Search Result
Results for "Acid-Sensing Ion Channel Peptides Inhibitors" in MCE Product Catalog:
8504
Inhibitors & Agonists
13
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-75867
-
-
- HY-131261
-
-
- HY-P1280
-
|
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.
|
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-130605
-
|
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.
|
-
- HY-12949
-
|
ML204
|
TRP Channel
|
Neurological Disease
|
|
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-12949A
-
|
ML204 hydrochloride
|
TRP Channel
|
Neurological Disease
|
|
ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-15736
-
-
- HY-U00135
-
-
- 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-101809
-
-
- HY-U00439
-
-
- HY-N2338
-
-
- HY-41076
-
-
- HY-N0172
-
-
- HY-100310
-
-
- HY-12082A
-
-
- HY-B0563A
-
-
- HY-P1264
-
|
α-Bungarotoxin
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.
|
-
- HY-B0563
-
|
Ropivacaine
|
Sodium Channel
Potassium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Ropivacain is a potent sodium channel blocker and acts as a local anesthetic agent. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also 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 is used for the research of regional anesthesia and neuropathic pain management.
|
-
- HY-B0563B
-
|
Ropivacaine hydrochloride
|
Sodium Channel
Potassium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also 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 is a local anesthetic agent widely used for regional anesthesia and neuropathic pain management in vivo.
|
-
- HY-P0189
-
-
- HY-11062
-
-
- HY-P0189A
-
-
- HY-U00280
-
|
Potassium Channel Activator 1
|
Others
|
Neurological Disease
|
|
Potassium Channel Activator 1 is an agent for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.
|
-
- HY-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-101238
-
-
- HY-B1221
-
|
Flufenamic acid
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-108505
-
-
- HY-101350
-
-
- HY-135407S
-
-
- HY-B1243
-
-
- HY-B0563C
-
|
Ropivacaine mesylate
|
Sodium Channel
Potassium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane.
|
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- 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.
|
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- HY-B0517A
-
|
Mepivacaine hydrochloride
|
Sodium Channel
|
Neurological Disease
|
|
Mepivacaine hydrochloride is an amide-type local anesthetic agent. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
|
-
- HY-B0517
-
|
Mepivacaine
|
Sodium Channel
|
Neurological Disease
|
|
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
|
-
- 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.
|
-
- HY-W040265
-
-
- HY-B0612D
-
-
- 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.
|
-
- HY-N0042
-
-
- 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.
|
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- HY-103310
-
-
- 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-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-B1090S
-
-
- HY-B0612E
-
-
- HY-16696
-
|
SN 2
|
TRP Channel
|
Infection
|
|
SN 2 is a potent activator of TRPML3 ion channel with an EC50 of 1.8 μM.
SN 2 also acts as a potent inhibitor of Dengue virus 2 (DENV2) and Zika virus (ZIKV).
|
-
- HY-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).
|
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- HY-B1704A
-
-
- HY-17611
-
|
Etripamil
MSP-2017; (-)-MSP-2017
|
Calcium Channel
|
Cardiovascular Disease
|
|
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist, can be used for the research of 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.
|
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- 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.
|
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- HY-P0274
-
|
PGLa
|
Bacterial
Antibiotic
|
Infection
|
|
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
-
|
PGLa TFA
|
Bacterial
Antibiotic
|
Infection
|
|
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-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.
|
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- HY-135412
-
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- 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).
|
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- HY-17451
-
-
- HY-131005
-
-
- 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.
|
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- 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.
|
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- HY-P1481
-
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- 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.
|
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- HY-107024
-
|
Osteogenic Growth Peptide (10-14)
OGP(10-14); Historphin
|
Src
|
Others
|
|
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-P1344A
-
-
- 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.
|
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- 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-131092
-
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- HY-P2244A
-
|
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).
|
-
- HY-P1249
-
|
Neuropeptide SF(mouse,rat)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide SF (mouse,rat) is a potent neuropeptide FF receptor agonist with Ki values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .
|
-
- 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-P0163
-
-
- HY-131094
-
-
- HY-B1546
-
|
Benzamil
Benzylamiloride
|
Sodium Channel
Na+/Ca2+ Exchanger
|
Neurological Disease
|
|
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-B1546A
-
|
Benzamil hydrochloride
Benzylamiloride hydrochloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
|
Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-17624
-
|
Framycetin
Neomycin B; Fradiomycin B
|
Bacterial
|
Infection
|
|
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.
|
-
- HY-P1249A
-
-
- HY-17624A
-
|
Framycetin sulfate
Neomycin B sulfate; Fradiomycin B sulfate
|
Bacterial
|
Infection
|
|
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.
|
-
- HY-P1481A
-
-
- 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-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-15419
-
|
RS-127445 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
|
-
- HY-15419A
-
|
RS-127445
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
|
-
- HY-121879
-
-
- 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-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-B1500
-
-
- HY-123834
-
|
FEN1-IN-1
|
Others
|
Cancer
|
|
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.
|
-
- HY-P1929
-
|
Bivalirudin
|
Thrombin
|
Cardiovascular Disease
|
|
Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
|
-
- HY-136909
-
|
SR33805
|
Calcium Channel
|
Cardiovascular Disease
|
|
SR33805 is a potent Ca 2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca 2+ channels. SR33805 can be used for the research of acute or chronic failing hearts.
|
-
- HY-B0908
-
-
- HY-122605
-
-
- HY-B1445
-
-
- HY-P0179
-
-
- HY-P1486
-
-
- 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-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-P0191
-
-
- 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-P0179A
-
-
- 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-128113
-
-
- 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-P0191A
-
-
- HY-P2292A
-
|
Omiganan-FITC TFA
|
Bacterial
Fungal
|
Infection
|
|
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.
|
-
- HY-131083
-
-
- HY-P2457
-
|
rCRAMP (rat)
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS.
|
-
- HY-P0281A
-
|
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.
|
-
- HY-A0176
-
-
- HY-P0281
-
|
TAT
|
HIV
|
Infection
|
|
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.
|
-
- HY-131326
-
-
- HY-P2292
-
|
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.
|
-
- HY-P1271
-
|
Catestatin
|
nAChR
|
Cardiovascular Disease
|
|
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.
|
-
- HY-133168
-
|
Englerin A
|
TRP Channel
|
Cancer
|
|
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.
|
-
- HY-19373
-
-
- 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-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-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-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-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-P1271A
-
|
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.
|
-
- 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-N0373
-
|
Licochalcone B
|
Amyloid-β
|
Neurological Disease
|
|
Licochalcone B is an extract from the root of Glycyrrhiza inflate. Licochalcone B inhibits amyloid β (Aβ42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ions.
|
-
- HY-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-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).
|
-
- HY-N7122A
-
|
Thymopentin acetate
|
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
|
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).
