ERK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	ERK1	ERK2	ERK5	ERK	Other
A12824	SCH772984	***	****
A12505	VX-11e		***			GSK3,AURA,CDK2
A15802	DEL-22379			*	*
A11794	Ulixertinib		****
A13420	GDC-0994	***	****
A14119	FR 180204	*	**
A11609	XMD8-92			**
A16232	ERK5-IN-1			**
A11225	Pluripotin (SC-1)	**				RasGAP

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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BAY885

Catalog No. A13765
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ERK5 inhibitor

BAY885 is a novel ERK5 inhibitor. 了解更多

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ERK5-IN-2

Catalog No. A18871
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ERK5 inhibitor

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. 了解更多

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SCH772984

Catalog No. A12824
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ERK 抑制剂

SCH772984是一种新型的ERK1/2特异性抑制剂，IC50分别为4 nM和1 nM。了解更多

Product Citations (6)

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Yajun Li, .et al. Urolithin B suppressed osteoclast activation and reduced bone loss of osteoporosis via inhibiting ERK/NF-??B pathway, Cell Prolif, 2022, Oct;55(10) PMID: 35708050
- Sergey A. Dyshlovoy, .et al. Activity of New Synthetic (2-Chloroethylthio)-1,4-naphthoquinones in Prostate Cancer Cells, Pharmaceuticals, 2021, 14(10), 949
- Sergey A Dyshlovoy, .et al. Marine alkaloid monanchoxymycalin C: a new specific activator of JNK1/2 kinase with anticancer properties, Sci Rep, 2020, Aug 6;10(1):13178 PMID: 32764580
- 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-205 transcription via Ras/Raf/MEK/ERK pathway in breast cancer, FEBS Open Bio, 2017, Aug; 7(8): 1154-1165 PMID: 28781955
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TCS ERK 11e (VX-11e)

Catalog No. A12505
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ERK2 抑制剂

TCS ERK 11e (VX-11e)是一种有效且选择性的细胞外信号相关激酶2（ERK2）抑制剂（ERK2，GSK-3，Aurora激酶A和Cdk2的Ki值分别<2、395、540和852 nM）。有效阻断HT29细胞的增殖（IC50 = 48 nM）。了解更多

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- 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.
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FR 180204

Catalog No. A14119
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ERK 抑制剂

FR 180204是细胞外信号调节激酶（ERK）的新型选择性抑制剂，它可能是类风湿关节炎的潜在新疗法。了解更多

Product Citations (2)

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- Sergey A Dyshlovoy, .et al. Marine alkaloid monanchoxymycalin C: a new specific activator of JNK1/2 kinase with anticancer properties, Sci Rep, 2020, Aug 6;10(1):13178 PMID: 32764580
- 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
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ERK-IN-1

Catalog No. A19080
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RAF/ERK1/2 inhibitor

ERK-IN-1 (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. 了解更多

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- 最新产品
AG-126

Catalog No. A17146
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ERK2 抑制剂

AG-126是一种ERK2抑制剂，它在25-50μM下选择性抑制ERK1（p44）和ERK2（p42）的磷酸化。了解更多

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LY3214996

Catalog No. A16843
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ERK 抑制剂

LY3214996是一种选择性的新型ERK1/2抑制剂，在生化分析中两种酶的IC50为5 nM。它有效抑制BRAF和RAS突变癌细胞系中的细胞磷酸RSK1。了解更多

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AZD0364

Catalog No. A16839
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ERK 抑制剂

AZD0364是一种临床前ERK1/2抑制剂，对ERK2的IC50为0.6 nM。了解更多

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MK-8353 (SCH900353)

Catalog No. A16838
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ERK 抑制剂

MK-8353 (SCH900353)是一种口服生物利用型，选择性和有效的ERK抑制剂，在体外抑制激活的ERK1和ERK2，IC50值分别为23.0 nM和8.8 nM（IMAP激酶测定），以及未激活的ERK2，具有IC50值 0.5 nM（MEK1-ERK2耦合测定）。了解更多

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CC-90003

Catalog No. A16837
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ERK1/2 抑制剂

CC-90003是ERK1/2的不可逆抑制剂，IC50在10-20 nM范围内，在258激酶生化分析中显示出良好的激酶选择性。了解更多

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Tomatidine

Catalog No. A16233
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ERK/Akt/NF-kB 抑制剂

Tomatidine抑制ERK，Akt的磷酸化以及NF-kB的核含量。具有抗炎特性。了解更多

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ERK5-IN-1

Catalog No. A16232
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ERK5 抑制剂

ERK5-IN-1表现出对ERK5的有效抑制，其细胞EC50值为0.19 uM，酶促IC50值为0.087 uM，LRRK2 [G2019S]具有酶促IC50值为0.026uM。了解更多

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APS-2-79

Catalog No. A16231
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KSR/Ras 抑制剂

APS-2-79是RAF通过直接结合KSR活性位点而使MEK磷酸化的拮抗剂。了解更多

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DEL-22379

Catalog No. A15802
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ERK 抑制剂

DEL-22379是一种有效的选择性ERK二聚体抑制剂，可抑制ERK二聚体而不影响ERK磷酸化，阻止由RAS-ERK途径癌基因驱动的肿瘤发生。了解更多

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TMCB

Catalog No. A13977
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CK2/ERK8 抑制剂

MCB抑制酪蛋白激酶2（CK2）和细胞外信号调节激酶8（ERK8/MAPK15）（CK2和ERK8的IC50 = 0.50 uM）。了解更多

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XMD8-92

Catalog No. A11609
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BMK1/ERK5 抑制剂

XMD8-92是一种有效的选择性BMK1/ERK5抑制剂。了解更多

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XMD 17-109

Catalog No. A14090
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ERK5 抑制剂

XMD17-109是一种新型的ERK-5特异性抑制剂，在HEK293细胞中的EC50值为4.2 uM。了解更多

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GDC0994 (Ravoxertinib)

Catalog No. A13420
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ERK1/2 抑制剂

GDC-0994是一种强效选择性Erk1/2抑制剂。GDC-0994抑制ERK磷酸化和ERK介导的信号转导通路的激活。了解更多

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Ulixertinib (BVD-523, VRT752271)

Catalog No. A11794
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ERK1/ERK2 抑制剂

Ulixertinib (BVD-523,VRT752271)是ERK蛋白激酶的吡咯抑制剂。了解更多

Product Citations (1)

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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Pluripotin (SC-1)

Catalog No. A11225
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ERK1/RasGAP 抑制剂

Pluripotin (SC-1)的活性是通过联合抑制RasGAP和ERK1介导的，其Kd值分别为98和212 nM。了解更多

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- Mohammad Azhar, .et al. Rational polypharmacological targeting of FLT3, JAK2, ABL, and ERK1 suppresses the adaptive resistance to FLT3 inhibitors in AML, Blood Adv, 2022, Aug 31 PMID: 36044389