Comanthoside A is a plant derived natural flavonoid glycoside isolated from the leaves of Comanthosphace japonica. Comanthoside A also serves as a key intermediate for the synthesis of Comanthoside B and Linaroside.
|
-
- HY-U00225
-
-
- HY-126708
-
Luisol A
|
ADC Cytotoxin
|
Infection
|
Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, anthraquinone antibiotic analog, is an ADC Cytotoxin.
|
-
- HY-18260
-
Bisphenol A
|
Endogenous Metabolite
|
Endocrinology
|
Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders.
|
-
- HY-100483
-
A-804598
|
P2X Receptor
|
Cancer
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
|
-
- HY-15568
-
A-317491
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
|
-
- HY-N2017
-
-
- HY-N4318
-
-
- HY-N6593
-
-
- HY-N4223
-
Sibirioside A
|
Others
|
Metabolic Disease
|
Sibirioside A is a phenylpropanoid glycoside isolated from Scrophulariae Radix. Sibirioside A has the potential for the treatment of diabetes.
|
-
- HY-N4274
-
-
- HY-U00142
-
A-802715
|
Others
|
Cancer
|
A802715 is a methylxanthine derivative. A802715 has a TD50 (toxic dose of 50%) of 0.9-1.1 mM.
|
-
- HY-N6994
-
Isoasatone A
|
Others
|
Infection
|
Isoasatone A is a natural product isolated from the plant Heterotropa takaoi M., with anti-insect activity. Isoasatone A againsts S. litura by acting on cytochrome P450 monoxygenases and glutathione transferases.
|
-
- HY-P1629
-
Temporin A
|
Bacterial
Fungal
Antibiotic
|
Infection
|
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
|
-
- HY-N2437
-
-
- HY-N2238
-
Dipsanoside A
|
Others
|
Metabolic Disease
|
Dipsanoside A is a novel tetrairidoid glucoside from Dipsacus asper. Dipsacus asper Wall., a perennial plant widespread in China, has been used in traditional Chinese medicine for hundreds of years as a tonic for refreshment, as a fissiparism promoter of the osseous cells, and as an embryo security agent, etc.
|
-
- HY-N0246
-
-
- HY-N6917
-
-
- HY-N2326
-
(±)-Anatoxin A fumarate
|
nAChR
|
Neurological Disease
|
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
|
-
- HY-131103
-
-
- HY-N7692
-
Polyporusterone A
|
Others
|
Others
|
Polyporusterone A is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone A has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
|
-
- HY-P2322
-