|
-
- HY-131091
-
-
- HY-P1333
-
|
Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-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.
|
-
- HY-P1045
-
|
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-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-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-125586
-
|
β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-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-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-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- 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-B1319
-
-
- HY-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-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.
|
-
- 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-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-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-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-105077A
-
|
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-106244A
-
|
DOTATATE acetate
|
Others
|
Cancer
|
|
DOTATATE acetate, a DOTA-conjugated peptide, and can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide therapy (PRRT).
|
-
- HY-P0256
-
-
- HY-131142
-
-
- 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-111828
-
|
TTA-A2
|
Calcium Channel
|
Neurological Disease
|
|
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
|
-
- HY-P1019A
-
-
- 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-P0256A
-
-
- HY-P1051
-
|
β-amyloid (12-28)
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-P1051A
-
|
β-amyloid (12-28) (TFA)
Amyloid β-Protein (12-28) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) TFA is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-B0407AS
-
-
- HY-128933
-
-
- HY-P1179
-
-
- HY-P1220
-
|
Huwentoxin-IV
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.
|
-
- HY-P0269
-
|
Magainin 1
Magainin I
|
Bacterial
Fungal
Antibiotic
|
Infection
|
|
Magainin 1 (Magainin I) 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.
|
-
- HY-P0082A
-
|
Glucagon hydrochloride
Porcine glucagon hydrochloride
|
Glucagon Receptor
|
Metabolic Disease
|
|
Glucagon hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone, produced by pancreatic α-cells. Glucagon hydrochloride stimulates gluconeogenesis. Glucagon hydrochloride activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-12796A
-
-
- HY-12796
-
-
- 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-P1179A
-
-
- HY-P2322
-
|
Iturin A
|
Fungal
|
|
|
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.
|
-
- HY-B0545
-
-
- HY-111325
-
|
Synta66
|
CRAC Channel
|
Neurological Disease
|
|
Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.
|
-
- HY-P1220A
-
|
Huwentoxin-IV TFA
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain.
|
-
- HY-P0269A
-
|
Magainin 1 TFA
Magainin I TFA
|
Bacterial
Fungal
Antibiotic
|
Infection
|
|
Magainin 1 TFA (Magainin I 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.
|
-
- 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-18728
-
-
- 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-N2077
-
-
- 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-13259
-
|
MG-132
Z-Leu-Leu-Leu-al; MG132
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
|
MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
|
-
- HY-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-15206
-
-
- HY-B0552A
-
-
- HY-B0552
-
-
- 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-P2315
-
|
Human β-defensin-1
HβD-1
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-1 (HβD-1) is a cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by all epithelial surfaces, but also by circulatory cells and cells of the reproductive tract. Human β-defensin-1 has antimicrobial activities against a broad-sperm bacteria.
|
-
- HY-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.
|
-
- HY-P0082
-
|
Glucagon
Porcine glucagon
|
Glucagon Receptor
|
Metabolic Disease
|
|
Glucagon (Porcine glucagon) is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-P1078A
-
|
Huwentoxin XVI TFA
|
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin XVI TFA, 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 TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.
|
-
- HY-14657
-
-
- HY-101942
-
|
CM-4620
|
CRAC Channel
|
Neurological Disease
|
|
CM-4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
|
-
- HY-18940A
-
-
- 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.
|
-
- 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-108335
-
|
Sipatrigine
619C89; BW 619C89
|
Sodium Channel
Calcium Channel
|
Neurological Disease
|
|
Sipatrigine (619C89), a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has the potential in the study for focal cerebral ischemia and stroke.
|
-
- 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-U00151
-
-
- HY-122697
-
|
ML418
|
Potassium Channel
|
Neurological Disease
|
|
ML418 is the first potent, selective and CNS penetrating blocker of Kir7.1 potassium channel (IC50, 310 nM), which also potently inhibits Kir6.2/SUR1, and exhibits superior selectivity over other Kir channels.
|
-
- HY-P1369
-
-
- HY-14462
-
-
- 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-15583
-
-
- 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).
|
-
- 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-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-12507
-
-
- HY-14656
-
-
- HY-P1369A
-
-
- 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-16126
-
-
- HY-N7511
-
-
- 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-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-P2458
-
|
CAP18 (rabbit)
|
Bacterial
|
Infection
|
|
CAP18 (rabbit) is a 37 amino acids antimicrobial peptide originally isolated from rabbit granulocytes. CAP18 (rabbit) has broad antimicrobial activity against both Gram-positive (IC50, 130-200 nM) and Gram-negative (IC50, 20-100 nM) bacteria. CAP18 (rabbit) has the potential for bacterial sepsis research.
|
-
- HY-126810A
-
|
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-P1080
-
|
ω-Agatoxin IVA
|
Calcium Channel
|
Neurological Disease
|
|
ω-Agatoxin IVA is a potent, selective P/Q type Ca 2+ channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels.
|
-
- 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-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-101096
-
-
- HY-107319
-
-
- HY-16723
-
-
- HY-P0318
-
-
- HY-P1471
-
-
- 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-P0290
-
-
- 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-100831
-
-
- HY-118628
-
-
- HY-111360
-
|
SPL-707
|
γ-secretase
|
Inflammation/Immunology
|
|
SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
|
-
- HY-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-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-P0052A
-
-
- HY-P0052
-
-
- HY-B0285
-
-
- HY-B0285A
-
-
- 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-P1416A
-
|
Foxy-5 TFA
|
Wnt
|
Cancer
|
|
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
|
-
- HY-P1514
-
-
- 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-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-N0601
-
-
- HY-W009724
-
-
- HY-P0215
-
-
- 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-16125
-
|
Carboxyamidotriazole Orotate
L-651582 Orotate; CAI Orotate
|
Calcium Channel
|
Cancer
Inflammation/Immunology
|
|
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.
|
-
- HY-P0139
-
-
- HY-W032013
-
-
- HY-P0215A
-
-
- HY-N0814A
-
|
Phytic acid dodecasodium salt hydrate
Inositol hexaphosphate dodecasodium salt hydrate; myo-Inositol, hexakis(dihydrogen phosphate) 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-15416
-
-
- HY-18723
-
-
- HY-B0703
-
-
- 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-B0285B
-
-
- HY-P0069A
-
-
- HY-15664
-
-
- 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-12545
-
|
Brevetoxin-3
PbTx-3
|
Sodium Channel
|
Inflammation/Immunology
|
|
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
|
-
- HY-12498
-
|
GV-58
|
Calcium Channel
|
Neurological Disease
|
|
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
|
-
- HY-100750
-
-
- HY-135328
-
-
- HY-14149
-
-
- 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-W010986
-
-
- HY-114424A
-
-
- HY-114424
-
-
- HY-B0653A
-
-
- HY-P0270
-
|
Magainin 2
Magainin II
|
Bacterial
Antibiotic
Fungal
|
Infection
|
|
Magainin 2 (Magainin II) is an antimicrobial peptide (AMP) isolated from the skin of the African clawed frog Xenopus laevis. Magainin 2 displays antibiotic activity against numerous gram-negative and gram-positive bacteria. Magainin 2 also is active against protozoa. Magainin 2 exerts its cytotoxicity effects by preferential interactions with anionic phospholipids abundant in bacterial membranes.
