Search Result
Results for "
ERK1/2 inhibitor
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
15
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-50706
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- HY-15816
-
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BVD-523; VRT752271
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ERK
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Cancer
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Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
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- HY-14187
-
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Potassium Channel
Autophagy
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Cardiovascular Disease
Infection
Neurological Disease
Cancer
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Amiodarone, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC50 of ∼45 nM . Amiodarone induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone can be used in the research of both supraventricular and ventricular arrhythmias .
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- HY-13241
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LY2228820 dimesylate
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p38 MAPK
Autophagy
Apoptosis
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Inflammation/Immunology
Cancer
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Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
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- HY-15312
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STAT
JAK
Apoptosis
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Cancer
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WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. WP1066 can cross the blood-brain barrier[1][2][3][4].
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- HY-14188
-
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Potassium Channel
Autophagy
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Cardiovascular Disease
Infection
Neurological Disease
Cancer
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Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC50 of ∼45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
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- HY-14463
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AT13387
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HSP
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Cancer
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Onalespib (AT13387) is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor. Onalespib inhibits the proliferation, survival and migration. Onalespib decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib shows antitumor activity. Onalespib has the potential for the research of non-small cell lung cancer (NSCLC) .
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- HY-136579
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ASN007
5 Publications Verification
ERK-IN-3
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ERK
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Cancer
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ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK. ASN007 inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 exhibits significant anti proliferative activity against various tumor cells. ASN007 can be used for the research of cancers driven by RAS mutations .
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- HY-15816A
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BVD-523 hydrochloride; VRT752271 hydrochloride
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ERK
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Cancer
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Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
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- HY-B1456A
-
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LILLY-53858
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COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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- HY-N10546
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iGluR
Trk Receptor
ERK
Apoptosis
Autophagy
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Neurological Disease
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Ganglioside GM1 is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease .
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- HY-112287
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ERK
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Cancer
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ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively .
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- HY-111407
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MK-8353
5 Publications Verification
SCH900353
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ERK
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Cancer
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MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
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- HY-14569
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- HY-107818
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ERK
Akt
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Cardiovascular Disease
Inflammation/Immunology
Endocrinology
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4-Hydroxychalcone is an orally active flavonoid precursor. 4-Hydroxychalcone inhibits VEGF- and bFGF-induced phosphorylation of ERK1/2 and Akt. 4-Hydroxychalcone suppresses resistant hypertension by alleviating hyperaldosteronism, inflammation and renal injury in cryptochrome gene knockout mice. 4-Hydroxychalcone possesses anti-angiogenic activity .\n
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- HY-D0205A
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Carbocysteine
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NF-κB
PERK
Keap1-Nrf2
Apoptosis
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Infection
Inflammation/Immunology
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Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
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- HY-126288
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ERK
Apoptosis
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Cancer
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ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity .
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- HY-10520
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MNK
Apoptosis
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Cancer
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CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
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- HY-50706A
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- HY-16697
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GPR55
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Cancer
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CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
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- HY-N0774
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ERK
COX
MMP
Toll-like Receptor (TLR)
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Inflammation/Immunology
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Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
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- HY-N12586
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ERK
Reactive Oxygen Species (ROS)
COX
PGE synthase
STAT
HCV
HCV Protease
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Infection
Neurological Disease
Cancer
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Pheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC50=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease .
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- HY-113509
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LXA4
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Interleukin Related
Endogenous Metabolite
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Inflammation/Immunology
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Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
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- HY-123037
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Environmental Pollutants
AMPK
Akt
PERK
Fungal
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Infection
Neurological Disease
Metabolic Disease
Endocrinology
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Triadimefon is an orally active fungicide. Triadimefon significantly reduces the phosphorylation of AKT1 and ERK1/2. Triadimefon significantly increases pAMPK levels, but does not affect total AMPK levels. Triadimefon inhibits the growth of Saccharomyces cerevisiae, disrupts hormone homeostasis (affecting the synthesis of testosterone, etc.), inhibits fetal adrenal development in rats, induces metabolic shifts in hepatocytes, and impairs spatial learning and memory .
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- HY-153738
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ERK
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Cancer
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ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
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- HY-112181
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KO-947
4 Publications Verification
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ERK
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Cancer
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KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
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- HY-N2283
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ERK
Akt
Endogenous Metabolite
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Cancer
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Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
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- HY-16642A
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- HY-122246
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GPR55
PKC
ERK
Arrestin
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Metabolic Disease
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ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation .
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- HY-13905
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HHGV678 mesylate
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Bcr-Abl
c-Kit
PDGFR
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Cancer
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Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .
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- HY-N0924
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Tetrahydrocoptisine
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Interleukin Related
NO Synthase
p38 MAPK
PERK
NF-κB
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Neurological Disease
Inflammation/Immunology
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(±)-Stylopine (Tetrahydrocoptisine) is an alkaloid compound. (±)-Stylopine can be isolated from the tubers of the plant Corydalis. (±)-Stylopine inhibits TNF-α, IL-6, and NO production, and attenuates phosphorylation of p38 MAPK, ERK1/2. (±)-Stylopine inhibits NF-κB expression. (±)-Stylopine exhibits anti-inflammatory activity. (±)-Stylopine has protective effects against foot edema, gastric ulcers, anxiety, depression, and acute lung injury .
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- HY-B0288B
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LILLY-53858 Calcium hydrate
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COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
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Fenoprofen (LILLY-53858) Calcium hydrate is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium hydrate is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium hydrate also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium hydrate has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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- HY-111083
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CID23612552
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GPR55
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Others
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ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC50=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM .
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- HY-151379
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Histone Methyltransferase
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Cancer
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EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .
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- HY-124740
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Melanocortin Receptor
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Cancer
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ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity .
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- HY-W001174
-
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ERK
NF-κB
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Inflammation/Immunology
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2,5-Dihydroxyacetophenone, isolated from Rehmannia glutinosa, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways .
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- HY-142433
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ERK
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Cancer
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ERK1/2 inhibitor 7 is a potent ERK inhibitor with an IC50 of 0.94 nM for ERK2 (WO2021110168A1, WX006) .
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- HY-P0178
-
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Integrin
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Inflammation/Immunology
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LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
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- HY-120006A
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ERK
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Cardiovascular Disease
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(rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS. (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor (CTGF) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor. (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure .
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- HY-76474A
-
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Apoptosis
Syk
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Inflammation/Immunology
Cancer
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BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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- HY-153864
-
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PROTACs
MEK
ERK
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Cancer
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PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
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- HY-76474
-
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Syk
Apoptosis
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Inflammation/Immunology
Cancer
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BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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- HY-145025
-
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ERK
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Inflammation/Immunology
Cancer
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ERK1/2 inhibitor 3 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1) .
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- HY-151367
-
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ERK
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Cancer
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SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer .
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- HY-153445
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MEK-IN-6
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ERK
MEK
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Cancer
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Polfurmetinib (MEK-IN-6) (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). Polfurmetinib can be used for research of cancer .
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- HY-136579A
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ERK-IN-3 benzenesulfonate
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ERK
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Cancer
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ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of ERK. ASN007 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 benzenesulfonate exhibits significant anti proliferative activity against various tumor cells. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations .
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- HY-N1987
-
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Apoptosis
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Inflammation/Immunology
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Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
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- HY-15816R
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BVD-523 (Standard); VRT752271 (Standard)
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ERK
Reference Standards
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Cancer
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Ulixertinib (Standard) is the analytical standard of Ulixertinib. This product is intended for research and analytical applications. Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
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- HY-162460
-
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ERK
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Cancer
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ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations .
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- HY-145026
-
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ERK
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Inflammation/Immunology
Cancer
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ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
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- HY-145027
-
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ERK
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Cancer
|
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ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
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- HY-142437
-
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ERK
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Cancer
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ERK1/2 inhibitor 8 is a potent ERK inhibitor with an IC50 of 0.48 nM for ERK2 (WO2021110168A1, WX007) .
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- HY-113916
-
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AT13387 lactate
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HSP
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Cancer
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Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) .
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- HY-B0288A
-
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LILLY-53858 Calcium
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COX
Melanocortin Receptor
ERK
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Inflammation/Immunology
|
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Fenoprofen (LILLY-53858) Calcium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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- HY-P0178A
-
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Integrin
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Inflammation/Immunology
|
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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 .
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- HY-14188R
-
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Reference Standards
Potassium Channel
Autophagy
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Cardiovascular Disease
Cancer
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Amiodarone (hydrochloride) (Standard) is the analytical standard of Amiodarone (hydrochloride). This product is intended for research and analytical applications. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
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- HY-13699
-
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GnRH Receptor
PERK
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Others
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NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .
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- HY-168171
-
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ERK
Caspase
Apoptosis
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Cancer
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ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2, lending to DSB accumulation and ERK1/2 expression degradation. ERK1/2 inhibitor 11 lowers the levels of BCL-2, and induces DNA damage by inhibiting PARP and ERK1/2. ERK1/2 inhibitor 11 activates caspase 3 to inducing apoptosis. .
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- HY-W838814
-
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ERK
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Cancer
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ERK1/2 inhibitor 12 (compound 76.3) is a ERK1/2 inhibitor which inhibits ERK-mediated phosphorylation of caspase-9 and the p90Rsk-1 kinase. ERK1/2 inhibitor 12 exhibits anti-cancer activity and can be utilized in cancer research .
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- HY-145028
-
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ERK
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Inflammation/Immunology
Cancer
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ERK1/2 inhibitor 6 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 6 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021063335A1, compound 1) .
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- HY-173060
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ERK
Apoptosis
Autophagy
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Cancer
|
|
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
|
-
- HY-N10047
-
|
|
NF-κB
PPAR
|
Cardiovascular Disease
|
|
7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis .
|
-
- HY-162616
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
|
-
- HY-19382
-
|
|
SOD
ERK
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
EUK-189 is a synthetic superoxide dismutase (SOD) and catalase mimetic. EUK-189 can block oxygen/glucose deprivation (OGD)-induced ERK1/2 dephosphorylation, ATP depletion and eliminate ROS production. EUK-189 exhibits neuroprotective effect and can inhibit delayed radiation injury. EUK-189 can be used for the research of neurological disease, such as ischemic stroke .
|
-
- HY-P5977
-
|
Ste-MPKKKPTPIQLNP-NH₂; ERK Activation inhibitor Peptide
|
ERK
|
Cancer
|
|
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
|
-
- HY-N3828
-
|
|
Apoptosis
ERK
JNK
|
Cancer
|
|
epi-Eriocalyxin A (Epieriocalyxin A), a diterpenoid isolated from Isodon eriocalyx, induces colon cancer apoptosis. epi-Eriocalyxin A also inhibits ERK1/2 and JNK activation, which suppresses Bcl-2 expression .
|
-
- HY-177802
-
|
|
ERK
|
Cancer
|
|
C3 sodium is an aptamer that binds to Erk2. C3 binds to the MAP kinase insert domain, a unique site on Erk1/2. Due to this recognition profile C3 inhibits Erk2 activation by its upstream kinase MKK1.
|
-
- HY-50706R
-
|
AZD6244 (Standard); ARRY-142886 (Standard)
|
MEK
Apoptosis
Reference Standards
|
Cancer
|
|
Selumetinib (Standard) is the analytical standard of Selumetinib. This product is intended for research and analytical applications. Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-W565924
-
|
|
mGluR
ERK
|
Neurological Disease
|
|
STX107 is a metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulator (NAM) with a pKi of 8.32. STX107 inhibits glutamate-induced Ca 2+ mobilization, IP1 accumulation, and ERK1/2 phosphorylation. STX107 also inhibits glutamate-induced mGlu5 internalization .
|
-
- HY-107640
-
|
|
MMP
|
Cancer
|
|
WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research .
|
-
- HY-146672
-
|
|
Itk
|
Cancer
|
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
|
-
- HY-137135
-
|
|
Phosphatase
Apoptosis
ERK
p38 MAPK
JNK
|
Cancer
|
|
Cantharidic acid is a selective inhibitor for protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). Cantharidic acid inhibits cell viability and arrest cell cycle at sub G1 phase, induces apoptosis in cells NPC-39 and HONE-1 through the upregulation of ERK1/2, p38, and JNK1/2 pathway .
|
-
- HY-14188S
-
|
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Amiodarone-d4 (hydrochloride) is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ~45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
|
-
- HY-12482
-
|
|
PI3K
Apoptosis
PDK-1
MEK
Akt
ERK
|
Cancer
|
|
X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL) .
|
-
- HY-N11439
-
|
|
CDK
Akt
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2 .
|
-
- HY-156393
-
|
|
ERK
|
Cancer
|
|
Laxiflorin B, a herbal compound, is a novel selective ERK1/2 inhibitor that has antitumor activity .
