Search Result
Results for "
MEK inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
10
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-12202
-
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MEK
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Cancer
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MEK inhibitor is a potent MEK inhibitor with antitumor potency.
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- HY-15610
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RG 7421; MEK inhibitor 1
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MEK
Apoptosis
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Cancer
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GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
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-
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- HY-139638
-
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MEK
|
Cancer
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MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
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-
-
- HY-139639
-
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MEK
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Cancer
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MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.
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-
-
- HY-157750
-
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MEK
Raf
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Cancer
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MEK1/C-Raf-IN-1 (Compound 14d) is a MEK1/C-Raf inhibitor with IC50 values of 97 and 23 nM, respectively. MEK1/C-Raf-IN-1 has antitumor activity .
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-
-
- HY-P4133
-
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ERK
MEK
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Cancer
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MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable .
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-
-
- HY-P4136
-
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ERK
|
Cancer
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Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM .
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-
-
- HY-160414
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(R,R)-TRX-COBI; TRX-cobimetinib
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MEK
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Cancer
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TRX-COBI ((R,R)-TRX-COBI; Trx-cobimetinib) is a MEK inhibitor targeting TRX fragments based on Fe 2+. TRX-COBI has antitumor activity .
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-
-
- HY-163173
-
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YAP
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Cancer
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TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
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-
-
- HY-P5977
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Ste-MPKKKPTPIQLNP-NH₂; ERK Activation inhibitor Peptide
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ERK
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Cancer
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STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
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-
-
- HY-15496
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ER-806201
|
MEK
FLT3
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Cancer
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E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
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-
-
- HY-15202
-
MEK162; ARRY-162; ARRY-438162
|
MEK
Autophagy
|
Cancer
|
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
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-
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- HY-145701
-
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MEK
|
Cancer
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MEK1/2-IN-2 is a potent ATP-competitive MEK1/2 inhibitor and shows equipotent inhibition of WT MEK1/2 and a panel of MEK1/2 mutant cell lines .
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-
-
- HY-14719
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CH4987655
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MEK
|
Cancer
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RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
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-
-
- HY-15202R
-
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MEK
Autophagy
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Cancer
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Binimetinib (Standard) is the analytical standard of Binimetinib. This product is intended for research and analytical applications. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
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-
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- HY-12058
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ARRY-424704; ARRY-704
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MEK
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Cancer
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AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.
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-
-
- HY-137881
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-
-
- HY-153445A
-
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MEK
|
Cancer
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MEK-IN-6 hydrate (compound 69) is a MEK inhibitor. MEK-IN-6 hydrate has an IC50 of 2 nM for A375 cells .
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-
-
- HY-132844
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HL-085
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MEK
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Cancer
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Tunlametinib, an antineoplastic agent, is a MEK1/2 inhibitor .
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-
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- HY-14691
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BAY 869766; RDEA119
|
MEK
|
Cancer
|
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
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-
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- HY-U00312
-
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MEK
|
Cancer
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MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1.
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-
-
- HY-153445
-
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ERK
MEK
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Cancer
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MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). MEK-IN-6 can be used for research of cancer .
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-
- HY-107622
-
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Others
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Metabolic Disease
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(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
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- HY-50706
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AZD6244; ARRY-142886
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MEK
Apoptosis
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Cancer
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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.
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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-15437
-
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MEK
|
Cancer
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SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
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-
-
- HY-143468
-
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Apoptosis
MEK
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Cancer
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MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
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- HY-10999
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GSK1120212; JTP-74057
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MEK
Autophagy
Apoptosis
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Cancer
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Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
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- HY-145702
-
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MEK
ERK
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Cancer
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MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
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- HY-13064A
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GDC-0973 hemifumarate; XL-518 hemifumarate
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MEK
Apoptosis
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Cancer
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Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
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- HY-18086
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SC 204330
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Pim
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Cancer
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TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM) .
