Search Result
Results for "Acid-Sensing Ion Channel Peptides Inhibitors" in MCE Product Catalog:
1165
Inhibitors & Agonists
5
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-75867
-
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- HY-131261
-
-
- HY-122135
-
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- HY-112217A
-
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PSEM 89S TFA
|
nAChR
|
Neurological Disease
|
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PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.
|
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- HY-136564A
-
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DAD
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Potassium Channel
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Neurological Disease
|
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DAD is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD is a third-generation photoswitch that responds to visible light. DAD has the potential for restoring visual function.
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- HY-136564
-
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DAD dichloride
|
Potassium Channel
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Neurological Disease
|
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DAD dichloride is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD dichloride is a third-generation photoswitch that responds to visible light. DAD dichloride has the potential for restoring visual function.
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- HY-P1280
-
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Margatoxin
|
Potassium Channel
|
Neurological Disease
|
|
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.
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- HY-130605
-
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BAY-1797
|
P2X Receptor
|
Neurological Disease
|
|
BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects.
|
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- HY-U00439
-
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- HY-16787
-
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ICA-121431
|
Sodium Channel
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Cardiovascular Disease
|
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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).
|
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- HY-110325
-
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- HY-P0274
-
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PGLa
|
Bacterial
Antibiotic
|
Infection
|
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PGLa, a 21-residue peptide, is an antimicrobial peptide. PGLa is a member of the magainin family of antibiotic peptides found in frog skin and its secretions.
|
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- HY-P0274A
-
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PGLa TFA
|
Bacterial
Antibiotic
|
Infection
|
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PGLa TFA, a 21-residue peptide, is an antimicrobial peptide. PGLa TFA is a member of the magainin family of antibiotic peptides found in frog skin and its secretions.
|
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- HY-136300
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- HY-P1481
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- HY-P1344A
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- HY-131092
-
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- HY-U00135
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-
- HY-131094
-
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- HY-P1481A
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- HY-101809
-
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- HY-P0179
-
-
- HY-N2338
-
-
- HY-P1486
-
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- HY-P0179A
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- HY-P2244A
-
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YAP-TEAD-IN-1 TFA
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM).
|
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- HY-P1486A
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- HY-107024
-
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Osteogenic Growth Peptide (10-14)
OGP(10-14); Historphin
|
Src
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Others
|
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Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
|
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- HY-128113
-
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- HY-P2292A
-
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Omiganan-FITC TFA
|
Bacterial
Fungal
|
Infection
|
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Omiganan-FITC TFA is a peptide-FITC complex composed of Omiganan and a FITC. Omiganan is a bactericidal and fungicidal cationic peptide being developed as a topical gel for prevention of catheter-associated infections.
|
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- HY-P0281A
-
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TAT TFA
|
HIV
|
Infection
|
|
TAT TFA (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins.
|
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- HY-P0281
-
|
TAT
|
HIV
|
Infection
|
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TAT (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus-1 (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins.
|
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- HY-108586
-
|
NS3623
|
Potassium Channel
|
Neurological Disease
|
|
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.
|
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- HY-P2292
-
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Omiganan-FITC
|
Bacterial
Fungal
|
Infection
|
|
Omiganan-FITC is a peptide-FITC complex composed of Omiganan and a FITC. Omiganan is a bactericidal and fungicidal cationic peptide being developed as a topical gel for prevention of catheter-associated infections. FITC is a derivative of fluorescein for the labeling of amines.
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- HY-100310
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- HY-15736
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- HY-U00280
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Potassium Channel Activator 1
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Others
|
Neurological Disease
|
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Potassium Channel Activator 1 is an agent for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.
|
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- HY-100257
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- HY-17624
-
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Framycetin
Neomycin B; Fradiomycin B
|
Bacterial
|
Infection
|
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Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
|
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- HY-P1333
-
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Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
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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).
|
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- HY-131005
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- HY-17624A
-
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Framycetin sulfate
Neomycin B sulfate; Fradiomycin B sulfate
|
Bacterial
|
Infection
|
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Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
|
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- HY-N7122
-
|
Thymopentin
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Thymopentin is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs).
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- HY-N7122A
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Thymopentin acetate
|
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
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Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs).
|
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- HY-123834
-
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FEN1-IN-1
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Others
|
Cancer
|
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FEN1-IN-1 (compound 1) is a flap endonuclease 1 (FEN1) inhibitor. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg 2+ ions.
|
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- HY-P2316
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Epinecidin-1 TFA
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Bacterial
Antibiotic
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Infection
|
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Epinecidin-1 TFA is a multi-functional antimicrobial peptide (AMP) from Orange-spotted grouper (Epinephelus coioides). Epinecidin-1 TFA has antibacterial, antifungal, antiviral, anti-tumor, and immunomodulatory effects. Epinecidin-1 TFA has the potential to be an alternative for current antibiotics.
|
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- HY-11062
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- HY-131091
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- HY-41076
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- HY-N0172
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- HY-B1319
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- HY-12082A
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- HY-P1929
-
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Bivalirudin
|
Thrombin
|
Cardiovascular Disease
|
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Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
|
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- HY-P2244
-
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YAP-TEAD-IN-1
|
YAP
|
Cancer
|
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YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM).
|
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- HY-B0908
-
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- HY-121879
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- HY-P1051
-
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β-amyloid (12-28)
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
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β-amyloid (12-28) is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
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- HY-P1051A
-
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β-amyloid (12-28) (TFA)
Amyloid β-Protein (12-28) (TFA)
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Amyloid-β
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Neurological Disease
|
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β-amyloid (12-28) TFA is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
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- HY-N0373
-
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Licochalcone B
|
Amyloid-β
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Neurological Disease
|
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Licochalcone B is an extract from the root of Glycyrrhiza inflate. Licochalcone B inhibits amyloid β (Aβ42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ions.
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- HY-131142
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- HY-16696
-
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SN 2
|
TRP Channel
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Others
|
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SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8±0.13 μM.
|
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- HY-P1271
-
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Catestatin
|
nAChR
|
Cardiovascular Disease
|
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Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
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- HY-P2272
-
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NLS-StAx-h
|
Wnt
β-catenin
|
Cancer
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NLS-StAx-h is a selective, stapled peptide inhibitor of Wnt signaling with an IC50 of 1.4 μM. NLS-StAx-h efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h inhibits proliferation and migration of colorectal cancer cells.
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- HY-P1179
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- HY-P0269
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Magainin 1
|
Bacterial
Fungal
Antibiotic
|
Infection
|
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Magainin 1 is an antimicrobial and amphipathic peptide isolated from the skin of Xenopus laevis. Magainin 1 exhibits antibiotic activity against numerous Gram-negative and Gram-positive bacteria.
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- HY-P1019A
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- HY-P1271A
-
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Catestatin TFA
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
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- HY-P0082A
-
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Glucagon hydrochloride
Porcine glucagon hydrochloride
|
Glucagon Receptor
|
Metabolic Disease
|
|
Glucagon hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone, produced by pancreatic α-cells. Glucagon hydrochloride stimulates gluconeogenesis. Glucagon hydrochloride decreases the activity of HNF-4. Glucagon hydrochloride increases HNF4α phosphorylation.
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- HY-P1179A
-
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Guanylin(human) TFA
|
Guanylate Cyclase
Endogenous Metabolite
|
|
|
Guanylin(human) TFA, a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) TFA is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism.
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- HY-P0269A
-
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Magainin 1 TFA
|
Bacterial
Fungal
Antibiotic
|
Infection
|
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Magainin 1 TFA is an antimicrobial and amphipathic peptide isolated from the skin of Xenopus laevis. Magainin 1 TFA exhibits antibiotic activity against numerous Gram-negative and Gram-positive bacteria.
|
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- HY-12949
-
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- HY-P2322
-
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Iturin A
|
Fungal
|
|
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IturinA exhibits strong antifungal activity against pathogenic yeast and fungi. Iturin A interacts with the cytoplasmic membrane of the target cell forming ion conducting pores.
|
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- HY-P2315
-
|
Human β-defensin-1
HβD-1
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-1 (HβD-1) is a cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by all epithelial surfaces, but also by circulatory cells and cells of the reproductive tract. Human β-defensin-1 has antimicrobial activities against a broad-sperm bacteria.
|
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- HY-101238
-
-
- HY-101350
-
-
- HY-108505
-
-
- HY-P0082
-
|
Glucagon
Porcine glucagon
|
Glucagon Receptor
|
Metabolic Disease
|
|
Glucagon (Porcine glucagon) is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon decreases the activity of HNF-4. Glucagon increases HNF4α phosphorylation.
|
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- HY-19373
-
-
- HY-17360
-
|
Tiotropium Bromide
BA679 BR
|
mAChR
|
Neurological Disease
|
|
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
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- HY-P1115A
-
|
AKTide-2T TFA
|
Akt
|
Others
|
|
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
|
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- HY-P1178
-
|
Cyclotraxin B
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
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- HY-U00151
-
-
- HY-P1178A
-
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Cyclotraxin B TFA
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
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- HY-107929
-
|
Calcium polystyrene sulfonate
Poly(styrenesulfonic Acid) calcium salt
|
Others
|
Cardiovascular Disease
|
|
Calcium polystyrene sulfonate is an ion-exchange resin used for reducing blood levels of potassium. Calcium polystyrene sulfonate is used to treat hyperkalemia in patients with chronic kidney disease (CKD).
|
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- 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-P1508A
-
|
Bactenecin TFA
Bactenecin, bovine TFA
|
Bacterial
Fungal
|
Infection
|
|
Bactenecin TFA (Bactenecin, bovine TFA) is a potent 12-aa looped antimicrobial peptide isolated from bovine neutrophils. Bactenecin TFA inhibits the growth of bacteria and yeast, and kills the fungus Trichophyton rubrum. Bactenecin TFA increass membrane permeability, inhibits the growth and biofilm formation of B. pseudomallei.
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-
- HY-105077A
-
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Nemifitide diTFA
INN 00835 diTFA
|
5-HT Receptor
|
Neurological Disease
|
|
Nemifitide diTFA (INN 00835 diTFA) is a synthetic pentapeptide antidepressant with a potential for rapid onset of action. Nemifitide diTFA is a peptide analog of melanocyte-inhibiting factor (MIF). Nemifitide diTFA can cross the blood-brain barrier.
|
-
- HY-W016349
-
|
Chelidamic acid
|
Others
|
Others
|
|
Chelidamic acid is a heterocyclic organic acid with a pyran skeleton. Chelidamic acid has good coordination ability with noble metal ions. Chelidamic acid is also one of the most potent inhibitors of glutamate decarboxylase, with a Ki of 33 μM.
|
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- HY-125586
-
|
β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
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- HY-P1471
-
-
- HY-126810A
-
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NP213 TFA
|
Fungal
|
Infection
|
|
NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections.
|
-
- HY-P1115
-
|
AKTide-2T
|
Akt
|
Others
|
|
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
|
-
- 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-N2197
-
|
Hirsuteine
|
Others
|
Neurological Disease
|
|
Hirsuteine is an indole alkaloid extracted from Uncaria genus. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.
|
-
- HY-P1508
-
|
Bactenecin
Bactenecin, bovine
|
Bacterial
Fungal
|
Infection
|
|
Bactenecin (Bactenecin, bovine) is a potent 12-aa looped antimicrobial peptide isolated from bovine neutrophils. Bactenecin inhibits the growth of bacteria and yeast, and kills the fungus Trichophyton rubrum. Bactenecin increass membrane permeability, inhibits the growth and biofilm formation of B. pseudomallei.
|
-
- HY-P1045
-
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187-1, N-WASP inhibitor
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-B0612D
-
-
- HY-108017
-
|
Ferric maltol
|
Others
|
Metabolic Disease
|
|
Ferric maltol is an orally active complex of a single ferric ion (Fe 3+). Ferric maltol has tha potential for iron deficiency anemia treatment in inflammatory bowel disease.
|
-
- HY-N0042
-
-
- HY-P0316
-
|
TP508
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-P1045A
-
|
187-1, N-WASP inhibitor TFA
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-B1221
-
-
- HY-12501A
-
|
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
|
-
- HY-P0316A
-
|
TP508 TFA
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-P1136
-
|
Gap19
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Gap19, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 has protective effects against myocardial.
|
-
- HY-P1471A
-
|
Adrenomedullin (AM) (22-52), human TFA
22-52-Adrenomedullin (human) (TFA)
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
|
-
- HY-14182
-
|
Vernakalant
RSD1235
|
Potassium Channel
|
Cardiovascular Disease
|
|
Vernakalant(RSD-1235) is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.
|
-
- HY-13259
-
|
MG-132
Z-Leu-leu-leu-al
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
|
MG-132 (Z-Leu-leu-leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
|
-
- HY-P1136A
-
|
Gap19 TFA
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Gap19 TFA, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 TFA inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 TFA is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 TFA has protective effects against myocardial.
|
-
- HY-130994
-
|
Aeruginosin 865
|
NF-κB
ADC Cytotoxin
|
Cancer
Inflammation/Immunology
|
|
Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp. Lukešová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect
|
-
- HY-126810
-
|
NP213
|
Fungal
|
Infection
|
|
NP213 is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 is effective and well-tolerated in resolving nail fungal infections.
|
-
- HY-12501
-
|
ITI214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
|
-
- 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-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-125777A
-
|
α-Conotoxin Vc1.1 TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.
|
-
- HY-106225
-
|
Rotigaptide
ZP123
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.
|
-
- HY-P0190
-
|
Iberiotoxin
|
Potassium Channel
|
Cardiovascular Disease
|
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
|
-
- HY-122700
-
|
Factor D inhibitor 6
|
Complement System
|
Inflammation/Immunology
|
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
|
-
- HY-P1237
-
-
- HY-P1815
-
-
- HY-B1090S
-
-
- HY-W040265
-
-
- HY-B1243
-
-
- HY-B0612E
-
-
- HY-12883A
-
-
- HY-N4097
-
|
Incensole
|
Others
|
Neurological Disease
|
|
Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.
|
-
- HY-P0027
-
|
Jasplakinolide
|
Arp2/3 Complex
Fungal
|
Cancer
Infection
|
|
Jasplakinolide is a potent actin polymerization inducer and stabilizes pre-existing actin filaments. Jasplakinolide binds to F-actin competitively with phalloidin with a Kd of 15 nM. Jasplakinolide, a naturally occurring cyclic peptide from the marine sponge, has both fungicidal and anti-cancer activity.