|
-
- HY-174128
-
|
|
ERK
Apoptosis
|
Cancer
|
|
Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor (IC50 values are 3.04 nM and 1.57 nM, respectively). Multi-target kinase-IN-5 significantly inhibits cancer cell proliferation, migration and invasion, and induces cell apoptosis and cell cycle arrest. Multi-target kinase-IN-5 inhibits the phosphorylation of ERK1/2 and downregulates the activity of its downstream substrate RSK to exert anti-tumor effects. Multi-target kinase-IN-5 can be used in cancer research .
|
-
- HY-111407A
-
|
SCH900353 hydrochloride; MK-8353-001
|
ERK
|
Cancer
|
|
MK-8353 (SCH900353) hydrochloride is a potent, selective, orally active ERK1/2 inhibitor with IC50 values of 23.0 nM and 8.8 nM, respectively. MK-8353 exhibits antitumor activity .
|
-
- HY-125522
-
|
|
ERK
Apoptosis
|
Inflammation/Immunology
|
|
Methyl helicterate is a triterpenoid, that can be isolated from Helicteres angustifolia (Sterculiaceae). Methyl helicterate inhibits hepatic stellate cell activation and promotes cell apoptosis through downregulating the ERK1/2 signaling pathway .
|
-
- HY-158098
-
|
|
FGFR
|
Metabolic Disease
|
|
FGFR1 inhibitor-11 (compound 5g) binds to FGFR1, inactivation of its downstream ERK1/2 and IκBα/NF-κB signaling inhibited RANKL-induced osteoclastogenesis. FGFR1 inhibitor-11 has oral bioactivity .
|
-
- HY-50706AR
-
|
AZD6244 sulfate (Standard); ARRY-142886 sulfate (Standard)
|
MEK
Apoptosis
Reference Standards
|
Cancer
|
|
Selumetinib (sulfate) (Standard) is the analytical standard of Selumetinib (sulfate). This product is intended for research and analytical applications. Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-155533
-
|
|
SHP2
|
Cancer
|
|
YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC50=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells .
|
-
- HY-162850
-
-
- 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-174274
-
|
|
ERK
|
Cancer
|
|
ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC50 value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAF V600E mutant cells (IC50=250 nM in A375 cells). ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma .
|
-
- HY-117982
-
|
|
GnRH Receptor
ERK
|
Endocrinology
|
|
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
|
-
- HY-180419
-
|
|
ERK
Apoptosis
c-Myc
|
Inflammation/Immunology
Cancer
|
|
SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup .
|
-
- HY-W001174R
-
-
- HY-138135
-
|
Fidaxomicin metabolite OP-1118
|
NF-κB
ERK
Apoptosis
Bacterial
|
Infection
|
|
OP-1118 (Fidaxomicin metabolite OP-1118) is an orally active dual inhibitor of NF-κB and ERK1/2, with low systemic plasma exposure, no accumulation, and primary excretion via feces. By inhibiting the phosphorylation of NF-κB and ERK1/2 and reducing the expression of pro-inflammatory cytokines, OP-1118 exerts significant anti-inflammatory, cytoprotective, anti-apoptotic and antibacterial activities. In Clostridium difficile infection models, OP-1118 effectively blocks toxin-mediated intestinal inflammation, cell rounding, histological damage and apoptosis, and its protective effect can be reversed by PMA (HY-18739) .
|
-
- HY-123795
-
|
|
Ras
Akt
ERK
VEGFR
|
Cancer
|
|
NY0123 is a EPAC1 inhibitor. NY0123 significantly inhibits the expression of EPAC1, phosphorylated AKT, phosphorylated ERK1/2 and phosphorylated VEGFR2. NY0123 inhibits angiogenesis and tumor growth of triple-negative breast cancer. NY0123 is applicable to relevant research on triple-negative breast cancer .
|
-
- HY-182299
-
|
|
Phosphatase
Tyrosinase
ERK
|
Inflammation/Immunology
|
|
LYP-IN-5 is a lymphoid tyrosine phosphatase (LYP) inhibitor with an IC50 value of 20.6 μM. LYP-IN-5 enhances the phosphorylation of ZAP70 and ERK1/2 following TCR stimulation, and promotes T cell activation. LYP-IN-5 can be used in the research of autoimmune diseases .
|
-
- HY-182389
-
-
- HY-15947G
-
|
GDC-0994
|
ERK
c-Myc
Hexokinase
Lactate Dehydrogenase
|
Cancer
|
|
Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
|
-
- HY-158969
-
|
|
EGFR
Apoptosis
Akt
ERK
|
Cancer
|
|
EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC50 of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer .
|
-
- HY-10520R
-
|
|
Reference Standards
MNK
Apoptosis
|
Cancer
|
|
CGP 57380 (Standard) is the analytical standard of CGP 57380 (HY-10520). This product is intended for research and analytical applications. CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
|
-
- HY-180226
-
|
|
Apoptosis
Akt
ERK
STAT
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
Apoptosis inducer 55 (Compound 10) is an Apoptosis inducer. Apoptosis inducer 55 induces rapid apoptosis via the intrinsic pathway. Apoptosis inducer 55 potently inhibits several signaling cascades including AKT, ERK1/2, STAT1, STAT3, and S6K. Apoptosis inducer 55 has anti-cancer activity against melanoma .
|
-
- HY-180794
-
|
|
FGFR
Akt
ERK
|
Cancer
|
|
LHQ766 is a highly selective, orally active, covalent FGFR2 inhibitor with an IC50 of 7.3 nM. LHQ766 significantly suppresses phosphorylation of FGFR2 and its downstream signaling molecules FRS2-a, Akt and ERK1/2. LHQ766 selectively suppresses the proliferation of FGFR2-driven cancer cells .
|
-
- HY-175870A
-
|
|
Ras
ERK
|
Cancer
|
|
(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer .
|
-
- HY-180949
-
|
|
EGFR
ERK
|
Cancer
|
|
EGFR-IN-189 (Compound 7) is a selective covalent epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 200 nM. EGFR-IN-189 can effectively inhibit the C797S mutant type of EGFR. EGFR-IN-189 can inhibit cancer cells proliferation and inhibit EGFR phosphorylation and downstream ERK1/2 phosphorylation. EGFR-IN-189 can be used for research of nonsmall cell lung cancer .
|
-
- HY-P11827
-
|
|
Collagen
ERK
TGF-beta/Smad
|
Metabolic Disease
|
|
C11 peptide-1 is an antifibrotic agent that binds directly to Collagen I. C11 peptide-1 physically disrupts Collagen I interaction with Lumican. C11 peptide-1 reduces inflammatory infiltration and inhibits the ERK1/2 and Smad2/3 signaling pathways. C11 peptide-1 can be used for the research of liver fibrosis .
|
-
- HY-B0493
-
|
|
Chloride Channel
COX
|
Inflammation/Immunology
Cancer
|
|
Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
|
-
- HY-14985
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-136778
-
|
|
PARP
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
ERK
p38 MAPK
|
Cardiovascular Disease
|
|
INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases .
|
-
- HY-17522
-
|
2,4-DNOPC
|
Fungal
ERK
JNK
p38 MAPK
Apoptosis
Mitochondrial Metabolism
|
Infection
Endocrinology
|
|
Meptyldinocap (2,4-DNOPC) is a fungicide and cytotoxic agent that acts against powdery mildew. Meptyldinocap upregulates the phosphorylation levels of ERK1/2, JNK and p38. Meptyldinocap induces apoptosis and endoplasmic reticulum stress, disrupts calcium homeostasis, inhibits cell proliferation and migration, downregulates the expression of proliferation- and pregnancy-related genes, and triggers mitochondrial dysfunction. Meptyldinocap can be used in studies related to powdery mildew and implantation failure .
|
-
- HY-B1456AR
-
|
LILLY-53858 (Standard)
|
Reference Standards
COX
Melanocortin Receptor
ERK
|
Inflammation/Immunology
|
|
Fenoprofen (Standard) (LILLY-53858 (Standard)) is the analytical standard of Fenoprofen (HY-B1456A). This product is intended for research and analytical applications. Fenoprofenc is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
|
-
- HY-181067
-
|
|
MEK
ERK
|
Cancer
|
|
IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC50 value of 0.1 nM. IK-595 has oral activity and blood-brain barrier penetration. IK-595 can be used for the research of Ras/MAPK pathway-altered cancers .
|
-
- HY-118817
-
|
|
Reactive Oxygen Species (ROS)
Calcium Channel
JNK
ERK
p38 MAPK
Apoptosis
|
Neurological Disease
|
|
Evariquinone is an anthraquinone compound isolated from the endophytic fungus Colletotrichum sp. JS-0367 of mulberry. Evariquinone possesses direct antioxidant activity. It inhibits excessive phosphorylation of the JNK, ERK1/2 and p38 MAPK signaling pathways by suppressing ROS and Ca 2+, thereby reducing neuronal apoptosis. Evariquinone can be used to study glutamate excitotoxicity-related neurological disorders (such as Alzheimer's disease, Parkinson's disease, cerebral ischemia, etc.) .
|
-
- HY-164551
-
|
|
VEGFR
STAT
ERK
Apoptosis
|
Cancer
|
YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth .
|
-
- HY-N0774R
-
|
|
ERK
Reference Standards
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Isofraxidin (Standard) is the analytical standard of Isofraxidin. This product is intended for research and analytical applications. Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
|
-
- HY-118824A
-
|
(E/Z)-Moschamine
|
Calcium Channel
PDGFR
ERK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
N-Feruloylserotonin ((E/Z)-Moschamine) is a serotonin hydroxycinnamic acid amide. It can be isolated from a variety of plants, particularly the seeds of safflower (Carthamus tinctorius L.). N-Feruloylserotonin inhibits KCl- and 5-HT-induced elevation of intracellular [Ca 2+]i. It suppresses PDGF-BB-induced phosphorylation of PDGFRβ and ERK1/2. N-Feruloylserotonin exerts anti-inflammatory effects on aortic endothelial cells. It inhibits atherosclerotic plaque formation in apolipoprotein E-deficient mice .
|
-
- HY-181020
-
|
|
Phosphodiesterase (PDE)
p38 MAPK
Akt
mTOR
ERK
|
Cancer
|
|
Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma .
|
-
- HY-16697R
-
|
|
GPR55
|
Cancer
|
|
CID 16020046 (Standard) is the analytical standard of CID 16020046. This product is intended for research and analytical applications. CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
|
-
- HY-W004486
-
|
|
HSV
MMP
ERK
p38 MAPK
JNK
|
Infection
|
|
Gallic aldehyde (3,4,5-Trihydroxybenzaldehyde) is a phenolic aldehyde. Gallic aldehyde can be isolated from Geum japonicum. Gallic aldehyde inhibits the gelatinolytic activity and expression of MMP-9. Gallic aldehyde also inhibits ERK1/2, p38, and JNK. Gallic aldehyde has potent anti-HSV-1 and antioxidant activities. Gallic aldehyde also exhibits antibacterial activity against Oenococcus oeni VF .
|
-
- HY-180327
-
|
|
Drug Derivative
Apoptosis
Keap1-Nrf2
Raf
MEK
ERK
|
Neurological Disease
Inflammation/Immunology
|
|
NEPP11 is a cyclopentenone prostaglandin analogue. NEPP11 can inhibit glutamate-induced HT22 cell death in mouse hippocampus and prevent manganese-induced apoptosis in PC12 cells. NEPP11 can activate Nrf2 and maintain MEK1/2 and ERK1/2 activity by inhibiting c-Raf downregulation. NEPP11 exerts a neuroprotective effect in a mouse model of focal cerebral ischemia caused by permanent middle cerebral artery occlusion .
|
-
- HY-D0205AS2
-
|
Carbocysteine-d3
|
Isotope-Labeled Compounds
|
Infection
Inflammation/Immunology
|
|
Carbocisteine-d3 (Carbocysteine-d3) is deuterium labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-B0288BR
-
|
LILLY-53858 Calcium hydrate (Standard)
|
Reference Standards
COX
Melanocortin Receptor
ERK
|
Inflammation/Immunology
|
|
Fenoprofen (LILLY-53858 (Standard)) (Standard) Calcium hydrate is the analytical standard of Fenoprofen Calcium hydrate (HY-B0288B). This product is intended for research and analytical applications. Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
|
-
- HY-N10546A
-
|
|
iGluR
Trk Receptor
ERK
Apoptosis
Autophagy
|
Neurological Disease
|
|
Ganglioside GM1 (bovine) ammonium is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 (bovine) ammonium exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 (bovine) ammonium can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease .
|
-
- HY-129636A
-
|
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
|
-
- HY-18318
-
|
|
Raf
VEGFR
PERK
|
Cancer
|
|
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity .
