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MAPK | MAPK 信号通路

MAPK | MAPK 信号通路

Catalog No.	Product Name	Application	Product Information
A10453 SALE	Honokiol	Antiangiogenic and Antitumor Agent	Honokiol is a lignan present in the cones, bark, and leaves of Magnolia grandiflora that has shown pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines.
A14137 SALE	SL-327	MKK/MEK 抑制剂	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.
A11264	Refametinib	MEK 抑制剂	Refametinib is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
A15050	Cobimetinib (racemate)	MEK 抑制剂	Cobimetinib is a potent, highly selective inhibitor of MEK1/2. Product Citations (1) Chun-Yu Liu, .et al. Varlitinib Downregulates HER/ERK Signaling and Induces Apoptosis in Triple Negative Breast Cancer Cells, Cancers (Basel), 2019, Jan 17;11(1) PMID: 30658422
A15051	Cobimetinib (R-enantiomer)	MEK 抑制剂	Cobimetinib R-enantiomer is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2).
A15157	MEK inhibitor	MEK 抑制剂	MEK inhibitor is a potent MEK inhibitor, antitumor agent.
A15762	BI-847325	MEK/Aurora 抑制剂	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.
A14380	G-479	MEK 抑制剂	G-479 is an potent MEK inhibitor. G-479 with polarity distributed throughout the molecule was shown improved bioactivity over GDC-0623 in many aspects.
A12974	GDC-0623	MEK1 抑制剂	GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
A16032	PD 198306	MEK 抑制剂	PD 198306 is a potent, selective and non-ATP competitive MAPK/ERK-kinase (MEK) inhibitor.
A16044	PD 334581	MEK1 抑制剂	PD 334581 is used in biological studies to evaluate halogen bonding as a novel interaction for rational drug design. It is also an inhibitor of MEK1.
A10256 SALE	PD0325901	MEK 抑制剂	PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2. Product Citations (3) Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246 Fukumoto S, .et al. Synergistic anti-proliferative effects of mTOR and MEK inhibitors in high-grade chondrosarcoma cell line OUMS-27, Acta Histochem, 2018, Feb;120(2):142-150 PMID: 29397960 Yoshiteru Yano, .et al. Non-neural and cardiac differentiating properties of Tbx6-expressing mouse embryonic stem cells, Regenerative Therapy, 2016, 3 (2016) 1-6
A10257	AZD6244 (Selumetinib)	MEK 抑制剂	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. Product Citations (1) Chia-Chi Chang, .et al. Upregulation of lactate dehydrogenase a by 14-3-3汎 leads to increased glycolysis critical for breast cancer initiation and progression, Oncotarget, 2016, Jun 7; 7(23): 35270每35283 PMID: 27150057
A10705	PD98059	MEK 抑制剂	PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Product Citations (3) Tsai CC, .et al. Protease-activated receptor 2 induces migration and promotes Slug-mediated epithelial-mesenchymal transition in lung adenocarcinoma cells, Biochim Biophys Acta Mol Cell Res, 2018, Oct 13. pii: S0167-4889(18)30452-X PMID: 30321617 Kim MH, .et al. C16?ceramide and sphingosine 1?phosphate/S1PR2 have opposite effects on cell growth through mTOR signaling pathway regulation, Oncol Rep, 2018, Nov;40(5):2977-2987 PMID: 30226616 Onozato D, .et al. Efficient Generation of Cynomolgus Monkey Induced Pluripotent Stem Cell-Derived Intestinal Organoids with Pharmacokinetic Functions, Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
A10212 SALE	PD184352 (CI-1040)	MEK1/2 抑制剂	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.
A10957 SALE	U0126-EtOH	MEK 抑制剂	U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively. Product Citations (2) Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055 Choe YJ, .et al. Nutlin-3 induces HO-1 expression by activating JNK in a transcription-independent manner of p53., Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
