Search Result
Results for "
blockade
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-13650
-
|
E 7070
|
Molecular Glues
Carbonic Anhydrase
|
Cancer
|
|
Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
|
-
-
- HY-153346
-
|
RMC-6291
|
Ras
ERK
Apoptosis
|
Cancer
|
|
Elironrasib is an orally active and covalent inhibitor of KRAS G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
|
-
-
- HY-156677
-
STC-15
4 Publications Verification
|
METTL3
|
Cancer
|
|
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
|
-
-
- HY-P9902A
-
|
MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)
|
PD-1/PD-L1
|
Cancer
|
|
Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
|
-
-
- HY-16961
-
|
MGCD516; MG-516
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
|
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
|
-
-
- HY-P99406
-
|
MCLA 158
|
EGFR
|
Cancer
|
|
Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
|
-
-
- HY-B0423
-
|
Eustigmin bromide; Neoserine bromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
|
-
-
- HY-129492
-
GNF4877
1 Publications Verification
|
DYRK
GSK-3
|
Metabolic Disease
|
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
|
-
-
- HY-N6636
-
|
|
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
Valencene is a sesquiterpene that can be isolated from Cyperus rotundus. Valencene possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene inhibits the production and expression of proinflammatory cytokines IL-1β and IL-6 in LPS-stimulated RAW 264.7 cells. Valencene can reduce atopic dermatitis symptoms and recover decreased expression of filaggrin in DNCB-sensitized mouse model .
|
-
-
- HY-B0292A
-
|
BW-33A
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
|
-
-
- HY-128679
-
|
|
IKK
|
Cancer
|
|
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
|
-
-
- HY-B0653A
-
|
(S)-(-)-Bupivacaine monohydrochloride
|
Sodium Channel
Ferroptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
-
- HY-121276
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
|
-
-
- HY-108594
-
|
|
Potassium Channel
|
Metabolic Disease
|
|
PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability .
|
-
-
- HY-13954
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
|
-
-
- HY-P990841
-
|
|
Glycoprotein VI
|
Cancer
|
|
Anti-pan-Glypican Antibody (HS20) is a kind of human IgG1 κ human antibody, targeting to human pan-Glypican. Anti-pan-Glypican Antibody (HS20) can neutralize the heparan sulfate (HS) chains on GPC3 thereby disrupting the Wnt3a-GPC3 interactions leading to blockade of the Wnt3a/β-catenin signaling. Anti-pan-Glypican Antibody (HS20) can be used for the research of cancer, such as hepatocellular carcinoma (HCC) .
|
-
-
- HY-P99406A
-
|
|
EGFR
|
Cancer
|
|
Petosemtamab (FUT8-KO) is an anti-EGFR and anti-LGR5 monoclonal antibody expressed in CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucosyl loss enhances the ADCC effect of the antibody. Petosemtamab (FUT8-KO) leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab (FUT8-KO) can be used for research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC) .
|
-
-
- HY-P99540
-
|
PSB-205; QL1706 (iparomlimab/tuvonralimab); PBS105
|
CTLA-4
|
Cancer
|
|
Tuvonralimab (PSB-205) is a humanized IgG1 monoclonal antibody against CTLA-4. Tuvonralimab can be used in the research of tumors. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
-
- HY-141549
-
-
-
- HY-45509
-
|
RAD150
|
Androgen Receptor
|
Neurological Disease
|
|
TLB 150 Benzoate (RAD150) is a nonsteroidal androgen receptor modulator with an IC50 value of 0.13 μM. TLB 150 Benzoate spontaneously cyclizes under physiological conditions to form RAD 179, resulting in a persistent, reversible, and slow neuronal conduction blockade. TLB 150 Benzoate can be used for research on neurological diseases .
|
-
-
- HY-103094
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression .
|
-
-
- HY-136310
-
|
|
PI5P4K
|
Cancer
|
|
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways .
|
-
-
- HY-P2265A
-
|
|
SOS1
Ras
|
Cancer
|
|
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
-
- HY-122140
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
ACG548B (compound 24) is a potent inhibitor of acetyl- and butyrylcholinesterase (AChE and BChE) with IC50s of 1.78 and 0.496 μM, respectively. ACG548B has higher AChE affinity and selectivity over BChE and ChoK (choline kinase). ACG548B can be uesd for the study of myasthenia gravis and neuromuscular blockade .
|
-
-
- HY-144501
-
|
|
Toll-like Receptor (TLR)
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50 = 24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 (HY-144497). D18 has strong immune activation and anti-tumor activity. D18 commonly used in cancer research, such as colon cancer .