|
-
- HY-N1987R
-
|
|
Reference Standards
Apoptosis
|
Inflammation/Immunology
|
|
Cucurbitacin IIb (Standard) is the analytical standard of Cucurbitacin IIb. This product is intended for research and analytical applications. Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
|
-
- HY-N2362R
-
|
DL-2-Aminopropionic acid (Standard)
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
|
|
Cucurbitacin IIb (Standard) is the analytical standard of Cucurbitacin IIb. This product is intended for research and analytical applications. Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
|
-
- HY-N7140
-
|
γ-Linolenic acid
|
Endogenous Metabolite
Apoptosis
NF-κB
ERK
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Gamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases .
|
-
- HY-183688
-
|
|
Bacterial
Phosphatase
p38 MAPK
ERK
|
Infection
|
|
MptpB-IN-3 is a selective inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with an IC50 of 0.19 μM. MptpB-IN-3 blocks MptpB-mediated inhibition of the macrophage MAPK pathway and restores the phosphorylation levels of Erk1/2 and p38. MptpB-IN-3 exhibits direct anti-tuberculosis activity against Mycobacterium tuberculosis and reduces the Mycobacterium tuberculosis load in mouse macrophages. MptpB-IN-3 can be used for tuberculosis research .
|
-
- HY-178211
-
|
|
Ras
MEK
ERK
Akt
|
Cancer
|
|
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
|
-
- HY-178194
-
|
|
Ras
MEK
ERK
Akt
|
Cancer
|
|
SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
|
-
- HY-145384
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca 2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases .
|
-
- HY-101546A
-
|
(+)-Cavidine
|
p38 MAPK
ERK
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
Cavidine ((+)-Cavidine) is an analgesic and anti-inflammatory agent. Cavidine can be isolated from Corydalis ternata f. yanhusuo (Y.H.Chou & Chun C.Hsu) Y.C.Zhu. Cavidine reduces the expression of inflammatory factors IL-1β, IL-6 and TNF-α, and inhibits calcium ion influx. Cavidine inhibits the phosphorylation of p38 and ERK1/2. Cavidine increases mechanical and thermal pain thresholds in chronic pain models. Cavidine can be used for the research of chronic pain .
|
-
- HY-N18197
-
|
|
Tyrosinase
NF-κB
AP-1
Interleukin Related
p38 MAPK
JNK
ERK
|
Infection
|
|
Norkurarinol is a prenylated flavonoid. Norkurarinol can be isolated from Sophora flavescens. Norkurarinol potently inhibits mushroom Tyrosinase DOPA oxidase activity with an IC50 of 2.1 μM. Norkurarinol inhibits poly(I:C)-induced NF-κB/AP-1 activation. Norkurarinol inhibits pro-inflammatory cytokines (TNF-α, IL-6). Norkurarinol inhibits phosphorylation of p38, JNK, and ERK1/2. Norkurarinol increases phosphorylation of IRF3. Norkurarinol has antiviral activity against Rotavirus KJ56-1
|
-
- HY-17522R
-
|
2,4-DNOPC (Standard)
|
Reference Standards
Bacterial
|
Infection
Endocrinology
|
|
Meptyldinocap (2,4-DNOPC) (Standard) is the analytical standard of Meptyldinocap. This product is intended for research and analytical applications. Meptyldinocap is a fungicide and cytotoxic agent that acts against powdery mildew. Meptyldinocap upregulates the phosphorylation levels of ERK1/2, JNK and p38. Meptyldinocap induces apoptosis and endoplasmic reticulum stress, disrupts calcium homeostasis, inhibits cell proliferation and migration, downregulates the expression of proliferation- and pregnancy-related genes, and triggers mitochondrial dysfunction. Meptyldinocap can be used in studies related to powdery mildew and implantation failure .
|
-
- HY-120089
-
|
|
FLT3
ERK
Akt
STAT
Apoptosis
|
Cancer
|
|
UNC1666 is an ATP-competitive dual-target Mer/Flt3 tyrosine kinase inhibitor with IC50 values of 0.55 nM and 0.69 nM, and Ki values of 0.16 nM and 0.67 nM, respectively. UNC1666 reduces the phosphorylation levels of Mer and Flt3, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt and Stat), induces cell apoptosis, and decreases colony formation of acute myeloid leukemia cells. UNC1666 is applicable to research related to acute myeloid leukemia .
|
-
- HY-P991964
-
|
Rendomab-B49
|
Endothelin Receptor
|
Cancer
|
|
Rendomab B4 (Rendomab-B49) is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research .
|
-
- HY-B1456AS
-
|
LILLY-53858-13C6 sodium hydrate
|
Isotope-Labeled Compounds
COX
Melanocortin Receptor
ERK
|
Inflammation/Immunology
|
|
Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
|
-
- HY-W1000105
-
|
(E)-3,7-Dimethylocta-2,6-dienal
|
TNF Receptor
Interleukin Related
ERK
JNK
IKK
COX
NO Synthase
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
Geranial is an aromatic compound. It can be isolated from the fruits of Litsea cubeba Lour and the rhizomes of ginger (Zingiber officinale). Geranial inhibits LPS-induced phosphorylation of ERK1/2, JNK1/3 and IκB in macrophages. It suppresses the secretion of IL-1β, TNF-α and IL-6, as well as the expression of pro-IL-1β, iNOS and COX-2. Geranial increases ROS. It can be used in the research of inflammatory diseases .
|
-
- HY-12927
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
|
-
- HY-13404A
-
|
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-160023
-
|
D3S-001
|
Ras
PERK
|
Cancer
|
|
Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
|
-
- HY-12028
-
PD98059
Maximum Cited Publications
391 Publications Verification
|
MEK
ERK
Aryl Hydrocarbon Receptor
Autophagy
|
Cancer
|
|
PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy .
|
-
- HY-148877
-
|
|
HSP
HSV
HIF/HIF Prolyl-Hydroxylase
VEGFR
NF-κB
ERK
Akt
FAK
|
Infection
Inflammation/Immunology
Cancer
|
|
AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs) .
|
-
- HY-13404C
-
|
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404
-
|
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404B
-
|
INC280 hydrochloride; INCB-28060 hydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-152087
-
|
|
ERK
p38 MAPK
|
Cardiovascular Disease
|
|
DCZ19931 is a potent multi-targeting kinase inhibitor. DCZ19931 has anti-angiogenic effects on ocular neovascularization. DCZ19931 also inhibits ERK1/2-MAPK and p38-MAPK signaling .
|
-
- HY-182899
-
|
|
PERK
Ras
COX
PD-1/PD-L1
Apoptosis
DNA/RNA Synthesis
Mitochondrial Metabolism
|
Cancer
|
|
DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma .
|
-
- HY-N2484
-
|
Astrapterocarpan
|
PDGFR
ERK
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Methylnissolin (Astrapterocarpan) is an osteoclast inhibitor with anti-inflammatory, neuroprotective and antioxidant activities. Methylnissolin downregulates the activation of the MAPK and PI3K/AKT pathways, inhibits the phosphorylation of MAPK1 and AKT1, and blocks PDGF-BB-induced phosphorylation of ERK1/2. Methylnissolin reduces the expression and secretion of proinflammatory mediators, decreases intracellular ROS levels, upregulates antioxidant enzymes, and downregulates osteoclastogenesis markers. Methylnissolin is applicable to research related to ischemic stroke, osteoporosis, cardiovascular diseases, skin aging, etc.
|
-
- HY-W050000
-
OR-1855
1 Publications Verification
|
Drug Metabolite
Reactive Oxygen Species (ROS)
ERK
p38 MAPK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
OR-1855, an active metabolite of Levosimendan (HY-14286), has effect on myometrial contractility. OR-1855 exerts anti-inflammatory effects by inhibiting IL-1β-induced ROS formation and NAD(P)H oxidase-dependent superoxide radical generation in HUVECs. OR-1855 inhibits IL-1β-induced phosphorylation p38 MAPK, ERK1/2, c-Jun and JNK in HUVECs. OR-1855 can be used for the study of inflammation .
|
-
- HY-113509S
-
|
LXA4-d5
|
Interleukin Related
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
|
-
- HY-175820
-
|
|
VEGFR
ERK
Apoptosis
EGFR
|
Cancer
|
|
AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer .
|
-
- HY-123037R
-
|
|
Reference Standards
Fungal
Akt
PERK
AMPK
|
Infection
Neurological Disease
Metabolic Disease
Endocrinology
|
|
Triadimefon (Standard) is the analytical standard of Triadimefon (HY-123037). This product is intended for research and analytical applications. Triadimefon is an orally active fungicide. Triadimefon significantly reduces the phosphorylation of AKT1 and ERK1/2. Triadimefon significantly increases pAMPK levels, but does not affect total AMPK levels. Triadimefon inhibits the growth of Saccharomyces cerevisiae, disrupts hormone homeostasis (affecting the synthesis of testosterone, etc.), inhibits fetal adrenal development in rats, induces metabolic shifts in hepatocytes, and impairs spatial learning and memory .
|
-
- HY-N10175
-
|
|
NO Synthase
NF-κB
ERK
Interleukin Related
TNF Receptor
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
keleyacetal C, a meroterpenoid compound with anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways. Berkeleyacetal C significantly inhibits the expression of iNOS and the following NO production by macrophages. Berkeleyacetal C inhibits expression and secretion of key pro-inflammatory factors and chemokines (TNF-α, IL-6, IL-1β, MIP-1α, and MCP-1). Berkeleyacetal C also inhibits activation of neutrophils and reactive oxygen species (ROS) production. Berkeleyacetal C can be used for the study of inflammatory disorders .
|
-
- HY-B1272A
-
-
- HY-12716A
-
|
|
Adrenergic Receptor
ERK
p38 MAPK
Dopamine Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
BRL-44408 maleate is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 maleate exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 maleate can be used in studies related to acute respiratory distress syndrome, depression and visceral pain .
|
-
- HY-D0205AS1
-
|
Carbocysteine-13C3-1
|
Isotope-Labeled Compounds
Keap1-Nrf2
NF-κB
PERK
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Carbocisteine- 13C3-1 (Carbocysteine- 13C3-1) is 13C labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-12716
-
|
|
Adrenergic Receptor
p38 MAPK
Dopamine Receptor
ERK
|
Cardiovascular Disease
Neurological Disease
|
|
BRL-44408 is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 can be used in studies related to acute respiratory distress syndrome, depression and visceral pain .
|
-
- HY-B1272
-
-
- HY-B0493R
-
|
|
Reference Standards
Chloride Channel
COX
|
Inflammation/Immunology
|
|
Niflumic acid (Standard) is the analytical standard of Niflumic acid. This product is intended for research and analytical applications. Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
|
-
- HY-120793
-
|
TRB-N0224
|
Ras
Apoptosis
MMP
|
Inflammation/Immunology
Cancer
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
|
-
- HY-183316
-
|
|
Akt
PI3K
PERK
p38 MAPK
ERK
Apoptosis
|
Cancer
|
|
Anticancer agent 319 is an anticancer agent. Anticancer agent 319 inhibits the proliferation of liver cancer cells. Anticancer agent 319 inhibits AKT phosphorylation and blocks the PI3K/AKT signaling axis; meanwhile, it inhibits ERK1/2 phosphorylation and blocks the MAPK/ERK signaling axis. Anticancer agent 319 induces G2/M phase cell cycle arrest, triggers apoptosis, and reduces mitochondrial membrane potential in liver cancer cells. Anticancer agent 319 can be used for the research of hepatocellular carcinoma .
|
-
- HY-125542
-
|
|
Apoptosis
JAK
STAT
ERK
PI3K
Akt
|
Cancer
|
|
DCZ3301 is an apoptosis inducer. DCZ3301 modulates JAK2/STAT3, ERK1/2, and PI3K/AKT pathways. DCZ3301 induces G2/M and M phase cell cycle arrest and inhibits cell proliferation and viability. DCZ3301 enhances DNA damage, inhibits DNA repair, and suppresses angiogenesis. DCZ3301 can be used for the research of diffuse large B-cell lymphoma, multiple myeloma and leukemia/lymphoma .
|
-
- HY-108543
-
|
|
Phosphatase
Apoptosis
|
Cancer
|
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)) . NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway .
|
-
- HY-122241
-
|
|
PKC
|
Cancer
|
|
MT477 is a potent protein kinase C (PKC) inhibitor. MT477 induces apoptosis and necrosis. MT477 decreases the protein expression of Ras-GTP, p-Erk1/2, p-Elk1. MT477 shows antitumor activity .
|
-
- HY-173119
-
|
|
ERK
Autophagy
Apoptosis
p62
mTOR
Reactive Oxygen Species (ROS)
Ferroptosis
|
Cancer
|
|
SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC50 of 38.69 nM and a Kd of 126.9 nM against human ERK1, an IC50 of 40.12 nM and a Kd of 209.8 nM against ERK2, and an IC50 of 59.72 nM and a Kd of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer .
|
-
- HY-159642
-
|
TYRA-300
|
FGFR
ERK
|
Metabolic Disease
Cancer
|
|
Dabogratinib (TYRA-300) is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia .
|
-
- HY-168438
-
|
|
EGFR
Akt
ERK
|
Cardiovascular Disease
|
|
ERBB agonist-1 (Compound EF-1) is an agonist for ERBB4, that activates the ERBB4 signaling pathway by inducing dimerization of the ERBB4 receptor with an EC50 of 10.5 μM. ERBB agonist-1 induces phosphorylation of Akt and ERK1/2, reduces the collagen expression in cardiac fibroblasts, inhibits H2O2-induced cardiomyocyte death and Ang II (HY-13948)-induced cardiomyocyte hypertrophy. ERBB agonist-1 prevents fibrosis and exhibits cardioprotective efficacy in mouse models .
|
-
- HY-P11147
-
|
|
Interleukin Related
FAK
Src
Akt
ERK
MMP
|
Cancer
|
|
IL13Rα2 D1 is an effective IL-13/IL13Rα2 signaling axis inhibitor. IL13Rα2 D1 can inhibit IL-13-induced cell adhesion, migration, invasion, and proliferation. IL13Rα2 D1 can inhibit FAK, Src, AKT, ERK1/2 phosphorylation, and MMP expression. IL13Rα2 D1 can be used for research on cancers such as colorectal cancer .
|
-
- HY-W004486R
-
|
|
Reference Standards
HSV
MMP
ERK
p38 MAPK
JNK
|
Infection
|
|
Gallic aldehyde (Standard) is an analytical standard of Gallic aldehyde (HY-W004486). This product is intended for research and analytical applications. Gallic aldehyde (3,4,5-Trihydroxybenzaldehyde) is a phenolic aldehyde. Gallic aldehyde can be isolated from Geum japonicum. Gallic aldehyde inhibits the gelatinolytic activity and expression of MMP-9. Gallic aldehyde also inhibits ERK1/2, p38, and JNK. Gallic aldehyde has potent anti-HSV-1 and antioxidant activities. Gallic aldehyde also exhibits antibacterial activity against Oenococcus oeni VF .
|
-
- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-168493
-
|
|
FLT3
VEGFR
HDAC
STAT
PERK
|
Cancer
|
|
FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia .
|
-
- HY-N2450R
-
-
- HY-N2450
-
|
|
Apoptosis
EGFR
ERK
NF-κB
Microtubule/Tubulin
|
Cancer
|
|
Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals .
|
-
- HY-B2162D
-
|
Chondroitin polysulfate (from chicken)
|
ERK
p38 MAPK
Interleukin Related
TNF Receptor
Prostaglandin Receptor
MMP
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Chondroitin sulfate (from chicken) (Chondroitin polysulfate (from chicken)) is an orally active, sulfated linear polysaccharide extracted from chickens, which belongs to glycosaminoglycans. Chondroitin sulfate (from chicken) reduces the phosphorylation levels of ERK1/2 and p38MAPK, inhibits the expression of inflammatory cytokines and MMP, and downregulates the levels of IL-1β, IL-6, TNF-α and PGE2. Chondroitin sulfate (from chicken) improves motor function, protects cartilage tissue, reverses chondrocyte aggregation, and regulates the structure of intestinal flora. Chondroitin sulfate (from chicken) can be used in research related to osteoarthritis .
|
-
- HY-B1272AS
-
-
- HY-B1272AS1
-
-
- HY-N17131
-
|
|
NF-κB
ERK
|
Inflammation/Immunology
|
|
24-O-Acetyllycoclavanol (compound 1) is a triterpenoid anti-inflammatory agent that selectively targets the NF-κB and ERK1/2 signaling pathways. It exerts its anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and COX-2 expression, reducing the production of inflammatory mediators such as nitric oxide (NO), IL-1β, and IL-8. 24-O-Acetyllycoclavanol can be used in research related to inflammatory bowel disease (IBD). 24-O-Acetyllycoclavanol can be biologically isolated from the ethyl acetate extract of Lycopodium clavatum .
|
-
- HY-134877
-
|
|
EGFR
ERK
Akt
|
Cancer
|
|
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .
|
-
- HY-12028R
-
|
|
MEK
ERK
Aryl Hydrocarbon Receptor
Autophagy
|
Cancer
|
|
PD98059 (Standard) is the analytical standard of PD98059. This product is intended for research and analytical applications. PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy .
|
-
- HY-12723
-
|
(-)-Apomorphine
|
Dopamine Receptor
Monoamine Oxidase
Reactive Oxygen Species (ROS)
JNK
ERK
Amyloid-β
Tau Protein
MMP
|
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Apomorphine ((-)-Apomorphine) is a potent dopamine receptor agonist. Apomorphine also inhibit MAO-A and MAO-B. Apomorphine exerts neuroprotective effect and can relax rat corpus cavernosum. Apomorphine can inhibit ROS production, DNA fragmentation and inibit JNK and ERK1/2 phosphorylation. Apomorphine can enhance degradation of intracellular Aβ40 and Aβ42, reduces tau protein levels and inhibit MMP-9 expression. Apomorphine is a highly potent radical scavenger and iron chelator. Apomorphine can be used for the researches of dementia, parkinson's disease, alzheimer disease, breast carcinoma, and erectile dysfunction .
|
-
- HY-13404CR
-
|
INC280 dihydrochloride hydrate (Standard); INCB-28060 dihydrochloride hydrate (Standard)
|
c-Met/HGFR
Apoptosis
Reference Standards
|
Cancer
|
|
Capmatinib (dihydrochloride hydrate) (Standard) is the analytical standard of Capmatinib (dihydrochloride hydrate). This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-173153
-
|
|
JNK
PERK
MEK
NO Synthase
|
Inflammation/Immunology
Cancer
|
|
BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities .
|
-
- HY-13404R
-
|
INC280 (Standard); INCB28060 (Standard)
|
Reference Standards
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-P991358
-
|
LFA-102; X213
|
Estrogen Receptor/ERR
STAT
Akt
|
Cancer
|
|
XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer .
|
-
- HY-W745090
-
|
|
Formyl Peptide Receptor (FPR)
Src
ERK
Akt
p38 MAPK
|
Others
|
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
- HY-W744699
-
|
(+)-Larixol
|
Src
ERK
Akt
|
Inflammation/Immunology
|
|
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
- HY-162888
-
|
|
PDGFR
ERK
|
Cardiovascular Disease
|
|
WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension .
|
-
- HY-B0916
-
|
|
Environmental Pollutants
MMP
Insecticide
Cholinesterase (ChE)
ERK
Keap1-Nrf2
Reactive Oxygen Species (ROS)
|
Infection
Neurological Disease
Cancer
|
|
Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
|
-
- HY-181965
-
|
|
Ras
ERK
p38 MAPK
|
Cancer
|
|
KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
|
-
- HY-B1272R
-
|
|
Reference Standards
Adrenergic Receptor
ERK
JNK
p38 MAPK
NF-κB
AP-1
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Desipramine hydrochloride (Standard) is the analytical standard of Desipramine hydrochloride (HY-B1272). This product is intended for research and analytical applications. Desipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .
|
-
- HY-N6664
-
|
Arabic gum
|
Environmental Pollutants
Parasite
Apoptosis
PERK
Transmembrane Glycoprotein
|
Infection
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Gum Arabic is an orally active complex branched polysaccharide. Gum Arabic can be isolated from the Acacia senegal tree. Gum Arabic upregulates the expression of maturation markers (CD86, CD40, and CD54), promotes ERK1/2 phosphorylation, and inhibits Apoptosis. Gum Arabic exhibits antimalarial effects against Plasmodium berghei ANKA. Gum Arabic exhibits hepatoprotective, renal, and cardiovascular protective activities. Gum Arabic improves obesity. Gum Arabic is commonly used as a stabilizer and thickener. Gum Arabic can be used in the research of brain tumor imaging .
|
-
- HY-N10133
-
|
3′-Prenylnaringenin
|
Bacterial
mTOR
Akt
PI3K
NF-κB
Caspase
JNK
ERK
COX
NO Synthase
Apoptosis
|
Others
|
Licoflavanone (3′-Prenylnaringenin) is a flavanone with antioxidant, anti-inflammatory and anticancer activities. Licoflavanone can be isolated from the leaf extract of Glycyrrhiza glabra. Licoflavanone downregulates the mTOR/PI3K/AKT signaling pathway to inhibit the proliferation, migration and invasion of cancer cells, while activates Bax, Bad and multiple caspase enzymes to induce apoptosis. Its anti-inflammatory effect is manifested by reducing the nuclear translocation of NF-κB, decreasing the phosphorylation levels of p38, JNK and ERK1/2, thereby inhibiting the expression of nitric oxide, proinflammatory cytokines, COX-2 and iNOS. Licoflavanone is used in studies on nasopharyngeal carcinoma and related mechanisms .
|
-
- HY-108543R
-
|
|
Reference Standards
Phosphatase
Apoptosis
|
Cancer
|
|
NSC 95397 (Standard) is the analytical standard of NSC 95397 (HY-108543). This product is intended for research and analytical applications. NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)) . NSC 95397 inhibits mitogen-activated protein Kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway .
|
-
- HY-P1650
-
|
B 9870
|
Bradykinin Receptor
ERK
|
Cancer
|
|
Breceptin (B 9870) is an antagonist of the bradykinin B1/B2 receptor (B1/B2R). Breceptin exhibits an irreversible antagonist effect on B2R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B2R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer .
|
-
- HY-N0526
-
|
|
Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
|
Neurological Disease
Inflammation/Immunology
|
|
2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
|
-
- HY-N1910
-
|
|
SARS-CoV
Virus Protease
Succinate Receptor 1
ERK
|
Infection
Neurological Disease
|
|
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy .
|
-
- HY-12723R
-
|
(-)-Apomorphine (Standard)
|
Reference Standards
Dopamine Receptor
Monoamine Oxidase
Reactive Oxygen Species (ROS)
JNK
ERK
Amyloid-β
Tau Protein
MMP
|
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Apomorphine ((-)-Apomorphine) (Standard) is the analytical standard of Apomorphine (HY-12723). This product is intended for research and analytical applications. Apomorphine is a potent dopamine receptor agonist. Apomorphine also inhibit MAO-A and MAO-B. Apomorphine exerts neuroprotective effect and can relax rat corpus cavernosum. Apomorphine can inhibit ROS production, DNA fragmentation and inibit JNK and ERK1/2 phosphorylation. Apomorphine can enhance degradation of intracellular Aβ40 and Aβ42, reduces tau protein levels and inhibit MMP-9 expression. Apomorphine is a highly potent radical scavenger and iron chelator. Apomorphine can be used for the researches of dementia, parkinson's disease, alzheimer disease, breast carcinoma, and erectile dysfunction .
|
-
- HY-15872
-
|
|
Farnesyl Transferase
Ras
ERK
mTOR
Caspase
Apoptosis
Akt
PI3K
Bacterial
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
FTI-277 is a farnesyltransferase (FTase) inhibitor. FTI-277 inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification .
|
-
- HY-156041
-
|
Lyso-PE (egg); LPE (egg); L-α-lysophosphatidylethanolamine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lysophosphatidylethanolamine (LPE) is a naturally-occurring lysophospholipid that can be generated via deacylation of phosphatidylethanolamine by phospholipase A2 (PLA2). It increases the phosphorylation of ERK1/2 in PC12 cells, an effect that can be blocked by the MEK inhibitors U-0126 (HY-12031A) and PD 98059 (HY-12028) and the EGFR inhibitor AG-1478 (HY-13524).1 LPE also increases neurite outgrowth and expression of neurofilament M in PC12 cells. LPE inhibits the activity of phospholipase D (PLD) partially purified from cabbage.3 This product contains lysophosphatidylethanolamine molecular species with variable fatty acyl chain lengths at the sn-1 position and a hydroxy group at the sn-2 position.
|
-
- HY-W750153
-
|
|
Isotope-Labeled Compounds
Insecticide
MMP
Cholinesterase (ChE)
Reactive Oxygen Species (ROS)
ERK
Keap1-Nrf2
|
Infection
Neurological Disease
Cancer
|
|
Propoxur-d7 is the deuterium labeled Propoxur. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
|
-
- HY-175286
-
|
|
Integrin
ERK
|
Inflammation/Immunology
Cancer
|
|
α4β1 antagonist-1 (Compound 4) is a highly selective α4β1 integrin antagonist (IC50=15 nM). α4β1 antagonist-1 inhibits integrin-mediated cell adhesion and ERK1/2 signaling activation. α4β1 antagonist-1 also exhibits partial agonism toward αMβ2 integrin (EC50=23 nM). α4β1 antagonist-1 is promising for research of chronic inflammatory diseases (e.g., rheumatoid arthritis, multiple sclerosis) and cancers .
