Search Result

Search Results for " mek1 "

Targets

Compounds

Natural Products

Recombinant Proteins

Cat No.	Product Name	Synonyms	Targets
T80543	STE-MEK1(13)	ERK Activation Inhibitor Peptide,Ste-MPKKKPTPIQLNP-NH₂	ERK
	STE-MEK1(13), a cell-permeable ERK1/2 inhibitor with IC50 values ranging from 13 to 30 μM, impedes the phosphorylation of ERK1/2, as demonstrated in studies [1] [2].		ERK
T63547	MEK1/2-IN-2
	MEK1/2-IN-2 is a potent, ATP-competitive MEK1/2 inhibitor that exhibits equal inhibitory effects on wild-type MEK1/2 and a group of MEK1/2 mutant cells.
T79144	PROTAC MEK1 Degrader-1		PROTACs
	PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferat...		PROTACs
T76556	MEK1 Derived Peptide Inhibitor 1
	MEK1 Derived Peptide Inhibitor 1, a peptide inhibitor, prevents the in vitro activation of ERK2 by MEK1, exhibiting an inhibitory concentration (IC 50) of 30 μM. It is utilized in the study of cell-permeable [1].
T76557	Myristoyl-MEK1 Derived Peptide Inhibitor 1
	Myristoyl-MEK1 Derived Peptide Inhibitor 1, the myristoylated variant of MEK1 Derived Peptide Inhibitor 1, effectively inhibits ERK activation, demonstrating an inhibitory concentration (IC50) of 10 μM [1].
T72407	C-Met/MEK1/Flt-3-IN-1
	Antiproliferative Against-3 (comp 33) demonstrates significant activity against Hela (IC 50 = 0.21 µM), A549 (IC 50 = 0.39 µM), and MCF-7 (IC 50 = 0.33 µM) cell lines. Additionally, it induces apoptosis in a dose-depende...
T6636	Refametinib	BAY 86-97661,BAY 869766,RDEA119	MEK
	Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).		MEK
T6692	TAK-733	TAK733,TAK 733	MEK
	TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.		MEK
T6131	Pimasertib	AS703026,MSC1936369B,SAR 245509	MEK
	Pimasertib (AS703026) is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.		MEK
T6218	Selumetinib	ARRY-142886,AZD6244	Apoptosis , ERK , MEK
	Selumetinib (AZD6244) (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM).		Apoptosis , ERK , MEK
T6843	GDC-0623	G-868,GDC0623,RG 7421,MEK inhibitor 1	Apoptosis , MEK
	GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.		Apoptosis , MEK
T5412	RO4987655	CH4987655,RG7167	MEK
	RO4987655 (RG7167) is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).		MEK
T2708	SL327	SL 327,SL-327	MEK , DNA/RNA Synthesis
	SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.		MEK , DNA/RNA Synthesis
T5857	Trametinib (DMSO solvate)	Trametinib DMSO solvate,GSK-1120212 (DMSO solvate),Trametinib dimethyl sulfoxide,JTP-74057 (DMSO solvate)	Apoptosis , MEK
	Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a Highly Potent and Selective MEK Inhibitor that specifically inhibits MEK1/2(IC50 :2 nM)		Apoptosis , MEK
T2443	CI-1040	PD 184352	Apoptosis , MEK
	CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM).		Apoptosis , MEK
T2125	Trametinib	GSK1120212,JTP-74057	Apoptosis , MEK , Autophagy
	Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.		Apoptosis , MEK , Autophagy
T6223	U0126-EtOH	U0126 Ethanol,U0126	Mitophagy , Influenza Virus , MEK , Autophagy
	U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).		Mitophagy , Influenza Virus , MEK , Autophagy
T2623	PD98059	PD 98059	ERK , Aryl Hydrocarbon Receptor , MEK , Autophagy
	PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.		ERK , Aryl Hydrocarbon Receptor , MEK , Autophagy
T6152	PD318088		MEK
	PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.		MEK
T2508	Binimetinib	ARRY-438162,ARRY-162,MEK162	MEK , Autophagy
	Binimetinib (ARRY-162) (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.		MEK , Autophagy
T6971	Ro 5126766	CH5126766,Avutometinib,VS-6766,RO5126766	Raf , MEK
	RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.		Raf , MEK
T6324	(E/Z)-BIX02188	334949-59-6	ERK , MEK , TGF-beta/Smad
	BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, JNK2, and ERK2.		ERK , MEK , TGF-beta/Smad
T6083	AZD8330	ARRY-424704,ARRY-704	ERK , MEK
	AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.		ERK , MEK
T3623	Cobimetinib	RG7420,XL518,GDC-0973	Apoptosis , MEK
	Cobimetinib (GDC-0973) is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of e...		Apoptosis , MEK
T6525	GW 5074	GW5074,Raf1 Kinase Inhibitor I	Apoptosis , Raf
	GW 5074 (Raf1 Kinase Inhibitor I)(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.		Apoptosis , Raf