|
-
-
- HY-P0142A
-
|
|
PKG
|
Cardiovascular Disease
|
|
DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
|
-
-
- HY-N2412
-
|
|
Chloride Channel
|
Neurological Disease
Cancer
|
|
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 (IC50=9.8 μM) .
|
-
-
- HY-155847
-
|
|
Phosphatase
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
LYP-IN-3 is a selective, orally active and reversible lymphoid-tyrosine phosphatase (LYP) inhibitor (IC50 = 2.55 μM, Ki = 0.93 μM). D34 exhibits high selectivity of PTP1B, PTPN12, PTPN5 and SSH2. LYP-IN-3 regulates the T-cell receptor (TCR) signaling by specifically inhibiting LYP. LYP-IN-3 does not significantly inhibit MC38 cell viability; its anti-tumor effect stems from immune regulation. LYP-IN-3 can significantly upregulate PD-L1 or PD-1 expression in different immune cells. LYP-IN-3 facilitates T-cell infiltration and enhances T-cell functions. LYP-IN-3 synergizes with PD-L1 blockade can significantly improve colorectal tumor regression. LYP-IN-3 can be used for the study of colorectal cancer .
|
-
-
- HY-W742955
-
|
|
mAChR
|
Neurological Disease
|
|
Pargeverine hydrochloride is an antispasmodic opioid alkaloid. Pargeverine hydrochloride has a moderate and non-selective blockade of muscarinic cholinergic fibers. Pargeverine hydrochloride can be used in the research of painful spasms .
|
-
-
- HY-159161
-
|
|
Orphan GPCR
|
Inflammation/Immunology
Cancer
|
|
PSB-CB-27 is a potent and selective GPR18 inhibitor with an IC50 of 0.65 μM. PSB-CB-27 shows selectivity over Human GPR55, Human CB1 receptor, and Human CB2 receptor. PSB-CB-27 leads to a complete blockade of Δ9-Tetrahydrocannabinol (THC)-induced GPR18 activation. PSB-CB-27 can be used for inflammatory diseases and cancer immunotherapy research .
|
-
-
- HY-B0653
-
|
(S)-(-)-Bupivacaine
|
Sodium Channel
Ferroptosis
|
Neurological Disease
Cancer
|
|
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
-
- HY-122664
-
|
|
BRK
Apoptosis
STAT
ERK
Akt
|
Cancer
|
|
XMU-MP-2 is a selective BRK/PTK6 inhibitor with an IC50 of 5.4 nM. XMU-MP-2 inhibits the proliferation of BRK-positive breast cancer cells and induces apoptosis. XMU-MP-2 is applicable to breast cancer-related research .
|
-
-
- HY-101809A
-
|
|
iGluR
|
Cardiovascular Disease
|
|
CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
-
- HY-P0142
-
|
|
PKG
|
Cardiovascular Disease
|
|
DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
|
-
-
- HY-14408
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade .
|
-
-
- HY-121037
-
|
EGM1
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
|
-
-
- HY-118387
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
AVE-0118 is a Kv1.5 potassium channel blocker and antiarrhythmic agent. AVE-0118 blocks neuronal Kv1.5 potassium channels, thereby enhancing the release of norepinephrine. AVE-0118 enhances field stimulation-induced neurogenic contraction, an effect sensitive to α1-adrenergic receptor blockade. AVE-0118 terminates persistent atrial fibrillation in some dogs. AVE-0118 is applicable to research related to atrial fibrillation and persistent atrial fibrillation .
|
-
-
- HY-16961A
-
|
MGCD516 malate; MG-516 malate
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
|
Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
|
-
-
- HY-P2265
-
|
|
SOS1
Ras
|
Cancer
|
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
-
- HY-135004
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Su-4029 is an agent that interacts with alpha receptors. It negates the blockade of norepinephrine by the reversible adrenergic blocker phentolamine but not by the irreversible blocker Dibenamine, suggesting Su-4029 acts at the same site as these blockers. Su-4029 pretreatment results in three categories of responses to pressor phenylalkylamines: irreversible blockade of amines with no or only p-hydroxylation, reversible blockade of amines with beta-carbon hydroxylation, and no blockade or augmentation of amines with m and p-hydroxylation or m or p plus beta-hydroxylation. Su-4029 may deform the alpha receptor site affected by adrenergic blocking agents .