|
-
- HY-20888
-
|
MNF
|
Aryl Hydrocarbon Receptor
Cytochrome P450
Apoptosis
Akt
ERK
TGF-beta/Smad
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
3'-Methoxy-4'-nitroflavone (MNF) is a specific aryl hydrocarbon receptor (AhR) antagonist. 3'-Methoxy-4'-nitroflavone activates AhR by inhibiting CYP1, the metabolic enzyme of the endogenous ligand FICZ (HY-12451), leading to the accumulation of FICZ. 3'-Methoxy-4'-nitroflavone reverses the anti-apoptotic effect of TCDD, attenuates the activation of Akt and Erk1/2 kinases and the expression of TGFα induced by TCDD. 3'-Methoxy-4'-nitroflavone can be used in research related to breast tumor promotion, rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease .
|
-
- HY-116504
-
|
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
|
-
- HY-P4866
-
|
|
Integrin
Transglutaminase
Akt
p38 MAPK
ERK
Caspase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Q-Peptide is an angiopoietin-1 derived peptide (QHREDGS). Q-Peptide interacts with β1-integrin, binds to integrins on the surface of osteoblasts, and serves as an acyl donor substrate for Streptomyces mobaraensis transglutaminase. Q-Peptide activates Akt, MAPKp42/44, ILK, ERK1/2, and downregulates caspase-3/7. Q-Peptide inhibits cell apoptosis, enhances cell adhesion and migration, and promotes osteoblast differentiation, bone matrix deposition and mineralization. Q-Peptide can be used in studies related to myocardial infarction, bone regeneration, diabetic wound repair and human induced pluripotent stem cells .
|
-
- HY-101460
-
|
|
E3 Ligase Ligand-Linker Conjugates
Drug Derivative
|
Cancer
|
|
Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research .
|
-
- HY-W050000R
-
|
|
Drug Metabolite
Reference Standards
Reactive Oxygen Species (ROS)
ERK
p38 MAPK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
OR-1855 (Standard) is an analytical standard of OR-1855 (HY-W050000). This product is intended for research and analytical applications. OR-1855, an active metabolite of Levosimendan (HY-14286), has effect on myometrial contractility. OR-1855 exerts anti-inflammatory effects by inhibiting IL-1β-induced ROS formation and NAD(P)H oxidase-dependent superoxide radical generation in HUVECs. OR-1855 inhibits IL-1β-induced phosphorylation p38 MAPK, ERK1/2, c-Jun and JNK in HUVECs. OR-1855 can be used for the study of inflammation .
|
-
- HY-10254
-
|
PD0325901; PD325901
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
|
-
- HY-168376
-
|
9(10)-Nitrated oleic acid
|
PPAR
ERK
Akt
NO Synthase
|
Metabolic Disease
Inflammation/Immunology
|
|
9 (10)-Nitrooleate (9(10)-Nitrated oleic acid) is an endogenous lipid signaling mediator with vasoprotective effects. 9 (10)-Nitrooleate enhances enzymatic activity and improves nitric oxide bioavailability by inducing phosphorylation of Akt and ERK1/2, regulating the multi-site phosphorylation status of eNOS and optimizing its interaction with Hsp90. 9 (10)-Nitrooleate also activates PPARα, PPARδ and PPARγ receptors, thereby regulating adipogenesis, glucose uptake and inflammation-related gene expression, and exhibits immunosuppressive effects by inhibiting neutrophil migration and cytokine secretion. 9 (10)-Nitrooleate is widely used in studies of sepsis and related inflammatory diseases .
|
-
- HY-159642G
-
|
TYRA-300
|
FGFR
ERK
|
Metabolic Disease
Cancer
|
|
Dabogratinib (TYRA-300) (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia .
|
-
- HY-13749B
-
|
MK-0431 phosphate monohydrate
|
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes .
|
-
- HY-59201
-
|
|
nAChR
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
- HY-59201A
-
|
|
ERK
5-HT Receptor
Epigenetic Reader Domain
nAChR
|
Neurological Disease
Metabolic Disease
|
|
A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
- HY-13749
-
|
MK-0431
|
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes .
|
-
- HY-13749A
-
|
MK-0431 phosphate
|
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes .
|
-
- HY-13749E
-
|
MK-0431 hydrochloride
|
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes .
|
-
- HY-B0380A
-
|
|
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-B0380
-
|
|
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-B0916S
-
|
|
Isotope-Labeled Compounds
Insecticide
Cholinesterase (ChE)
MMP
Reactive Oxygen Species (ROS)
ERK
Keap1-Nrf2
|
Infection
Neurological Disease
Cancer
|
|
Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
|
-
- HY-120406
-
|
|
Btk
Akt
mTOR
p38 MAPK
ERK
CCR
Apoptosis
|
Cancer
|
|
LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research .
|
-
- HY-110038
-
|
|
Farnesyl Transferase
Ras
ERK
mTOR
Apoptosis
Caspase
Akt
PI3K
Bacterial
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
FTI-277 TFA is a farnesyltransferase (FTase) inhibitor. FTI-277 TFA inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 TFA activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 TFA activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 TFA can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification .
|
-
- HY-B0916R
-
|
|
Reference Standards
MMP
Insecticide
Cholinesterase (ChE)
Reactive Oxygen Species (ROS)
ERK
Keap1-Nrf2
|
Infection
Neurological Disease
Cancer
|
|
Propoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
|
-
- HY-147183
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
|
-
- HY-147183A
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
|
-
- HY-P991219
-
|
EnX209
|
Interleukin Related
ERK
MMP
|
Inflammation/Immunology
|
|
Anti-IL11RA Antibody (X209) (EnX209) is a human-derived IgG4, κ-type antibody inhibitor targeting IL11RA, with a KD of 6 nM. Anti-IL11RA Antibody (X209) blocks the IL11RA signaling pathway, inhibits ERK-dependent activation, and reduces the activation level of ERK1/2. Anti-IL11RA Antibody (X209) exerts a protective effect against fibrosis. Anti-IL11RA Antibody (X209) is applicable to studies related to liver fibrosis, cardiac fibrosis and other related conditions. Recommended isotype control: Human IgG4 kappa, Isotype Control (HY-P99003) .
|
-
- HY-147183B
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
|
-
- HY-149577
-
|
|
EBV
|
Cancer
|
|
Epstein-Barr virus (EBV) lytic cycle inducer-1 Dp44mT (compound C7) is an iron-chelatoe-like compound. Dp44mT cooperates with HDAC inhibitor Romidespin (HY-15149) and SAHA to induce EBV lytic cycle. Dp44mT reactivates EBV lytic cycle by activating the ERK1/2-autophagy axis in epithelial cancers .
|
-
- HY-B0380S2
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-B0380S1
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-13749R
-
|
MK-0431 (Standard)
|
Reference Standards
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749). This product is intended for research and analytical applications. Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
|
-
- HY-13749AR
-
|
MK-0431 phosphate (Standard)
|
Reference Standards
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin (MK-0431) phosphate (Standard) is the analytical standard of Sitagliptin phosphate (HY-13749A). This product is intended for research and analytical applications. Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
|
-
- HY-13749AS
-
|
MK-0431-d4 phosphate
|
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin-d4 phosphate (MK-0431-d4) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
|
-
- HY-13749S3
-
|
MK-0431-d6
|
Isotope-Labeled Compounds
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
|
-
- HY-13749S2
-
|
MK-0431-d4
|
Isotope-Labeled Compounds
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
|
-
- HY-13749S1
-
|
MK-0431-d4 hydrochloride
|
Isotope-Labeled Compounds
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin-d4 hydrochloride is the deuterium labeled Sitagliptin hydrochloride (HY-13749E). Sitagliptin hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
|
-
- HY-13749BR
-
|
MK-0431 phosphate monohydrate (Standard)
|
Reference Standards
Dipeptidyl Peptidase
GLP Receptor
Endogenous Metabolite
PKA
ERK
|
Metabolic Disease
|
|
Sitagliptin (MK-0431) phosphate monohydrate (Standard) is the analytical standard of Sitagliptin phosphate monohydrate (HY-13749B). This product is intended for research and analytical applications. Sitagliptin phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.
|
-
- HY-181931
-
|
|
Phosphodiesterase (PDE)
p38 MAPK
LPL Receptor
ERK
JNK
|
Inflammation/Immunology
|
|
Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC50 of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis .
|
-
- HY-113016
-
|
|
Apoptosis
Wnt
ERK
Bacterial
Interleukin Related
|
Infection
Metabolic Disease
Cancer
|
|
Elaidic acid is an orally active trans fatty acid. Elaidic acid enhances the stemness of colorectal cancer cells by activating the Wnt/ERK1/2 pathway, thereby promoting cell proliferation, invasion and metastasis, and inhibiting apoptosis. Elaidic acid also inhibits the growth of Lactobacillus and alters the cell surface hydrophobicity of Lactobacillus. Elaidic acid reduces basal 2-deoxyglucose uptake in muscle cells and adipocytes. Elaidic acid can be used in research on colorectal cancer, insulin and other related areas .
|
-
- HY-120281
-
|
|
MEK
PI3K
Akt
Apoptosis
Caspase
|
Cancer
|
|
ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
|
-
- HY-181964
-
|
|
|
Cancer
|
|
KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
|
-
- HY-101349A
-
|
|
Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
|
Neurological Disease
Cancer
|
|
L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .
|
-
- HY-101349
-
|
|
Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
|
Neurological Disease
Cancer
|
|
L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .
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-
- HY-N0526R
-
|
|
Reference Standards
Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
|
Neurological Disease
Inflammation/Immunology
|
|
2"-O-Galloylhyperin (Standard) is the analytical standard of 2"-O-Galloylhyperin (HY-N0526). This product is intended for research and analytical applications. 2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
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-
- HY-122214
-
|
|
Autophagy
|
Cancer
|
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells . AC-73 is also an anti-proliferative agent and an inducer of autophagy in leukemic cells .
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-
- HY-N12561
-
|
|
ERK
p38 MAPK
JNK
|
Others
|
|
Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .
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-
- HY-B0380AR
-
|
|
Reference Standards
Opioid Receptor
Apoptosis
Potassium Channel
NF-κB
Akt
IRAK
JNK
Toll-like Receptor (TLR)
ERK
Calcium Channel
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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-
- HY-B0380R
-
|
|
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
Reference Standards
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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-
- HY-178020
-
|
|
FLT3
ERK
Akt
Apoptosis
|
Cancer
|
|
FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML) .
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-
- HY-181587
-
|
|
PDGFR
Carbonic Anhydrase
STAT
Akt
ERK
Apoptosis
Caspase
|
Cancer
|
|
PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia .
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-
- HY-181726
-
|
|
PERK
P-glycoprotein
Apoptosis
|
Cancer
|
|
BRAFV600E/ABL2-IN-2 is a dual BRAFV 600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV 600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma .
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-
- HY-P11642
-
|
|
ERK
Androgen Receptor
Opioid Receptor
Enteropeptidase
mTOR
Aminopeptidase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
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-
- HY-N6796
-
|
|
Antibiotic
Exosomes
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
TNF Receptor
Atg8/LC3
|
Infection
Inflammation/Immunology
Cancer
|
|
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
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-
- HY-10254R
-
|
PD0325901 (Standard); PD325901 (Standard)
|
Reference Standards
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Mirdametinib (Standard) is the analytical standard of Mirdametinib (HY-10254). This product is intended for research and analytical applications. Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Kiapp of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
|
-
- HY-N6857
-
|
|
AP-1
NF-κB
p38 MAPK
ERK
JNK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia .
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-
- HY-P5762A
-
-
- HY-119013
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
VPC32183 is a competitive antagonist of LPA1 and LPA3 receptors. The activity of VPC32183 can inhibit lipid phosphatase 1 (LPP1), thereby preventing the activation of ERK(1/2) by dioctanoic acid diglyceride (DGPP 8:0). By reducing the expression of LPP1, VPC32183 can further reduce DGPP 8:0-induced ERK(1/2) activation. The effects of VPC32183 suggest that it may have a positive regulatory function in cell signaling processes .
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-
- HY-N12378A
-
|
|
AMPK
FASTK
Sirtuin
ROCK
Keap1-Nrf2
Toll-like Receptor (TLR)
Apoptosis
PKA
ERK
NF-κB
Epigenetic Reader Domain
Caspase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
α-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. α-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. α-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. α-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma .
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-
- HY-P11642A
-
|
|
Enteropeptidase
Aminopeptidase
Opioid Receptor
ERK
mTOR
Androgen Receptor
|
Inflammation/Immunology
|
|
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
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-
- HY-N12378
-
|
|
NF-κB
Toll-like Receptor (TLR)
PKA
Epigenetic Reader Domain
Keap1-Nrf2
Sirtuin
AMPK
Caspase
FASTK
ERK
ROCK
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
β-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. β-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. β-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. β-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma .
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-
- HY-180200
-
|
|
Ras
ERK
|
Cancer
|
|
RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
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-
- HY-P10641
-
|
|
Exosomes
STAT
ERK
Akt
|
Cardiovascular Disease
|
|
Heart-homing peptide is a heart-targeting peptide with the sequence CRPPR that mediates cardiac endothelial targeting and accumulates in cardiac tissues. Heart-homing peptide mediates the translocation of liposomal and exosomal cargos across cardiac endothelium into interstitial tissues, enhances the accumulation of exosomes in the heart, and inhibits the GP130-STAT3/ERK1/2/AKT pathway. Heart-homing peptide accumulates at sites of ischemia/reperfusion, myocardial infarction and hypertrophy in mice. Heart-homing peptide can be used for the research of cardiovascular diseases .
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-
- HY-117720
-
|
|
PKC
Apoptosis
|
Cancer
|
|
OSU-2S is a potent PKCδ activator. OSU-2S inhibits cell proliferation and migration. OSU-2S decreases the expression of p-ERK1/2, increases the expression of PKCδ (38 kDa) when combined with Sorafenib (HY-10201). OSU-2S induces Apoptosis. OSU-2S slao is a non-immunosuppressive analogue of FTY720. OSU-2S shows anticancer activity .
|
-
- HY-182068
-
|
|
iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
NFI23 is a blood-brain barrier-penetrant GluN2B-NMDAR inhibitor, with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 reduces NMDA-induced Ca 2+ influx and ROS production, maintains mitochondrial membrane potential, inhibits neuronal apoptosis, and restores the expression of p-ERK1/2. NFI23 exerts neuroprotective effects against NMDA-induced cytotoxicity and in the rat middle cerebral artery occlusion (MCAO) model. NFI23 can be used for the research of ischemic stroke .
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-
- HY-178061
-
|
|
ERK
RET
|
Cancer
|
|
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
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-
- HY-161966
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
VEGFR
|
Cancer
|
|
VEGFR-2-IN-52 (compound 14d) is a potent VEGFR-2 inhibitor with an IC50 value of 191.1 nM. VEGFR-2-IN-52 decreases the protein expression of p-VEGFR-2, MMP9, p-ERK1/2 and p-MEK1. VEGFR-2-IN-52 shows cytotoxicity. VEGFR-2-IN-52 induces apoptosis and cell cycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
|
-
- HY-P10102
-
Kp7-6
2 Publications Verification
|
Apoptosis
PERK
NF-κB
Caspase
JNK
|
Inflammation/Immunology
Cancer
|
|
Kp7-6 is a Fas mimetic peptide and also a Fas/FasL antagonist. Kp7-6 specifically binds to Fas and FasL, disrupts receptor complexes, and blocks downstream apoptosis signaling pathways. Kp7-6 inhibits the phosphorylation of ERK1-2, induces the phosphorylation of IκBα, and activates NF-κB. Kp7-6 inhibits the activation of caspase-8, caspase-3 and JNK, and suppresses human amylin-induced β-cell apoptosis. Kp7-6 inhibits FasL-induced lymphoid cytotoxicity and apoptosis. Kp7-6 reduces local tumor FasL expression, increases CD8 +Fas + T cell infiltration, and decreases tumor volume in pancreatic neuroendocrine tumor models. Kp7-6 prevents concanavalin A-induced liver injury in mice. Kp7-6 is applicable to research related to type 2 diabetes, concanavalin A-induced hepatitis and pancreatic neuroendocrine tumors .
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-
- HY-N12445
-
|
|
Topoisomerase
Caspase
Apoptosis
SOD
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Quercetin-3'-O-glucoside is an orally active flavonoid glycoside. Quercetin-3'-O-glucoside reduces liver glucose-6-phosphatase activity, alters serum insulin and glucose levels, and regulates the activities of antioxidant enzymes in the liver and kidney. Quercetin-3'-O-glucoside inhibits DNA topoisomerase II, induces S-phase cell cycle arrest and caspase-3-mediated apoptosis in hepatocellular carcinoma cells. Quercetin-3'-O-glucoside selectively inhibits EGFR-mediated signaling pathways targeting AKT, ERK1/2, FAK and MEK1/2. Quercetin-3'-O-glucoside inhibits growth factor-induced migration and invasion in pancreatic cancer cells. Quercetin-3'-O-glucoside exerts free radical scavenging effects. Quercetin-3'-O-glucoside is applicable to research related to pancreatic cancer, diabetes, hepatocellular carcinoma and malignant tumors .
|
-
- HY-178812
-
|
|
PI3K
PAK
mTOR
PERK
Apoptosis
|
Cancer
|
|
PI3Kα-IN-27 (Compound 50b) is an orally active PI3K-α inhibitor, with an IC50 of 40 nM. PI3Kα-IN-27 effectively inhibits PAK3, p110α, phospho-mTOR and phospho-ERK1/2. PI3Kα-IN-27 induces early Apoptosis. PI3Kα-IN-27 shows anticancer activity against pancreatic cancer, lung cancer, breast cancer .
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-
- HY-N9541
-
|
|
Others
|
Inflammation/Immunology
|
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-N0910
-
-
- HY-N0226
-
|
|
Cholinesterase (ChE)
Beta-secretase
|
Neurological Disease
Metabolic Disease
|
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
|
-
- HY-135319
-
|
|
Bacterial
Antibiotic
ERK
JNK
NF-κB
ROR
Apoptosis
Caspase
GSK-3
Akt
PI3K
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .
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-
- HY-N0226A
-
|
|
Cholinesterase (ChE)
Beta-secretase
Reactive Oxygen Species (ROS)
|
Neurological Disease
Metabolic Disease
|
|
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .
|
-
- HY-P10833
-
|
|
VEGFR
PI3K
Akt
mTOR
ERK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer .
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-
- HY-W923189
-
|
|
Interleukin Related
COX
TNF Receptor
NOD-like Receptor (NLR)
NO Synthase
PERK
p38 MAPK
Reactive Oxygen Species (ROS)
Caspase
Autophagy
Herbicide
|
Inflammation/Immunology
Cancer
|
|
Neral is a plant-derived anti-inflammatory, antioxidant and anticancer agent. Neral inhibits the phosphorylation of ERK1/2, p38 MAPK and IκB in macrophages induced by LPS (HY-D1056), suppresses the secretion of TNF-α and IL-6, as well as the expression of pro-IL-1β, iNOS and COX-2 in cells, and reduces the production of ROS in cells. Neral inhibits the activation of the NLRP3 inflammasome, and decreases the activation of caspase-1 and the secretion of IL-1β in mouse macrophages. Neral induces autophagy, and exhibits antiproliferative activity both in in vitro breast cancer cell models and mouse xenograft models. Neral regulates brassinosteroid, jasmonic acid and ethylene signaling pathways, and induces the expression of AP2/ERF-ERF and bHLH family genes in rice roots. Neral acts as a herbicide safener, alleviates the damage induced by Fenoxaprop-P-ethyl (HY-B2013), and promotes the elongation of rice roots. Neral can be used in research related to breast cancer, inflammatory and immune system diseases, and herbicide safeners .
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-
- HY-182902
-
|
|
BMX Kinase
Apoptosis
|
Cancer
|
|
IHMT-15137 is a BMX inhibitor with an IC50 of 26.97 nM. IHMT-15137 covalently binds to BMX Cys496 within the ATP-binding pocket, inhibits BMX phosphorylation at Tyr566, and disrupts the BMX-ERK1/2-Cyclin D1/CDK4/6-E2F1 signaling axis. IHMT-15137 reduces E2F1 protein stability via decreased Ser332/337 phosphorylation, increased ubiquitination, and ubiquitin-proteasome pathway degradation. IHMT-15137 induces cell cycle arrest, apoptosis, DNA damage, and suppresses cell migration and invasion. IHMT-15137 can be used for the research of small cell lung cancer .
|
-
- HY-149824
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity .
|
-
- HY-N0493
-
|
|
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
|
-
- HY-N0493R
-
|
|
Reference Standards
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
Inflammation/Immunology
|
|
Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
|
-
- HY-N0745
-
|
|
Caspase
ERK
Keap1-Nrf2
Heme Oxygenase (HO)
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A) . Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury .
|
-
- HY-178382
-
|
|
Raf
Bcr-Abl
P-glycoprotein
PERK
Apoptosis
|
Cancer
|
|
BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma .
|
-
- HY-N3097R
-
-
- HY-N3097
-
-
- HY-13032B
-
|
GSK 525762C; I-BET 762 besylate
|
Epigenetic Reader Domain
ERK
|
Cancer
|
|
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
|
-
- HY-W715812
-
|
|
Fungal
Apoptosis
Caspase
Reactive Oxygen Species (ROS)
MDM-2/p53
SOD
Bcl-2 Family
PERK
JNK
p38 MAPK
|
Cardiovascular Disease
Infection
Endocrinology
Cancer
|
|
Bromuconazole is a triazole fungicide with oral efficacy and blood-brain barrier permeability . Bromuconazole protects crops from various fungal contaminations. Bromuconazole exhibits cytotoxicity against a variety of cancer cells, induces G0/G1 cell cycle arrest and inhibits DNA synthesis in cancer cells, and triggers cytoskeletal structural disorder, genotoxic damage, apoptotic (apoptosis) cell death, and mitochondrial membrane depolarization. Bromuconazole activates caspase-3, induces excessive production of ROS, p53 and Bax, lipid peroxidation, increased activities of SOD and CAT, and downregulates Bcl-2. By upregulating p-ERK1/2 and p-JNK, Bromuconazole disrupts the MAPK signaling pathway, impairs the cellular stress response of human trophoblast cells and endometrial cells, and damages the implantation process . Bromuconazole is applicable to research related to glioma, colon cancer, reproductive injury (implantation dysfunction), and cardiac dysfunction .
|
-
- HY-N5084
-
|
|
TRP Channel
HDAC
p38 MAPK
JNK
ERK
NF-κB
TNF Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a TRPV1 antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8 + T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer .
|
-
- HY-112570
-
|
|
ERK
|
Cancer
|
|
CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
|
-
- HY-N0909
-
|
20(S)-Notoginsenoside R2; Ginsenoside Ng-R2
|
Apoptosis
MEK
ERK
Reactive Oxygen Species (ROS)
Caspase
COX
β-catenin
Src
MDM-2/p53
JAK
STAT
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Notoginsenoside R2 (20(S)-Notoginsenoside R2; Ginsenoside Ng-R2) is an orally active notoginsenoside . Notoginsenoside R2 activates P90RSK and Nrf2 via the MEK1/2-ERK1/2 pathway to inhibit 6-OHDA-induced apoptotic damage in nerve cells. Notoginsenoside R2 upregulates SOX8/β-catenin by reducing miR-27a, thereby suppressing Aβ25-35-induced neuronal apoptosis and inflammatory responses . Notoginsenoside R2 alleviates lipid accumulation and mitochondrial dysfunction in diabetic nephropathy by inhibiting c-Src. Notoginsenoside R2 alleviates hepatic fibrosis by inducing hepatic stellate cell senescence and inhibiting the inflammatory microenvironment via JAK/STAT3 suppression . Notoginsenoside R2 can be used in research related to Parkinson's disease, Alzheimer's disease, diabetic nephropathy and hepatic fibrosis .
|
-
- HY-N2270
-
|
|
p38 MAPK
ERK
IKK
|
Inflammation/Immunology
|
|
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .
|
-
- HY-19696
-
|
Tauroursodeoxycholic acid; TUDCA; UR 906
|
ERK
Caspase
Endogenous Metabolite
Apoptosis
|
Cancer
|
|
Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an orally active endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK .
|
-
- HY-156549
-
|
|
ERK
Ras
|
Cancer
|
|
KRAS G12C inhibitor 61 (Example 3) inhibits phospho-ERK 1/2 in MIA PaCa-2 cells with an IC50 value of 9 nM. KRAS G12C inhibitor 61 can be used for research of pancreatic, colorectal, and lung cancers .
|
-
- HY-107753
-
|
|
Ras
|
Inflammation/Immunology
Cancer
|
|
XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2 . XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules .
|
-
- HY-19696BR
-
|
Tauroursodeoxycholic acid dihydrate (Standard); TUDCA dihydrate (Standard); UR 906 dihydrate (Standard)
|
ERK
Caspase
Apoptosis
Endogenous Metabolite
Reference Standards
|
Cancer
|
|
Tauroursodeoxycholate (dihydrate) (Standard) is the analytical standard of Tauroursodeoxycholate (dihydrate). This product is intended for research and analytical applications. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK .
|
-
- HY-162575
-
|
|
ERK
|
Cancer
|
|
Anticancer agent 231 (Compound P5) is a tyrosine protein kinase inhibitor with a IC50 value of 3.95 μM. Anticancer agent 231 inhibits the cell viability, cell proliferation, cell migration and cancer dryness of triple negative breast cancer (TNBC) cells by targeting EGFR-ERK 1/2 signaling pathway, and is expected to play an important role in the field of TNBC disease therapy .
|
-
- HY-101798
-
|
|
PI3K
|
Cancer
|
|
MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
|
-
- HY-107753R
-
|
|
Reference Standards
Ras
|
Inflammation/Immunology
Cancer
|
|
XRP44X (Standard) is the analytical standard of XRP44X (HY-107753). This product is intended for research and analytical applications. XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2 . XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules .
|
-
- HY-N9980
-
|
|
PI3K
Akt
NF-κB
p38 MAPK
AP-1
|
Inflammation/Immunology
|
|
Antcin K is a selective inhibitor targeting the PI3K/Akt, NF-κB, MEK1/2-ERK, p38 and AP-1 pathways. Antcin K upregulates IL-10 expression, thereby inhibiting the production of pro-inflammatory factors, blocking monocyte adhesion, reducing tissue damage, and promoting myogenesis. Antcin K has significant anti-inflammatory, anti-damage and tissue protective activities. Antcin K is mainly used in the research of inflammation-related diseases such as periodontitis, rheumatoid arthritis, and skeletal muscle injury .
|
-
- HY-119272
-
EF24
2 Publications Verification
|
ERK
Caspase
NF-κB
Apoptosis
p38 MAPK
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
|
-
- HY-N7110
-
|
|
Akt
ERK
JNK
GABA Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
|
-
- HY-N12060
-
|
|
Bcl-2 Family
Caspase
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Akt
JNK
ERK
|
Cardiovascular Disease
Neurological Disease
|
|
Ginkgo biloba extract is a natural product that can be isolated from Ginkgo biloba leaves . Ginkgo biloba extract alleviates oxidative stress-induced neuronal apoptosis (Apoptosis) by stabilizing mitochondrial function, regulating Bcl-2 family proteins and inhibiting caspase activation. Ginkgo biloba extract alleviates testicular injury by upregulating SKP2 and inhibiting Beclin1-independent autophagy (Autophagy) . Ginkgo biloba extract alleviates various types of neuronal damage in animal models. Ginkgo biloba extract reduces behavioral sensitization in rats. Ginkgo biloba extract counteracts Aβ-induced neurotoxicity by blocking a series of Aβ-triggered events, including glucose uptake, ROS accumulation, AKT activation, mitochondrial dysfunction, JNK and ERK 1/2 pathways, and apoptosis, and also interferes with the formation of Aβ oligomers. Ginkgo biloba extract is applicable to research related to cerebral hypoperfusion, testicular injury, Alzheimer's disease, Parkinson's disease, multi-infarct dementia, stroke, traumatic brain injury and amyotrophic lateral sclerosis .
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-
-
-
HY-L010
-
|
|
1,063 compounds
|
|
MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers.
MCE designs a unique collection of 1,063 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.
|
| Cat. No. |
Product Name |
Type |
-
- HY-159642G
-
|
TYRA-300
|
Fluorescent Dyes
|
|
Dabogratinib (TYRA-300) (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia .
|
-
- HY-15947G
-
|
GDC-0994
|
Fluorescent Dyes
|
|
Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
|
| Cat. No. |
Product Name |
Type |
-
- HY-B2162D
-
|
Chondroitin polysulfate (from chicken)
|
Biochemical Assay Reagents
|
|
Chondroitin sulfate (from chicken) (Chondroitin polysulfate (from chicken)) is an orally active, sulfated linear polysaccharide extracted from chickens, which belongs to glycosaminoglycans. Chondroitin sulfate (from chicken) reduces the phosphorylation levels of ERK1/2 and p38MAPK, inhibits the expression of inflammatory cytokines and MMP, and downregulates the levels of IL-1β, IL-6, TNF-α and PGE2. Chondroitin sulfate (from chicken) improves motor function, protects cartilage tissue, reverses chondrocyte aggregation, and regulates the structure of intestinal flora. Chondroitin sulfate (from chicken) can be used in research related to osteoarthritis .
|
-
- HY-159642G
-
|
TYRA-300
|
Biochemical Assay Reagents
|
|
Dabogratinib (TYRA-300) (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia .
|
-
- HY-W745090
-
|
|
Biochemical Assay Reagents
|
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
- HY-15947G
-
|
GDC-0994
|
Biochemical Assay Reagents
|
|
Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10102
-
Kp7-6
2 Publications Verification
|
Apoptosis
PERK
NF-κB
Caspase
JNK
|
Inflammation/Immunology
Cancer
|
|
Kp7-6 is a Fas mimetic peptide and also a Fas/FasL antagonist. Kp7-6 specifically binds to Fas and FasL, disrupts receptor complexes, and blocks downstream apoptosis signaling pathways. Kp7-6 inhibits the phosphorylation of ERK1-2, induces the phosphorylation of IκBα, and activates NF-κB. Kp7-6 inhibits the activation of caspase-8, caspase-3 and JNK, and suppresses human amylin-induced β-cell apoptosis. Kp7-6 inhibits FasL-induced lymphoid cytotoxicity and apoptosis. Kp7-6 reduces local tumor FasL expression, increases CD8 +Fas + T cell infiltration, and decreases tumor volume in pancreatic neuroendocrine tumor models. Kp7-6 prevents concanavalin A-induced liver injury in mice. Kp7-6 is applicable to research related to type 2 diabetes, concanavalin A-induced hepatitis and pancreatic neuroendocrine tumors .
|
-
- HY-P0178
-
|
|
Integrin
|
Inflammation/Immunology
|
|
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
|
-
- HY-P10641
-
|
|
Exosomes
STAT
ERK
Akt
|
Cardiovascular Disease
|
|
Heart-homing peptide is a heart-targeting peptide with the sequence CRPPR that mediates cardiac endothelial targeting and accumulates in cardiac tissues. Heart-homing peptide mediates the translocation of liposomal and exosomal cargos across cardiac endothelium into interstitial tissues, enhances the accumulation of exosomes in the heart, and inhibits the GP130-STAT3/ERK1/2/AKT pathway. Heart-homing peptide accumulates at sites of ischemia/reperfusion, myocardial infarction and hypertrophy in mice. Heart-homing peptide can be used for the research of cardiovascular diseases .
|
-
- HY-P0178A
-
|
|
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-P11147
-
|
|
Interleukin Related
FAK
Src
Akt
ERK
MMP
|
Cancer
|
|
IL13Rα2 D1 is an effective IL-13/IL13Rα2 signaling axis inhibitor. IL13Rα2 D1 can inhibit IL-13-induced cell adhesion, migration, invasion, and proliferation. IL13Rα2 D1 can inhibit FAK, Src, AKT, ERK1/2 phosphorylation, and MMP expression. IL13Rα2 D1 can be used for research on cancers such as colorectal cancer .
|
-
- HY-P5977
-
|
Ste-MPKKKPTPIQLNP-NH₂; ERK Activation inhibitor Peptide
|
ERK
|
Cancer
|
|
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
|
-
- HY-P4866
-
|
|
Integrin
Transglutaminase
Akt
p38 MAPK
ERK
Caspase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Q-Peptide is an angiopoietin-1 derived peptide (QHREDGS). Q-Peptide interacts with β1-integrin, binds to integrins on the surface of osteoblasts, and serves as an acyl donor substrate for Streptomyces mobaraensis transglutaminase. Q-Peptide activates Akt, MAPKp42/44, ILK, ERK1/2, and downregulates caspase-3/7. Q-Peptide inhibits cell apoptosis, enhances cell adhesion and migration, and promotes osteoblast differentiation, bone matrix deposition and mineralization. Q-Peptide can be used in studies related to myocardial infarction, bone regeneration, diabetic wound repair and human induced pluripotent stem cells .
|
-
- HY-P11642A
-
|
|
Enteropeptidase
Aminopeptidase
Opioid Receptor
ERK
mTOR
Androgen Receptor
|
Inflammation/Immunology
|
|
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
|
-
- HY-P10833
-
|
|
VEGFR
PI3K
Akt
mTOR
ERK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer .
|
-
- HY-P5762A
-
-
- HY-P11827
-
|
|
Collagen
ERK
TGF-beta/Smad
|
Metabolic Disease
|
|
C11 peptide-1 is an antifibrotic agent that binds directly to Collagen I. C11 peptide-1 physically disrupts Collagen I interaction with Lumican. C11 peptide-1 reduces inflammatory infiltration and inhibits the ERK1/2 and Smad2/3 signaling pathways. C11 peptide-1 can be used for the research of liver fibrosis .
|
-
- HY-P11642
-
|
|
ERK
Androgen Receptor
Opioid Receptor
Enteropeptidase
mTOR
Aminopeptidase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991219
-
|
EnX209
|
Interleukin Related
ERK
MMP
|
Inflammation/Immunology
|
|
Anti-IL11RA Antibody (X209) (EnX209) is a human-derived IgG4, κ-type antibody inhibitor targeting IL11RA, with a KD of 6 nM. Anti-IL11RA Antibody (X209) blocks the IL11RA signaling pathway, inhibits ERK-dependent activation, and reduces the activation level of ERK1/2. Anti-IL11RA Antibody (X209) exerts a protective effect against fibrosis. Anti-IL11RA Antibody (X209) is applicable to studies related to liver fibrosis, cardiac fibrosis and other related conditions. Recommended isotype control: Human IgG4 kappa, Isotype Control (HY-P99003) .
|
-
(5)
-
- HY-P991358
-
|
LFA-102; X213
|
Estrogen Receptor/ERR
STAT
Akt
|
Cancer
|
|
XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer .
|
-
(5)
-
- HY-P991964
-
|
Rendomab-B49
|
Endothelin Receptor
|
Cancer
|
|
Rendomab B4 (Rendomab-B49) is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-19696
-
-
-
- HY-N7140
-
-
-
- HY-113016
-
-
-
- HY-N6796
-
-
-
- HY-N10546
-
|
|
Structural Classification
Natural Products
Animals
|
iGluR
Trk Receptor
ERK
Apoptosis
Autophagy
|
|
Ganglioside GM1 is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease .
|
-
-
- HY-107818
-
-
-
- HY-D0205A
-
-
-
- HY-N6664
-
-
-
- HY-N0526
-
|
|
Flavonols
Structural Classification
Classification of Application Fields
Plants
Flavonoids
Pyrola calliantha H. Andr.
Pyrolaceae
Phenols
Polyphenols
Pyrola incarnata Fisch. ex DC.
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
|
|
2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
|
-
-
- HY-N0226A
-
-
-
- HY-N0774
-
-
-
- HY-N0226
-
-
-
- HY-N0493
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Campylotropis hirtella (Franch.) Schindl.
Phenols
Polyphenols
Plants
Compositae
Inflammation/Immunology
Disease Research Fields
Source Classification
|
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
|
Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
|
-
-
- HY-N0745
-
-
-
- HY-N12586
-
|
|
Suaeda vermiculata Forssk. ex J.F.Gmel.