T2253	TCS PIM-1 1	SC 204330	Pim
	TCS PIM-1 1 (SC 204330)(sc-204330) is a effective and specific ATP-competitive Pim-1 kianse inhibitor (IC50: 50 nM) , exhibits good specific over MEK1/MEK2 and Pim-2(IC50s >20, 000 nM).		Pim
T6039	TAK-285	TAK285,TAK 285	EGFR , MEK , HER , Aurora Kinase
	TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.		EGFR , MEK , HER , Aurora Kinase
T27242	EF24	EF 24,EF-24,3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone	ERK , MEK , Caspase
	EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral ...		ERK , MEK , Caspase
T6077	ZM-447439		Apoptosis , MEK , Src , Aurora Kinase
	ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect aga...		Apoptosis , MEK , Src , Aurora Kinase
T6760	APS-2-79 hydrochloride	APS-2-79 HCl,APS-2-79	MEK , MAPK
	APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activ...		MEK , MAPK
T2378	RGB-286638 free base		GSK-3 , MEK , JAK , CDK
	RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 a...		GSK-3 , MEK , JAK , CDK
T21635	PD184161		MEK
	PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].		MEK
T35610	2,5-dimethyl Celecoxib		Apoptosis , Wnt/beta-catenin , Prostaglandin Receptor
	2,5-dimethyl Celecoxib is a derivative of celecoxib that does not inhibit COX-2 (IC50 = >100 μM).1 It does inhibit microsomal prostaglandin E synthase-1 (mPGES-1) in HeLa cells (IC50 = 15.6 μM) and reduces prostaglandin ...		Apoptosis , Wnt/beta-catenin , Prostaglandin Receptor
T13782	MS432		MEK
	MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.		MEK
T23129	PD 334581		Others
	MEK1 inhibitor		Others
T63929	Selumetinib sulfate
	Selumetinib (AZD6244) is a potent, selective, non-ATP-competitive MEK1/2 inhibitor that inhibits MEK1/2 phosphorylation levels with an IC50 value of 14 nM for MEK1.
T64001	MAP855
	MAP855 is a potent, selective, orally active, ATP-competitive MEK1/2 kinase inhibitor with an IC50 value of 3 nM for MEK1 ERK2 cascade and a pERKEC50 value of 5 nM. MAP855 exhibits equal inhibition of wild-type and mutan...
T71163	Pimasertib HCl
	Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1/2, preventing the acti...
T64175	Cobimetinib hemifumarate
	Cobimetinib hemifumarate is a potent and selective MEK1 inhibitor with an IC50 value of 4.2 nM for MEK1.
T61755	E6201
	E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-ind...
T68267	RO5068760
	RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen...
T69826	U-0126
	U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase M...
T68459	RO4927350
	RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a bro...
T31126	CX-659S	CX659S,UNII-YG2F04AVMQ,CX 659S
	CX-659S is a novel diaminuracil derivative that indirectly inhibits Langerhans cell function by blocking the MEK1/2 -- ERK1/2 pathway in keratinocytes. CX-659S can inhibit the contact hypersensitivity induced by haptens ...
T78209	Nedometinib		MEK
	Nedometinib, a tyrosine kinase inhibitor, specifically targets MEK1 and exhibits antineoplastic effects. It is utilized in research related to dermatosis, cutaneous fibroneruroma, and neurofibromatosis [1].		MEK
T40217	PD0325901-O-C2-dioxolane	PD0325901-O-C2-dioxolane
	PD0325901-O-C2-dioxolane is a chemical compound primarily composed of the MEK inhibitor PD0325901. It can be utilized, in conjunction with either a VHL or CRBN E3 ligase ligand, for the synthesis of MEK1/2 degrader.
T28862	ST-168	ST168,ST 168
	ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ i...
T18668	(S,R,S)-AHPC-Me-C10-Br		Others
	(S,R,S)-AHPC-Me-C10-Br is a chemically synthesized conjugate that functions as a ligand-linker for E3 ligases. This compound incorporates a VHL E3 ligase linker and MS432, derived from the MEK1/2 inhibitor PD0325901[1].		Others
T71722	Angiogenesis inhibitor BT2
	Angiogenesis inhibitor BT2 is a novel inhibitor of angiogenesis and vascular permeability, inhibiting ERK phosphorylation and the expression of FosB/ΔFosB, VCAM-1, and many genes involved in proliferation, migration, ang...
T74361	MEK/PI3K-IN-2
	MEK/PI3K-IN-2 (compound 6s), a potent inhibitor of both MEK and PI3K, demonstrates IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ). This compound effectively reduces pAKT and pERK1/2 levels, exhibiting a...