|
-
- HY-B0267A
-
-
- HY-B0267
-
-
- HY-100244
-
-
- HY-14183
-
|
Vernakalant Hydrochloride
RSD1235 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
|
-
- HY-110153
-
|
NS19504
|
Potassium Channel
|
Neurological Disease
|
|
NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
|
-
- HY-100623
-
-
- HY-N6778
-
|
Paxilline
|
Potassium Channel
Calcium Channel
|
Neurological Disease
|
|
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca 2+ ATPase (SERCA) with IC50s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity.
|
-
- HY-111747
-
|
TBAJ-587
|
Bacterial
|
Infection
Cardiovascular Disease
|
|
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization.
|
-
- 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-P1237
-
-
- HY-15125
-
-
- HY-P1452A
-
-
- HY-103309
-
|
ML218
|
Calcium Channel
|
Neurological Disease
|
|
ML218 is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
|
-
- HY-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-P1815
-
-
- HY-101547
-
|
TRPC6-IN-1
|
TRP Channel
|
Cancer
|
|
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
|
-
- HY-B0575
-
-
- HY-15763
-
|
Erastin
|
Ferroptosis
VDAC
|
Cancer
|
|
Erastin is a ferroptosis inducer. Erastin binds and inhibits voltage-dependent anion channels (VDAC2/VDAC3).
|
-
- HY-106855
-
-
- HY-P0224
-
-
- HY-Z0816
-
-
- HY-101674
-
-
- HY-B0495
-
|
Lamotrigine
LTG; BW430C
|
Sodium Channel
Autophagy
|
Neurological Disease
|
|
Lamotrigine(BW430C) is a novel anticonvulsant drug for inhibition of 5-HT and sodium channel
Target: Sodium Channel
Lamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate [1].
|
-
- HY-W015977
-
|
Prion Protein 106-126 (human)
PrP 106-126 (human)
|
Apoptosis
|
Neurological Disease
|
|
Prion Protein 106-126 (human) is a peptide fragment of prion, it can induct neuronal apoptosis, antiproteinase K digestion, fiber formation, and mediate the conversion of normal cellular prion protein (PrP c) into pathogenic isoform (PrP Sc). Prion Protein 106-126 (human) is generally used as the model to investigate neural degeneration of prion disease.
|
-
- 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-101840
-
-
- HY-101840A
-
-
- HY-P1247
-
-
- HY-100545
-
|
BAPTA-AM
|
Potassium Channel
|
Cardiovascular Disease
|
|
BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
|
-
- HY-P1036
-
-
- HY-P0276
-
-
- HY-B0211
-
-
- HY-B0211A
-
-
- HY-15707
-
-
- HY-19062
-
-
- 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-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-B0246
-
-
- HY-B0984
-
-
- HY-101621
-
-
- HY-14290A
-
-
- HY-B0837
-
|
Emamectin Benzoate
MK-244
|
GABA Receptor
|
Infection
|
|
Emamectin Benzoate (MK-244) works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.
|
-
- HY-101383
-
-
- HY-P2505
-
-
- HY-101507
-
|
Pico145
HC-608
|
TRP Channel
|
Cancer
|
|
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
|
-
- HY-P0214
-
-
- HY-50694
-
|
Senicapoc
ICA-17043
|
Potassium Channel
|
Others
|
|
Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
|
-
- HY-P1247A
-
-
- 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-16671
-
|
CFTR(inh)-172
|
CFTR
Autophagy
|
Others
|
|
CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.
|
-
- HY-108585
-
-
- HY-108585A
-
|
VU591
|
Potassium Channel
|
Others
|
|
VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
|
-
- HY-100230A
-
-
- HY-100611
-
-
- HY-B0407A
-
-
- HY-B1798A
-
|
Tocainide hydrochloride
|
Sodium Channel
|
Inflammation/Immunology
|
|
Tocainide hydrochloride is a sodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.
|
-
- HY-17631A
-
-
- HY-P1282
-
-
- HY-B0114
-
|
Oxcarbazepine
GP 47680
|
Sodium Channel
|
Neurological Disease
|
|
Oxcarbazepine (GP 47680) inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.
|
-
- 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-108584
-
|
Flindokalner
BMS-204352
|
Potassium Channel
|
Neurological Disease
|
|
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
|
-
- HY-135809
-
|
A2764 dihydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.
|
-
- HY-B0317
-
-
- HY-B0341
-
-
- HY-101012
-
-
- HY-B0317A
-
-
- HY-105117
-
-
- HY-B0612A
-
-
- HY-B0612
-
-
- HY-101069
-
-
- HY-B0437
-
-
- HY-P0214A
-
-
- HY-19960
-
|
BCTC
|
TRP Channel
|
Cancer
|
|
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
|
-
- HY-135328S
-
-
- HY-P1282A
-
-
- HY-P1663A
-
-
- HY-P0081
-
-
- 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-P1546
-
-
- HY-113618A
-
|
RO2959 hydrochloride
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
|
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
|
-
- HY-103371
-
|
DCPIB
|
Chloride Channel
Potassium Channel
|
Neurological Disease
|
|
DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK and inhibits TRESK, TASK1 and TASK3 (IC50s of 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM in CPAE cells.
|
-
- HY-13103
-
|
NS 11021
|
Potassium Channel
|
Others
|
|
NS 11021 is a potent and specific Ca 2-activated big-conductance K ＋ Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
|
-
- HY-A0016
-
|
Dronedarone
SR 33589
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
|
Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
|
-
- 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-15580
-
-
- HY-U00218
-
-
- HY-B0768A
-
-
- HY-U00315
-
-
- HY-B0567
-
-
- HY-101740
-
-
- HY-B0317B
-
-
- HY-B0424
-
-
- HY-B0419
-
-
- HY-12515A
-
-
- HY-101428
-
|
NS-638
|
Calcium Channel
|
Neurological Disease
|
|
NS-638 is a small nonpeptide molecule with Ca 2+-channel blocking properties. K +-stimulated intracellular Ca 2+-elevation is blocked with an IC50 value of 3.4 μM.
|
-
- HY-100727
-
-
- HY-20587
-
-
- HY-N0252
-
-
- HY-108465
-
|
Pyr3
|
TRP Channel
|
Others
|
|
Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca 2+ influx.