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-
-
- HY-152156
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
|
-
-
- HY-153543
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC50s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade .
|
-
-
- HY-P991738
-
|
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
LM-299 is a PD-1/VEGF bispecific antibody. LM-299 achieves its dual binding activity through the effective binding of the anti-VEGF-A antibody at the fab end to human VEGF-A, coupled with the blockade of the PD-1/PD-L1 pathway by the anti-PD-1 antibody at the-Fc end. LM-299 can be used for the study of non-small cell lung cancer (NSCLC).
|
-
-
- HY-13650R
-
|
E 7070 (Standard)
|
Molecular Glues
Carbonic Anhydrase
Reference Standards
|
Cancer
|
|
Indisulam (Standard) is the analytical standard of Indisulam. This product is intended for research and analytical applications. Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
|
-
-
- HY-135698
-
|
M-CAM
|
Opioid Receptor
|
Neurological Disease
|
|
Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction .
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-
-
- HY-10383
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications [1][3].
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-
-
- HY-165407
-
|
|
Elastase
CFTR
|
Inflammation/Immunology
|
|
Neltenexine, a mucolytic agent, is an Elastase inhibitor. Neltenexine diminishes anion secretion in in bronchial epithelial cells by inhibiting the Cl− and HCO3- uptake via Na/K/2Cl++− and Na+/HCO3- cotransporter without blockade of the CFTR channel, and also diminishes anion secretion via stimulation of Cl−/HCO3- exchanger. Neltenexine significantly prevents pulmonary emphysema with a reduction of alveolar deformation in rat models induced by Elastase. Neltenexine can be used for lung diseases such as chronic obstructive pulmonary disease (COPD) research .
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-
-
- HY-N6636R
-
|
|
Reference Standards
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
Valencene (Standard) is the analytical standard of Valencene. This product is intended for research and analytical applications. Valencene is a sesquiterpene that can be isolated from Cyperus rotundus. Valencene possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene inhibits the production and expression of proinflammatory cytokines IL-1β and IL-6 in LPS-stimulated RAW 264.7 cells. Valencene can reduce atopic dermatitis symptoms and recover decreased expression of filaggrin in DNCB-sensitized mouse model .
|
-
-
- HY-153544
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC50s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy .
|
-
-
- HY-B0292
-
|
BW-33A free acid
|
nAChR
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation .
|
-
- HY-124047
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue .
|
-
- HY-B0292AR
-
|
BW-33A (Standard)
|
Reference Standards
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atracurium (besylate) (Standard) is the analytical standard of Atracurium (besylate). This product is intended for research and analytical applications. Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
|
-
- HY-163844
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1, with the IC50 of 77 nM. PD-1/PD-L1-IN-49 activates Jurkat T cells, reflecting successful blockade of the PD-1/PD-L1 immune checkpoint .
|
-
- HY-129254
-
-
- HY-116738
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Trimecaine, a local neural blockade agent, has a strong depressant effect on the cerebral cortex and the ascending reticular formation of the brain stem .
|
-
- HY-B0098B
-
|
(R)-UK 33274
|
Adrenergic Receptor
|
Metabolic Disease
|
|
(R)-Doxazosin ((R)-UK 33274) is an isomer of Doxazosin, a selective and orally active a1-adrenoceptor agonist. Doxazosin can be used for systemic antihypertensive and ocular hypotensive. Doxazosin exerts its antihypertensive effect by reducing total peripheral resistance by selective postsynaptic a1-blockade, without reducing cardiac output. Doxazosin can significantly lower both standing and supine blood pressure .
|
-
- HY-101809
-
|
CNS 5161A
|
iGluR
|
Cardiovascular Disease
|
|
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
- HY-113858
-
|
Brefanolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Brefonalol (Brefanolol) is an orally active, non-selective β-adrenergic receptor blocker with vasodilatory properties. Brefonalol exhibits an optimal balance between β-blockade and vasodilatory effects at low doses: it reduces blood pressure and slows heart rate, while increasing stroke volume instead of decreasing it, causing no significant elevation in peripheral resistance and increasing reactive hyperemia; at high doses, the β-blockade effect dominates. Brefonalol can be used in the research of arterial hypertension .
|
-
- HY-B0098C
-
|
(S)-UK 33274
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
(S)-Doxazosin is a long-acting selective α1-adrenoceptor antagonist. (S)-Doxazosin exhibits antihypertensive activity through lowering total perioheral resistance by selective postsynaptic α1-blockade. (S)-Doxazosin reduces blood pressure in dog model with experimentally induced renal hypertension. (S)-Doxazosin can alleviate bladder outflow obstruction. (S)-Doxazosin can also be studied in mental health disorder-related research .
|
-
- HY-107728
-
-
- HY-107697
-
|
|
iGluR
|
Neurological Disease
|
|
N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity .
|
-
- HY-126635
-
|
|
Dopamine Receptor
Adrenergic Receptor
|
Others
|
|
Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
|
-
- HY-121276R
-
|
|
Dopamine Receptor
Reference Standards
|
Neurological Disease
|
|
Benperidol (Standard) is the analytical standard of Benperidol. This product is intended for research and analytical applications. Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
|
-
- HY-106305A
-
|
CI 958 trihydrochloride
|
DNA/RNA Synthesis
|
Cancer
|
|
Ledoxantrone (CI 958) trihydrochloride is a DNA helicases inhibitor with an IC50 of 0.17 μM. Ledoxantrone trihydrochloride can be used in the study of prostate cancer .
|
-
- HY-106305
-
|
CI 958
|
DNA/RNA Synthesis
|
Cancer
|
|
Ledoxantrone (CI 958) is a DNA helicases inhibitor with an IC50 of 0.17 μM. Ledoxantrone can be used in the study of prostate cancer .
|
-
- HY-14828
-
|
SMP-986
|
mAChR
|
Metabolic Disease
|
|
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB) .
|
-
- HY-172348
-
|
|
Bacterial
|
Infection
|
|
BRD-9327 is an inhibitor of EfpA. BRD-9327 binds in the outer vestibule without complete blockade of the substrate path to the outside, suggesting its possible inhibition of the movement necessary for alternate access of the transporter. BRD-9327 can be used for anti-tuberculosis study .
|
-
- HY-126635R
-
|
|
Adrenergic Receptor
Dopamine Receptor
Reference Standards
|
Others
|
|
Mafoprazine (Standard) is the analytical standard of Mafoprazine. This product is intended for research and analytical applications. Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
|
-
- HY-119385
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Savoxepin mesylate is a D2 dopamine receptor (D2 Dopamine Receptor) antagonist with antipsychotic activity. Savoxepin mesylate selectively blocks dopamine D2 receptors in the hippocampus while having no significant effect on D2 receptors in the striatum. This selective blockade helps reduce the risk of extrapyramidal side effects (EPS) .
|
-
- HY-B0284A
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
Nifedipine hydrochloride is a potent vasodilator with calcium antagonist activity. Nifedipine hydrochloride is a useful antianginal compound that can also lower blood pressure. Nifedipine hydrochloride exhibits comparable antihypertensive properties to some new compounds, especially in calcium channel blockade. Nifedipine hydrochloride is used in biological activity studies to develop new antihypertensive and/or antianginal compounds .
|
-
- HY-105925
-
|
MCN 2378
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Mefenidil (MCN 2378) is a selective cerebral vasodilator that is not affected by beta-adrenergic blockade. Mefenidil can be used in the study of cardiovascular disease. In monkey models, mefenidil preferentially increases cerebral blood flow over systemic (femoral) blood flow. Mefenidil is also able to reduce systemic arterial pressure in anesthetized dogs.
|
-
- HY-P4042
-
|
hepatitis B peptide 4980
|
HBV
|
Infection
Inflammation/Immunology
|
|
Hepatitis B Virus Receptor Binding Fragment (hepatitis B peptide 4980) is a synthetic peptide analog which specifically binds to Hep G2 cells. Hepatitis B Virus Receptor Binding Fragment is a promising immunogen expected to elicit protective antibodies based on the concept of the attachment blockade pathway of virus neutralization .
|
-
- HY-131340
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
|
-
- HY-117223
-
|
|
Potassium Channel
|
Neurological Disease
|
|
GEA 857 is a structural analog of the Serotonin (HY-B1473A) uptake blocker Alaproclate (HY-164011). GEA 857 enhances responses induced by muscarinic receptor agonists by inhibiting certain calcium-dependent potassium channels on membranes, a blockade that can enhance or prolong the muscarinic cholinergic effects. GEA 857 can be used in research on neurodegenerative diseases .
|
-
- HY-W424918
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Opromazine hydrochloride is an antipsychotic medication that exhibits sedative and antiemetic pharmacological effects, making it effective for treating psychiatric disorders such as schizophrenia and psychosis. Opromazine hydrochloride functions by reducing dopaminergic activity through the blockade of dopamine receptors in the brain. Opromazine hydrochloride has been analyzed for its metabolites in various microsomal enzymes, revealing differences in formation rates that underscore the variability of drug-metabolizing enzymes in human liver and placenta microsomes.
|
-
- HY-132246
-
|
|
MAGL
|
Neurological Disease
|
|
WWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM . WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice .
|
-
- HY-P5487
-
|
|
iGluR
|
Others
|
|
GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
|
-
- HY-150587
-
|
|
ERK
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver .
|
-
- HY-122171
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .
|
-
- HY-161818
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
|
|
LLW-018 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 2.61 nM. LLW-018 can interrupt PD-1/PD-L1 interaction with an IC50 value of 0.88 μM by cell-based PD-1/PD-L1 blockade bioassays. LLW-018 has the potential for immunotherapy research .
|
-
- HY-113695
-
|
|
Angiotensin-converting Enzyme (ACE)
Adrenergic Receptor
|
Cardiovascular Disease
|
|
BW A575C is a dual inhibitor against angiotensin converting enzyme (ACE) and β-adrenoceptor. BW A575C produces a competitive blockade of Isoprenaline (HY-108353)-induced tachycardia in a guinea-pig right atrial. BW A575C also inhibits Angiotensin I (HY-P1032)-induced pressor responses in rats. BW A575C is promising for research of hypertensive diseases .
|
-
- HY-19904A
-
|
(+/-)-LY2409021
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(+/-)-Adomeglivant ((+/-)-LY2409021) is a potent and selective glucagon receptor antagonist with hypoglycemic activity. (+/-)-Adomeglivant is effective in lowering blood sugar levels in both healthy people and people with type 2 diabetes. (+/-)-Adomeglivant is well tolerated by glucagon signaling blockade in patients with type 2 diabetes and significantly reduces fasting and postprandial blood glucose with a concomitant reversible elevation of aminotransferases. Glucagon signaling inhibition by (+/-)-Adomeglivant is a promising potential inhibitory approach for patients with type 2 diabetes and warrants further evaluation of its benefits and risks in longer clinical trials .
|
-
- HY-170525
-
|
|
CD73
|
Inflammation/Immunology
|
|
CD73-IN-19 (Compound 4ab) is a CD73 inhibitor (with a 44% inhibition rate of CD73 enzymatic activity at 100 μM). CD73-IN-19 (at 10 μM and 100 μM) can completely antagonize the blockade of T cell proliferation induced by TCR (T cell receptor) triggering (which is induced by CD73 activity), and it can also inhibit the hA2A receptor activity in HEK-293 cells (Ki is 3.31 μM). CD73-IN-19 holds promise for research in the field of immune diseases .
|
-
- HY-119800
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Setoperone is an orally active and potent 5-HT₂ receptor antagonist and a moderate dopamine D₂ receptor blocker. Setoperone dissociates from the receptors relatively quickly, but it is easily "captured" by serotonin receptors in the body, resulting in persistent receptor inhibition even after elution. Setoperone can be used to study the negative symptoms of type II schizophrenia and associated mood disorders .
|
-
- HY-178016
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist (IC50 = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity (IC50 = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50 = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy .
|
-
- HY-B0653AS
-
|
(S)-(–)-Bupivacaie-d9hydrochloride
|
Isotope-Labeled Compounds
Ferroptosis
Sodium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
- HY-182537
-
|
|
Drug Derivative
|
Neurological Disease
|
|
Org 9616 bromide is a non-depolarizing neuromuscular blocker with a structure similar to Pancuroniam. Org 9616 bromide induces rapid-onset, short-duration neuromuscular blockade .
|
-
- HY-126635A
-
-
- HY-180379
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Pelanserin (Compound 1) is an orally active antihypertensive agent. Pelanserin is a potent 5-HT2 receptor antagonist. Pelanserin has the ability to block the activity of α-adrenergic receptor, with its ED50 being 0.03 μg/mL. Pelanserin has vasodilatory activity, with its ED100 being 5 μg. Pelanserin exhibits antihypertensive activity in hypertensive rats and renal hypertensive dog breeds. Pelanserin can be used for research on hypertension .
|
-
- HY-107728R
-
|
|
Reference Standards
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
S 25585 (Standard) is the analytical standard of S 25585 (HY-107728). This product is intended for research and analytical applications. S 25585 is a potent and selective neuropeptide Y (NPY) Y5 receptor antagonist. S 25585 reduces food intake but not through blockade of the NPY Y5 receptor .
|
-
- HY-108594R
-
|
|
Reference Standards
Potassium Channel
|
Metabolic Disease
|
|
PD-118057 (Standard) is the analytical standard of PD-118057 (HY-108594). This product is intended for research and analytical applications. PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability .
|
-
- HY-183856
-
|
|
MEK
|
Cancer
|
|
MEK4 IN-4 is a MEK4 inhibitor (IC50 = 0.041 μM) that inhibits the kinase catalytic activity of MEK4 via competitive blockade of ATP binding. MEK4 IN-4 can be used to investigate cell proliferative diseases and disorders associated with MEK4 activity, including cancer .