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- HY-12042A
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AS703026 hydrochloride; MSC1936369B hydrochloride
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MEK
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Cancer
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Pimasertib hydrochloride is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
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- HY-164474
-
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MEK
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Cancer
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DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
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- HY-50295
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PD 184352
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MEK
Apoptosis
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Cancer
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CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
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- HY-13064
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GDC-0973; XL518
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MEK
Apoptosis
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Cancer
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Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
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- HY-10999S
-
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MEK
Autophagy
Apoptosis
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Cancer
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Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-12055
-
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MEK
ERK
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Cancer
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BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
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- HY-10999A
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GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
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MEK
Apoptosis
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Cancer
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Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis .
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- HY-12042
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AS703026; MSC1936369B
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MEK
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Cancer
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Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
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- HY-10999S1
-
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MEK
Autophagy
Apoptosis
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Cancer
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Trametinib- 13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-10999R
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MEK
Autophagy
Apoptosis
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Cancer
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Trametinib (Standard) is the analytical standard of Trametinib. This product is intended for research and analytical applications. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
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- HY-10999S2
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GSK1120212-13C,d3; JTP-74057-13C,d3
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Isotope-Labeled Compounds
MEK
Autophagy
Apoptosis
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Cancer
|
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-50706A
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AZD6244 sulfate; ARRY-142886 sulfate
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MEK
Apoptosis
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Cancer
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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.
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- HY-18652
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Ro 5126766; CH5126766
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MEK
Raf
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Cancer
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Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
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-
-
- HY-12031A
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U0126
Maximum Cited Publications
366 Publications Verification
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MEK
Autophagy
Mitophagy
Influenza Virus
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Cancer
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U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
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- HY-13303
-
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MEK
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Cancer
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RO 4927350 is a potent and selective non-ATP-competitive MEK1/2 inhibitor. RO 4927350 exhibits significant antitumor efficacy in a broad spectrum of tumor models .
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-
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- HY-107619
-
-
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- HY-12062
-
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MEK
|
Cancer
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PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .
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-
-
- HY-107417
-
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VEGFR
MEK
FLT3
PDGFR
ERK
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Cancer
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Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively .
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-
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- HY-107621
-
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MEK
|
Cancer
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U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM .
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- HY-P10074
-
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ERK
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Inflammation/Immunology
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TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC50 in vitro for ERK2 is 29 μM .
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- HY-12028
-
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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 .
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- HY-162873
-
|
MEK
Raf
|
Cancer
|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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-
- HY-126048
-
|
MEK
|
Cancer
|
JTP-70902, a p15 INK4b-inductive compound, is a MEK1/2 inhibitor. JTP-70902 exhibits potent antitumor effect .
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- HY-12031B
-
|
Others
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Inflammation/Immunology
|
(2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
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- HY-131295
-
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MEK
Ligands for Target Protein for PROTAC
|
Cancer
|
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader .
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-
- HY-144692
-
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MEK
PI3K
PERK
|
Cancer
|
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
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-
- HY-144693
-
|
MEK
PI3K
PERK
|
Cancer
|
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
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-
- HY-13064S1
-
GDC-0973-d4 hydrochloride; XL518-d4 hydrochloride
|
MEK
Apoptosis
Isotope-Labeled Compounds
|
Cancer
|
Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
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-
- HY-12031
-
U0126-EtOH
Maximum Cited Publications
366 Publications Verification
|
MEK
Autophagy
Mitophagy
Influenza Virus
|
Cancer
|
U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
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-
- HY-100627
-
|
MEK
|
Cancer
|
APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .
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-
- HY-100627A
-
|
MEK
|
Cancer
|
APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .
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-
- HY-10174
-
|
MEK
Apoptosis
|
Neurological Disease
Cancer
|
PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior .
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-
- HY-159846
-
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MEK
|
Cancer
|
Luvometinib is a mitogen-activated protein kinase (MEK) inhibitor with antitumor activity .
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-
- HY-10254
-
PD0325901; PD325901
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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 .
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-
- HY-13079
-
GDC-0973 (R-enantiomer); XL-518 (R-enantiomer)
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MEK
|
Cancer
|
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
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-
- HY-18652A
-
Ro 5126766 potassium; CH5126766 potassium
|
Raf
MEK
|
Cancer
|
Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) .