|
-
- HY-P1075
-
|
CALP3
|
Calcium Channel
|
Cancer
Neurological Disease
|
|
CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
|
-
- 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-18728
-
-
- HY-16974
-
|
Afoxolaner
|
GABA Receptor
Chloride Channel
|
Infection
|
|
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
|
-
- HY-B1009
-
|
Ethylenediaminetetraacetic acid trisodium salt
EDTA trisodium salt; Trisodium EDTA
|
Ferroptosis
|
Others
|
|
Ethylenediaminetetraacetic acid trisodium salt (EDTA trisodium salt) is used to bind metal ions in the practice of chelation therapy, for treating mercury and lead poisoning, used in a similar manner to remove excess iron from the body, for treating the complication of repeated blood transfusions, as would be applied to treat thalassaemia.
|
-
- HY-15084B
-
|
Dizocilpine
MK-801
|
iGluR
|
Neurological Disease
|
|
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux.
|
-
- HY-P1075A
-
|
CALP3 TFA
|
Calcium Channel
|
Cancer
Neurological Disease
|
|
CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
|
-
- HY-P1459
-
-
- HY-P1758
-
-
- HY-N1673
-
|
2,5-Dihydroxybenzaldehyde
Gentisaldehyde
|
Bacterial
|
Infection
|
|
2,5-Dihydroxybenzaldehyde (Gentisaldehyde) is a naturally occurring antimicrobial that inhibits the growth of Mycobacterium avium subsp. paratuberculosis. 2,5-Dihydroxybenzaldehyde is active against S. aureus strains with a MIC50 of 500 mg/L.
|
-
- HY-P1546
-
-
- HY-P2311
-
-
- HY-P2321
-
-
- HY-P0318
-
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-P2321A
-
-
- HY-135407S
-
-
- HY-117825
-
|
RU-TRAAK-2
|
Potassium Channel
|
Neurological Disease
|
|
RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K + channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).
|
-
- HY-135013
-
|
Umbellulone
|
TRP Channel
|
Neurological Disease
|
|
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.
|
-
- HY-P1565
-
|
Transdermal Peptide
TD 1 (peptide)
|
Na+/K+ ATPase
|
Inflammation/Immunology
|
|
Transdermal Peptide (TD 1 peptide) is a 11-amino acid peptide, binds toNa +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide can enhance the transdermal delivery of many macromolecules.
|
-
- HY-107642
-
|
MA-2029
|
Motilin Receptor
|
Metabolic Disease
|
|
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility.
|
-
- HY-P2251
-
|
T-peptide
|
Microtubule/Tubulin
|
|
|
T-peptide is a peptide derived from microtubule binding repeat of Tau protein. T-peptide self-assembles into 30-55 nm paired helical filaments (PHFs) even in the absense of inducers. T-peptide is cytotoxic in multiple cell lines including cortical neurons, cerebellar granular neurons, neuroblastoma cells, kidney fibroblasts and HEK293 cells. T-peptide co-localizes with pathological hyperphosphorylated forms of tau in vitro.
|
-
- HY-107732
-
|
JNJ-5207787
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors.
|
-
- HY-P1847
-
|
IKKγ NBD Inhibitory Peptide
|
NF-κB
|
Cancer
|
|
IKKγ NBD Inhibitory Peptide is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-13443
-
-
- HY-13443A
-
-
- HY-15583
-
-
- HY-P0189
-
-
- HY-P0189A
-
-
- HY-113952
-
|
Actinonin
(-)-Actinonin
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
|
-
- HY-P1362
-
|
β-Amyloid (42-1), human
Amyloid β Peptide (42-1)(human)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (42-1), human is the inactive form of Amyloid β Peptide (1-42). Amyloid β Peptide (42-1) is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
|
-
- HY-P1847A
-
-
- HY-108512
-
|
PD 144418
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity.
|
-
- HY-P1565A
-
|
Transdermal Peptide TFA
TD 1 (peptide) (TFA)
|
Na+/K+ ATPase
|
Others
|
|
Transdermal Peptide TFA (TD 1 peptide TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide TFA can enhance the transdermal delivery of many macromolecules.
|
-
- HY-P1144
-
-
- HY-P1144A
-
-
- HY-P1186
-
-
- HY-P1454A
-
|
Fz7-21 TFA
Ac-LPSDDLEFWCHVMY-NH2 TFA
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
|
-
- HY-P1454
-
|
Fz7-21
Ac-LPSDDLEFWCHVMY-NH2
|
Wnt
|
Cancer
|
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
|
-
- HY-P1841
-
-
- HY-103473A
-
|
Boc-MLF TFA
Boc-Met-Leu-Phe-OH (TFA)
|
Others
|
Inflammation/Immunology
|
|
Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
|
-
- HY-P0215
-
-
- HY-P1497
-
-
- HY-P1378
-
-
- HY-P1514
-
-
- HY-108512A
-
|
PD 144418 oxalate
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity.
|
-
- HY-N0814
-
|
Phytic acid
Inositol hexaphosphate; myo-Inositol, hexakis(dihydrogen phosphate)
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Phytic acid is a phosphorus storage compound of seeds and cereal grains. Phytic acid is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- 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-P1113
-
-
- HY-P1113A
-
-
- HY-P0215A
-
-
- HY-P1398
-
-
- HY-P1345
-
|
TLQP-21
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-P1378A
-
-
- HY-P1046
-
|
β-Amyloid 1-15
Amyloid β-Protein (1-15)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-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-P0119A
-
-
- HY-P0119
-
-
- HY-103310
-
-
- HY-101436A
-
|
Sematilide hydrochloride
CK-1752 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Sematilide hydrochloride (CK-1752 hydrochloride) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent.
|
-
- HY-B1546
-
|
Benzamil
Benzylamiloride
|
Sodium Channel
Na+/Ca2+ Exchanger
|
Neurological Disease
|
|
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-101436
-
|
Sematilide
CK-1752
|
Potassium Channel
|
Cardiovascular Disease
|
|
Sematilide (CK-1752) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent.
|
-
- HY-B1546A
-
|
Benzamil hydrochloride
Benzylamiloride hydrochloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
|
Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-P1398A
-
-
- HY-P1219A
-
|
Jingzhaotoxin-III TFA
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-III TFA is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III TFA can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype[1] [2] .
|
-
- HY-P1219
-
|
Jingzhaotoxin-III
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype[1] [2] .
|
-
- HY-19765
-
|
GSK2798745
|
TRP Channel
|
Cardiovascular Disease
|
|
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 is used in research for the treatment of pulmonary edema associated with congestive heart failure.
|
-
- HY-N0814A
-
|
Phytic acid dodecasodium salt hydrate
myo-Inositol, hexakis(dihydrogen phosphate) dodecasodium salt hydrate; Inositol hexaphosphate dodecasodium salt hydrate
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid dodecasodium salt hydrate is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid dodecasodium salt hydrate inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- HY-P1119
-
|
WRW4
|
Others
|
Neurological Disease
|
|
WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
|
-
- 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.
|
-
- HY-W012479
-
-
- HY-129658A
-
-
- HY-P2294
-
|
pm26TGF-β1 peptide
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
|
-
- HY-P1345A
-
|
TLQP-21 TFA
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-P0272
-
|
Peptide T
|
HIV
|
Infection
|
|
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
-
- HY-12523
-
|
Peptide M
|
Others
|
Others
|
|
Peptide M is a 50 aa synthetic peptide derived from a streptococcal M protein containing an additional C-terminal cysteine residue.
|
-
- HY-112679
-
-
- HY-P1231
-
-
- HY-P0290
-
-
- HY-P1229
-
-
- HY-P1329
-
-
- HY-P2294A
-
|
pm26TGF-β1 peptide TFA
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
|
-
- HY-P0272A
-
|
Peptide T TFA
|
HIV
|
Infection
|
|
Peptide T (TFA) is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
-
- HY-P1083
-
-
- HY-B1500
-
-
- HY-114426
-
-
- HY-P0014
-
-
- HY-114424A
-
-
- HY-P1363
-
-
- HY-114424
-
-
- HY-129658
-
-
- HY-P0052A
-
-
- HY-P1246
-
-
- HY-P0136
-
-
- HY-P1329A
-
-
- HY-P1522
-
-
- HY-P1063
-
-
- HY-P0052
-
-
- HY-114426A
-
-
- HY-P0224
-
-
- HY-P1083A
-
-
- 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-P2268
-
|
RAGE antagonist peptide
|
Amyloid-β
|
|
|
RAGE antagonist peptide is an antagonist of Receptor for advanced glycation end products (RAGE). RAGE blocks S100P, S100A4 and HMGB-1 mediated RAGE activation. RAGE antagonist peptide inhibits growth and metastasis of rat glioma tumors. RAGE antagonist peptide also reduces cell growth and RAGE-mediated NF-κB activity in human PDAC cell lines.
|
-
- HY-P1116A
-
|
PBP10 TFA
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects.
|
-
- HY-N1391
-
|
10-Deacetyltaxol
10-Deacetylpaclitaxel
|
Microtubule/Tubulin
|
Cancer
|
|
10-Deacetyltaxol (10-Deacetylpaclitaxel) is a taxane derivative isolated from Taxus wallichiana Zucc. 10-Deacetyltaxol (10-Deacetylpaclitaxel) promotes the polymerization of tubulin and to inhibit the depolymerization of microtubules induced by cold or by calcium ions in vitro. 10-Deacetyltaxol (10-Deacetylpaclitaxel) exhibits cytotoxicity in human glial and neuroblastoma cell-lines.
|
-
- HY-17611
-
|
Etripamil
MSP-2017; (-)-MSP-2017
|
Calcium Channel
|
Cardiovascular Disease
|
|
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.
|
-
- HY-17409
-
|
Nystatin
|
Fungal
Antibiotic
|
Infection
|
|
Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasma membranes to small monovalent ions, including chloridion. Nystatin is a cholesterol-sequestering agent, partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis.
|
-
- HY-P1731
-
|
Tirzepatide
LY3298176
|
Glucagon Receptor
|
Metabolic Disease
|
|
Tirzepatide (LY3298176) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist that is being developed for the treatment of type 2 diabetes.
|
-
- HY-P1731B
-
|
Tirzepatide hydrochloride
LY3298176 hydrochloride
|
Glucagon Receptor
|
Metabolic Disease
|
|
Tirzepatide hydrochloride (LY3298176 hydrochloride) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist that is being developed for the treatment of type 2 diabetes.
|
-
- HY-P0139
-
-
- HY-P1063A
-
-
- HY-P1880
-
-
- HY-P0270
-
-
- HY-P1891
-
-
- HY-P1879
-
-
- HY-P1893
-
-
- HY-P0133
-
|
(Arg)9
Nona-L-arginine; Peptide R9
|
Others
|
Neurological Disease
|
|
(Arg)9 (Nona-L-arginine;Peptide R9) is a cell-penetrating peptide; exhibits neuroprotective activity with an IC50 of 0.78 μM in the glutamic acid model.
|
-
- HY-125824
-
-
- HY-P1418
-
|
DPC-AJ1951
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
DPC-AJ1951, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
|
-
- HY-P1495
-
-
- HY-P1000
-
-
- HY-12811
-
|
PF-04856264
|
Sodium Channel
|
Neurological Disease
|
|
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.
|
-
- HY-D0143B
-
|
Quinine hemisulfate hydrate
|
Parasite
Potassium Channel
|
Infection
|
|
Quinine hemisulfate hydrate is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine hemisulfate hydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
|
-
- HY-D0143
-
|
Quinine
|
Parasite
Potassium Channel
|
Infection
|
|
Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
|
-
- HY-107641
-
|
α-Cyano-4-hydroxycinnamic acid
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
|
-
- HY-P1418A
-
|
DPC-AJ1951 TFA
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
DPC-AJ1951 TFA, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
|
-
- HY-P1401
-
|
Protein Kinase C (19-36)
|
PKC
|
Metabolic Disease
|
|
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response.
|
-
- HY-P2319
-
-
- HY-P2281
-
|
Atrial natriuretic factor (1-28) (human, porcine)
Atrial natriuretic peptide (1-28)
|
Endogenous Metabolite
|
|
|
Atrial natriuretic factor (1-28) (human, porcine) (Atrial natriuretic peptide (1-28)) is an endogenous peptide produced by the heart, involved in blood pressure regulation. Atrial natriuretic factor (1-28) (human, porcine) produces natriuresis, diuresis and vasorelaxation in vivo.
|
-
- HY-P1731A
-
|
Tirzepatide TFA
LY3298176 TFA
|
Glucagon Receptor
|
Metabolic Disease
|
|
Tirzepatide TFA (LY3298176 TFA) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist that is being developed for the treatment of type 2 diabetes.
|
-
- HY-P1872
-
|
OV-1, sheep
|
Bacterial
|
Infection
|
|
OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa.
|
-
- 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-N7432
-
|
DIMBOA
|
Bacterial
Fungal
Antibiotic
|
Infection
|
|
DIMBOA, an antibiotic, is a benzoxazinoid, part of the chemical defense system of graminaceous plants such as maize, wheat, and rye. DIMBOA possess growth inhibitory properties against many strains of studied bacteria and fungi, such as Staphylococcus aureus, Escherichia coli as well as against Saccharomyces cerevisiae. DIMBOA exhibits a potent free-radical scavenging activity and a weaker iron (III) ions reducing activity. Antioxidant activity.
|
-
- HY-A0095
-
|
Flibanserin
BIMT-17; BIMT-17BS
|
5-HT Receptor
|
Neurological Disease
|
|
Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD).
|
-
- HY-N0322
-
|
Cholesterol
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Metabolic Disease
|
|
Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
|
-
- HY-P0069A
-
-
- HY-P0080
-
-
- HY-15664
-
-
- HY-P1255
-
-
- HY-P2264
-
|
KYL peptide
|
Ephrin Receptor
|
|
|
KYL peptide is an EphA4 receptor tyrosine kinase inhibitor (Kd=0.8 μM). KYL peptide inhibits EphA4-EphrinA5 interactions (IC50=6.34 μM). KYL peptide prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. KYL peptide also exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively).