|
-
- HY-130354
-
|
Dibutyryl-cGMP sodium
Bt2cGMP sodium
|
Potassium Channel
|
Cardiovascular Disease
|
|
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
|
-
- HY-P2504
-
-
- HY-P2547
-
-
- 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-113618B
-
|
RO2959 monohydrochloride
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
|
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
|
-
- HY-P1077
-
|
CALP1
|
Calcium Channel
mGluR
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.
|
-
- 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-P2321
-
-
- HY-N5006
-
-
- HY-N1469
-
-
- HY-N0252A
-
-
- HY-15292
-
|
S107
|
Others
|
Cardiovascular Disease
|
|
S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca 2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold.
|
-
- HY-14255
-
-
- HY-B0347
-
-
- HY-66012
-
-
- HY-101422
-
-
- HY-U00173
-
-
- HY-100001
-
-
- HY-103315
-
-
- HY-U00201
-
-
- HY-B0437AS
-
-
- HY-12515
-
|
Nicardipine
YC-93 free base
|
Calcium Channel
|
Neurological Disease
|
|
Nicardipine (YC-93 free base) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
|
-
- 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-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-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-P1758
-
-
- HY-P2311
-
-
- HY-P2321A
-
-
- HY-N1462
-
|
Atractyloside potassium salt
|
Others
|
Others
|
|
Atractyloside potassium salt is a toxic diterpenoid glycoside isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart.
|
-
- HY-P2502
-
-
- 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-112075
-
-
- HY-W011509
-
-
- HY-P1728A
-
-
- HY-P1284
-
|
ZIP
|
PKC
|
Neurological Disease
|
|
ZIP is a selective peptide inhibitor of PKMζ. ZIP injections can block the impairment in morphine conditioned place preference induced.
|
-
- HY-P1565
-
|
Transdermal Peptide Disulfide
TD 1 Disulfide(peptide)
|
Na+/K+ ATPase
|
Inflammation/Immunology
|
|
Transdermal Peptide Disulfide (TD 1 Disulfide(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 Disulfide can enhance the transdermal delivery of many macromolecules.
|
-
- HY-13443
-
-
- HY-13443A
-
-
- HY-14470
-
-
- HY-18600A
-
-
- HY-18600
-
-
- HY-N6691
-
|
Veratridine
3-Veratroylveracevine
|
Sodium Channel
|
Neurological Disease
|
|
Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM.
|
-
- 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-P1029
-
-
- HY-116448
-
-
- HY-B0401
-
-
- HY-B1109
-
-
- HY-B2136
-
-
- HY-100572
-
-
- HY-14256
-
-
- HY-U00236
-
-
- HY-B0233
-
-
- HY-101843
-
-
- HY-108582
-
|
Y-27152
|
Potassium Channel
|
Cardiovascular Disease
|
|
Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
|
-
- 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-114161
-
-
- HY-112705
-
|
VU0529331
|
Potassium Channel
|
Neurological Disease
|
|
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
|
-
- HY-B0166
-
-
- HY-B0166A
-
|
L-Ascorbic acid sodium salt
Sodium L-ascorbate; Vitamin C sodium salt
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
|
-
- HY-B0551
-
-
- HY-B0551A
-
-
- HY-15553A
-
-
- 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-P1565A
-
|
Transdermal Peptide Disulfide TFA
TD 1 Disulfide(peptide) TFA
|
Na+/K+ ATPase
|
Others
|
|
Transdermal Peptide Disulfide TFA (TD 1 Disulfide(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 Disulfide TFA can enhance the transdermal delivery of many macromolecules.
|
-
- HY-N6688
-
|
Verruculogen
|
Potassium Channel
Bacterial
Antibiotic
|
Infection
|
|
Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
|
-
- HY-108577
-
-
- HY-P1144
-
-
- 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-N3463
-
-
- HY-U00044
-
-
- HY-14284
-
-
- HY-B1448
-
-
- HY-P1284A
-
|
ZIP TFA
|
PKC
|
Neurological Disease
|
|
ZIP TFA is a selective peptide inhibitor of PKMζ. ZIP TFA injections can block the impairment in morphine conditioned place preference induced.
|
-
- HY-114161A
-
-
- HY-136589
-
-
- HY-P1186
-
-
- HY-P1497
-
-
- HY-P1144A
-
-
- HY-15553
-
|
Mibefradil
Ro 40-5967
|
Calcium Channel
|
Cardiovascular Disease
|
|
Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca 2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
|
-
- HY-N2433
-
|
Paederosidic acid methyl ester
|
Potassium Channel
|
Neurological Disease
|
|
Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
|
-
- HY-P1841
-
-
- HY-13422
-
|
Zatebradine hydrochloride
UL-FS-49; UL-FS-49CL
|
HCN Channel
|
Cardiovascular Disease
|
|
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
|
-
- HY-10341A
-
|
Fasudil
HA-1077; AT877
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+channel antagonist and vasodilator.
|
-
- 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-B1386
-
|
Halazone
|
Bacterial
Carbonic Anhydrase
Sodium Channel
|
Infection
|
|
Halazone is an atypical antimicrobial sulfonamide derivative and a carbonic anhydrase II inhibitor with a Kd value of 1.45 µM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water.
|
-
- HY-13812
-
-
- HY-101346
-
-
- HY-B0265
-
-
- HY-14187
-
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-14188
-
-
- HY-12515AS
-
|
Nicardipine D3 hydrochloride
YC-93 D3
|
Calcium Channel
|
Neurological Disease
|
|
Nicardipine D3 hydrochloride (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
|
-
- 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-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-108573
-
|
P-1075
|
Potassium Channel
|
Cardiovascular Disease
|
|
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
|
-
- HY-P1113
-
-
- HY-P1113A
-
-
- HY-12515B
-
|
(S)-Nicardipine
(S)-YC-93 free base
|
Others
|
Neurological Disease
Cardiovascular Disease
|
|
(S)-Nicardipine ((S)-YC-93 free base) is the less active S enantiomer of Nicardipine. Nicardipine is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
|
-
- HY-50722
-
|
NNC 55-0396
NNC 55-0396 dihydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.
|
-
- HY-P1789
-
-
- 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-16664
-
-
- HY-B0682A
-
-
- HY-B1140
-
-
- HY-B0284
-
-
- HY-U00212
-
-
- HY-B0162A
-
-
- HY-N1378
-
-
- HY-B1304
-
-
- HY-P0119A
-
-
- HY-P2519
-
-
- HY-W012479
-
-
- HY-14275
-
|
Verapamil
(±)-Verapamil; CP-16533-1
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Metabolic Disease
|
|
Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
|
-
- HY-A0064
-
|
Verapamil hydrochloride
(±)-Verapamil hydrochloride; CP-16533-1 hydrochloride
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Cardiovascular Disease
|
|
Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
|
-
- 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-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-P1789A
-
-
- 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-P1378
-
-
- HY-P2538
-
-
- HY-10340B
-
-
- HY-12465
-
-
- 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-B0422
-
|
Nateglinide
A4166; Senaglinide
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1] [2] .