A10089 SALE	AS703026 (Pimasertib)	MEK1/2 抑制剂	AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that inhibits growth and survival of MM cells and cytokine-induced osteoclast differentiation.
A11029 SALE	GSK1120212 (JTP-74057, Trametinib)	MEK 抑制剂	GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. Product Citations (5) Chul Min Park, .et al. Mechanisms for DNA-damaging agent-induced inactivation of ErbB2 and ErbB3 via the ERK and p38 signaling pathways, Oncol Lett, 2018, Feb; 15(2): 1758每1762 PMID: 29434871 Sumi T, .et al. Trametinib downregulates survivin expression in RB1-positive KRAS-mutant lung adenocarcinoma cells, Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601 Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33每46 PMID: 29658609 Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358 Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
A10151 SALE	BIX 02189	MEK 抑制剂	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. Product Citations (1) Mitsunori Miyazaki, .et al. TSC2/Rheb signaling mediates ERK坼dependent regulation of mTORC1 activity in C2C12 myoblasts, FEBS Open Bio, 2017, Mar; 7(3): 424每433 PMID: 28286738
A11040 SALE	TAK-733	MEK 抑制剂	TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
A10115	AZD8330	MEK 抑制剂	AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
A10704	PD318088	MEK 抑制剂	PD318088 is an inhibitor of MEK1 AND MEK2.
A10150	BIX02188	MEK5 抑制剂	BIX02188 is a potent and selective inhibitor of MEK5.
A11441 SALE	GDC-0973 (Cobimetinib)	MEK1 抑制剂	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. Product Citations (1) Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
A11493 SALE	MEK162 (ARRY-438162, Binimetinib)	MEK1/2 抑制剂	MEK162 (ARRY-438162) is a potent, selective, ATP uncompetitive inhibitor of MEK1/2. Product Citations (2) Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332 Alquezar C, .et al. Increasing progranulin levels and blockade of the ERK1/2 pathway: Upstream and downstream strategies for the treatment of progranulin deficient frontotemporal dementia, Eur Neuropsychopharmacol, 2015, Mar;25(3):386-403 PMID: 25624003
A11247	RO4927350	MEK1/2 抑制剂	RO4927350 a potent and highly selective non-ATP-competitive MEK1/2 inhibitor.
A12866	Refametinib (RDEA-119, BAY 86-9766)	MEK1/2 抑制剂	Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. Product Citations (1) Estelle Daudigeos-Dubus, etc. Regorafenib: Antitumor Activity upon Mono and Combination Therapy in Preclinical Pediatric Malignancy Models. PLoS One. 2015; 10(11): e0142612.
A13119	Balamapimod (MKI-833)	Ras/Raf/MEK 抑制剂	Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor.
A14019	RO5126766 (CH5126766)	Raf/MEK dual 抑制剂	RO5126766, also known as CH5126766, is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity.
A13750	Hypothemycin	-	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.
A13272	RO4987655	MEK1 抑制剂	RO4987655 is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity.
A11225	Pluripotin (SC-1)	ERK1/RasGAP 抑制剂	The activity of Pluripotin (SC-1) is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.
A11794 SALE	Ulixertinib (BVD-523, VRT752271)	ERK1/ERK2 抑制剂	VRT752271 is a pyrrole inhibitors of ERK protein kinase.
A12824 SALE	SCH772984	ERK 抑制剂	SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively. Product Citations (2) Guo X, .et al. PDGF-induced migration of synthetic vascular smooth muscle cells through c-Src-activated L-type Ca2+ channels with full-length CaV1.2 C-terminus, Pflugers Arch, 2018, Jun;470(6):909-921 PMID: 29441404 Takuya Hasegawa, .et al. ErbB2 signaling epigenetically suppresses microRNA坼205 transcription via Ras/Raf/MEK/ERK pathway in breast cancer, FEBS Open Bio, 2017, Aug; 7(8): 1154每1165 PMID: 28781955