|
-
- HY-P2319A
-
-
- HY-19574
-
-
- HY-103546
-
-
- HY-P2278
-
-
- HY-P1013
-
-
- HY-114118
-
-
- HY-W010986
-
-
- HY-P0080A
-
-
- HY-P0261
-
-
- HY-P0241
-
-
- HY-P1895
-
-
- HY-P1595
-
-
- HY-P1818
-
-
- HY-P0315
-
|
Crosstide
|
Akt
|
Others
|
|
Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt.
|
-
- HY-P1903
-
-
- HY-P0122
-
|
iRGD peptide
c(CRGDKGPDC)
|
Integrin
|
Cancer
|
|
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
|
-
- HY-P1111A
-
|
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-P1860
-
-
- HY-I1112
-
-
- HY-P1524
-
-
- HY-P1226
-
-
- HY-P1224
-
-
- HY-P1601
-
-
- HY-P1228
-
-
- HY-P1774
-
-
- HY-P1223
-
-
- HY-P0092
-
-
- HY-P0198
-
-
- HY-114118A
-
-
- HY-P1116
-
|
PBP10
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects.
|
-
- HY-10095A
-
|
Olcegepant hydrochloride
BIBN-4096 hydrochloride; BIBN4096BS hydrochloride
|
CGRP Receptor
|
Neurological Disease
|
|
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
|
-
- HY-10095
-
|
Olcegepant
BIBN-4096; BIBN 4096BS
|
CGRP Receptor
|
Neurological Disease
|
|
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
|
-
- HY-P0128
-
|
β-Amyloid (25-35)
Amyloid beta-peptide (25-35); Aβ25-35; β-Amyloid peptide (25-35)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (25-35) (Amyloid beta-peptide (25-35)) is the fragment Aβ(25-35) of the Alzheimer's amyloid β-peptide, has shown neurotoxic activities in cultured cells.
|
-
- HY-50844
-
-
- HY-P0276
-
-
- HY-P1145
-
-
- HY-P1521
-
-
- HY-P1053
-
-
- HY-P1593
-
-
- HY-P1036
-
-
- HY-P1331
-
-
- HY-P1510
-
-
- HY-P1560
-
-
- HY-P0311
-
|
LAH4
|
Bacterial
|
Infection
|
|
LAH4 is an antimicrobial peptide that strongly interacts with phospholipid membranes, exhibiting in vitro transfection efficiency.
|
-
- HY-P1517
-
-
- HY-N0630
-
-
- HY-P1235
-
|
Carperitide
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-135412
-
-
- HY-124906
-
|
JAMI1001A
|
iGluR
|
Neurological Disease
|
|
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
|
-
- HY-P1214
-
-
- HY-P1341
-
-
- HY-P1341A
-
-
- HY-P1214A
-
-
- HY-107625A
-
|
SNAP 94847 hydrochloride
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-107625
-
|
SNAP 94847
|
MCHR1 (GPR24)
|
Neurological Disease
Endocrinology
|
|
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-P1740
-
|
RGD peptide (GRGDNP)
|
Integrin
Apoptosis
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
|
-
- HY-111778
-
|
EHMT2-IN-1
|
Histone Methyltransferase
|
Cancer
|
|
EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
|
-
- HY-111904
-
|
EHMT2-IN-2
|
Histone Methyltransferase
|
Cancer
|
|
EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
|
-
- HY-P0214
-
-
- HY-P0245
-
-
- HY-P0291
-
|
Kemptide Phospho-Ser5
|
PKA
|
Others
|
|
Kemptide (Phospho-Ser5) is a phosphate acceptor peptide that serves as a specific substrate for cAMP-dependent protein kinase (PKA).
|
-
- HY-P1145A
-
-
- HY-P1014
-
-
- HY-P1580
-
-
- HY-P1593A
-
-
- HY-P1334
-
-
- HY-P2283
-
-
- HY-P1572
-
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-19406
-
-
- HY-P0163
-
-
- HY-17631A
-
-
- HY-P1740A
-
|
RGD peptide (GRGDNP) (TFA)
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
|
-
- HY-111191
-
|
ONO-2952
|
Others
|
Neurological Disease
|
|
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
|
-
- HY-N2600
-
|
Kuwanon H
|
Bombesin Receptor
|
Cancer
|
|
Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
|
-
- HY-P2317
-
-
- HY-P0228
-
-
- HY-P1452A
-
-
- HY-P1334A
-
-
- HY-P1261
-
-
- HY-P0214A
-
-
- HY-P1484
-
-
- HY-P1062
-
-
- HY-P1262
-
-
- HY-P0173A
-
|
Chlorotoxin
|
Chloride Channel
|
Cancer
|
|
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
|
-
- HY-P1751
-
|
Ceratotoxin B
|
Bacterial
|
Infection
|
|
Ceratotoxins B is antibacterial peptide produced by the sexually mature females of Ceratitis capitata. Lytic and antibacterial activity .
|
-
- HY-P1832
-
|
PTD-p65-P1 Peptide
|
NF-κB
|
Cancer
Inflammation/Immunology
|
|
PTD-p65-P1 Peptide is a nuclear transcription factor NF-kappaB inhibitor, composed of a membrane-translocating peptide sequence generated from antennapedia (PTD) conjugated with p65-P1, which selectively inhibits activation induced by various inflammatory stimuli.
|
-
- HY-D0889
-
-
- HY-101177
-
-
- HY-W008555
-
-
- HY-116819
-
|
VU0453379
|
Glucagon Receptor
|
Metabolic Disease
|
|
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
|
-
- HY-P1832A
-
|
PTD-p65-P1 Peptide TFA
|
NF-κB
|
Cancer
Inflammation/Immunology
|
|
PTD-p65-P1 Peptide TFA is a nuclear transcription factor NF-kappaB inhibitor, composed of a membrane-translocating peptide sequence generated from antennapedia (PTD) conjugated with p65-P1, which selectively inhibits activation induced by various inflammatory stimuli.
|
-
- HY-P1884
-
|
LL-37, acetylated,amidated
|
Bacterial
|
Infection
|
|
LL-37, acetylated, amidated is a cathelicidin peptide LL-37 acetylated on the N-terminus and amidated on the C-terminus. The single human cathelicidin peptide LL-37 has antimicrobial and anti-biofilm activity against multiple Gram-positive and Gram-negative human pathogens, and has wound-healing effects on the host.
|
-
- HY-P1218A
-
|
Phrixotoxin 3 TFA
|
Sodium Channel
|
Neurological Disease
|
|
Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current[1] .
|
-
- HY-P1164
-
-
- HY-P1244
-
-
- HY-P1262A
-
-
- HY-P1581
-
|
Ceratotoxin A
|
Bacterial
|
Infection
|
|
Ceratotoxin A, a 29-residue peptide isolated from the accessory gland secretion fluid, with strong anti-bacterial activity.
|
-
- HY-P1261A
-
-
- HY-P1534
-
-
- HY-P1034
-
|
DAPTA
D-Ala-peptide T-amide; Adaptavir
|
CCR
HIV
|
Infection
Endocrinology
|
|
DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.
|
-
- HY-P1062A
-
-
- HY-P1082
-
-
- HY-P1490
-
-
- HY-15580
-
-
- HY-13760
-
-
- HY-P1663A
-
-
- HY-P1164A
-
-
- HY-P0225
-
-
- HY-P0250
-
-
- HY-P1772
-
-
- HY-17451
-
-
- HY-16952A
-
|
Bepridil hydrochloride hydrate
(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
|
-
- HY-129361
-
-
- HY-131095
-
-
- HY-P1141A
-
|
GLP-1(9-36)amide TFA
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1(9-36)amide TFA is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide TFA acts as an antagonist to the human pancreatic GLP-1 receptor.
|
-
- HY-P1728
-
|
Super-TDU 1-31
|
YAP
|
Cancer
|
|
Super-TDU (1-31) is a peptide of Super-TDU, which is an inhibitor of YAP-TEADs, shows potent anti-tumor activity.
|
-
- HY-P0206
-
-
- HY-114161
-
-
- HY-P1592A
-
|
G3-C12 TFA
|
Galectin
|
Cancer
|
|
G3-C12 (TFA) is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
|
-
- HY-P0191
-
-
- HY-P1469
-
-
- HY-P1728A
-
-
- HY-P1562
-
|
PUMA BH3
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- HY-P2318
-
|
Bac2A TFA
|
Fungal
|
|
|
Bac2A TFA is an antimicrobial and immunomodulatory peptide. Bac2A TFA is a linear variant of bactenecin and is very effective against fungal pathogens.
|
-
- HY-P1746
-
|
Protein Kinase C (19-31)
PKC (19-31)
|
PKC
|
Inflammation/Immunology
|
|
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-P0069
-
|
D-JNKI-1
AM-111; XG-102
|
JNK
|
Others
|
|
D-JNKI-1 (AM-111) is a highly potent and cell-permeable peptide inhibitor of JNK.
|
-
- HY-126488
-
-
- HY-P0173B
-
|
Chlorotoxin TFA
|
Chloride Channel
|
Cancer
|
|
Chlorotoxin TFA is a peptide isolated from the venom of the scorpion Leiurus quinquestriatus, acts as a chloride channel blocker. Anti-cancer activity.
|
-
- HY-P1388
-
-
- HY-P1462
-
-
- HY-P0313
-
|
CEF6
|
Influenza Virus
|
Infection
|
|
CEF6 is a 9-aa-long peptide corresponding to aa 418-426 of the influenza A virus (H1N1) nucleocapsid protein.
|
-
- HY-114161A
-
-
- HY-P1225
-
-
- HY-P0191A
-
-
- HY-P0263
-
-
- HY-P1746A
-
|
Protein Kinase C (19-31) (TFA)
PKC (19-31) (TFA)
|
PKC
|
Inflammation/Immunology
|
|
Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) TFA is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-P0081
-
-
- HY-17566
-
-
- HY-P0078
-
-
- HY-B0780
-
-
- HY-129360
-
-
- HY-128067
-
|
5-(N,N-Hexamethylene)-amiloride
Hexamethylene amiloride; HMA
|
Sodium Channel
HIV
Apoptosis
|
Cancer
Infection
|
|
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
|
-
- HY-P1462A
-
-
- HY-P0324
-
|
Parasin I
|
Bacterial
|
Infection
|
|
Parasin I is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
|
-
- HY-P1388A
-
-
- HY-129657
-
|
GLP-1 receptor agonist 4
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist extracted from patent WO2009111700A2, compound 87, has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.
|
-
- HY-P1854
-
|
β-Amyloid (1-9)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
|
-
- HY-P2231A
-
|
Cotadutide acetate
MEDI0382 acetate
|
Glucagon Receptor
|
Metabolic Disease
|
|
Cotadutide acetate (MEDI0382 acetate) is a potent peptide dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate (MEDI0382 acetate) exhibits ability to facilitate both weight loss and glycaemic control, has the potential for obesity and type 2 diabetes (T2D) treatment.
|
-
- HY-P1218
-
|
Phrixotoxin 3
|
Sodium Channel
|
Neurological Disease
|
|
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current[1] .
|
-
- HY-A0176
-
-
- HY-P1567
-
-
- HY-P1170
-
-
- HY-P0228A
-
-
- HY-P1244A
-
-
- HY-P0263A
-
|
Dermaseptin TFA
|
Bacterial
Fungal
|
Infection
|
|
Dermaseptin TFA, a peptide isolated from frog skin, exhibits potent antimicrobial activity against bacteria, fungi, and protozoa at micromolar concentration.
|
-
- HY-P2203
-
|
SAHM1
|
Notch
|
|
|
SAHM1 is a Notch pathway inhibitor. SAHM1 stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 targets the protein-protein interface and prevents Notch complex assembly.
|
-
- HY-P0054A
-
-
- HY-B0990
-
|
Thiostrepton
|
Bacterial
Antibiotic
|
Infection
|
|
Thiostrepton is a natural cyclic oligopeptide antibiotic, is a natural product of the ribosomally synthesized and post-translationally modified peptide (RiPP) class.
|
-
- HY-W007970
-
-
- HY-P1097
-
-
- HY-P2039
-
-
- HY-P1141
-
|
GLP-1(9-36)amide
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor.
|
-
- HY-P1468
-
|
β-Amyloid 1-28
Amyloid β-Protein (1-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-28) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-P1308
-
-
- HY-P1752
-
-
- HY-P1504
-
-
- HY-P0283
-
-
- HY-P1043A
-
|
NGR peptide Trifluoroacetate
|
Aminopeptidase
|
Cancer
|
|
NGR peptide Trifluoroacetate containing the asparagine-glycine-arginine (NGR) motif is recognized by CD13/aminopeptidase N (APN) receptor isoforms that are selectively overexpressed in tumor neovasculature.
|
-
- HY-P1333A
-
|
Dynorphin A TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-P1801
-
|
Cys-TAT(47-57)
Cys-[HIV-Tat (47-57)]
|
HIV
|
Infection
|
|
Cys-TAT(47-57) (Cys-[HIV-Tat (47-57)]) is an arginine rich cell penetrating peptide derived from the HIV-1 transactivating protein.
|
-
- HY-P1742
-
-
- HY-P1466
-
|
β-Amyloid 1-16
Amyloid β-Protein (1-16)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-16) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-P1866
-
-
- HY-P0288
-
-
- HY-108896
-
-
- HY-P0199
-
-
- HY-P1562A
-
|
PUMA BH3 TFA
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- HY-P1789
-
-
- HY-101986
-
-
- HY-U00171
-
|
SQ28603
SQ28,603; Squibb 28603
|
Neprilysin
|
Metabolic Disease
|
|
SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).
|
-
- HY-B0643
-
|
Dirithromycin
LY237216
|
Bacterial
Antibiotic
|
Infection
|
|
Dirithromycin(LY 237216) is a macrolide glycopeptide antibiotic by binding to the 50S subunit of the 70S bacterial ribosome to inhibit the translocation of peptides.