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-
- HY-13078
-
GDC-0973 racemate; XL518 racemate
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MEK
|
Cancer
|
Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
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-
- HY-13449
-
TAK-733
5 Publications Verification
|
MEK
|
Cancer
|
TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
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-
- HY-14947
-
MKI 833
|
MEK
|
Cancer
|
Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
|
-
- HY-111368
-
|
MEK
|
Cancer
|
EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
|
-
- HY-113592
-
|
ERK
|
Cancer
|
ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .
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-
- HY-10216
-
BAY 869766 R enantiomer; RDEA119 R enantiomer
|
MEK
|
Cancer
|
Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.
|
-
- HY-12056
-
|
MEK
ERK
|
Cancer
|
BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
|
-
- HY-18955
-
|
MEK
Aurora Kinase
Apoptosis
|
Cancer
|
BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-114189
-
UNC10225170
|
MEK
|
Cancer
|
GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein .
|
-
- HY-114189A
-
UNC10225170 hydrochloride
|
MEK
|
Cancer
|
GW284543 (UNC10225170) hydrochloride is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein .
|
-
- HY-B0023
-
CS 905
|
Calcium Channel
MEK
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
Azelnidipine (CS 905) is a dihydropyridine calcium channel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects .
|
-
- HY-130642
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(S,R,S)-AHPC-Me-C10-Br is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-Me-C10-Br incorporates a VHL E3 ligase linker and MS432 based on the MEK1/2 inhibitor PD0325901 .
|
-
- HY-148507
-
|
MEK
|
Cancer
|
GSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis .
|
-
- HY-156625
-
NFX-179
|
MEK
|
Cancer
|
Nedometinib is a tyrosine kinase inhibitor targeting to MEK1. Nedometinib has antineoplastic effect and can be used for research in dermatosis, cutaneous fibroneuroma, neurofibromatosis .
|
-
- HY-164428
-
|
PKC
|
Cancer
|
AE 51310 is an OPN4 inhibitor. AE 51310 inhibits the activation of PKC and the downstream BRAF/MEK/ERKs signaling pathway. AE 51310 can be used for cancer research, such as NSCLC .
|
-
- HY-19700
-
|
MEK
ERK
Endogenous Metabolite
|
Others
|
trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
|
-
- HY-10338A
-
|
c-Met/HGFR
VEGFR
|
Cancer
|
Foretinib phosphate is an orally bioavailable small molecule with potential anti-tumor activity. Foretinib phosphate can selectively inhibit hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib phosphate shows different anti-cancer activity from cabozantinib in lung cancer cells and has stronger inhibitory effects on targets such as MEK1/2, FER and AURKB .
|
-
- HY-107620
-
|
MEK
|
Neurological Disease
|
PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects .
|
-
- HY-139558
-
PD0184264; ATR-002
|
MEK
Influenza Virus
Bacterial
|
Infection
Cancer
|
Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities .
|
-
- HY-N12740
-
|
MEK
ERK
|
Others
|
Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis .
|
-
- HY-32718
-
EKB-569; WAY-EKB 569
|
EGFR
Src
|
Cancer
|
Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
|
-
- HY-110171
-
iMDK
2 Publications Verification
|
PI3K
|
Cancer
|
iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
- HY-110171A
-
|
PI3K
|
Cancer
|
iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice .
|
-
- HY-10508
-
|
MEK
|
Cancer
|
(R)-PD 0325901CL is an isomer of PD 0325901CL. PD 0325901CL is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) involved in cancer research. PD 0325901CL inhibits the growth of cancer cells in vitro and in vivo .
|
-
- HY-W065835
-
|
HIV
|
Infection
|
2-Bromoaldisine is a pyrrole alkaloid that can be isolated from the Red Sea: marine sponge Stylissa carter. 2-Bromoaldisine inhibits HIV-1 vector infection. 2-Bromoaldisine inhibits Raf/MEK/MAPK pathway .
|
-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
|
-
- HY-19700S
-
|
MEK
ERK
Endogenous Metabolite
|
Others
|
trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
|
-
- HY-162658
-
|
HDAC
Apoptosis
|
Cancer
|
Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models .
|
-
- HY-10254G
-
PD0325901; PD325901
|
MEK
|
Cancer
|
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
|
-
- HY-14590
-
-
- HY-13078S
-
GDC-0973-13C66 racemate; XL518-13C6 racemate
|
Isotope-Labeled Compounds
|
Others
|
Cobimetinib- 13C6 (GDC-0973- 13C6; XL518- 13C6) racemateis the deuterium labeledCobimetinib (racemate)(HY-13078) . Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor .
|
-
- HY-120454
-
|
MEK
Potassium Channel
|
Cancer
|
G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
|
-
- HY-10542
-
|
Raf
Apoptosis
|
Cancer
|
GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms .
|
-
- HY-B0185A
-
Lignocaine hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence . Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor .
|
-
- HY-B0185
-
Lignocaine
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-B0185B
-
Lignocaine hydrochloride hydrate
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-142160
-
|
Raf
|
Cancer
|
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
|
-
- HY-157740
-
|
HDAC
|
Cancer
|
XSJ-10 is a HDAC inhibitor containing a RAS/RAF protein interfering unit, with IC50s of 0.05 and 0.04 μM in PANC-1 cells and HT-29 cells. XSJ-10 can effectively induce the apoptosis of cancer cells and suppress the tumor by strongly inhibiting the RAS-RAF-MEK-ERK signaling pathway and the acetylation level of HDAC3 .
|
-
- HY-141523
-
RMC-4630; SHP2-IN-7
|
SHP2
Phosphatase
|
Cancer
|
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
|
-
- HY-14590R
-
Kempferol(Standard); Robigenin (Standard)
|
Estrogen Receptor/ERR
Autophagy
Mitophagy
Apoptosis
HIV
Parasite
Endogenous Metabolite
|
Cancer
|
Kaempferol (Standard) is the analytical standard of Kaempferol. This product is intended for research and analytical applications. Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer .
|
-
- HY-149380
-
|
Raf
|
Cancer
|
Vem-L-Cy5 (compound 3),modified with the NIR fluorophore cyanine-5 (Cy5),is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAF V600E,and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability,and inhibits cell growth of many types of cancer .
|
-
- HY-B0185AS1
-
Lignocaine-d6 hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
|
-
- HY-158115
-
|
Molecular Glues
Raf
MEK
|
Cancer
|
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .
|
-
- HY-12010
-
AC480 Hydrochloride
|
EGFR
|
Cancer
|
BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
- HY-10251
-
AC480
|
EGFR
|
Cancer
|
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
- HY-B0185AS
-
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine-d10 (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride, an amide derivative, has the potential for the research of the ventricular arrhythmia[2].
|
-
- HY-B0185S1
-
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
|
-
- HY-B0185S
-
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
N-Oxide Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
|
-
- HY-B0185R
-
Lignocaine (Standard)
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine (Standard) is the analytical standard of Lidocaine. This product is intended for research and analytical applications. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-164400
-
|
MEK
ERK
Akt
Apoptosis
|
Cancer
|
SIJ1777 is a GNF-7 (HY-10943) derivative, possesses potent anti-cancer effects on melanoma cells harboring BRAF class I/II/III mutations. SIJ1777 substantially inhibits the activation of MEK, ERK, and AKT. SIJ1777 remarkably induces apoptosis and significantly blocks migration, invasion, and anchorage-independent growth of melanoma cells harboring BRAF class I/II/II mutations .
|
-
- HY-B0185BR
-
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
Lidocaine (hydrochloride hydrate) (Standard) is the analytical standard of Lidocaine (hydrochloride hydrate). This product is intended for research and analytical applications. Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-108635
-
PAF (C16)
|
p38 MAPK
MEK
ERK
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
|
C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability .
|
-
- HY-142042
-
|
MEK
TGF-beta/Smad
|
Neurological Disease
Inflammation/Immunology
Cancer
|
3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is an inhibitor for bone morphogenetic protein 2 (BMP2) with an IC50 of 2.2 μM. 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is inhibitor for mitogen-activated protein kinase 1 (MEK1). 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles exhibits anti-inflammatory and neuroprotective activity in EAE mouse model .