|
-
- HY-183539
-
|
|
DGK
Interleukin Related
|
Cancer
|
|
INCB191358 is a selective and orally active inhibitor of diacylglycerol kinase α/ζ/ι (DGKα/ζ/ι ) with IC50 values of 0.12, 0.36 and 0.36 nM. INCB191358 induces antigen-dependent T-cell activation, induces IL-2 production and enhances antitumor efficacy in combination with PD-1 blockade. INCB191358 can be used for the research of cancer, such as colon carcinoma .
|
-
- HY-P991952
-
|
|
CTLA-4
|
Cancer
|
|
ADU-1604 is a humanized IgG1 CTLA-4 antibody. ADU-1604 binds to a unique epitope on CTLA-4 and achieves full blockade of both CD80 and CD86 interactions. ADU-1604 enhances human T cell responses. ADU-1604 demonstrates a favorable tolerability profile. ADU-1604 can be used for melanoma research. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-103094R
-
|
|
Reference Standards
5-HT Receptor
|
Inflammation/Immunology
|
|
LY266097 hydrochloride (Standard) is the analytical standard of LY266097 hydrochloride (HY-103094). This product is intended for research and analytical applications. LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression .
|
-
- HY-134483
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases .
|
-
- HY-131691
-
|
|
iGluR
Calcium Channel
|
Neurological Disease
|
|
NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca 2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases .
|
-
- HY-180892
-
|
|
Calcium Channel
Cholinesterase (ChE)
|
Neurological Disease
|
|
Multi-kinase-IN-10 (Compound IIIk) is a multi-kinase inhibitor. Multi-kinase-IN-10 exhibits significant calcium channel blocking activity, with its IC50 being 26.67 μM. Multi-kinase-IN-10 is a potent dual cholinesterase inhibitor, with its IC50 values for hAChE and hBuChE being 0.304 μM and 1.033 μM respectively. Multi-kinase-IN-10 has antioxidant and neuroprotective activities, and shows significant anti-amnesia activity. Multi-kinase-IN-10 can be used for research on Alzheimer's disease .
|
-
- HY-180891
-
|
|
Cholinesterase (ChE)
Calcium Channel
|
Neurological Disease
|
|
Multitarget AD-IN-4 (compound IIIj) is a multitarget-directed ligand (MTDL), with the ability to simultaneously inhibit ChE enzymes (EeAChE IC50 = 0.157 μM, eqBuChE IC50 = 0.147 μM, hAChE IC50 = 1.551 μM, hBuChE IC50 = 2.152 μM), exhibit antioxidant activity, provide neuroprotection, and inhibit calcium channels (Ca 2+ channel blockade: IC50 = 30.59 μM). Multitarget AD-IN-4 reverses Scopolamine (HY-N0296)-induced amnesia in a mouse model. Multitarget AD-IN-4 can be used for Alzheimer’s disease (AD) research .
|
-
- HY-183845
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
HTL0039732 is an orally active antagonist of the prostaglandin EP4 receptor (Prostaglandin E2 Receptor EP4). HTL0039732 reverses PGE2-induced differentiation toward M2-like macrophages. HTL0039732 exhibits efficacy in syngeneic tumor models and acts synergistically with PD-1/PD-L1 pathway blockers. HTL0039732 can be used for the research of advanced solid tumors .
|
-
- HY-175188
-
|
BPN-0027490
|
Myosin
|
Neurological Disease
|
MT-110 (BPN-0027490) is a non-muscle myosin NMIIB-selective inhibitor with high brain penetration and favorable safety profile. MT-110 specifically disrupts NMIIB-dependent actin dynamics in dendritic spines, while it exerts no significant adverse effects on cardiac myosin II and cardiac functions (such as cardiac output and heart rate) at tested concentrations. A single administration of MT-110 produces long-lasting (sustained for several weeks) blockade of methamphetamine motivation associated with environmental cues. MT-110 exhibits extremely high specificity, with no interference with cocaine motivation, hippocampus-dependent memory, fear memory, or locomotor and anxiety-like behaviors. MT-110 serves as a valuable tool compound for investigating the mechanisms of methamphetamine use disorder .