|
-
- HY-111360
-
-
- HY-P1592
-
|
G3-C12
|
Galectin
|
Cancer
|
|
G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
|
-
- HY-106268A
-
-
- HY-100200
-
|
SMER28
|
Autophagy
|
Cancer
|
|
SMER28 is a positive regulator of autophagy acting via an mTOR-independent mechanism. SMER28 prevents the accumulation of amyloid beta peptide.
|
-
- HY-14789
-
|
(R)-Elagolix
NBI-56418
|
GNRH Receptor
|
Cancer
Endocrinology
|
|
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
|
-
- HY-135859
-
|
NH2-MPAA-NODA
|
Others
|
Cancer
|
|
NH2-MPAA-NODA is a nitroveratryl-based photocleavable linker, it has a NODA motif and a methyl phenyl acetic acid (MPAA) backbone. NH2-MPAA-NODA can be used as a radiolabel by labeling with 18F-fluoride.
|
-
- HY-P0324A
-
|
Parasin I TFA
|
Bacterial
|
Infection
|
|
Parasin I (TFA) is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
|
-
- HY-P1789A
-
-
- HY-P1504A
-
-
- HY-P2323
-
-
- HY-P1866A
-
-
- HY-P1752A
-
-
- HY-112295
-
|
AzKTB
|
Others
|
Infection
|
|
AzKTB is a capture reagent which bears a short trypsin-cleavable peptide sequence between the azide module and the TAMRA/PEG-biotin labels.
|
-
- HY-101844
-
-
- HY-16664
-
-
- HY-18347A
-
-
- HY-P1029
-
-
- HY-P2004
-
|
FFAGLDD
|
MMP
|
Cancer
|
|
FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.
|
-
- HY-P1763
-
|
Urechistachykinin II
Uru-TK II
|
Bacterial
|
Infection
|
|
Urechistachykinin II (Uru-TK II), an invertebrate tachykinin-related peptides (TRPs) isolated from echiuroid worms, shows antimicrobial activities without a hemolytic effect.
|
-
- HY-P1519B
-
-
- HY-P1768
-
|
Urechistachykinin I
Uru-TK I
|
Bacterial
|
Infection
|
|
Urechistachykinin I (Uru-TK I), an invertebrate tachykinin-related peptides (TRPs) isolated from echiuroid worms, shows antimicrobial activities without a hemolytic effect.
|
-
- HY-P2203A
-
|
SAHM1 TFA
|
Notch
|
|
|
SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.
|
-
- HY-P1519
-
-
- HY-P2310
-
|
Defensin HNP-1 human
|
Endogenous Metabolite
|
|
|
Defensin HNP-1 human is a Human neutrophil peptides (HNPs), involved in endothelial cell dysfunction at the time of early atherosclerotic development.Defensin HNP-1 human can regulate the growth of atherosclerosis.
|
-
- HY-P1868
-
|
α2β1 Integrin Ligand Peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-P1308A
-
-
- HY-10340B
-
-
- HY-16141
-
|
Cilengitide
EMD 121974
|
Integrin
Autophagy
|
Cancer
|
|
Cilengitide, a cyclic RGD-containing peptide, is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50s of 4 and 79 nM, respectively.
|
-
- HY-12465
-
-
- HY-12366
-
-
- HY-10340
-
-
- HY-10340A
-
|
Tirbanibulin dihydrochloride
KX2-391 (dihydrochloride); KX-01 (dihydrochloride)
|
Src
Microtubule/Tubulin
|
Cancer
|
|
Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
|
-
- HY-110105
-
|
NS8593 hydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
|
-
- HY-110237
-
|
BX430
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-B0563C
-
|
Ropivacaine mesylate
|
Potassium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Ropivacaine mesylate is an aminoamide compound, effectively blocks neuropathic pain. Ropivacaine mesylate is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine mesylate inhibits pressure-induces lung endothelial hyperpermeability in models of acute hypertension.
|
-
- HY-116330A
-
|
Hyperforin dicyclohexylammonium salt
Hyperforin DCHA
|
TRP Channel
Calcium Channel
|
Neurological Disease
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
|
-
- HY-B0563A
-
|
Ropivacaine hydrochloride monohydrate
|
Potassium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Ropivacaine hydrochloride monohydrate is an aminoamide compound, effectively blocks neuropathic pain. Ropivacaine hydrochloride monohydrate is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine hydrochloride monohydrate inhibits pressure-induces lung endothelial hyperpermeability in models of acute hypertension.
|
-
- HY-103369
-
|
PG01
|
CFTR
|
Endocrinology
|
|
PG01 is a potent CFTR Cl - channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl - current after adding Forskolin.
|
-
- HY-12537
-
-
- HY-P1868A
-
|
α2β1 Integrin Ligand Peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-P1536
-
-
- HY-P1955
-
|
Etelcalcetide
AMG 416; KAI-4169
|
CaSR
|
Endocrinology
|
|
Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis.
|
-
- HY-P0097A
-
-
- HY-P0271
-
-
- HY-P2291
-
-
- HY-P1596
-
-
- HY-P2004A
-
|
FFAGLDD TFA
|
MMP
|
Cancer
|
|
FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.
|
-
- HY-P1955A
-
|
Etelcalcetide hydrochloride
AMG 416 hydrochloride; KAI-4169 hydrochloride
|
CaSR
|
Endocrinology
|
|
Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide hydrochloride is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis.
|
-
- HY-P1236
-
-
- HY-12946
-
|
BI 653048
|
Glucocorticoid Receptor
Cytochrome P450
HCV Protease
|
Infection
Inflammation/Immunology
|
|
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
|
-
- HY-12946A
-
|
BI 653048 phosphate
|
Glucocorticoid Receptor
Cytochrome P450
HCV Protease
|
Infection
Inflammation/Immunology
|
|
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
|
-
- HY-112544
-
|
IK1 inhibitor PA-6
PA-6
|
Potassium Channel
|
Cardiovascular Disease
|
|
IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
|
-
- HY-N6708
-
|
Alamethicin
|
Bacterial
Antibiotic
|
Infection
|
|
Alamethicin, isolated from Trichoderma viride, is a channel-forming peptide antibiotic and induces voltage-gated conductance in model and cell membranes.
|
-
- HY-130976
-
-
- HY-N1476
-
|
Heterophyllin B
|
PI3K
|
Cancer
|
|
Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer.
|
-
- HY-112999
-
-
- HY-112862
-
|
Arg-AMS
|
Aminoacyl-tRNA Synthetase
|
Others
|
|
Arg-AMS is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.
|
-
- HY-19214
-
-
- HY-P1564
-
-
- HY-P1674A
-
|
Murepavadin TFA
POL7080 TFA
|
Bacterial
Antibiotic
|
Infection
|
|
Murepavadin (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa. Murepavadin (TFA) targets the lipopolysaccharide transport portin D .
|
-
- HY-P1236A
-
-
- HY-P0107
-
-
- HY-P1263
-
-
- HY-P0271A
-
|
Syntide 2 TFA
|
CaMK
Calcium Channel
|
Neurological Disease
|
|
Syntide 2 (TFA), a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected.
|
-
- HY-P2291A
-
-
- HY-P0107B
-
-
- HY-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-P2246
-
|
JTP10-△-TATi TFA
|
JNK
|
Cancer
|
|
JTP10-△-TATi TFA is a selective JNK2 peptide inhibitor, with an IC50 of 92 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3.
|
-
- HY-P1586
-
|
HIV-1 Rev 34-50
HIV-1 rev Protein (34-50)
|
HIV
|
Infection
|
|
HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.
|
-
- HY-P1277
-
-
- HY-117819
-
|
TMP920
|
ROR
|
Inflammation/Immunology
|
|
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
|
-
- HY-16711
-
-
- HY-32709
-
|
Telcagepant
MK-0974
|
CGRP Receptor
|
Neurological Disease
|
|
Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
|
-
- HY-135717
-
|
Norbiotinamine
|
Others
|
Cancer
|
|
Norbiotinamine is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
|
-
- HY-P1350
-
|
H-Lys-Trp-Lys-OH
|
Bacterial
|
Infection
|
|
H-Lys-Trp-Lys-OH is a small molecule peptide which displays antibacterial and antiviral activities extracted from patent CN 104072579 A, Compound AMP12.
|
-
- HY-135717A
-
|
Norbiotinamine hydrochloride
|
Others
|
Cancer
|
|
Norbiotinamine hydrochloride is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
|
-
- HY-P1277A
-
-
- HY-P1263A
-
-
- HY-P1348
-
-
- HY-P0107A
-
-
- HY-112080
-
-
- HY-N2403
-
|
Dihydrolycorine
|
Others
|
Neurological Disease
|
|
Dihydrolycorine is isolated from Lycoris radiate Herb with antihypertensive and neuroprotective activities. Dihydrolycorine is an inhibitor of protein synthesis in eukarytic cells by inhibiting the peptide bone formation step.
|
-
- HY-120261
-
-
- HY-17446
-
-
- HY-P0202
-
-
- HY-B1493
-
|
Bentiromide
|
Others
|
Endocrinology
|
|
Bentiromide is a peptide that is broken down in the pancreas by chymotrypsin.
The bentiromide test is an excellent means of confirming the diagnosis of pancreatic exocrine insufficiency by outpatient test of chymotrypsin function.
|
-
- HY-P0256
-
-
- HY-P2247
-
|
JTP10-△-R9 TFA
|
JNK
|
Cancer
|
|
JTP10-△-R9 TFA is a selective JNK2 peptide inhibitor, with an IC50 of 89 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3.
|
-
- HY-P0175A
-
|
740 Y-P TFA
740YPDGFR TFA; PDGFR 740Y-P TFA
|
PI3K
Autophagy
|
Cancer
|
|
740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
|
-
- HY-107094
-
-
- HY-A0162
-
|
Quinupristin
|
Bacterial
|
Infection
|
|
Quinupristin is a streptogramin antibiotic. Quinupristin blocks peptide bond synthesis to prevent the extension of polypeptide chains and promote the detachment of incomplete protein chains in the bacterial ribosomal subunits .
|
-
- HY-P1502
-
|
β-Endorphin, human
|
Opioid Receptor
|
Neurological Disease
|
|
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
|
-
- HY-128356
-
|
SPL-410
|
Others
|
Inflammation/Immunology
|
|
SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC50 of 9 nM.
|
-
- HY-70068
-
-
- HY-12480
-
|
Lanopepden
GSK 1322322
|
Bacterial
|
Infection
|
|
Lanopepden (GSK 1322322) is a peptide deformylase inhibitor active against Staphylococcus aureus strains with MICs of 1 and 1 mg/L for ATCC 29213 and ATCC 25923 strain, respectively.
|
-
- HY-15498
-
|
Rimegepant
BMS-927711
|
CGRP Receptor
|
Neurological Disease
|
|
Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.
|
-
- HY-100529
-
|
PD150606
|
Proteasome
|
Cancer
|
|
PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.
|
-
- HY-P0222
-
|
PKI(5-24)
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-P1235A
-
-
- HY-W048688
-
|
Fmoc-Trp(Me)-OH
|
Others
|
Others
|
|
Fmoc-Trp(Me)-OH is synthesized by N-(9-Fluorenylmethoxycarbonyloxy)succinimide (Fmoc-ONSu) and 1-Methyl-Ltrypthophan and can be used for protein or peptide synthesis.
|
-
- HY-18678A
-
-
- HY-10898
-
-
- HY-19593
-
|
Nikkomycin Z
|
Fungal
Antibiotic
|
Infection
|
|
Nikkomycin Z, a nucleoside-peptide, is a selective competitive chitin synthesis inhibitor. Nikkomycin Z has antifungal effects and acts as a competitive analogue of the chitin synthase substrate UDP-N-acetylglucosamine.
|
-
- HY-76612
-
-
- HY-112606
-
|
ML-290
|
Others
|
Others
|
|
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM.
|
-
- HY-P0242
-
-
- HY-P0256A
-
-
- HY-13631E
-
-
- HY-107094A
-
-
- HY-P1602
-
|
Apidaecin IB
|
Bacterial
|
Infection
|
|
Apidaecin IB is a insect antimicrobial peptide, with minimum inhibitory concentration (MIC) values of 8 μM for E. coli (ML35, O18K1H7 and ATCC 25922).
|
-
- HY-19529
-
-
- HY-17369
-
-
- HY-P0222A
-
|
PKI(5-24) TFA
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-P1191
-
|
JIP-1(153-163)
T1-JIP
|
JNK
|
Others
|
|
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
|
-
- HY-P0242A
-
-
- 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-103286
-
|
PD176252
|
Bombesin Receptor
|
Cancer
|
|
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
|
-
- HY-P1176
-
|
NTR 368
|
Apoptosis
|
Neurological Disease
|
|
NTR 368 is a peptide derived from p75 neurotrophin receptor (p75NTR) corresponding to residues 368-381 of the human receptor. NTR 368 has helix forming propensity in the presence of micellar lipid. NTR 368 is a potent inducer of neural apoptosis.
|
-
- HY-P2289
-
|
pBD-1
|
Bacterial
|
Infection
|
|
pBD-1 is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. pBD-1 has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs.
|
-
- HY-108677
-
|
L-368,899 hydrochloride
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent.
|
-
- HY-12286
-
|
PI-1840
|
Proteasome
|
Cancer
|
|
PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
|
-
- HY-P1548
-
-
- HY-P1222
-
|
LL-37, Human
|
Bacterial
|
Infection
|
|
LL-37, Human is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, Human could help protect the cornea from infection and modulates wound healing.
|
-
- HY-P1050A
-
|
COG 133 TFA
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM.
|
-
- HY-P1548B
-
-
- HY-P2324
-
|
Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
|
|
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).
|
-
- HY-P2290
-
|
Beta-defensin 1, pig
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Beta-defensin 1, pig is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig is active against bacteria such as Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis and Candida albicans.
|
-
- HY-P1453
-
|
CMD178
|
STAT
|
Cancer
|
|
CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 also is an inhibitor of STAT5 and inhibit Treg cell development.
|
-
- HY-P1293
-
|
Conantokin G
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties.