|
-
- HY-B0023
-
-
- HY-12502B
-
-
- HY-12502
-
-
- HY-19721
-
-
- HY-B0369A
-
-
- HY-17001A
-
-
- HY-15551
-
-
- HY-12515C
-
|
(R)-Nicardipine
(R)-YC-93 free base
|
Others
|
Neurological Disease
Cardiovascular Disease
|
|
(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
|
-
- HY-P1231
-
-
- HY-P1229
-
-
- HY-P1378A
-
-
- HY-P1083
-
-
- HY-P2468
-
|
BAD (103-127) (human)
|
Bcl-2 Family
|
Cancer
|
|
BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. BAD (103-127) (human) is reported to have almost 800-fold higher affinity for Bcl-XL than the 16-mer peptide.
|
-
- 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-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-13422A
-
|
Zatebradine
UL-FS-49 free base; UL-FS-49CL free base
|
HCN Channel
|
Cardiovascular Disease
|
|
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
|
-
- HY-22044
-
|
ICA
N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinamine
|
Parasite
|
Infection
Cardiovascular Disease
|
|
ICA (N-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine) is a SK channel inhibitor that has antileishmanial activity with an IC50 of 2.1 µM.
|
-
- 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-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-P2518
-
-
- HY-19408
-
|
Pyr10
|
TRP Channel
|
Others
|
|
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.
|
-
- 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-P0014
-
-
- HY-112679
-
-
- HY-114426A
-
-
- HY-17001
-
-
- HY-16973
-
|
Fluralaner
A1443; AH252723
|
Parasite
|
Infection
|
|
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
|
-
- HY-B1302
-
-
- HY-12496
-
-
- HY-W016498
-
-
- HY-N7395
-
-
- 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-P1063
-
-
- 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-P1083A
-
-
- HY-P1289
-
|
[Ala113]MBP(104-118)
|
PKC
|
Others
|
|
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM.
|
-
- HY-P1289A
-
|
[Ala107]MBP(104-118)
|
PKC
|
Others
|
|
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM.
|
-
- HY-129658
-
-
- 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-127106
-
|
VU0810464
|
Potassium Channel
|
Neurological Disease
|
|
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration.
|
-
- HY-130976
-
-
- HY-16711
-
-
- HY-P2466
-
-
- HY-P1084
-
-
- HY-12693
-
|
R(+)-IAA-94
R(+)-Methylindazone
|
Chloride Channel
|
Others
|
|
R(+)-IAA-94 (R(+)-Methylindazone) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-IAA-94 inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef).
|
-
- 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-P1236
-
-
- HY-P1289C
-
-
- HY-P1289B
-
-
- HY-100612
-
|
T16Ainh-A01
|
Chloride Channel
|
Others
|
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-17404
-
-
- HY-18996
-
-
- HY-17403
-
-
- HY-12502A
-
-
- 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-P1063A
-
-
- HY-P1246
-
-
- HY-P1329
-
-
- 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-P1495
-
-
- 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-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-120261
-
-
- HY-B0112
-
|
Minoxidil
U10858
|
Potassium Channel
|
Cardiovascular Disease
|
|
Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM.
|
-
- HY-N1934
-
-
- HY-P2319
-
-
- HY-P1363
-
-
- HY-P0271
-
-
- HY-P1236A
-
-
- HY-125824
-
-
- HY-108235
-
-
- HY-101396
-
-
- HY-A0093
-
-
- HY-B0284S
-
-
- HY-B0887
-
|
Permethrin
NRDC-143
|
Parasite
|
Infection
|
|
Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
|
-
- HY-P0136
-
-
- HY-P1329A
-
-
- HY-P1522
-
-
- HY-P2319A
-
-
- 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-117639
-
|
AUT1
|
Potassium Channel
|
Cancer
|
|
AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
|
-
- 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-P1084A
-
-
- 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-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-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis.
|
-
- HY-B0422S
-
|
Nateglinide D5
A4166 D5; Senaglinide D5
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1] [2] .
|
-
- 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-P1000
-
-
- HY-N0239
-
-
- HY-17398
-
-
- HY-16916
-
-
- HY-14744
-
|
Levamlodipine
(S)-Amlodipine; Levoamlodipine
|
Calcium Channel
|
Others
|
|
Levamlodipine ((S)-Amlodipine) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
|
-
- HY-B0493
-
-
- HY-U00137
-
-
- HY-103318
-
-
- HY-13519
-
-
- 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-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-P0261
-
-
- HY-P1880
-
-
- HY-P0241
-
-
- HY-P1595
-
-
- HY-P1818
-
-
- HY-P1879
-
-
- HY-P1255
-
-
- 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-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-114118
-
-
- 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-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-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-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-17612
-
-
- HY-108594
-
-
- HY-W011641
-
-
- HY-B0799
-
-
- HY-Y0258
-
-
- HY-135356
-
-
- HY-107301
-
-
- HY-19664
-
-
- HY-131281
-
|
Ivabradine impurity 1
|
Others
|
Others
|
|
Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-131282
-
|
Ivabradine impurity 2
|
Others
|
Others
|
|
Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-108690
-
|
Fluxametamide
|
GABA Receptor
|
Others
|
|
Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
|
-
- HY-N0714
-
|
Berbamine
|
NF-κB
Autophagy
|
Cancer
|
|
Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
|
-
- HY-P1263A
-
-
- HY-P2548
-
|
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated
|
EGFR
|
Others
|
|
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification.
|
-
- HY-I1112
-
-
- HY-19574
-
-
- 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-P1226
-
-
- HY-P1224
-
-
- HY-P1601
-
-
- HY-P1228
-
-
- HY-P1223
-
-
- HY-P0092
-
-
- 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-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-12048
-
-
- HY-122560A
-
|
VU0134992 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
|
-
- HY-102070
-
|
NS13001
|
Potassium Channel
|
Neurological Disease
|
|
NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.
|
-
- HY-114118A
-
-
- HY-103546
-
-
- HY-107212
-
|
Selamectin
|
Parasite
Chloride Channel
P-glycoprotein
|
Infection
|
|
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
|
-
- HY-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-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-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-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-B1090
-
-
- HY-108593
-
-
- HY-B0612DS
-
-
- HY-17436
-
-
- HY-10388
-
-
- HY-108590
-
-
- HY-131283
-
-
- HY-B1793
-
-
- HY-14744A
-
|
Levamlodipine besylate
(S)-Amlodipine besylate; Levoamlodipine besylate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
|
-
- HY-B1494
-
-
- HY-B0239
-
|
Chloramphenicol
|
Bacterial
Antibiotic
|
Infection
|
|
Chloramphenicol, a broad-spectrum antibiotic, acts as a potent inhibitor of bacterial protein biosynthesis. Chloramphenicol acts primarily on the 50S subunit of bacterial 70S rihosomes and inhibits peptide bond formation by suppressing peptidyl transferase activity.