Structural Classification
Alkaloids
Other Alkaloids
Amaranthaceae
Plants
Source Classification
|
ERK
Reactive Oxygen Species (ROS)
COX
PGE synthase
STAT
HCV
HCV Protease
|
|
Pheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC50=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease .
|
-
-
- HY-113509
-
-
-
- HY-N2450
-
-
-
- HY-N12060
-
|
|
Structural Classification
Natural Products
Ginkgoaceae
Plants
Ginkgo biloba
Source Classification
|
Bcl-2 Family
Caspase
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Akt
JNK
ERK
|
|
Ginkgo biloba extract is a natural product that can be isolated from Ginkgo biloba leaves . Ginkgo biloba extract alleviates oxidative stress-induced neuronal apoptosis (Apoptosis) by stabilizing mitochondrial function, regulating Bcl-2 family proteins and inhibiting caspase activation. Ginkgo biloba extract alleviates testicular injury by upregulating SKP2 and inhibiting Beclin1-independent autophagy (Autophagy) . Ginkgo biloba extract alleviates various types of neuronal damage in animal models. Ginkgo biloba extract reduces behavioral sensitization in rats. Ginkgo biloba extract counteracts Aβ-induced neurotoxicity by blocking a series of Aβ-triggered events, including glucose uptake, ROS accumulation, AKT activation, mitochondrial dysfunction, JNK and ERK 1/2 pathways, and apoptosis, and also interferes with the formation of Aβ oligomers. Ginkgo biloba extract is applicable to research related to cerebral hypoperfusion, testicular injury, Alzheimer's disease, Parkinson's disease, multi-infarct dementia, stroke, traumatic brain injury and amyotrophic lateral sclerosis .
|
-
-
- HY-N2283
-
-
-
- HY-N3097
-
-
-
- HY-N5084
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Flavonones
Other Diseases
Phenols
Polyphenols
Saxifragaceae
Plants
Penthorum chinense Pursh
Disease Research Fields
Source Classification
|
TRP Channel
HDAC
p38 MAPK
JNK
ERK
NF-κB
TNF Receptor
Interleukin Related
|
|
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a TRPV1 antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8 + T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer .
|
-
-
- HY-N0924
-
-
-
- HY-N2484
-
|
Astrapterocarpan
|
Cardiovascular Disease
Structural Classification
Monophenols
Flavonoids
Classification of Application Fields
Leguminosae
Phenols
Astragalus membranaceus var. mongholicus (Bunge)P.K.Hsiao
Plants
Other Flavonoids
Disease Research Fields
Source Classification
|
PDGFR
ERK
|
|
Methylnissolin (Astrapterocarpan) is an osteoclast inhibitor with anti-inflammatory, neuroprotective and antioxidant activities. Methylnissolin downregulates the activation of the MAPK and PI3K/AKT pathways, inhibits the phosphorylation of MAPK1 and AKT1, and blocks PDGF-BB-induced phosphorylation of ERK1/2. Methylnissolin reduces the expression and secretion of proinflammatory mediators, decreases intracellular ROS levels, upregulates antioxidant enzymes, and downregulates osteoclastogenesis markers. Methylnissolin is applicable to research related to ischemic stroke, osteoporosis, cardiovascular diseases, skin aging, etc.
|
-
-
- HY-N7110
-
-
-
- HY-N6857
-
-
-
- HY-N1910
-
-
-
- HY-N12445
-
|
|
Malvaceae
Structural Classification
Flavonols
Flavonoids
Abelmoschus manihot (Linn.) Medicus
Plants
Source Classification
|
Topoisomerase
Caspase
Apoptosis
SOD
|
|
Quercetin-3'-O-glucoside is an orally active flavonoid glycoside. Quercetin-3'-O-glucoside reduces liver glucose-6-phosphatase activity, alters serum insulin and glucose levels, and regulates the activities of antioxidant enzymes in the liver and kidney. Quercetin-3'-O-glucoside inhibits DNA topoisomerase II, induces S-phase cell cycle arrest and caspase-3-mediated apoptosis in hepatocellular carcinoma cells. Quercetin-3'-O-glucoside selectively inhibits EGFR-mediated signaling pathways targeting AKT, ERK1/2, FAK and MEK1/2. Quercetin-3'-O-glucoside inhibits growth factor-induced migration and invasion in pancreatic cancer cells. Quercetin-3'-O-glucoside exerts free radical scavenging effects. Quercetin-3'-O-glucoside is applicable to research related to pancreatic cancer, diabetes, hepatocellular carcinoma and malignant tumors .
|
-
-
- HY-N0910
-
-
-
- HY-W001174
-
-
-
- HY-N0909
-
-
-
- HY-118824A
-
-
-
- HY-N1987
-
-
-
- HY-101546A
-
-
-
- HY-N12378
-
|
|
Other Terpenoids
Structural Classification
Entada phaseoloides (L.) Merr.
Terpenoids
Labiatae
Plants
Source Classification
|
NF-κB
Toll-like Receptor (TLR)
PKA
Epigenetic Reader Domain
Keap1-Nrf2
Sirtuin
AMPK
Caspase
FASTK
ERK
ROCK
Apoptosis
|
|
β-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. β-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. β-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. β-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma .
|
-
-
- HY-135319
-
|
|
Structural Classification
Phenols
Polyphenols
Camellia sinensis (L.) O. Ktze.
Plants
Source Classification
Theaceae
|
Bacterial
Antibiotic
ERK
JNK
NF-κB
ROR
Apoptosis
Caspase
GSK-3
Akt
PI3K
|
|
Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .
|
-
-
- HY-N2270
-
-
-
- HY-N10047
-
-
-
- HY-N10133
-
|
3′-Prenylnaringenin
|
Structural Classification
Glycyrrhiza glabra Linn.
Flavonoids
Leguminosae
Flavonones
Plants
Source Classification
|
Bacterial
mTOR
Akt
PI3K
NF-κB
Caspase
JNK
ERK
COX
NO Synthase
Apoptosis
|
Licoflavanone (3′-Prenylnaringenin) is a flavanone with antioxidant, anti-inflammatory and anticancer activities. Licoflavanone can be isolated from the leaf extract of Glycyrrhiza glabra. Licoflavanone downregulates the mTOR/PI3K/AKT signaling pathway to inhibit the proliferation, migration and invasion of cancer cells, while activates Bax, Bad and multiple caspase enzymes to induce apoptosis. Its anti-inflammatory effect is manifested by reducing the nuclear translocation of NF-κB, decreasing the phosphorylation levels of p38, JNK and ERK1/2, thereby inhibiting the expression of nitric oxide, proinflammatory cytokines, COX-2 and iNOS. Licoflavanone is used in studies on nasopharyngeal carcinoma and related mechanisms .
|
-
-
- HY-N3828
-
-
-
- HY-N11439
-
-
-
- HY-N0774R
-
-
-
- HY-N2450R
-
-
-
- HY-W744699
-
|
(+)-Larixol
|
Larix decidua Miller
Natural Products
Pinaceae
Plants
Source Classification
|
Src
ERK
Akt
|
|
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
-
- HY-156393
-
-
-
- HY-125522
-
-
-
- HY-N1987R
-
|
|
Triterpenes
Structural Classification
Terpenoids
Cucurbitaceae
Plants
Hemsleya amabilis Diels
|
Reference Standards
Apoptosis
|
|
Cucurbitacin IIb (Standard) is the analytical standard of Cucurbitacin IIb. This product is intended for research and analytical applications. Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
|
-
-
- HY-N0526R
-
|
|
Flavonols
Structural Classification
Flavonoids
Pyrola calliantha H. Andr.
Pyrolaceae
Phenols
Polyphenols
Plants
Pyrola incarnata Fisch. ex DC.
Source Classification
|
Reference Standards
Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
|
|
2"-O-Galloylhyperin (Standard) is the analytical standard of 2"-O-Galloylhyperin (HY-N0526). This product is intended for research and analytical applications. 2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
|
-
-
- HY-N12561
-
|
|
Microorganisms
Terpenoids
Diterpenoids
Source Classification
|
ERK
p38 MAPK
JNK
|
|
Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .
|
-
-
- HY-W001174R
-
-
-
- HY-N0493R
-
|
|
Structural Classification
Flavonoids
Flavones
Campylotropis hirtella (Franch.) Schindl.
Phenols
Polyphenols
Plants
Compositae
Source Classification
|
Reference Standards
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
|
Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
|
-
- HY-N3097R
-
-
- HY-19696BR
-
|
Tauroursodeoxycholic acid dihydrate (Standard); TUDCA dihydrate (Standard); UR 906 dihydrate (Standard)
|
Structural Classification
Endogenous metabolite
Steroids
Source Classification
|
ERK
Caspase
Apoptosis
Endogenous Metabolite
Reference Standards
|
|
Tauroursodeoxycholate (dihydrate) (Standard) is the analytical standard of Tauroursodeoxycholate (dihydrate). This product is intended for research and analytical applications. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK .
|
-
- HY-118817
-
-
- HY-N2362R
-
-
- HY-N18197
-
-
- HY-N10175
-
-
- HY-N17131
-
|
|
Lycopodiaceae
Triterpenes
Structural Classification
Ketones, Aldehydes, Acids
Terpenoids
Plants
Source Classification
|
NF-κB
ERK
|
|
24-O-Acetyllycoclavanol (compound 1) is a triterpenoid anti-inflammatory agent that selectively targets the NF-κB and ERK1/2 signaling pathways. It exerts its anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and COX-2 expression, reducing the production of inflammatory mediators such as nitric oxide (NO), IL-1β, and IL-8. 24-O-Acetyllycoclavanol can be used in research related to inflammatory bowel disease (IBD). 24-O-Acetyllycoclavanol can be biologically isolated from the ethyl acetate extract of Lycopodium clavatum .
|
-
- HY-N12378A
-
|
|
Structural Classification
Entada phaseoloides (L.) Merr.
Terpenoids
Labiatae
Sesquiterpenes
Plants
Source Classification
|
AMPK
FASTK
Sirtuin
ROCK
Keap1-Nrf2
Toll-like Receptor (TLR)
Apoptosis
PKA
ERK
NF-κB
Epigenetic Reader Domain
Caspase
|
|
α-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. α-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. α-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. α-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma .
|
-
- HY-N9541
-
|
|
Alkaloids
Microorganisms
Pyrrole Alkaloids
Source Classification
|
Others
|
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-N9980
-
|
|
Structural Classification
Microorganisms
Steroids
Source Classification
|
PI3K
Akt
NF-κB
p38 MAPK
AP-1
|
|
Antcin K is a selective inhibitor targeting the PI3K/Akt, NF-κB, MEK1/2-ERK, p38 and AP-1 pathways. Antcin K upregulates IL-10 expression, thereby inhibiting the production of pro-inflammatory factors, blocking monocyte adhesion, reducing tissue damage, and promoting myogenesis. Antcin K has significant anti-inflammatory, anti-damage and tissue protective activities. Antcin K is mainly used in the research of inflammation-related diseases such as periodontitis, rheumatoid arthritis, and skeletal muscle injury .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13749AS
-
|
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Sitagliptin-d4 phosphate (MK-0431-d4) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
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- HY-13749S1
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Sitagliptin-d4 hydrochloride is the deuterium labeled Sitagliptin hydrochloride (HY-13749E). Sitagliptin hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
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- HY-14188S
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Amiodarone-d4 (hydrochloride) is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ~45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
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- HY-113509S
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Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
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- HY-B0916S
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Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
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- HY-B0380S1
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Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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- HY-B1456AS
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Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
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- HY-D0205AS1
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Carbocisteine- 13C3-1 (Carbocysteine- 13C3-1) is 13C labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
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- HY-B1272AS
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Desipramine-d4 is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .
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- HY-B1272AS1
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Desipramine-d3 is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .
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- HY-B0380S2
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Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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- HY-13749S3
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Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
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- HY-13749S2
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Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
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- HY-D0205AS2
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Carbocisteine-d3 (Carbocysteine-d3) is deuterium labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
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- HY-W750153
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Propoxur-d7 is the deuterium labeled Propoxur. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
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Classification |
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- HY-101460
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Tetrazine
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Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research .
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- HY-180200
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Alkynes
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RNK08954 is an orally active KRASG12D inhibitor with a Kd of 0.0395 nM. RNK08954 selectively binds the inactive GDP-bound KRASG12D form, suppresses downstream KRAS-mediated signaling pathways p-ERK1/2 experssion. RNK08954 inhibits KRASG12D-mutant cell proliferation, induces G0-G1 cell cycle arrest, and inhibits tumor growth in mouse xenograft models. RNK08954 can be used for the research of non-small cell lung cancer, pancreatic ductal adenocarcinoma .
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Product Name |
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Classification |
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- HY-N6664
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Arabic gum
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Emulsifiers
Suspending Agents
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Gum Arabic is an orally active complex branched polysaccharide. Gum Arabic can be isolated from the Acacia senegal tree. Gum Arabic upregulates the expression of maturation markers (CD86, CD40, and CD54), promotes ERK1/2 phosphorylation, and inhibits Apoptosis. Gum Arabic exhibits antimalarial effects against Plasmodium berghei ANKA. Gum Arabic exhibits hepatoprotective, renal, and cardiovascular protective activities. Gum Arabic improves obesity. Gum Arabic is commonly used as a stabilizer and thickener. Gum Arabic can be used in the research of brain tumor imaging .
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- HY-177802
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Aptamers
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C3 sodium is an aptamer that binds to Erk2. C3 binds to the MAP kinase insert domain, a unique site on Erk1/2. Due to this recognition profile C3 inhibits Erk2 activation by its upstream kinase MKK1.
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Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15947G
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GDC-0994
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ERK
c-Myc
Hexokinase
Lactate Dehydrogenase
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Cancer
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Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma .
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- HY-159642G
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TYRA-300
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FGFR
ERK
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Metabolic Disease
Cancer
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Dabogratinib (TYRA-300) (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia .
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