|
-
- HY-P1191A
-
|
JIP-1(153-163) TFA
T1-JIP TFA
|
JNK
|
Others
|
|
JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
|
-
- HY-14184
-
-
- HY-P1453A
-
|
CMD178 TFA
|
STAT
|
Inflammation/Immunology
|
|
CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
|
-
- HY-P1346
-
|
APETx2
|
Sodium Channel
|
Inflammation/Immunology
Neurological Disease
|
|
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
|
-
- HY-P1303
-
|
CART(62-76)(human,rat)
|
5-HT Receptor
|
Neurological Disease
|
|
CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
|
-
- HY-100566
-
-
- HY-P1176A
-
|
NTR 368 TFA
|
Apoptosis
|
Neurological Disease
|
|
NTR 368 TFA is a peptide derived from p75 neurotrophin receptor (p75NTR) corresponding to residues 368-381 of the human receptor. NTR 368 TFA has helix forming propensity in the presence of micellar lipid. NTR 368 TFA is a potent inducer of neural apoptosis.
|
-
- HY-P1548A
-
-
- HY-P2290A
-
|
Beta-defensin 1, pig TFA
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Beta-defensin 1, pig TFA is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig TFA is active against bacteria such as Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis and Candida albicans.
|
-
- HY-P1222A
-
|
LL-37, Human TFA
|
Bacterial
|
Infection
|
|
LL-37, Human TFA is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, Human TFA could help protect the cornea from infection and modulates wound healing.
|
-
- HY-122051
-
|
AC1903
|
TRP Channel
|
Metabolic Disease
|
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.
|
-
- HY-110358
-
|
QAQ dichloride
|
Sodium Channel
|
Inflammation/Immunology
|
|
QAQ dichloride, a photoswitchable voltage-gated Nav and Kv channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain.
|
-
- HY-106916
-
|
Unoprostone
|
Potassium Channel
|
Neurological Disease
|
|
Unoprostone, a prostaglandin F2α analogs (PGAs), activates BK channels to reduce oxidative stress- and light-induced retinal cell death, and phagocytotic dysfunction. Unoprostone reduces intraocular pressure and is used topically for glaucoma or ocular hypertension.
|
-
- HY-14184A
-
-
- HY-17369B
-
|
Tirofiban
L700462; MK383
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist
Target: integrin IIb/IIIa
Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation.
|
-
- HY-12048
-
-
- HY-13987
-
-
- HY-133125
-
|
ERAP1-IN-1
|
Others
|
Inflammation/Immunology
|
|
ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates.
|
-
- HY-P1416
-
|
Foxy-5
|
Wnt
|
Cancer
|
|
Foxy-5 is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 is a WNT5A agonist and effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
|
-
- HY-P2312
-
|
Human β-defensin-3
HβD-3
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml.
|
-
- HY-P1293A
-
|
Conantokin G TFA
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties.
|
-
- HY-P2282
-
|
APTSTAT3-9R
|
STAT
|
Cancer
|
|
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
|
-
- HY-P1791
-
|
Lactoferrin (17-41)
Lactoferricin B; Lfcin B
|
Bacterial
Fungal
Apoptosis
|
Cancer
Infection
|
|
Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities.
|
-
- HY-P1303A
-
|
CART(62-76)(human,rat) TFA
|
5-HT Receptor
|
Neurological Disease
|
|
CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
|
-
- HY-P1791B
-
|
Lactoferrin (17-41) (acetate)
Lactoferricin B acetate; Lfcin B acetate
|
Bacterial
Fungal
Apoptosis
|
Cancer
Infection
|
|
Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities.
|
-
- HY-P0175
-
|
740 Y-P
740YPDGFR; PDGFR 740Y-P
|
PI3K
Autophagy
|
Cancer
|
|
740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
|
-
- HY-12080A
-
-
- HY-B1190A
-
|
Cefadroxil hydrate
BL-S 578 hydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Cefadroxil hydrate (BL-S 578 hydrate) is an orally active and first-generation cephalosporin with a broad spectrum antibacterial activity. Cefadroxil hydrate (BL-S 578 hydrate) also acts as a substrate of the peptide transporter PEPT1 and PEPT2.
|
-
- HY-12080
-
|
BX471
ZK-811752
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
|
-
- HY-N2319
-
|
Dihydroergocristine mesylate
DHEC (mesylate)
|
Amyloid-β
|
Neurological Disease
|
|
Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively.
|
-
- HY-128941
-
-
- HY-P1143
-
-
- HY-P1531
-
-
- HY-P0323
-
|
GP(33-41)
|
Arenavirus
|
Infection
|
|
GP(33-41), a 9-aa-long peptide, is the optimal sequence of the GP1 epitope of lymphocytic choriomeningitis virus, and can upregulate H-2D b molecules at the RMA-S (Db Kb) cell surface with a SC50 of 344 nM.
|
-
- HY-P1422
-
|
Spadin
|
Potassium Channel
|
Neurological Disease
|
|
Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.
|
-
- HY-P1250
-
|
RFRP-3(human)
Neuropeptide VF(124-131)(human)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca 2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.
|
-
- HY-P1050
-
|
COG 133
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM.
|
-
- HY-101116
-
-
- HY-10235
-
|
Telaprevir
VX-950
|
HCV Protease
HCV
|
Infection
|
|
Telaprevir is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide.
|
-
- HY-12220
-
|
MM-102
HMTase Inhibitor IX
|
Histone Methyltransferase
|
Cancer
|
|
MM-102 (HMTase Inhibitor IX) is a potent WDR5/MLL interaction inhibitor, achieves IC50= 2.4 nM with an estimated Ki< 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
|
-
- HY-P2307
-
|
Tat-NR2Baa
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-P1098
-
|
Ac2-26
|
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-P1382
-
|
Rac1 Inhibitor W56
|
Ras
|
|
|
Rac1 Inhibitor W56 is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.
|
-
- HY-P1954
-
|
Piscidin-1 (22-42)
|
Bacterial
|
Cancer
Infection
|
|
Piscidin-1 (22-42) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides). Piscidin-1 (22-42) has many functional usages including antibacterial, antifungal, antiviral, antiprotozoal, anticancer, immunomodulatory, and wound healing properties.
|
-
- HY-P2048A
-
|
MOTS-c(human) acetate
|
AMPK
GLUT
|
Metabolic Disease
|
|
MOTS-c(human) acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.
|
-
- HY-P1143A
-
-
- 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-16474
-
|
Relugolix
TAK-385
|
GNRH Receptor
|
Cancer
Endocrinology
|
|
Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.
|
-
- HY-P1328
-
|
TAT-14
|
Keap1-Nrf2
|
Others
|
|
TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-P7061A
-
|
ALX 40-4C Trifluoroacetate
|
CXCR
|
Infection
Endocrinology
|
|
ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
-
- HY-P1309
-
-
- HY-P7061
-
|
ALX 40-4C
|
CXCR
|
Infection
Endocrinology
|
|
ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
|
-
- HY-P1098A
-
|
Ac2-26 TFA
|
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-108795A
-
|
Albiglutide TFA
|
Glucagon Receptor
|
Metabolic Disease
|
|
Albiglutide TFA, a glucagon-like peptide (GLP)-1 mimetic, is a long acting GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus (T2DM). Albiglutide TFA is generated by the genetic fusion of a DPP-4-resistant GLP-1 dimer to human albumin.
|
-
- HY-P1422A
-
|
Spadin TFA
|
Potassium Channel
|
Neurological Disease
|
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.
|
-
- HY-P1954A
-
|
Piscidin-1 (22-42) (TFA)
|
Bacterial
|
Infection
|
|
Piscidin-1 (22-42) (TFA) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides). Piscidin-1 (22-42) (TFA) has many functional usages including antibacterial, antifungal, antiviral, antiprotozoal, anticancer, immunomodulatory, and wound healing properties.
|
-
- HY-P1382A
-
|
Rac1 Inhibitor W56 TFA
|
Ras
|
|
|
Rac1 Inhibitor W56 TFA is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 TFA selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.
|
-
- HY-P1858
-
-
- HY-106783
-
|
Polymyxin B nonapeptide
|
Bacterial
Antibiotic
|
Infection
|
|
Polymyxin B nonapeptide is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
|
-
- HY-P2343
-
|
BH3 hydrochloride
|
Apoptosis
|
Cancer
|
|
BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian.
|
-
- HY-12220A
-
|
MM-102 TFA
HMTase Inhibitor IX TFA
|
Histone Methyltransferase
|
Cancer
|
|
MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
|
-
- HY-100374
-
|
Val-Cit-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.
|
-
- HY-125976
-
|
ML233
|
Others
|
Cardiovascular Disease
|
|
ML233 is a non-peptide based potent apelin receptor (APJ) agonist (EC50=3.7 μM). ML233 displays >21-fold selective over the closely related angiotensin 1 (AT1) receptor (>79 μM).
|
-
- HY-P1978
-
|
CysHHC10
|
Bacterial
|
Infection
|
|
CysHHC10 is a synthetic antimicrobial peptide (AMP), and exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of CysHHC10 against E. coli, P. aeruginosa, S. aureus and S. epidermidis are 10.1 mM, 20.2 mM, 2.5 mM and 1.3 mM, respectively.
|
-
- HY-P1858A
-
-
- HY-P1328A
-
|
TAT-14 TFA
|
Keap1-Nrf2
|
Others
|
|
TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-106783A
-
|
Polymyxin B nonapeptide TFA
|
Bacterial
|
Infection
|
|
Polymyxin B nonapeptide TFA is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide TFA is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
|
-
- HY-14184S
-
|
Macitentan D4
ACT-064992 D4
|
Endothelin Receptor
Apoptosis
|
Cardiovascular Disease
|
|
Macitentan D4 (ACT-064992 D4) is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
|
-
- HY-111583
-
|
RXFP3/4 agonist 1
|
Others
|
Metabolic Disease
|
|
RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC50s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats.
|
-
- HY-103374
-
|
Phenserine
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
AChE
Amyloid-β
|
Neurological Disease
|
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
|
-
- HY-P2289A
-
|
pBD-1 TFA
|
Bacterial
|
Infection
|
|
pBD-1 TFA is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. pBD-1 TFA has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs.
|
-
- HY-W010041
-
|
Scyllo-Inositol
|
Amyloid-β
Endogenous Metabolite
|
Neurological Disease
|
|
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and loweres amyloid plaques in an Alzheimer's disease mouse model.
|
-
- HY-P1792A
-
|
Angiotensin II (1-4), human TFA
|
Angiotensin Receptor
|
Endocrinology
Metabolic Disease
|
|
Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-P1365
-
|
α-Conotoxin MII
α-CTxMII
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-P1792
-
|
Angiotensin II (1-4), human
|
Angiotensin Receptor
|
Metabolic Disease
Endocrinology
|
|
Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-P2320
-
|
IDR-1
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release.
|
-
- HY-P0178
-
|
LXW7
|
Integrin
|
Inflammation/Immunology
|
|
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
|
-
- HY-P1978A
-
|
CysHHC10 TFA
|
Bacterial
|
Infection
|
|
CysHHC10 TFA is a synthetic antimicrobial peptide (AMP), and exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of CysHHC10 TFA against E. coli, P. aeruginosa, S. aureus and S. epidermidis are 10.1 mM, 20.2 mM, 2.5 mM and 1.3 mM, respectively.
|
-
- HY-P1346A
-
|
APETx2 TFA
|
Sodium Channel
|
Inflammation/Immunology
Neurological Disease
|
|
APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
|
-
- 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-128945
-
|
CL2A
|
ADC Linker
|
Cancer
Inflammation/Immunology
|
|
CL2A is a claevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker.
|
-
- HY-114645
-
|
PDK1-IN-RS2
|
PDK-1
|
Cancer
|
|
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.
|
-
- HY-P1052
-
|
Myelin Basic Protein(87-99)
|
Others
|
Inflammation/Immunology
|
|
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
|
-
- HY-10119
-
|
Vorapaxar
SCH 530348
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-P2313
-
|
Human β-defensin-2
HβD-2
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-2 (HβD-2) is a small cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by a number of epithelial cells.Human β-defensin-2 has antimicrobial activity against gram-negative bacteria and Candida, but not gram-positive Staphylococcus aureus. Human β-defensin-2 can be used for the study of colitis.
|
-
- HY-P0178A
-
|
LXW7 TFA
|
Integrin
|
Inflammation/Immunology
|
|
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
|
-
- HY-P1309A
-
-
- HY-P1769
-
|
Angiotensin II (5-8), human
|
Angiotensin Receptor
|
Metabolic Disease
Endocrinology
|
|
Angiotensin II (5-8), human is an endogenous C-terminal fragment of the peptide vasoconstrictor angiotensin II. Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-128865
-
|
BPR1M97
|
Opioid Receptor
|
Neurological Disease
|
|
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.
|
-
- HY-10119A
-
|
Vorapaxar sulfate
SCH 530348 sulfate
|
Protease-Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-131180
-
|
BMS-986235
LAR-1219
|
Others
|
Cardiovascular Disease
|
|
BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure.
|
-
- HY-P1365A
-
|
α-Conotoxin MII TFA
α-CTxMII TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-P1812
-
|
AUNP-12
NP-12
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
|
-
- HY-P1649
-
|
SPR741
NAB741
|
Bacterial
Antibiotic
|
Infection
|
|
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741.
|
-
- HY-P1105
-
|
GaTx2
|
Others
|
Neurological Disease
|
|
GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types.
|
-
- HY-43869
-
|
Vipivotide tetraxetan Linker
PSMA-617 Linker
|
ADC Linker
|
Cancer
|
|
Vipivotide tetraxetan Linker (PSMA-617 Linker) is a nonclaevable peptide linker for synthesis of Vipivotide tetraxetan (PSMA-617). Vipivotide tetraxetan (PSMA-617) is a ligand used to synthesize 177Lu-PSMA-617, which is a radioactive molecule for the treatment of prostate cancer.
|
-
- HY-108625
-
|
SHA 68
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
|
-
- HY-110166
-
|
PD 90780
|
Others
|
Neurological Disease
|
|
PD 90780 is a non peptide antagonist of nerve growth factor (NGF) binding to the P75 NGF receptor, inhibits NGF-p75 NTR interaction with IC50s values of 23.1 µM and 1.8 µM in PC12 cells and PC12 nnr5 cells, respectively .