A12505 SALE	TCS ERK 11e (VX-11e)	ERK2 抑制剂	TCS ERK 11e (VX-11e) is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM). Product Citations (1) Qi-sang Guo, etc. Involvement of FAK-ERK2 signaling pathway in CKAP2-induced proliferation and motility in cervical carcinoma cell lines. Sci Rep. 2017; 7: 2117.
A13420 SALE	GDC0994	ERK1/2 抑制剂	GDC-0994 is a potent and selective Erk1/2 inhibitor. GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways.
A14090	XMD 17-109	ERK5 抑制剂	XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 uM in HEK293 cells.
A14119 SALE	FR 180204	ERK 抑制剂	FR 180204 is a novel and selective inhibitor of extracellular signal-regulated kinase (ERK), which may be a potential new therapy for rheumatoid arthritis. Product Citations (1) Dyshlovoy SA, .et al. Proteomic-based investigations on the mode of action of the marine anticancer compound rhizochalinin, Proteomics, 2017, Jun;17(11) PMID: 28445005
A11609 SALE	XMD8-92	BMK1/ERK5 抑制剂	XMD8-92 is a potent and selective BMK1/ERK5 inhibitor .
A13977	TMCB	CK2/ERK8 抑制剂	MCB has been shown to inhibit both casein kinase 2 (CK2) and extracellular-signal-regulated kinase 8 (ERK8/MAPK15) (IC50 = 0.50 uM for both CK2 and ERK8).
A15802 SALE	DEL-22379	ERK 抑制剂	DEL-22379 is a potent and selective ERK Dimerization inhibitor that inhibits ERK Dimerization without affecting ERK phosphorylation, forestalls tumorigenesis driven by RAS-ERK pathway oncogenes.
A16231	APS-2-79	KSR/Ras 抑制剂	APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.
A16232	ERK5-IN-1	ERK5 抑制剂	ERK5-IN-1 exhibits potent inhibition of ERK5 with cellular EC50 values of 0.19 uM and enzymatic IC50 values of 0.087 uM and of LRRK2[G2019S] with enzymatic IC50 values of 0.026uM.
A16233	Tomatidine	ERK/Akt/NF-kB 抑制剂	Tomatidine inhibits the phosphorylation of ERK, Akt, and the nuclear content of NF-kB. possess anti-inflammatory properties.
A13678	SB-242235	p38 MAPK 抑制剂	SB-242235 is a potent and selective p38 MAP kinase inhibitor that may be an effective therapy for cytokine-mediated diseases such as autoimmune or inflammatory diseases.
A13552	RWJ-67657	p38 MAPK 抑制剂	RWJ-67657 is a potent p38 MAPK inhibitor.
A13563	BMS-582949	p38 MAPK 抑制剂	BMS-582949 Is a Dual Action p38 Kinase Inhibitor Well Suited To Avoid Resistance Mechanisms That Increase p38 Activation in Cells.
A10895	Pexmetinib (ARRY-614)	p38 MAPK 抑制剂	Pexmetinib is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase.
A10970	AMG 548	p38 MAPK 抑制剂	AMG 548 is a potent and selective inhibitor of p38α. It displays >1000-fold selectivity against 36 other kinases, and it inhibits whole blood LPS-stimulated TNFα.
A11101	SKF 86002 Dihydrochloride	p38 MAPK 抑制剂	SKF 86002 Dihydrochloride is inhibitor of p38 MAP kinase (IC50 = 0.1 - 1 uM). Potently inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 uM).

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MAPK | MAPK 信号通路

A10453 SALE

A14137 SALE

A11264

A15050

A15051

A15157

A15762

A14380

A12974

A16032

A16044

A10256 SALE

A10257

A10705

A10212 SALE

A10957 SALE

A10089 SALE

A11029 SALE

A10151 SALE

A11040 SALE

A10115

A10704

A10150

A11441 SALE

A11493 SALE

A11247

A12866

A13119

A14019

A13750

A13272

A11225

A11794 SALE

A12824 SALE

A12505 SALE

A13420 SALE

A14090

A14119 SALE

A11609 SALE

A13977

A15802 SALE

A16231

A16232

A16233

A13678

A13552

A13563

A10895

A10970

A11101