|
-
- HY-182372
-
|
|
Epoxide Hydrolase
|
Neurological Disease
|
|
SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
|
-
- HY-P991740
-
|
|
PD-1/PD-L1
Interleukin Related
|
Cancer
|
|
IBI-363 is a PD-1/IL-2 bispecific antibody with functions of blocking the PD-1/PD-L1 pathway and activating the IL-2 pathway. The IL-2 arm of IBI-363 retains affinity for IL-2Rα but attenuates binding ability to IL-2Rβ and IL-2Rγ to reduce toxicity. The PD-1 binding arm of IBI-363 enables PD-1 blockade and selective delivery of IL-2. IBI-363 can be used in cancer research, such as non-small cell lung cancer .
|
-
- HY-13654
-
|
|
Smo
Hedgehog
|
Cancer
|
|
IPI-269609 is an orally effective Smoothed (SMO) inhibitor that targets the Hedgehog (Hh) signaling pathway. IPI-269609 specifically reduces the ALDH-bright (high aldehyde dehydrogenase activity) cell subset, which is considered the "cancer stem cells" in pancreatic cancer. IPI-269609 significantly inhibits the migration and colony formation of pancreatic cancer cells. IPI-269609 effectively inhibits pancreatic cancer metastasis in a mouse model. IPI-269609 can be used for pancreatic cancer research .
|
-
- HY-P99916
-
|
AMG-427
|
FLT3
CD3
TNF Receptor
|
Inflammation/Immunology
Cancer
|
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
|
-
- HY-12502B
-
|
NZ-105 hydrochloride; (±)-Efonidipine hydrochloride
|
Calcium Channel
SARS-CoV
|
Cardiovascular Disease
Cancer
|
|
Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
|
-
- HY-12502
-
|
NZ-105; (±)-Efonidipine
|
Calcium Channel
SARS-CoV
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Efonidipine (NZ-105) is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine inhibits SARS-CoV-2 main protease. Efonidipine modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine reduces plasma aldosterone levels in vivo. Efonidipine improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
|
-
- HY-P992353
-
|
|
LILRB
|
Cancer
|
|
ES009 is a high-affinity LILRB2 antagonist, with IC50 values of 14.07 nM and 18.61 nM for inhibiting hLILRB2-huANGPTL3 and hLILRB2-huANGPTL4, respectively. ES009 specifically blocks the interactions between LILRB2 and MHC class I as well as non-MHC ligands, thereby effectively inhibiting receptor activation. ES009 can reprogram anti-inflammatory myeloid cells and induce their conversion to a pro-inflammatory phenotype, and also reverse the T cell suppression mediated by macrophages. When combined with anti-PD-1 blockade therapy, ES009 synergistically enhances T cell activation. ES009 can be used in research related to advanced solid tumors and ovarian cancer .
|
-
- HY-P991193
-
|
|
TNF Receptor
|
Cancer
|
|
NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a Ka of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkey LAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to PD-1 blockade, increases the content of intratumoral CD8 + T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer .
|
-
- HY-12502A
-
|
NZ-105 hydrochloride monoethanolate; (±)-Efonidipine hydrochloride monoethanolate
|
Calcium Channel
SARS-CoV
|
Cardiovascular Disease
Neurological Disease
Cancer
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Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
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- HY-136933
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Na+/K+ ATPase
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Cardiovascular Disease
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Gitoxin is a degradation metabolite of Digitoxin (HY-B1357) and a non-competitive Na +/K +-ATPase inhibitor, with an IC50 of 1.18e-6 M against the porcine high-affinity subtype and an IC50 of 2.85e-5 M against the porcine low-affinity subtype. Gitoxin regulates atrial contractility and rhythmicity. Gitoxin is applicable to research related to congestive heart failure .
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- HY-181932
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MAP4K
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Cancer
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HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer .
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- HY-12502AR
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NZ-105 hydrochloride monoethanolate (Standard); (±)-Efonidipine hydrochloride monoethanolate (Standard)
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Reference Standards
Calcium Channel
SARS-CoV
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Cardiovascular Disease
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Efonidipine (NZ-105) hydrochloride monoethanolate (Standard) is the analytical standard of Efonidipine hydrochloride monoethanolate (HY-12502AR). This product is intended for research and analytical applications. Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
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- HY-132184
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5,6-EET; (±)5,6-EpETrE
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Adrenergic Receptor
Calcium Channel
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Endocrinology
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5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2265A
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SOS1
Ras
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Cancer
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SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-P0142A
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PKG
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Cardiovascular Disease
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DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
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- HY-P0142
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PKG
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Cardiovascular Disease
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DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
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- HY-P2265
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SOS1
Ras
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Cancer
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SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
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- HY-P11062
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MUT30
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Peptides
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Cancer
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M30 peptide is an MHC class II epitope antigen that can be used in cancer nanovaccine research .
