Catalog No.
Product Name
Application
Product Information
Citations
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MEK1/2 inhibitor
AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that inhibits growth and survival of MM cells and cytokine-induced osteoclast differentiation. -
MEK Inhibitor
AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
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MEK inhibitor
BIX 02189 is a selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Mitsunori Miyazaki, .et al. , FEBS Open Bio, 2017, Mar; 7(3): 424-433 PMID: 28286738
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MEK1/2 inhibitor
PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.- Sachio Suzuki, .et al. , Cell Chem Biol, 2022, Sep 15;29(9):1446-1464 PMID: 35835118
- Masaru Yoshikawa, .et al. , J Am Chem Soc, 2021, May 5;143(17):6434-6446 PMID: 33890764
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MEK inhibitor
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.- Tadaaki Nakajima, .et al. , FEBS Open Bio, 2024, Jan;14(1):37-50 PMID: 37953493
- Jan Langkabel, .et al. , bioRxiv, 2021, January 25
- Ryan Clarke, .et al. , Mol Cell, 2021, Jan 21;81(2):226-238.e5 PMID: 33378644
- Tzeng SF, .et al. , FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fukumoto S, .et al. , Acta Histochem, 2018, Feb;120(2):142-150 PMID: 29397960
- Yoshiteru Yano, .et al. , Regenerative Therapy, 2016, 3 (2016) 1-6
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MEK inhibitor
AZD6244 (Selumetinib) also known as Selumetinib, ARRY142886, AZD-6244 & ARRY-142886 is MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nm.- Chia-Chi Chang, .et al. , Oncotarget, 2016, Jun 7; 7(23): 35270-35283 PMID: 27150057
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MEK Inhibitor
PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase.- Masayuki Harada, .et al. , Cell Cycle, 2024, Feb;23(3):308-327 PMID: 38461418
- Shota Mizuno, .et al. , Biol Pharm Bull, 2024, 47(1):120-129 PMID: 38171772
- Anna Nakanishi, .et al. , Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Isamu Ogawa, .et al. , Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Hanna Galganska, .et al. , Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Akinobu Nakamura, .et al. , ACS Chem Biol, 2020, Apr 17;15(4):1004-1015 PMID: 32162909
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Kwang Woon Kim, .et al. , Oncotarget, 2019, Sep 24; 10(54): 5645-5659 PMID: 31608140
- Tsai CC, .et al. , Biochim Biophys Acta Mol Cell Res, 2018, Oct 13. pii: S0167-4889(18)30452-X PMID: 30321617
- Kim MH, .et al. , Oncol Rep, 2018, Nov;40(5):2977-2987 PMID: 30226616
- Onozato D, .et al. , Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
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MEK inhibitor
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.- Ji Wang, .et al. , Acta Pharmacol Sin, 2024, Nov 20 PMID: 39567750
- Hanna Galganska, .et al. , Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. , Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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MEK Inhibitor
Trametinib (GSK1120212, JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.
- Yue Zhou, .et al. , Biol Pharm Bull, 2025, 48(7):1089-1095 PMID: 40721370
- Song Han, .et al. , Neoplasia, 2025, Jan:59:101070 PMID: 39541736
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Meenu Kesarwani, .et al. , Blood Adv, 2024, Jun 11;8(11):2765-2776 PMID: 38531054
- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
- Tsung-Ming Chang, .et al. , Journal of Biomedical Science, 2022, 29:92
- Nao Yamagishi, .et al. , Biol Pharm Bull, 2022, 45(10):1553-1558 PMID: 36184515
- Hayato Mizuta, .et al. , Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Keisuke Yanagida, .et al. , Dev Cell, 2020, 52 (6), 779-793 PMID: 32059774
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Kanemaru Y, .et al. , Acta Neuropathol Commun, 2019, Jul 25;7(1):119 PMID: 31345255
- Chul Min Park, .et al. , Oncol Lett, 2018, Feb; 15(2): 1758-1762 PMID: 29434871
- Sumi T, .et al. , Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601
- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Yuki Kawasaki, .et al. , Sci Rep, 2016, 6: 31502 PMID: 27531070
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MEK Inhibitor
TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
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MEK inhibitor
Refametinib is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. -
MEK1 inhibitor
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases.- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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MEK1/2 inhibitor
MEK162 (ARRY-438162) is a potent, selective, ATP uncompetitive inhibitor of MEK1/2.- S Shahab, .et al. , J Neuropathol Exp Neurol, 2020, Jul 1;79(7):746-753
- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
- Alquezar C, .et al. , Eur Neuropsychopharmacol, 2015, Mar;25(3):386-403 PMID: 25624003
- trans-Zeatin is a member of the plant hormone family known as ??cytokinins??, which regulate cell division, development, and nutrient processing.
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MEK1/2 inhibitor
Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. -
Ras/Raf/MEK inhibitor
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. - Hypothemycin is a resorcylic acid lactone polyketide. It was found to inhibit the proliferation of mouse and human T cells stimulated with anti-CD3 mAb + PMA and of human PBMC stimulated with anti-CD3 mAb alone.