|
-
- HY-12307
-
|
(-)-Indolactam V
Indolactam V
|
PKC
|
Cancer
|
|
(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
|
-
- HY-P2307A
-
|
Tat-NR2Baa TFA
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-15536
-
|
Cebranopadol
GRT6005
|
Opioid Receptor
|
Neurological Disease
|
|
Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
|
-
- HY-P1061
-
|
Colivelin
|
STAT
Amyloid-β
|
Neurological Disease
|
|
Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
|
-
- HY-P2260
-
|
Tat-beclin 1
|
Autophagy
HIV
|
Infection
|
|
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
|
-
- HY-120006A
-
|
(rel)-AR234960
|
ERK
|
Cardiovascular Disease
|
|
(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
|
-
- HY-P1039
-
|
R18
PHCVPRDLSWLDLEANMCLP
|
Others
|
Cancer
|
|
R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.
|
-
- HY-124071
-
|
ACT-389949
|
Others
|
Inflammation/Immunology
|
|
ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders.
|
-
- HY-15023
-
|
Cligosiban
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
|
Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents.
|
-
- HY-P1812A
-
|
AUNP-12 TFA
NP-12 TFA
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
|
-
- HY-P1061A
-
|
Colivelin TFA
|
STAT
Amyloid-β
|
Neurological Disease
|
|
Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
|
-
- HY-P2260A
-
|
Tat-beclin 1 TFA
|
Autophagy
HIV
|
Infection
|
|
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
|
-
- HY-P1649A
-
|
SPR741 TFA
NAB741 TFA
|
Bacterial
Antibiotic
|
Infection
|
|
SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA.
|
-
- HY-19676
-
|
Pralnacasan
VX-740; HMR 3480
|
Caspase
|
Inflammation/Immunology
|
|
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
|
-
- HY-15039
-
|
SSR240612
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
|
-
- HY-18962
-
|
AMI-1
|
Histone Methyltransferase
|
Cancer
|
|
AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
|
-
- HY-108466
-
|
Ro 08-2750
|
Apoptosis
|
Cancer
Neurological Disease
|
|
Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 µM. Ro 08-2750 inhibits NGF binding to p75 NTR selectively over TRKA. Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM.
|
-
- HY-B0290A
-
|
Pranlukast hemihydrate
ONO-1078 hemihydrate
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-B0290
-
|
Pranlukast
ONO-1078
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-P1906
-
|
[pThr3]-CDK5 Substrate
|
CDK
|
Neurological Disease
|
|
[pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM.
|
-
- HY-P1135A
-
|
M1145 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
M1145 TFA, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 TFA shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 TFA has an additive effect on the signal transduction of galanin.
|
-
- HY-103080
-
|
CMF019
|
Others
|
Cardiovascular Disease
|
|
CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin.
|
-
- HY-18962A
-
|
AMI-1 free acid
|
Histone Methyltransferase
|
Cancer
|
|
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
|
-
- HY-N0061
-
|
Ethyl ferulate
|
Reactive Oxygen Species
|
Neurological Disease
|
|
Ethyl ferulate, a naturally lipophilic derivative of ferulic acid originally derived from giant fennel (F. communis), induces heme oxygenase-1 (HO-1) and protects rat neurons against oxidative stress. Ethyl ferulate also protects neurons against amyloid β peptide (1-42)-induced oxidative stress and neurotoxicity.
|
-
- HY-P1906A
-
|
[pThr3]-CDK5 Substrate TFA
|
CDK
|
Neurological Disease
|
|
[pThr3]-CDK5 Substrate TFA is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM.
|
-
- HY-100383
-
|
BH3I-1
BHI1; BH 3I1
|
Bcl-2 Family
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
|
-
- HY-Y0265
-
|
Isatin
Indoline-2,3-dIone
|
Monoamine Oxidase
Apoptosis
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM). Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity. Shows effect on the serotonergic system.
|
-
- HY-16908A
-
|
Lefamulin acetate
BC-3781 acetate
|
Bacterial
Antibiotic
|
Infection
|
|
Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment. Lefamulin acetate (BC-3781 acetate) is the first semi-synthetic pleuromutilin for systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer.
|
-
- HY-135773
-
-
- HY-P1723A
-
|
Spexin TFA
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
|
|
|
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
|
-
- HY-P1205A
-
|
MCH(human, mouse, rat) TFA
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
MCH (human, mouse, rat) TFA is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
|
-
- HY-P1205
-
|
MCH(human, mouse, rat)
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
|
-
- HY-106994
-
|
Nebentan free base
YM598 free base
|
Endothelin Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
|
-
- HY-N2346
-
|
Tubulysin E
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin E is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin E is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-N7049
-
|
Tubulysin F
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin F is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin F is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-N7052
-
|
Tubulysin I
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin I is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-P1649B
-
|
SPR741 acetate
NAB741 acetate
|
Bacterial
Antibiotic
|
Infection
|
|
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate.
|
-
- HY-N7050
-
|
Tubulysin G
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin G is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin G is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-N2347
-
|
Tubulysin C
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin C is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin C is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-N2359
-
|
Chelerythrine
|
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
|
-
- HY-101764
-
|
Lintitript
SR 27897
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin.
|
-
- HY-N1243
-
|
Tubulysin B
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties.Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-N7053
-
|
Tubulysin M
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin M is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin M is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-101283
-
|
HCH6-1
|
Others
|
Inflammation/Immunology
|
|
HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1), an emerging therapeutic target for the discovery of drugs to treat neutrophilic inflammatory diseases. HCH6-1 is a selective FPR1 inhibitor and has protective effects against acute lung injury (ALI). HCH6-1 inhibits superoxide anion generation, elastase release, and chemotaxis in human neutrophils activated by fMLF (an FPR1 agonist).
|
-
- HY-N7051
-
|
Tubulysin H
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin H is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin H is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-N6680
-
|
Virginiamycin S1
|
Bacterial
Antibiotic
|
Infection
|
|
Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections[1][2].
|
-
- HY-101202
-
|
SNC80
NIH 10815
|
Opioid Receptor
|
Neurological Disease
|
|
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.
|
-
- HY-P1135
-
|
M1145
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
M1145, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 has an additive effect on the signal transduction of galanin.
|
-
- HY-107380A
-
|
PGlu-3-methyl-His-Pro-NH2 TFA
A-42872 TFA
|
Others
|
Endocrinology
|
|
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.
|
-
- HY-127090
-
|
Muramyl dipeptide
MDP
|
p38 MAPK
ERK
JNK
|
Inflammation/Immunology
|
|
Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide is an inducer of bone formation through induction of Runx2. Muramyl dipeptide directly enhances osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide indirectly attenuates osteoclast differentiation through a decreased RANKL/OPG ratio.
|
-
- HY-P1723
-
|
Spexin
Neuropeptide Q
|
Neuropeptide Y Receptor
|
|
|
Spexin is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin exhibits no significant activity at galanin receptor 1. Spexin is an endogenous satiety-inducing peptide; Spexin inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin attenuates LH secretion in goldfish. Spexin exhibits anxiolytic effects in vivo.
|
-
- HY-P0165
-
|
Taspoglutide
ITM077; R1583; BIM51077
|
Glucagon Receptor
|
Metabolic Disease
|
|
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM. Sequence: His-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-{Aib}-Arg-NH2.
|
-
- 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-120944
-
|
BAY-7598
|
MMP
|
Inflammation/Immunology
|
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
|
-
- HY-14743B
-
|
Golotimod hydrochloride
SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
|
|
Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
|
-
- HY-107691
-
|
GR 159897
|
Neurokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
|
-
- HY-P1695
-
|
Cinnamycin
Ro 09-0198
|
Bacterial
Antibiotic
|
|
|
Cinnamycin is tetracyclic lantibiotic produced from S. cinnamoneus that contains four unusual amino acids: erythro-β-hydroxyaspartic acid, mesolanthionine, threo-β-methyllanthionine, and lysinoalanine.1 Cinnamycin has demonstrated antiviral activity against herpes simplex virus type 1 KOS strain infection in Vero cells via a cytopathic effect reduction assay. Cinnamycin recognizes the structure of phosphatidylethanolamine and forms an equimolar complex with the phospholipid on biological membranes. This peptide has been used as a probe for analyzing the transbilayer movement of phosphatidylethanolamine.
|
-
- HY-13803C
-
|
Tazemetostat hydrobromide
EPZ-6438 hydrobromide; E-7438 hydrobromide
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-13803A
-
|
Tazemetostat trihydrochloride
EPZ-6438 trihydrochloride; E-7438 trihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-125837A
-
|
MS31 trihydrochloride
|
Epigenetic Reader Domain
|
Cancer
|
|
MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.
|
-
- HY-125837
-
|
MS31
|
Epigenetic Reader Domain
|
Cancer
|
|
MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells.
|
-
- 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-14743A
-
|
Golotimod TFA
SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
|
|
Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
|
-
- HY-14743
-
|
Golotimod
SCV 07; Gamma-D-glutamyl-L-tryptophan
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
|
|
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
|
-
- HY-13803
-
|
Tazemetostat
EPZ-6438; E-7438
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-101117
-
|
EED226
|
Histone Methyltransferase
|
Cancer
|
|
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
|
-
- HY-125728
-
|
Micrococcin P1
|
Bacterial
Parasite
HCV
|
Infection
|
|
Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor with an EC50 range of 0.1-0.5 μM. Micrococcin P1 has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Micrococcin P1 against S. aureus 1974149, E. faecalis 1674621 and S. pyogenes 1744264 are 2 μg/mL, 1 μg/mL and 1 μg/mL, respectively. Micrococcin P1 is also a potent inhibitor of the malaria parasite Plasmodium falciparum.
|
-
- HY-14994
-
|
SCH79797 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-P1404
-
|
R8-T198wt
|
Pim
|
|
|
R8-T198wt is a cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. R8-T198wt inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. R8-T198wt also inhibits Pim-1-dependent growth of DU145 cells in vitro and in vivo. R8-T198wt displays no effect on the growth of normal prostate epithelial RPWE-1 cells at concentrations of 10 and 20 μM.
|
-
- HY-128946
-
|
CL2A-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
Inflammation/Immunology
|
|
CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
|
-
- HY-108556
-
|
RWJ-56110
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessel in vivo. RWJ-56110 induces cell apoptosis.
|
-
- HY-P1110
-
|
AF12198
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
|
-
- HY-P1750
-
|
Shepherdin (79-87)
|
HSP
Survivin
|
Cancer
|
|
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity.
|
-
- HY-A0182A
-
-
- HY-P1440A
-
|
BeKm-1 TFA
|
Potassium Channel
|
|
|
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.
|
-
- HY-P1467A
-
-
- HY-128434
-
-
- HY-P1267
-
|
α-Conotoxin PnIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-P1314
-
-
- HY-P1449
-
|
Boc-Gly-Gly-Phe-Gly-OH
|
ADC Linker
|
Cancer
|
|
Boc-Gly-Gly-Phe-Gly-OH, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC).
|
-
- HY-P1076A
-
|
CALP2 TFA
|
Calcium Channel
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
|
-
- HY-P1335
-
|
CTAP
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID).
|
-
- HY-P1067
-
-
- HY-P1474
-
|
β-Amyloid (22-35)
Amyloid β-Protein (22-35)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-P1435A
-
|
NoxA1ds TFA
|
NADPH Oxidase
|
|
|
NoxA1ds TFA is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds TFA inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.
|
-
- HY-P1268A
-
|
α-Conotoxin PIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-P1846
-
|
Jagged-1 (188-204)
|
Notch
|
Cancer
|
|
Jagged-1 (188-204) is a fragment of the Jagged-1 (JAG-1) protein. JAG-1 is a Notch ligand highly expressed in cultured and primary multiple myeloma (MM) cells. JAG-1 induces maturation of monocyte-derived human dendritic cells.
|
-
- HY-P1869
-
-
- HY-P1260
-
-
- HY-P1294A
-
-
- HY-P0289
-
|
CEF3
|
Influenza Virus
|
Infection
|
|
CEF3 (SIIPSGPLK) corresponds to aa 13-21 of the influenza A virus M1 protein. The matrix (M1) protein of influenza A virus is a multifunctional protein that plays essential structural and functional roles in the virus life cycle.
|
-
- HY-P1483
-
-
- HY-P1568
-
|
Flagelin 22
Flagellin 22
|
Bacterial
|
Infection
|
|
Flagelin 22 (Flagellin 22), a fragment of bacterial flagellin, is an effective elicitor in both plants and algae.
|
-
- HY-P1390A
-
|
d[Cha4]-AVP TFA
|
Vasopressin Receptor
|
|
|
d[Cha4]-AVP TFA is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP TFA stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
|
-
- HY-P1428A
-
|
RFRP-1(human) TFA
|
Neuropeptide Y Receptor
|
|
|
RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-P0002A
-
-
- HY-P1198A
-
-
- HY-P0184
-
-
- HY-P1717B
-
|
AMY-101 acetate
Cp40 acetate
|
Complement System
SARS-CoV
|
Inflammation/Immunology
|
|
AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
|
-
- HY-P1375A
-
|
[D-Trp7,9,10]-Substance P TFA
|
mAChR
|
|
|
[D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-P1483A
-
-
- HY-P1525A
-
-
- HY-P2242A
-
-
- HY-P1420
-
|
TAT-cyclo-CLLFVY
|
HIF/HIF Prolyl-Hydroxylase
|
|
|
TAT-cyclo-CLLFVY is a selective HIF-1 dimerization inhibitor. TAT-cyclo-CLLFVY blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50=1.3 μM). TAT-cyclo-CLLFVY inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY also reduces tubularization of hypoxic HUVECs.
|
-
- HY-P1533
-
-
- HY-P0172A
-
|
ATI-2341 TFA
|
CXCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
|
-
- HY-P1091
-
|
Hemopressin (human, mouse)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.
|
-
- HY-P1081
-
-
- HY-P1215
-
-
- HY-P0108
-
-
- HY-P1537
-
-
- HY-P0079
-
-
- HY-P0298
-
-
- HY-P1485A
-
-
- HY-P1505A
-
-
- HY-P0121
-
|
ReACp53
|
MDM-2/p53
|
Cancer
|
|
ReACp53 could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.
|
-
- HY-P1887
-
|
p5 Ligand for Dnak and DnaJ
|
HSP
|
Infection
|
|
p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ.
|
-
- HY-P1126
-
|
Dolastatin 15
DLS 15
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin.
