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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T63547	MEK1/2-IN-2
	MEK1/2-IN-2 是有效的、ATP 竞争性的 MEK1/2 抑制剂，对野生型 MEK1/2 和一组 MEK1/2 突变细胞表现出同等的抑制效果。
T6152	PD318088	MEK	MAPK
	PD318088 是非 ATP 竞争性的MEK1/2变构抑制剂，是 PD184352 的结构类似物。它在MEK1 活性位点与 ATP 结合位点相邻的区域与 ATP 同时结合，可用于癌症研究。
T2508	Binimetinib ARRY-438162,ARRY-162,MEK162	MEK; Autophagy	Autophagy; MAPK
	Binimetinib (ARRY-162) 是一种可口服的选择性 MEK1/2抑制剂，抑制MEK 的IC50为 12 nM。
T3623	Cobimetinib 可美替尼,考比替尼,RG7420,XL518,GDC-0973	Apoptosis; MEK	Apoptosis; MAPK
	Cobimetinib (GDC-0973) 是一种可口服的 MEK1选择性抑制剂，抑制MEK1的IC50为4.2 nM。
T27242	EF24 EF 24,EF-24,3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone	ERK; MEK; Caspase	Apoptosis; MAPK; Proteases/Proteasome
	EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) 是姜黄素类似物，口服生物利用度高，抗肿瘤作用强。它可增强活化的 Caspase3 及 Caspase9 的水平，并抑制 MEK1 及 ERK 的磷酸化形式的表达。它可以抑制口腔鳞状细胞癌细胞的 MAPK/ERK 信号通路，从而发挥抗肿瘤作用。
T35610	2,5-dimethyl Celecoxib	Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor	Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
	2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂，mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
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 activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activati...
T80543	STE-MEK1(13) ERK Activation Inhibitor Peptide,Ste-MPKKKPTPIQLNP-NH₂	ERK	MAPK
	STE-MEK1(13)（Ste-MPKKKPTPIQLNP-NH2）为一细胞渗透性ERK1/2抑制剂，IC50值为13-30μM，可抑制ERK1/2磷酸化。
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 in mice.
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 broad spectrum of tumor models. RO4927350 inhibits not only ERK1/2 but also MEK1/2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1/2 rather than phospho-ERK1/2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback inc...
T74361	MEK/PI3K-IN-2
	MEK/PI3K-IN-2 (compound 6s) 是一种有效的 MEK/PI3K 抑制剂，其 IC50值分别为 352 nM (MEK1), 107 nM (PI3Kα), 和 137 nM (PI3Kδ)。MEK/PI3K-IN-2 抑制 pAKT 和 pERK1/2 水平。MEK/PI3K-IN-2 对肿瘤细胞具有抗增殖活性。
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-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2].
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-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf/MEK/ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation.
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.
TMIH-0117	Binimetinib-13C-d3
	Binimetinib-13C-d3 是 Binimetinib 的 13C 和氘代化合物。Binimetinib 的 CAS 号为 606143-89-9。Binimetinib 是一种可口服的选择性MEK1/2抑制剂，抑制MEK的IC50为 12 nM。
T74360	MEK/PI3K-IN-1
	MEK/PI3K-IN-1（compound 6r）是一种高效的MEK/PI3K抑制剂，IC50值为124 nM（MEK1）、130 nM（PI3Kα）及236 nM（PI3Kδ）。该化合物能够降低pAKT和pERK1/2的活性，并展现对肿瘤细胞的抗增殖作用。

化合物

Cat.No: T63547

Cat.No: T6152

Target: MEK

Cat.No: T2508

Synonym: ARRY-438162,ARRY-162,MEK162

Target: MEK, Autophagy

Cat.No: T3623

Synonym: 可美替尼,考比替尼,RG7420,XL518,GDC-0973

Target: Apoptosis, MEK

Cat.No: T27242

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

Target: ERK, MEK, Caspase

2,5-dimethyl Celecoxib

Cat.No: T35610

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

Cat.No: T71163

Cat.No: T80543

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

Target: ERK

Cat.No: T31126

Synonym: CX659S,UNII-YG2F04AVMQ,CX 659S

Cat.No: T68459

MEK/PI3K-IN-2

Cat.No: T74361

Cat.No: T61755

Cat.No: T68267

PD0325901-O-C2-dioxolane

Cat.No: T40217

Synonym: PD0325901-O-C2-dioxolane

Binimetinib-13C-d3

Cat.No: TMIH-0117

MEK/PI3K-IN-1

Cat.No: T74360

Cat. No.	Product Name	Target	Signaling Pathways
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 cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...

天然产物

Cat.No: T36954

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