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Raf/MEK dual inhibitor
Avutometinib (RO5126766, CH5126766), is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity.
- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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MKK/MEK inhibitor
SL-327 is a selective inhibitor of MEK1 and MEK2 (IC50 values are 0.18 and 0.22 μM respectively); blocks hippocampal LTP in vitro. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration. -
MEK inhibitor
Cobimetinib is a potent, highly selective inhibitor of MEK1/2.- Chitra Subramanian, .et al. , J Cell Mol Med, 2025, Mar;29(6):e70489 PMID: 40135438
- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Chun-Yu Liu, .et al. , Cancers (Basel), 2019, Jan 17;11(1) PMID: 30658422
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MEK inhibitor
Cobimetinib R-enantiomer is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2). -
MEK/Aurora Inhibitor
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.- Hilda Samimi, .et al. , Cancer Cell Int, 2022, Dec 8;22(1):388 PMID: 36482411
- Hilda Samimi, .et al. , Thyroid Res, 2021, Dec 3;14(1):27 PMID: 34861882
- Hilda Samimi, .et al. , DARU J Pharm Sci, 2019, 1-7 PMID: 31077090
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MEK1 inhibitor
Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM. - Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
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MEK inhibitor
Trametinib DMSO solvate (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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ALK/MET inhibitor
Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. -
MEK5 inhibitor
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.- Mitsunori Miyazaki, .et al. , FEBS Open Bio, 2017, Mar; 7(3): 424-433 PMID: 28286738
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PAF activator
C16-PAF (PAF (C16)) is a phospholipid mediator and a potent platelet-activating factor that functions as a ligand for the PAF G-protein-coupled receptor (PAFR). It exhibits anti-apoptotic effects by inhibiting caspase-dependent cell death through PAFR activation. C16-PAF is a strong activator of the MAPK and MEK/ERK signaling pathways and is known to induce increased vascular permeability. -
MEK1/2 inhibitor
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor with an IC50 of 1.9 nM against MEK1. It effectively blocks the RAS-RAF-MEK-ERK signaling cascade, inducing cell cycle arrest and apoptosis. Tunlametinib exhibits strong antiproliferative activity against RAS/RAF mutant cancer cells, including BRAF^V600E and KRAS^G12C mutants, and shows synergistic anti-tumor effects when combined with BRAF, KRAS^G12C, or SHP2 inhibitors, as well as Docetaxel. It is a promising agent for the study of targeted therapies in RAS/RAF-driven malignancies such as melanoma, colorectal cancer, and non-small cell lung cancer. -
MEK1/2 inhibitor
MAP855 is a highly potent, selective, ATP-competitive, and orally active MEK1/2 kinase inhibitor, with an IC50 of 3 nM for the MEK1–ERK2 cascade and a pERK EC50 of 5 nM. It exhibits equipotent inhibitory activity against both wild-type and mutant forms of MEK1/2, making it a valuable tool for MAPK pathway research. -
PROTAC MEK1/2 Degrader
MS432 is a first-in-class, highly selective PROTAC degrader targeting MEK1 and MEK2, based on PD0325901 and a von Hippel-Lindau (VHL) E3 ligase ligand. It demonstrates favorable plasma exposure in mice and induces MEK1 and MEK2 degradation in HT29 cells with DC₅₀ values of 31 nM and 17 nM, respectively. -
MEK 1/2 Degrader
MS934 is a VHL-recruiting PROTAC degrader that targets MEK 1/2, facilitating their degradation alongside CRAF. This compound demonstrates significant biological activity in various cancer models, including melanoma, non-small cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma. MS934 serves as an important tool for research into targeted cancer therapies and the mechanistic understanding of these oncogenic pathways. -
MEK/PI3K Inhibitor
ST-168 is an orally bioavailable inhibitor of MEK and PI3K, exhibiting IC50 values of 182 nM for MEK1 and showing varying potency against PI3K isoforms with values of 69.2 nM, 41.7 nM, 1482 nM, and 2293 nM for PI3Kα, PI3Kδ, PI3Kβ, and PI3Kγ, respectively. It effectively inhibits ERK1/2 and AKT phosphorylation, inducing apoptosis in cancer cells within a 3D tumor sphere model. In vivo studies demonstrate its substantial antitumor efficacy in A375 melanoma mouse models. Additionally, ST-168 displays an improved ocular safety profile compared to conventional MEK inhibitors, evidenced by reduced caspase activation and apoptosis levels, making it a valuable tool for melanoma research. -
MEK1/2 Inhibitor
RO5068760 is a potent non-ATP-competitive inhibitor of MEK1/2, demonstrating an IC50 of 0.025 μM for MEK1. This compound effectively inhibits MAPK pathway activity, leading to G1 cell cycle arrest and apoptosis, thereby reducing cancer cell proliferation. RO5068760 is applicable in research on various tumors characterized by dysregulation of the MAPK pathway, including melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer.