|
-
- HY-P1340A
-
-
- HY-P1106A
-
|
K41498 TFA
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively hypotension. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
|
-
- HY-P0062
-
|
Ziconotide
|
Calcium Channel
|
Neurological Disease
|
|
Ziconotide is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.
|
-
- HY-P1276A
-
-
- HY-P1017
-
-
- HY-P1749
-
-
- HY-P7060
-
|
NT 13
TPPT
|
iGluR
|
Neurological Disease
|
|
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.
|
-
- HY-P1204A
-
|
[Ala17]-MCH TFA
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
[Ala17]-MCH TFA, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu 3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.
|
-
- HY-P1337
-
-
- HY-P0251
-
-
- HY-P1441
-
|
Mambalgin 1
|
Sodium Channel
|
|
|
Mambalgin 1 is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 binds to closed/inactive channel. Mambalgin 1 is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
|
-
- HY-P1216A
-
|
HS014 TFA
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
|
-
- HY-W016887
-
-
- HY-P1377
-
-
- HY-P1582
-
|
ACTH (1-14)
Adrenocorticotropic Hormone Fragment 1-14
|
Adrenergic Receptor
|
Cancer
|
|
ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
|
-
- HY-P0035
-
-
- HY-P2093
-
|
S961
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
|
-
- HY-P1180A
-
-
- HY-P0252
-
-
- HY-P1317
-
-
- HY-P0297
-
-
- HY-P1031
-
-
- HY-P1297
-
|
CRF(6-33)(human)
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect.
|
-
- HY-P1073
-
|
ProTx-I
|
Calcium Channel
Sodium Channel
Potassium Channel
|
Cancer
|
|
ProTx-I, a venom toxin of the tarantula Thrixopelma pruriens, is a potent, selective CaV3.1 channel blocker with IC50 values of 0.2 μM and 31.8 μM for hCaV3.1 and hCaV3.2 respectively. ProTx-I is also a potent blocker for voltage-gated Na + channels and inhibits KV 2.1 channels.
|
-
- HY-P0177
-
-
- HY-P2266
-
|
SAH-EZH2
|
Histone Methyltransferase
|
|
|
SAH-EZH2 is an EZH2/EPP interaction inhibitor (Kd = 320 nM). SAH-EZH2 suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. SAH-EZH2 arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.
|
-
- HY-P2286
-
|
D-3
|
Phosphatase
|
|
|
D-3 is a selective PSC eliminating agent, inducing toxicity in cultured iPSCs and ESCs after 1 h of incubation, via an alkaline phosphatase-dependent mechanism.
|
-
- HY-P2259
-
|
TAT-GluA2 3Y
|
iGluR
|
|
|
TAT-GluA2 3Y is an inhibitor of AMPA receptor endocytosis. TAT-GluA2 3Y induces increased hind paw withdrawal latencies following thermal and mechanical stimuli in rats. TAT-GluA2 3Y also exhibits antinociceptive effects in a rat model of neuropathic pain. TAT-GluA2 3Y rescues pentobarbital-induced memory retrieval deficits in a rat model of learning and memory.
|
-
- HY-P1470
-
-
- HY-P1103
-
|
CTCE-9908
|
CXCR
|
Cancer
|
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, inhibits migration and induces cytotoxicity in CXCR4-expressing ovarian cancer cells.
|
-
- HY-P1485
-
-
- HY-P1012A
-
-
- HY-100866A
-
|
F1324 TFA
|
Bcl-2 Family
|
Cancer
|
|
F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
|
-
- HY-P2336
-
|
CCZ01048
|
Melanocortin Receptor
|
Cancer
|
|
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma.
|
-
- HY-P1298A
-
|
Sauvagine TFA
|
CRFR
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
|
-
- HY-P1077A
-
|
CALP1 TFA
|
Calcium Channel
mGluR
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.
|
-
- HY-P1932
-
-
- HY-101399
-
|
γ-Glu-Phe
γ-Glutamylphenylalanine
|
Endogenous Metabolite
|
Others
|
|
γ-Glu-Phe (γ-Glutamylphenylalanine) is synthesized by Bacillus amyloliquefaciens (GBA) and Aspergillus oryzae (GAO). γ-Glu-Phe or the post-enzymatic reaction mixture enhances the umami intensity of commercial soy sauce and model chicken broth.
|
-
- HY-P1160
-
-
- HY-P1542
-
|
Urotensin I
Catostomus urotensin I
|
CRFR
|
Cardiovascular Disease
Endocrinology
|
|
Urotensin I is, 41-aa neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively.
|
-
- HY-P1380A
-
|
Difopein TFA
|
Apoptosis
|
Cancer
|
|
Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells.
|
-
- HY-P1216
-
|
HS014
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
|
-
- HY-P1477
-
-
- HY-P1558
-
-
- HY-P1189
-
|
Echistatin
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-P1175A
-
-
- HY-13581A
-
-
- HY-P1268
-
|
α-Conotoxin PIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-P1850
-
-
- HY-P1252A
-
-
- HY-P1209
-
-
- HY-P2274
-
|
Argifin
|
Parasite
|
Infection
|
|
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively.
|
-
- HY-19870A
-
-
- HY-P2285
-
|
AC 253
|
Amyloid-β
|
|
|
AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
|
-
- HY-P1539
-
-
- HY-B2196
-
-
- HY-P1424
-
|
Lei-Dab7
|
Potassium Channel
|
|
|
Lei-Dab7 is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
|
-
- HY-P1132A
-
-
- HY-136563
-
|
RA375
|
Proteasome
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.
|
-
- HY-P1296
-
|
Urocortin, rat
Urocortin (Rattus norvegicus); Rat urocortin
|
CRFR
|
Neurological Disease
Endocrinology
|
|
Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.
|
-
- HY-P1316
-
|
Ac-RYYRWK-NH2
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
|
-
- HY-P1103A
-
|
CTCE-9908 TFA
|
CXCR
|
Cancer
|
|
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, inhibits migration and induces cytotoxicity in CXCR4-expressing ovarian cancer cells.
|
-
- HY-P0054
-
-
- HY-P0188A
-
-
- HY-P2276
-
|
Pep2-8
|
Ser/Thr Protease
|
|
|
Pep2-8 is a proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor, with an IC50 of 0.8 μM for PCSK9 binding to LDL receptor.
|
-
- HY-108742A
-
|
Abaloparatide TFA
BA 058 TFA; BIM 44058 TFA
|
Thyroid Hormone Receptor
|
Metabolic Disease
Endocrinology
|
|
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue selected to be a potent and selective activator of the PTHR1 signaling pathway. Abaloparatide TFA enhances Gs/cAMP signaling (EC50 of 0.3 nM) and β-arrestin recruitment (EC50 of 0.9 nM) in MC3T3-E1 osteoblast cells.
|
-
- HY-P1302A
-
|
Orphanin FQ(1-11) TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice.
|
-
- HY-P1194A
-
|
Spantide I TFA
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
|
-
- HY-P1127
-
-
- HY-P1184
-
-
- HY-P1060A
-
-
- HY-P1505
-
-
- HY-P1022A
-
|
Kisspeptin-54(human) TFA
Metastin(human) TFA
|
GNRH Receptor
|
Cancer
Endocrinology
|
|
Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion.
|
-
- HY-P0073
-
-
- HY-P1260A
-
-
- HY-P1320A
-
|
[Nphe1]Nociceptin(1-13)NH2 TFA
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
|
-
- HY-P1488
-
-
- HY-106224
-
|
Orexin A (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-P2108
-
|
Lysobactin
|
Antibiotic
Bacterial
|
Infection
|
|
Lysobactin, produced by several genera of Gram-negative gliding bacteria found in soil, is a potent antibiotic with in vivo efficacy against Staphylococcus aureus and Streptococcus pneumoniae.
|
-
- HY-P1022
-
|
Kisspeptin-54(human)
Metastin(human)
|
GNRH Receptor
|
Cancer
Endocrinology
|
|
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion.
|
-
- HY-P0198A
-
-
- HY-P1200A
-
|
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA
|
Src
|
Cancer
|
|
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions.
|
-
- HY-P1301
-
|
[Arg14,Lys15]Nociceptin
|
Opioid Receptor
|
Neurological Disease
|
|
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
|
-
- HY-P1415
-
|
Norleual
|
c-Met/HGFR
|
|
|
Norleual is an angiotensin IV analog. Norleual is a highly potent HGF/c-MET inhibitor (IC50=3 pM). Norleual inhibits HGF-induced MDCK cell proliferation and invasion in vitro. Norleual also is an AT4 receptor antagonist; disrupts LTP stabilization. Antiangiogenic.
|
-
- HY-P1424A
-
|
Lei-Dab7 TFA
|
Potassium Channel
|
|
|
Lei-Dab7 TFA is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
|
-
- HY-P1102A
-
|
TC14012 TFA
|
CXCR
HIV
|
Cancer
Infection
|
|
TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity.
|
-
- HY-P1441A
-
|
Mambalgin 1 TFA
|
Sodium Channel
|
|
|
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
|
-
- HY-103048A
-
|
PD-1/PD-L1-IN 3 TFA
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN 3 TFA is a PD-1/PD-L1 interaction inhibitor extracted from patent WO2014151634A1, compound 1. PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.
|
-
- HY-P1420A
-
|
TAT-cyclo-CLLFVY TFA
|
HIF/HIF Prolyl-Hydroxylase
|
|
|
TAT-cyclo-CLLFVY TFA is a selective HIF-1 dimerization inhibitor. TAT-cyclo-CLLFVY TFA blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50=1.3 μM). TAT-cyclo-CLLFVY TFA inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY TFA also reduces tubularization of hypoxic HUVECs.
|
-
- HY-P1492
-
-
- HY-P0086
-
-
- HY-100563A
-
-
- HY-P1064A
-
|
Apelin-36(human) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-P2329
-
-
- HY-P1016A
-
-
- HY-P0231
-
-
- HY-P1060
-
|
LPYFD-NH2
|
Amyloid-β
|
Neurological Disease
|
|
LPYFD-NH2, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 can be used for the research of Alzheimer’s disease.
|
-
- HY-100866B
-
|
F1324 acetate
|
Bcl-2 Family
|
Cancer
|
|
F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
|
-
- HY-P1506
-
-
- HY-P2228
-
|
Chlamydocin
|
HDAC
Apoptosis
|
Cancer
|
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
|
-
- HY-P1780
-
|
CEF20
|
CMV
|
Infection
|
|
CEF20 is an HLA-A*0201-restricted epitope from cytomegalovirus pp65 (495-503).
|
-
- HY-P1112A
-
-
- HY-P2344
-
-
- HY-41189
-
-
- HY-P1187A
-
|
HSDVHK-NH2 TFA
|
Integrin
|
Cancer
|
HSDVHK-NH2 TFA is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
|
-
- HY-P1762A
-
-
- HY-P1175
-
-
- HY-P1209A
-
-
- HY-P1090
-
|
Hemopressin(rat)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.
|
-
- HY-P2076
-
|
Dusquetide
SGX942
|
Bacterial
|
Cancer
Infection
|
|
Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
|
-
- HY-P2267
-
|
LDV
|
Integrin
|
|
|
LDV, a non-fluorescent derivative of LDV FITC, is a α4β1 integrin (VLA-4) ligand (Kd ~ 12 nM).
|
-
- HY-P1163A
-
|
D[LEU4,LYS8]-VP TFA
|
Vasopressin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
|
-
- HY-P0063
-
|
Copper tripeptide
GHK-Cu
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Copper tripeptide (GHK-Cu), a naturally occurring tripeptide, is first isolated from human plasma, but can be found in saliva and urine. During wound healing, Copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a Natural Modulator of Multiple Cellular Pathways in Skin Regeneration.
|
-
- HY-P1076
-
|
CALP2
|
Calcium Channel
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
|
-
- HY-P0205B
-
-
- HY-P1437A
-
|
Neuropeptide S(Mouse) TFA
|
Neuropeptide Y Receptor
|
|
|
Neuropeptide S(Mouse) TFA is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) TFA induces mobilization of intracellular Ca 2+. Neuropeptide S(Mouse) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) TFA also reduces anxiety-like behavior in mice.
|
-
- HY-P1306
-
|
Obestatin(rat)
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-P2080
-
|
GIP (1-30) amide,Human
|
Glucagon Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,Human is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide (Human) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M.
|
-
- HY-P1012
-
-
- HY-P2287
-
|
Cortagine
|
CRFR
|
Neurological Disease
|
|
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
|
-
- HY-P2036
-
|
FSL-1
|
Toll-like Receptor (TLR)
Antibiotic
|
Infection
|
|
FSL-1 is a TLR2/6 agonist (also a putative TLR10 ligand). FSL-1 activates NF-κB. FSL-1 induces pro-inflammatory cytokines including IL-8, IL-1β, CCL20 and TNF-α in vitro. FSL-1 synergizes with IFNγ to induce CXCL10 release from melanoma cells.
|
-
- HY-P0210B
-
-
- HY-P1799
-
|
[pTyr5] EGFR (988-993)
|
Phosphatase
|
Others
|
|
[pTyr5] EGFR (988-993) is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B).
|
-
- HY-P1479
-
-
- HY-P1528
-
-
- HY-P1010A
-
-
- HY-P1846A
-
|
Jagged-1 (188-204) (TFA)
|
Notch
|
Cancer
|
|
Jagged-1 (188-204) TFA is a fragment of the Jagged-1 (JAG-1) protein. JAG-1 is a Notch ligand highly expressed in cultured and primary multiple myeloma (MM) cells. JAG-1 induces maturation of monocyte-derived human dendritic cells.
|
-
- HY-P2233
-
|
Globomycin
|
Bacterial
|
Infection
|
|
Globomycin is a lipopeptide antibiotic and a signal peptidase II (LspA) inhibitor. Globomycin inhibits processing of the prolipoprotein by binding irreversibly to the peptidase. Globomycin has toxic for the mollicute Spiroplasma melliferum with a MIC in the range 6.25-12.5 μM.