|
-
- HY-B0185G
-
Lignocaine
|
Apoptosis
Sodium Channel
MEK
ERK
NF-κB
|
Cancer
|
Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-15504A
-
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-15504
-
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-148907
-
|
CaMK
MEK
Mixed Lineage Kinase
|
Cancer
|
CS640 is a selective inhibitor of calmodulin-dependent kinases. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, PIP5K1C, MEK5, RIPK4 and MLK3 with IC50 values of 0.08, 0.03, 0.001, 0.001, 11.2, 0.025, 5.69 and 2.75 μM, respectively. CS640 also shows inhibitory effects to CYP450 2C9 and CYP450 2C19 with IC50 values of 6 and 10 μM, respectively .
|
-
- HY-128634
-
|
Apoptosis
PI3K
MEK
|
Cancer
|
CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer .
|
-
- 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-164529
-
|
Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
|
-
- HY-153863
-
|
PROTACs
MEK
|
Cancer
|
MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma . (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078))
|
-
- HY-N0226A
-
|
Cholinesterase (ChE)
Beta-secretase
Reactive Oxygen Species
|
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-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-161966
-
|
Apoptosis
Reactive Oxygen Species
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-164473
-
|
ERK
Akt
STAT
Apoptosis
|
Cancer
|
DETD-35 is an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways, which promotes cancer cell apoptosis (Apoptosis) and reduces cancer cell resistance to Vemurafenib (HY-12057). The IC50 values of DETD-35 against wild-type and mutant melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c are 2.7, 6.0, 3.9, 3.1, and 2.5 μM, respectively. DETD-35 holds promise for research in the field of anti-melanoma therapy .
|
-
- HY-167854
-
|
Others
|
Cancer
|
KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
|
-
- HY-B0766
-
SY801
|
Autophagy
Apoptosis
HBV
HCV
HSP
Reactive Oxygen Species
Bcl-2 Family
Glutathione S-transferase
p38 MAPK
NF-κB
Microtubule/Tubulin
ERK
JNK
TNF Receptor
Interleukin Related
CDK
Cyclin G-associated Kinase (GAK)
mTOR
P-glycoprotein
Ferroptosis
|
Infection
Inflammation/Immunology
Cancer
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Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .
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HY-L010
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544 compounds
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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 544 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.
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Cat. No. |
Product Name |
Type |
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- HY-10254G
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PD0325901 (GMP); PD325901 (GMP)
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Fluorescent Dye
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Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
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- HY-B0185G
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Lignocaine (GMP)
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Fluorescent Dye
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Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
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Cat. No. |
Product Name |
Type |
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- HY-10254G
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PD0325901 (GMP); PD325901 (GMP)
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Biochemical Assay Reagents
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Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
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- HY-B0185G
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Lignocaine (GMP)
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Biochemical Assay Reagents
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Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P4133
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ERK
MEK
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Cancer
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MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable .
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- HY-P4136
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ERK
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Cancer
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Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM .
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- HY-P5977
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Ste-MPKKKPTPIQLNP-NH₂; ERK Activation inhibitor Peptide
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ERK
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Cancer
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STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
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- HY-P10074
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ERK
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Inflammation/Immunology
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TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC50 in vitro for ERK2 is 29 μM .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-107417
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Structural Classification
Monophenols
Microorganisms
Antifungal
Macrolide Antibiotics
Classification of Application Fields
Antibiotics
Source classification
Phenols
Disease Research
Disease Research Fields
Cancer
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VEGFR
MEK
FLT3
PDGFR
ERK
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Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively .
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- HY-19700
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- HY-14590
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- HY-108635
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- HY-N0226A
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- HY-N12740
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- HY-W065835
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- HY-14590R
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- HY-N0226
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Alkaloids
Source classification
Ranunculaceae
Coptis chinensis Franch.
Plants
Isoquinoline Alkaloids
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Cholinesterase (ChE)
Beta-secretase
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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 .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-19700S
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trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
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- HY-B0185AS
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Lidocaine-d10 (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride, an amide derivative, has the potential for the research of the ventricular arrhythmia[2].
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- HY-B0185S1
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Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
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- HY-10999S
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Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-10999S1
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Trametinib- 13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-10999S2
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Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
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- HY-13064S1
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Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
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- HY-13078S
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Cobimetinib- 13C6 (GDC-0973- 13C6; XL518- 13C6) racemateis the deuterium labeledCobimetinib (racemate)(HY-13078) . Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor .
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- HY-B0185AS1
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Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
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- HY-B0185S
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N-Oxide Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
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