|
-
- HY-P1013
-
-
- HY-P1331
-
-
- HY-P1560
-
-
- HY-P0311
-
|
LAH4
|
Bacterial
|
Infection
|
|
LAH4 is an antimicrobial peptide that strongly interacts with phospholipid membranes, exhibiting in vitro transfection efficiency.
|
-
- HY-P1774
-
-
- HY-P0198
-
-
- HY-P1274A
-
|
ShK-Dap22 TFA
|
Potassium Channel
|
Inflammation/Immunology
|
|
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.
|
-
- 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-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-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-N0630
-
-
- HY-N0663
-
-
- HY-13044
-
-
- HY-B1378
-
-
- HY-B0575S
-
-
- HY-17402
-
-
- HY-B1640
-
|
Ethacrynic acid
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Cancer
Inflammation/Immunology
|
|
Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
|
-
- HY-P1250A
-
|
RFRP-3(human) TFA
Neuropeptide VF(124-131)(human) TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
RFRP-3 (Neuropeptide VF(124-131))(human) TFA, 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-P0188
-
-
- HY-P1214
-
-
- HY-P1341
-
-
- HY-P1341A
-
-
- HY-P1214A
-
-
- HY-119322
-
|
Tifenazoxide
NN414
|
Potassium Channel
|
Metabolic Disease
|
|
Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K ATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.
|
-
- HY-P0245
-
-
- HY-P2559
-
-
- HY-P1895
-
-
- HY-P1903
-
-
- HY-P1235A
-
-
- HY-B0185A
-
|
Lidocaine hydrochloride
Lignocaine hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
|
-
- HY-100566
-
-
- HY-19529
-
-
- 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-P0188A
-
-
- HY-131018
-
-
- HY-101437A
-
-
- HY-112729
-
|
HC-056456
3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide
|
Others
|
Others
|
|
HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na +]i rise is slowed by HC-056456 (IC50~3 µM).
|
-
- HY-W013093
-
-
- HY-103368
-
|
Eact
|
Chloride Channel
|
Neurological Disease
|
|
Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity.
|
-
- HY-12343
-
-
- HY-B1655
-
|
Fluspirilene
R 6218; Redeptin
|
Calcium Channel
|
Neurological Disease
|
|
Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.
|
-
- 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-P1145
-
-
- HY-P2317
-
-
- HY-P1521
-
-
- HY-P1510
-
-
- HY-P1580
-
-
- HY-P1484
-
-
- HY-P1062
-
-
- HY-P1334
-
-
- 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-P1517
-
-
- HY-D0889
-
-
- HY-P1860
-
-
- HY-W008555
-
-
- HY-50844
-
-
- 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-116790A
-
-
- HY-B1288
-
|
Oxybuprocaine hydrochloride
Benoxinate hydrochloride
|
Sodium Channel
|
Neurological Disease
|
|
Oxybuprocaine hydrochloride (Benoxinate hydrochloride) reversibly blocks sodium channels and prevents propagation of painful nerve impulses in the cornea, conjunctiva, and sclera. Oxybuprocaine hydrochloride is used especially in ophthalmology and otolaryngology.
|
-
- HY-119373
-
-
- HY-A0084
-
|
Procainamide hydrochloride
|
Autophagy
|
Cancer
|
|
Procainamide hydrochloride is an anti-arrhythmic agent and is used to treat cardiac arrhythmia; induces rapid block of the batrachotoxin(BTX)-activated sodium channels of the heart muscle and acts as antagonist to long gating closures.
|
-
- HY-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-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-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-13295
-
-
- HY-B0185
-
|
Lidocaine
Lignocaine
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative commonly used to anesthetize. Lidocaine is a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
|
-
- HY-N0603
-
-
- HY-108538
-
|
Ethacrynic acid D5
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
|
|
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
|
-
- HY-B1671
-
|
(+)-Kavain
|
GABA Receptor
Sodium Channel
Calcium Channel
|
Metabolic Disease
Neurological Disease
|
|
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
|
-
- HY-12546
-
|
Brevetoxin B
Brevetoxin-2; PbTx-2
|
Sodium Channel
|
|
|
Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.
|
-
- HY-P1274
-
|
ShK-Dap22
|
Potassium Channel
|
Inflammation/Immunology
|
|
ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 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.
|
-
- HY-P1053
-
-
- HY-P1593
-
-
- 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-P1334A
-
-
- 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-P1062A
-
-
- 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-P1082
-
-
- HY-P1490
-
-
- HY-12533
-
|
Disopyramide
Dicorantil; SC-7031
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
|
|
Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.
|
-
- HY-112723
-
-
- HY-107372
-
-
- HY-12809
-
|
Optovin
|
TRP Channel
|
Others
|
|
Optovin is a reversible photoactive TRPA1 activator; stimulates human TRPA1 channels in vitro and enables repeated photoactivation of motor behaviors in wild-type zebrafish (EC50 = 2 μM).
|
-
- HY-P2496
-
-
- HY-P1259
-
|
PR-39
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-P0228
-
-
- HY-P0250
-
-
- HY-P1593A
-
-
- 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-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-133614
-
|
Dihydroisopimaric acid
|
Potassium Channel
|
Others
|
|
Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.
|
-
- HY-15065
-
-
- HY-114301
-
-
- HY-A0148A
-
|
Halofantrine hydrochloride
SKF-102886; WR-171669
|
Parasite
|
Infection
|
|
Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound.
|
-
- HY-129361
-
-
- HY-101177
-
-
- HY-131095
-
-
- 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-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-W013712
-
|
GI-530159
|
Potassium Channel
|
Neurological Disease
|
|
GI-530159 is a selective, mechanosensitive opener of TREK1 (K2P2.1) and TREK2 (K2P10.1) channels, with an EC50 of 0.76 μM for TREK1. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels. GI-530159 reduces rat dorsal root ganglion neuron excitability.
|
-
- HY-P1259A
-
|
PR-39 TFA
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-P1164
-
-
- HY-P0206
-
-
- 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-P1534
-
-
- HY-P1469
-
-
- HY-P2416
-
-
- 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-A0170
-
|
Trovafloxacin
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
|
-
- HY-N1483
-
|
Guanfu base A
|
Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.
|
-
- HY-103399
-
|
Trovafloxacin mesylate
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
|
-
- 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-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-15124
-
-
- HY-105170B
-
|
ABT-418 hydrochloride
|
nAChR
|
Neurological Disease
|
|
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.