Compounds

STE-MEK1(13)

T80543

Synonym: ERK Activation Inhibitor Peptide,Ste-MPKKKPTPIQLNP-NH₂

PROTAC MEK1 Degrader-1

T79144

Synonym:

Target: PROTACs

MEK1 Derived Peptide Inhibitor 1

T76556

Synonym:

Target:

Myristoyl-MEK1 Derived Peptide Inhibitor 1

T76557

Synonym:

Target:

c-Met/MEK1/Flt-3-IN-1

Synonym: BAY 86-97661,BAY 869766,RDEA119

Target: MEK

TAK-733

T6692

Synonym: TAK733,TAK 733

Target: MEK

Pimasertib

T6131

Synonym: AS703026,MSC1936369B,SAR 245509

Target: MEK

Selumetinib

T6218

Synonym: ARRY-142886,AZD6244

Target: Apoptosis, ERK, MEK

GDC-0623

T6843

Synonym: G-868,GDC0623,RG 7421,MEK inhibitor 1

Target: Apoptosis, MEK

RO4987655

T5412

Synonym: CH4987655,RG7167

Target: MEK

SL327

T2708

Synonym: SL 327,SL-327

Target: MEK, DNA/RNA Synthesis

Trametinib (DMSO solvate)

T5857

Synonym: Trametinib DMSO solvate,GSK-1120212 (DMSO solvate),Trametinib dimethyl sulfoxide,JTP-74057 (DMSO solvate)

Target: Apoptosis, MEK

CI-1040

T2443

Synonym: PD 184352

Target: Apoptosis, MEK

Trametinib

T2125

Synonym: GSK1120212,JTP-74057

Target: Apoptosis, MEK, Autophagy

U0126-EtOH

T6223

Synonym: U0126 Ethanol,U0126

Target: Mitophagy, Influenza Virus, MEK, Autophagy

PD98059

T2623

Synonym: PD 98059

Target: ERK, Aryl Hydrocarbon Receptor, MEK, Autophagy

Synonym: ARRY-438162,ARRY-162,MEK162

Target: MEK, Autophagy

Ro 5126766

T6971

Synonym: CH5126766,Avutometinib,VS-6766,RO5126766

Target: ERK, MEK, TGF-beta/Smad

AZD8330

T6083

Synonym: ARRY-424704,ARRY-704

Target: ERK, MEK

Cobimetinib

T3623

Synonym: RG7420,XL518,GDC-0973

Target: Apoptosis, MEK

GW 5074

T6525

Synonym: GW5074,Raf1 Kinase Inhibitor I

Target: Apoptosis, Raf

Synonym: TAK285,TAK 285

Target: EGFR, MEK, HER, Aurora Kinase

EF24

T27242

Synonym: EF 24,EF-24,3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone

Target: ERK, MEK, Caspase

ZM-447439

T6077

Synonym:

Target: Apoptosis, MEK, Src, Aurora Kinase

APS-2-79 hydrochloride

T6760

Synonym: APS-2-79 HCl,APS-2-79

Target: GSK-3, MEK, JAK, CDK

2,5-dimethyl Celecoxib

T35610

Synonym:

Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor

Cobimetinib hemifumarate

Synonym: CX659S,UNII-YG2F04AVMQ,CX 659S

PD0325901-O-C2-dioxolane

T40217

Synonym: PD0325901-O-C2-dioxolane

Target:

ST-168

T28862

Synonym: ST168,ST 168

Target:

(S,R,S)-AHPC-Me-C10-Br

T18668

Synonym:

Target: Others

Angiogenesis inhibitor BT2

Cat No.	Product Name	Synonyms	Targets
T6S1587	Notoginsenoside R2	20(S)-Notoginsenoside R2,Ginsenoside Ng-R2	Others , Nrf2
	Notoginsenoside R2 (20(S)-Notoginsenoside R2) has neuroprotection against 6-OHDA-induced neurotoxicity, is associated with Notoginsenoside R2-mediated P90RSK and Nrf2 activation through MEK1/2-ERK1/2 pathways.		Others , Nrf2
T5S2361	Epiberberine		ERK , Beta-Secretase , MEK , BACE , AMPK , AChR , AChE
	1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during 3T3-L1 adipocyte diffe...		ERK , Beta-Secretase , MEK , BACE , AMPK , AChR , AChE
T2836	Isorhamnetin	3-methylquercetin,3'-Methylquercetin,Isorhamnetol,3'-Methoxyquercetin	MEK , PI3K , Endogenous Metabolite
	Isorhamnetin (3-methylquercetin) is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents endothelial cell injuries from oxidized LD...		MEK , PI3K , Endogenous Metabolite
T15542	Hypothemycin		Others
	Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 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).		Others
T14055	5Z-7-Oxozeaenol	FR148083,L783279,LL-Z 1640-2	VEGFR , FLT , MEK , MAPK , PDGFR , Antibiotic , Src
	5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is ...		VEGFR , FLT , MEK , MAPK , PDGFR , Antibiotic , Src
T36954	Nemorosone
	Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma ce...

Natural Products

Notoginsenoside R2

T6S1587

Synonym: 20(S)-Notoginsenoside R2,Ginsenoside Ng-R2

Target: ERK, Beta-Secretase, MEK, BACE, AMPK, AChR, AChE

Isorhamnetin

T2836

Synonym: 3-methylquercetin,3'-Methylquercetin,Isorhamnetol,3'-Methoxyquercetin

Target: MEK, PI3K, Endogenous Metabolite

Synonym: FR148083,L783279,LL-Z 1640-2

Target: VEGFR, FLT, MEK, MAPK, PDGFR, Antibiotic, Src

Recombinant Proteins

Species：

Expression System：

Tag：

Cat No.	Product Name	Species	Expression System
TMPY-04756	MEK1 Protein, Mouse, Recombinant	Mouse	Baculovirus Insect Cells
	MEK1 Protein, Mouse, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 43.6 kDa and the accession number is P31938.
TMPY-04569	MEK1 Protein, Mouse, Recombinant (His & GST)	Mouse	Baculovirus Insect Cells
	MEK1 Protein, Mouse, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 71.3 kDa and the accession number is P31938.
TMPJ-01378	Mp1 Protein, Human, Recombinant (His)	Human	E. coli
	Mitogen-Activated Protein Kinase Scaffold Protein 1 (MAPKSP1) was identified as an interacting protein that belongs to the LAMTOR3 family. MAPKSP1 restricted to late endosomes by the mitogen-activated protein-binding pro...
TMPY-04544	MEK2 Protein, Human, Recombinant (GST)	Human	Baculovirus Insect Cells
	Dual specificity mitogen-activated protein kinase kinase 2, also known as MAP kinase kinase 2, MAPKK2, ERK activator kinase 2, MAPK / ERK kinase 2, MEK2 and MAP2K2, is a member of the protein kinase superfamily, STE Ser/...
TMPY-05095	RAF1 Protein, Human, Recombinant (His & GST)	Human	Baculovirus Insect Cells
	RAF1 gene is the cellular homolog of viral raf gene (v-raf). The encoded protein is a MAP kinase kinase kinase (MAP3K), which functions downstream of the Ras family of membrane associated GTPases to which it binds direct...