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- HY-P11061
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Peptides
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Cancer
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M27 peptide is an MHC class I epitope antigen that can be used in cancer nanovaccine research .
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- HY-P4042
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hepatitis B peptide 4980
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HBV
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Infection
Inflammation/Immunology
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Hepatitis B Virus Receptor Binding Fragment (hepatitis B peptide 4980) is a synthetic peptide analog which specifically binds to Hep G2 cells. Hepatitis B Virus Receptor Binding Fragment is a promising immunogen expected to elicit protective antibodies based on the concept of the attachment blockade pathway of virus neutralization .
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- HY-P5487
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iGluR
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Others
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GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P9902A
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MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)
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PD-1/PD-L1
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Cancer
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Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
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(5)
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- HY-P99406
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MCLA 158
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EGFR
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Cancer
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Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
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(5)
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- HY-P990841
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Glycoprotein VI
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Cancer
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Anti-pan-Glypican Antibody (HS20) is a kind of human IgG1 κ human antibody, targeting to human pan-Glypican. Anti-pan-Glypican Antibody (HS20) can neutralize the heparan sulfate (HS) chains on GPC3 thereby disrupting the Wnt3a-GPC3 interactions leading to blockade of the Wnt3a/β-catenin signaling. Anti-pan-Glypican Antibody (HS20) can be used for the research of cancer, such as hepatocellular carcinoma (HCC) .
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(5)
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- HY-P99406A
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EGFR
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Cancer
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Petosemtamab (FUT8-KO) is an anti-EGFR and anti-LGR5 monoclonal antibody expressed in CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucosyl loss enhances the ADCC effect of the antibody. Petosemtamab (FUT8-KO) leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab (FUT8-KO) can be used for research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC) .
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(5)
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- HY-P991740
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PD-1/PD-L1
Interleukin Related
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Cancer
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IBI-363 is a PD-1/IL-2 bispecific antibody with functions of blocking the PD-1/PD-L1 pathway and activating the IL-2 pathway. The IL-2 arm of IBI-363 retains affinity for IL-2Rα but attenuates binding ability to IL-2Rβ and IL-2Rγ to reduce toxicity. The PD-1 binding arm of IBI-363 enables PD-1 blockade and selective delivery of IL-2. IBI-363 can be used in cancer research, such as non-small cell lung cancer .
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(5)
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- HY-P99916
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AMG-427
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FLT3
CD3
TNF Receptor
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Inflammation/Immunology
Cancer
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Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
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-
(5)
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- HY-P99540
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PSB-205; QL1706 (iparomlimab/tuvonralimab); PBS105
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CTLA-4
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Cancer
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Tuvonralimab (PSB-205) is a humanized IgG1 monoclonal antibody against CTLA-4. Tuvonralimab can be used in the research of tumors. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001) .
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(5)
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- HY-P991193
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TNF Receptor
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Cancer
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NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a Ka of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkey LAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to PD-1 blockade, increases the content of intratumoral CD8 + T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer .
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-
(5)
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- HY-P991738
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PD-1/PD-L1
VEGFR
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Cancer
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LM-299 is a PD-1/VEGF bispecific antibody. LM-299 achieves its dual binding activity through the effective binding of the anti-VEGF-A antibody at the fab end to human VEGF-A, coupled with the blockade of the PD-1/PD-L1 pathway by the anti-PD-1 antibody at the-Fc end. LM-299 can be used for the study of non-small cell lung cancer (NSCLC).
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(5)
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- HY-P991952
-
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CTLA-4
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Cancer
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ADU-1604 is a humanized IgG1 CTLA-4 antibody. ADU-1604 binds to a unique epitope on CTLA-4 and achieves full blockade of both CD80 and CD86 interactions. ADU-1604 enhances human T cell responses. ADU-1604 demonstrates a favorable tolerability profile. ADU-1604 can be used for melanoma research. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001) .
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(5)
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- HY-P992353
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LILRB
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Cancer
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ES009 is a high-affinity LILRB2 antagonist, with IC50 values of 14.07 nM and 18.61 nM for inhibiting hLILRB2-huANGPTL3 and hLILRB2-huANGPTL4, respectively. ES009 specifically blocks the interactions between LILRB2 and MHC class I as well as non-MHC ligands, thereby effectively inhibiting receptor activation. ES009 can reprogram anti-inflammatory myeloid cells and induce their conversion to a pro-inflammatory phenotype, and also reverse the T cell suppression mediated by macrophages. When combined with anti-PD-1 blockade therapy, ES009 synergistically enhances T cell activation. ES009 can be used in research related to advanced solid tumors and ovarian cancer .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0653AS
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Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
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