|
-
- HY-W042039
-
-
- HY-B0448A
-
-
- HY-114301A
-
-
- HY-B0448
-
-
- 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-126488
-
-
- 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-P1164A
-
-
- HY-P0225
-
-
- HY-P1244
-
-
- HY-P1772
-
-
- HY-P1225
-
-
- HY-P2283
-
-
- HY-P0263
-
-
- HY-135746
-
|
OR-1896
|
Potassium Channel
Phosphodiesterase (PDE)
Drug Metabolite
|
Cardiovascular Disease
|
|
OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
|
-
- HY-N0747
-
|
Oxypeucedanin
|
Potassium Channel
|
Cancer
Cardiovascular Disease
|
|
Oxypeucedanin is a furocoumarin derivative isolated from Angelica dahurica. Oxypeucedanin is a selective open-channel blocker, inhibits the hKv1.5 current with an IC50 value of 76 nM. Oxypeucedanin prolongs cardiac action potential duration (APD), is a potential antiarrhythmic agent for atrial fibrillation. Oxypeucedanin induces cell apoptosis through inhibition of cancer cell migration.
|
-
- 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-100783A
-
|
(-)-Bicuculline methochloride
l-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-N2412
-
|
Irisolidone
|
Chloride Channel
|
Cancer
Neurological Disease
|
|
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade.
|
-
- HY-B0834
-
|
Indoxacarb
(±)-Indoxacarb
|
Sodium Channel
|
|
|
Indoxacarb ((±)-Indoxacarb) is a broad-spectrum oxadiazine insecticide. Indoxacarb is metabolized in vivo to its active N-decarbomethoxyllated metabolite DCJW. Indoxacarb suppresses voltage-gated sodium channel currents in rat dorsal root ganglion neurons.
|
-
- HY-33350
-
-
- HY-100783
-
|
(-)-Bicuculline methobromide
l-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-A0093S
-
|
Mexiletine D6 hydrochloride
KOE-1173 D6 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
|
|
Mexiletine D6 hydrochloride (KOE-1173 D6 hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.
|
-
- 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-17566
-
-
- HY-129360
-
-
- HY-P2523
-
|
Temporin L
|
Bacterial
Fungal
|
Infection
|
|
Temporin L is a potent antimicrobial peptide and is active against Gram-negative bacteria and yeast strains. Temporin L also has antiendotoxin properties.
|
-
- 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-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-16915
-
|
RPR-260243
|
Potassium Channel
|
Cardiovascular Disease
|
|
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
|
-
- HY-130353
-
|
Desethylamiodarone hydrochloride
N-desethylamiodarone hydrochloride; LB 33020 hydrochloride
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
|
Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.
|
-
- HY-17429
-
|
Flecainide acetate
R-818
|
Sodium Channel
|
Cardiovascular Disease
|
|
Flecainide acetate (R-818) is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.
|
-
- HY-B0432B
-
|
(S)-Propafenone
(S)-SA-79
|
Others
|
Cardiovascular Disease
|
|
(S)-Propafenone ((S)-SA-79) is the S-enantiomer of Propafenone. (S)-Propafenone ((S)-SA-79) exerts beta-blocking action and the sodium channel-dependent antiarrhythmic class 1 activity.
|
-
- HY-15598
-
-
- 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-14600
-
-
- HY-126010
-
|
Dooku1
|
Others
|
Cardiovascular Disease
|
|
Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
|
-
- 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-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-P1388
-
-
- HY-P1462
-
-
- HY-P0078
-
-
- HY-B0780
-
-
- HY-W007970
-
-
- 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-N6868
-
-
- HY-11079
-
-
- 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-P1567
-
-
- HY-P1170
-
-
- HY-P1308
-
-
- HY-P1462A
-
-
- HY-P0283
-
-
- HY-P1388A
-
-
- HY-P2039
-
-
- 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-N1072
-
|
Wilforgine
|
Others
|
Inflammation/Immunology
|
|
Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.
|
-
- HY-19608
-
-
- HY-N7126
-
|
Citronellal
|
Others
|
Neurological Disease
|
|
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, hypnotic, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway.
|
-
- HY-100641
-
-
- HY-101253
-
|
AM-92016 hydrochloride
|
Others
|
Cardiovascular Disease
|
|
AM-92016 hydrochloride is a specific blocker of rectifier potassium current (IK). AM-92016 hydrochloride delays rectifier potassium channel (IK), repolarizes the membrane thereby restricting the duration of the nerve impulse thereby restricting the duration of the nerve impulse.
|
-
- HY-101622
-
-
- HY-136615
-
-
- HY-B1837
-
|
Cyfluthrin
|
Sodium Channel
|
Infection
|
|
Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.
|
-
- 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-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-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-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-P0228A
-
-
- HY-P2323
-
-
- 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-P1742
-
-
- HY-P0288
-
-
- HY-108896
-
-
- 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-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-101986
-
-
- 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-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-P1097
-
-
- 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.
|
-
- HY-10341
-
|
Fasudil Hydrochloride
HA-1077 Hydrochloride; AT-877 Hydrochloride
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-P1244A
-
-
- 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-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-P1308A
-
-
- HY-P0199
-
-
- 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-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-18779
-
|
PF-4840154
|
TRP Channel
|
Inflammation/Immunology
|
|
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.
|
-
- HY-111613
-
|
Pinaverium bromide
|
Calcium Channel
|
Others
|
|
Pinaverium bromide is an L-type calcium channel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients.
|
-
- HY-101844
-
-
- 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-13750
-
-
- 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-P1866
-
-
- HY-19282A
-
-
- HY-N6016
-
|
Bacopaside II
|
Apoptosis
|
Cancer
|
|
Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis.
|
-
- HY-75161
-
|
(-)-Menthol
|
TRP Channel
Endogenous Metabolite
|
Cancer
|
|
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i. Antitumor activity.
|
-
- HY-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-12366
-
-
- HY-P1564
-
-
- HY-12537
-
-
- 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-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-P1504
-
-
- HY-P2563
-
-
- HY-P1519B
-
-
- HY-P2291
-
-
- HY-P1866A
-
-
- HY-P1519
-
-
- 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-P2558
-
-
- HY-102052
-
|
DCEBIO
|
Potassium Channel
|
Inflammation/Immunology
|
|
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl － secretion in T84 colonic cells. DCEBIO stimulates Cl － secretion via the activation of hIK1 K ＋ channels and the activation of an apical membrane Cl － conductance.
|
-
- HY-N2941
-
|
Bisandrographolide C
|
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Bisandrographolide C is an unusual dimer of ent-labdane diterpenoid isolated and identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels with Kd values of 289 and 341 μM respectively, and protects cardiomyocytes from hypoxia-reoxygenation injury.
|
-
- HY-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-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-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-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-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-133012
-
|
GFB-8438
|
TRP Channel
|
Neurological Disease
|
|
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
|
-
- HY-19214
-
-
- HY-P1504A
-
-
- HY-P1596
-
-
- 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-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-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-P0107
-
-
- HY-P2291A
-
-
- HY-B0562
-
|
Methyclothiazide
|
Carbonic Anhydrase
|
Metabolic Disease
Cardiovascular Disease
|
|
Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro.