|
-
- HY-P1588
-
-
- HY-P0201A
-
-
- HY-P1081A
-
-
- HY-P0036
-
-
- HY-P0298A
-
-
- HY-P1607
-
-
- HY-P1474A
-
|
β-Amyloid (22-35) (TFA)
Amyloid β-Protein (22-35) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-P1065A
-
|
Apelin-36(rat, mouse) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-P1449A
-
-
- HY-P1335A
-
|
CTAP TFA
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).
|
-
- HY-P1189A
-
|
Echistatin TFA
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-106224A
-
|
Orexin A (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-P1192
-
-
- HY-P1194
-
|
Spantide I
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
|
-
- HY-P0273
-
-
- HY-P1149A
-
|
Epithalon TFA
|
Telomerase
|
Cancer
Neurological Disease
|
|
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa.
|
-
- HY-P1217A
-
|
[D-Trp8]-γ-MSH TFA
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
[D-Trp8]-γ-MSH TFA is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH TFA could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis[1] [2] .
|
-
- HY-P1202A
-
|
CYN 154806 TFA
|
Somatostatin Receptor
|
Endocrinology
|
|
CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
|
-
- HY-P1525
-
-
- HY-P0234
-
-
- HY-P0299
-
|
LSKL, Inhibitor of Thrombospondin (TSP-1)
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.
|
-
- HY-P0295
-
|
Gly-Arg-Gly-Asp-Ser
|
Integrin
|
Others
|
|
Gly-Arg-Gly-Asp-Ser is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM
|
-
- HY-P0265
-
-
- HY-100538A
-
|
DTP3 TFA
|
DNA/RNA Synthesis
JNK
|
Cancer
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
|
-
- HY-P1437
-
|
Neuropeptide S(Mouse)
|
Neuropeptide Y Receptor
|
|
|
Neuropeptide S(Mouse) is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) induces mobilization of intracellular Ca 2+. Neuropeptide S(Mouse) increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) also reduces anxiety-like behavior in mice.
|
-
- HY-P0031
-
|
Cyclo(RADfK)
|
Integrin
|
Others
|
|
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis.
|
-
- HY-P1717A
-
|
AMY-101 TFA
Cp40 TFA
|
Complement System
SARS-CoV
|
Inflammation/Immunology
|
|
AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
|
-
- HY-P1180
-
-
- HY-P1156
-
-
- HY-P1291
-
|
PKI 14-22 amide,myristoylated
|
PKA
|
Cancer
|
|
PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
|
-
- HY-P1269A
-
-
- HY-P1339A
-
-
- HY-P1114A
-
|
2B-(SP) (TFA)
|
GSK-3
|
Cancer
|
|
2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3.
|
-
- HY-P1532
-
-
- HY-P1206A
-
|
CH 275 TFA
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 TFA is a potent and selective somatostatin receptor 1 (sst1) agonist and display IC50 values of 30.9 nM, 345 nM, >1 μM, >10 μM for human human sst1, sst3, sst4, sst2 and sst5 respectively. CH 275 can be used for the research of Alzheimer’s disease.
|
-
- HY-P1079
-
|
ω-Agatoxin TK
|
Calcium Channel
|
Neurological Disease
|
|
ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca 2+ channel blocker. ω-Agatoxin TK inhibits the high K + depolarisation-induced rise in internal Ca 2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels.
|
-
- HY-P2080B
-
|
GIP (1-30) amide,Human acetate
|
Glucagon Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,Human acetate is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide (Human) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M.
|
-
- HY-P2336A
-
|
CCZ01048 TFA
|
Melanocortin Receptor
|
Cancer
|
|
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma.
|
-
- HY-P2036A
-
|
FSL-1 TFA
|
Toll-like Receptor (TLR)
Antibiotic
|
Infection
|
|
FSL-1 TFA is a TLR2/6 agonist (also a putative TLR10 ligand). FSL-1 TFA activates NF-κB. FSL-1 TFA induces pro-inflammatory cytokines including IL-8, IL-1β, CCL20 and TNF-α in vitro. FSL-1 TFA synergizes with IFNγ to induce CXCL10 release from melanoma cells.
|
-
- HY-P1319
-
|
Nociceptin(1-7)
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.
|
-
- HY-19870B
-
-
- HY-P1091A
-
|
Hemopressin(human, mouse) TFA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.
|
-
- HY-P2344A
-
-
- HY-P1727A
-
|
Super-TDU TFA
|
YAP
|
Cancer
|
|
Super-TDU TFA is a specific YAP antagonist therapy against gastric cancer targeting YAP-TEADs interaction.
|
-
- HY-P2123A
-
-
- HY-P1009
-
|
Z-YVAD-FMK
|
Caspase
|
Cancer
|
|
AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.
|
-
- HY-P0172
-
|
ATI-2341
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
|
-
- HY-P0299A
-
|
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
|
-
- HY-P1682A
-
|
Balixafortide TFA
POL6326 TFA
|
CXCR
|
Cancer
|
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
|
-
- HY-P1066A
-
|
Apelin-17(human, bovine) TFA
|
HIV
|
Infection
|
|
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-P1533A
-
-
- HY-P0089
-
-
- HY-P2328
-
-
- HY-P0300
-
-
- HY-P1064
-
|
Apelin-36(human)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
|
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-100866
-
|
F1324
|
Bcl-2 Family
|
Cancer
|
|
F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
|
-
- HY-P1390
-
|
d[Cha4]-AVP
|
Vasopressin Receptor
|
|
|
d[Cha4]-AVP is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
|
-
- HY-P1440
-
|
BeKm-1
|
Potassium Channel
|
|
|
BeKm-1 is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 dose-dependently prolongs QTc interval in isolated rabbit heart.
|
-
- HY-P0219
-
|
Microcystin-LA
|
Phosphatase
|
Cancer
|
|
Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.
|
-
- HY-P1068
-
|
Lysozyme
Muramidase
|
Bacterial
|
Infection
|
|
Lysozyme is an antimicrobial enzyme produced by animals that forms part of the innate immune system.
|
-
- HY-P1578A
-
-
- HY-P1318
-
|
Ac-RYYRIK-NH2
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-106178
-
|
PMX-53
3D53
|
Complement System
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.
|
-
- HY-P1852
-
-
- HY-P1300
-
-
- HY-P1423A
-
|
BA 1 TFA
|
Bombesin Receptor
|
|
|
BA 1 TFA is a potent bombesin receptor agonist (IC50 values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). BA 1 TFA enhances glucose transport in obese and diabetic primary myocytes. BA 1 TFA also stimulates NCI-H1299 lung cancer cell proliferation in vitro.
|
-
- HY-P1163
-
|
D[LEU4,LYS8]-VP
|
Vasopressin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
|
-
- HY-P1295
-
|
Urocortin, human
Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I
|
CRFR
|
Neurological Disease
Endocrinology
|
|
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
|
-
- HY-105240
-
|
Delparantag
PMX-60056
|
Factor Xa
|
Cardiovascular Disease
|
|
Delparantag (PMX-60056) is a salicylamide derivative and an effective unfractionated heparin (UFH) and low molecular weight heparin (LMWH) reversing agent. Delparantag shows ability to neutralize the anticoagulation and bleeding effects of UFH and LMWH.
|
-
- HY-P1072
-
|
PHM-27 (human)
|
CGRP Receptor
|
Metabolic Disease
Cardiovascular Disease
|
|
PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.
|
-
- HY-P1321
-
|
GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
|
-
- HY-B2237
-
-
- HY-P1167A
-
-
- HY-P0049
-
|
Argipressin
Vasopressin; Arg8-vasopressin; AVP
|
Vasopressin Receptor
|
Neurological Disease
|
|
Argipressin binds to the V1, V2, V3-vascular arginine vasopressin receptor, with a Kd value of 1.31 nM in A7r5 rat aortic smooth muscle cells for V1. Argipressin is a selective V2 agonist.
|
-
- HY-P0184A
-
-
- HY-P0236
-
-
- HY-P1269
-
|
α-Conotoxin AuIB
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
|
-
- HY-P0197
-
-
- HY-P0226
-
-
- HY-P1428
-
|
RFRP-1(human)
|
Neuropeptide Y Receptor
|
|
|
RFRP-1(human) is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-P1340
-
-
- HY-P1405
-
-
- HY-P1435
-
|
NoxA1ds
|
NADPH Oxidase
|
|
|
NoxA1ds is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.
|
-
- HY-P1755
-
-
- HY-P1438A
-
|
Neuropeptide S(Rat) TFA
|
Neuropeptide Y Receptor
|
|
|
Neuropeptide S(Rat) TFA is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) TFA also reduces anxiety-like behavior in mice.
|
-
- HY-P1840
-
-
- HY-P0183
-
-
- HY-P1682
-
|
Balixafortide
POL6326
|
CXCR
|
Cancer
|
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
|
-
- HY-P0055A
-
-
- HY-P1206
-
|
CH 275
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 is a potent and selective somatostatin receptor 1 (sst1) agonist and display IC50 values of 30.9 nM, 345 nM, >1 μM, >10 μM for human human sst1, sst3, sst4, sst2 and sst5 respectively. CH 275 can be used for the research of Alzheimer’s disease.
|
-
- HY-P1074
-
|
SNX-482
|
Calcium Channel
|
Neurological Disease
|
|
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect.
|
-
- HY-P1467
-
-
- HY-P1160A
-
-
- HY-P1166
-
|
UFP-803
|
Urotensin Receptor
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Cardiovascular Disease
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UFP-803 is a potent urotensin-II receptor (UT) ligand. UFP-803 has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.
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- HY-P2213
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GPLGIAGQ
|
MMP
Apoptosis
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Cancer
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GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT).
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- HY-P0266
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- HY-P1438
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Neuropeptide S(Rat)
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Neuropeptide Y Receptor
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Neuropeptide S(Rat) is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) also reduces anxiety-like behavior in mice.
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- HY-P1294
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- HY-P1167
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-
- HY-P0244
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-
- HY-107532
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-
- HY-P1274A
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ShK-Dap22 TFA
|
Potassium Channel
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Inflammation/Immunology
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ShK-Dap22 TFA is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 TFA is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.
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- HY-P1301A
-
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[Arg14,Lys15]Nociceptin TFA
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Opioid Receptor
|
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[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
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- HY-P1024
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-
- HY-P1787
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-
- HY-P1783A
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M2e, human TFA
|
Influenza Virus
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Infection
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M2e, human TFA, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A. M2e, human TFA is a valid and versatile vaccine candidate to protect against any strain of human influenza A.
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- HY-P1480
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-
- HY-P1252
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-
- HY-P1215A
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-
- HY-P0248
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Kemptide
|
PKA
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Metabolic Disease
|
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Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
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- HY-P0210
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-
- HY-125747
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Actinomycin X2
Actinomycin V
|
Bacterial
|
Cancer
Infection
|
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Actinomycin X2 (Actinomycin V), produced by many Streptomyces sp., shows strong inhibition of MRSA with a minimum inhibitory concentration (MIC) value of 0.25 μg/mL. Actinomycin X2 can be used for cancer and bacterial infection.
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- HY-P1597A
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Malantide TFA
|
PKA
PKC
|
Cancer
|
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Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM.
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- HY-P1540
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-
- HY-P0162
-
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HCV-IN-4
|
HCV
|
Infection
|
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HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively.
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-
- HY-P1221
-
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ProTx II
|
Sodium Channel
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Neurological Disease
|
|
ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.
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-
- HY-P0249
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-
- HY-P0088
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-
- HY-P1545A
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-
- HY-P0295A
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-
- HY-P1784
-
|
Secretin, canine
|
Src
|
Endocrinology
|
|
Secretin, canine is an endocrine hormone that stimulates the secretion of bicarbonate-rich pancreatic fluids. Secretin, canine can regulates gastric chief cell function and paracellular permeability in canine gastric monolayers by a Src kinase-dependent pathway.
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-
- HY-P0201
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-
- HY-P1717
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|
AMY-101
Cp40
|
Complement System
SARS-CoV
|
Inflammation/Immunology
|
|
AMY-101 (Cp40), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
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- HY-P0051
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- HY-P0166A
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Alexamorelin Met 1
(D-Mrp)-Ala-Trp-(D-Phe)
|
GHSR
|
Metabolic Disease
Endocrinology
|
|
Alexamorelin Met 1 is one of the metabolites of alexamorelin. The heptapeptide Ala-His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2 (Alexamorelin) is a synthetic molecule which inhibits growth hormone secretagogue binding in vitro.
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-
- HY-P1762
-
-
- HY-B0686A
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-
- 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.
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-
- HY-P2222
-
-
- HY-P1432A
-
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K-(D-1-Nal)-FwLL-NH2 TFA
|
GHSR
|
|
|
K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
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-
- HY-P0062A
-
|
Ziconotide TFA
|
Calcium Channel
|
Neurological Disease
|
|
Ziconotide TFA is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide TEA acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.
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-
- HY-P1213
-
|
JKC363
|
Melanocortin Receptor
|
Neurological Disease
|
|
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.
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-
- HY-P1078
-
|
Huwentoxin XVI
|
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.
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-
- HY-P1738
-
-
- HY-P1423
-
|
BA 1
|
Bombesin Receptor
|
|
|
BA 1 is a potent bombesin receptor agonist (IC50 values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). BA 1 enhances glucose transport in obese and diabetic primary myocytes. BA 1 also stimulates NCI-H1299 lung cancer cell proliferation in vitro.
|
-
- HY-P1339
-
-
- HY-P1757
-
-
- HY-P1568A
-
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Flagelin 22 TFA
Flagellin 22 TFA
|
Bacterial
|
Infection
|
|
Flagelin 22 TFA (Flagellin 22 TFA), a fragment of bacterial flagellin, is an effective elicitor in both plants and algae.
|
-
- HY-P1166A
-
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UFP-803 TFA
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
UFP-803 TFA is a potent urotensin-II receptor (UT) ligand. UFP-803 TFA has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.
|
-
- HY-P1037
-
-
- HY-P1185
-
|
Antagonist G
|
Vasopressin Receptor
Apoptosis
|
Cancer
|
|
Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
|
-
- HY-P1594
-
-
- HY-P1432
-
|
K-(D-1-Nal)-FwLL-NH2
|
GHSR
|
|
|
K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
|
-
- HY-P1578
-
-
- HY-P1299A
-
|
UFP-101 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.
|
-
- HY-P0098
-
-
- HY-P1306A
-