|
-
- HY-108464A
-
|
Phenamil methanesulfonate
|
Sodium Channel
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
|
-
- 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-P2497
-
-
- 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-18662
-
|
RQ-00203078
|
TRP Channel
|
Cancer
|
|
RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
|
-
- HY-12650
-
|
Mirogabalin
DS5565
|
Calcium Channel
|
Neurological Disease
|
|
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
|
-
- HY-P0165
-
-
- 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-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-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-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-P1536
-
-
- HY-P0097A
-
-
- HY-P1348
-
-
- HY-P1277
-
-
- 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-B0309
-
|
Felodipine
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
|
-
- HY-18347A
-
-
- HY-17446
-
-
- HY-17369
-
-
- 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-10015
-
|
PAP-1
5-(4-Phenoxybutoxy)psoralen
|
Potassium Channel
|
Inflammation/Immunology
|
|
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.
|
-
- 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-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-P1277A
-
-
- HY-12361
-
|
PF 1022A
|
Parasite
|
Infection
|
|
PF 1022A is a cyclooctadepsipeptide with broadspectrum anthelmintic properties produced by fermentation of the fungus Mycelia sterilia. PF 1022A is a channel-forming ionophore. PF 1022A showes strong anthelmintic activities against Ascaridia galli in chickens. PF 1022A also can be used for angiostrongyliasis research.
|
-
- 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-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-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-112999
-
-
- 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-16953
-
|
JNJ 303
|
Potassium Channel
|
Cardiovascular Disease
|
|
JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM. JNJ 303 does not have any effects on other cardiac channels at concentrations of 3.3 μM for INa, Ica, Ito, and IKr. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).
|
-
- HY-13631E
-
-
- HY-70068
-
-
- 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-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-115681
-
|
(2R/S)-6-PNG
6-Prenylnaringenin
|
Calcium Channel
|
|
|
(2R/S)-6-PNG (6-Prenylnaringenin) is a Cav3.2 (T-type) Ca 2+ channel blocker (IC50=991 nM). (2R/S)-6-PNG suppresses neuropathic allodynia in mouse pain models.
|
-
- HY-100973A
-
-
- HY-B0824
-
|
Bifenthrin
|
Sodium Channel
|
Neurological Disease
|
|
Bifenthrin is a synthetic pyrethroid insecticide that prolongs opening of sodium channels resulting in membrane depolarization and conductance block in the insect nervous system. Bifenthrin is effective against A. gambiae and C. quinquefasciatus mosquitos (LD50s = 0.15 and 0.16 ng/mg, respectively) and increases O. insidiosus mortality in treated corn and sorghum plants.
|
-
- HY-B0122
-
-
- 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-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-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-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-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-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-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-18678A
-
-
- HY-10898
-
-
- 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-P0242A
-
-
- HY-B0836
-
|
λ-Cyhalothrin
|
Parasite
Sodium Channel
|
Infection
Endocrinology
Neurological Disease
|
|
λ-Cyhalothrin is a high efficiency, broad-spectrum type II synthetic pyrethroid insecticide containing α-cyano group. λ-Cyhalothrin is used to control a wide range of pests in a variety of applications. λ-Cyhalothrin is a neurotoxin that targets sodium channels in the membranes of neurons in the central nervous system.
|
-
- HY-12532
-
-
- HY-12962
-
|
NMDA-IN-1
|
iGluR
|
Neurological Disease
|
|
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
|
-
- HY-N6776
-
|
Penitrem A
|
Potassium Channel
|
Cancer
Neurological Disease
|
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.
|
-
- HY-110199
-
|
TC-I 2014
|
TRP Channel
|
Neurological Disease
|
|
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.
|
-
- HY-108588
-
|
NS5806
|
Potassium Channel
|
Cardiovascular Disease
|
|
NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
|
-
- HY-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-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-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-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-P1278A
-
|
GR 64349 TFA
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
|
-
- HY-P1278
-
|
GR 64349
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
|
-
- HY-P2460
-
|
SMAP-29
|
Bacterial
Fungal
|
Infection
Inflammation/Immunology
|
|
SMAP-29, a promising antiinfective agent, is a broad spectrum antibacterial and antifungal α-helical cathelicidin-derived peptide. SMAP-29 acts by permeabilizing bacterial membranes and inducing remarkable changes in the surface morphology of susceptible microorganism.
|
-
- HY-P0202
-
-
- 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-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-P2539
-
-
- HY-135897
-
-
- HY-B1193
-
-
- HY-B0254
-
|
Glipizide
CP 28720; K 4024
|
Potassium Channel
|
Metabolic Disease
|
|
Glipizide (K 4024; CP 2872) a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2 diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium (KATP) channels among β cells of pancreatic islets of Langerhans.
|
-
- 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-14184
-
-
- HY-106994A
-
|
Nebentan potassium
YM598
|
Endothelin Receptor
|
Inflammation/Immunology
|
|
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium 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-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-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-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-70057
-
|
Safinamide
FCE 26743; EMD 1195686
|
Monoamine Oxidase
|
Neurological Disease
|
|
Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
|
-
- 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-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-133596
-
|
12,14-Dichlorodehydroabietic acid
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
|
-
- HY-122114
-
|
ICA-27243
|
Potassium Channel
|
Neurological Disease
|
|
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects.
|
-
- HY-106994
-
|
Nebentan
YM598 free base
|
Endothelin Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Nebentan (YM598 free base) 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-14184A
-
-
- 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-13987
-
-
- 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-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-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-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-12080A
-
-
- HY-P2454
-
|
CSP1
|
Bacterial
|
Infection
|
|
CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent.
|
-
- HY-P1143
-
-
- HY-P2499
-
|
BAD (103-127) (human), FAM-labeled
|
Bcl-2 Family
|
Cancer
|
|
BAD (103-127) (human), FAM-labeled is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL.
|
-
- 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-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-110234
-
-
- HY-19976
-
|
RN-1747
|
TRP Channel
|
Cardiovascular Disease
|
|
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM.
|
-
- HY-12323
-
|
ISX-9
Isoxazole 9
|
Others
|
Neurological Disease
|
|
ISX-9 is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+ influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).
|
-
- HY-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-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-70057A
-
|
Safinamide mesylate
FCE 26743 mesylate; EMD 1195686 mesylate
|
Monoamine Oxidase
|
Neurological Disease
Cardiovascular Disease
|
|
Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 nM). Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al.
|
-
- 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-P2159
-
|
Dynorphin A (1-8)
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
|
-
- 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-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-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-P1548
-
-
- 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-P1548B
-
-
- 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-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-P1143A
-
-
- 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-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 BH |
