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MAPK

MAPK

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BI-78D3

Catalog No. A13683
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JNK 抑制剂

BI-78D3是一种竞争性JNK（c-Jun N端激酶）抑制剂（IC50 = 280 nM），其选择性是p38α的100倍以上，在mTOR和PI-3K上无活性。 BI 78D3抑制JIP1（JNK相互作用蛋白1）JNK结合（IC50 = 500 nM）。了解更多

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CC-930 (Tanzisertib)

Catalog No. A13564
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JNK 抑制剂

CC-930在蛋白底物c-Jun的JNK依赖性磷酸化中与ATP动力学竞争，并且对JNK的所有同工型均有效（Ki（JNK1）= 44±3 nM，IC50（JNK1）= 61 nM，Ki（JNK2 ）= 6.2±0.6 nM，IC50（JNK2）= 5 nM，IC50（JNK3）= 5 nM），对MAP激酶ERK1和p38a具有选择性，IC50分别为0.48和3.4μM。了解更多

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CEP-1347

Catalog No. A13565
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JNK 抑制剂

CEP-1347是c-jun N末端激酶（JNK）信号传导的抑制剂。它可以挽救经历凋亡的运动神经元（EC50 = 20 nM）。了解更多

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CC-401 hydrochloride

Catalog No. A15037
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JNK 抑制剂

CC-401 hydrochloride是具有潜在抗肿瘤活性的第二代ATP竞争性蒽并吡喃酮c-Jun N末端激酶（JNK）抑制剂。了解更多

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DB07268

Catalog No. A15061
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JNK1 抑制剂

DB07268是一种有效的选择性JNK1抑制剂，IC50值为9 nM。了解更多

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JNK-IN-7

Catalog No. A15136
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JNK 抑制剂

JNK-IN-7是一种相对选择性的JNKs抑制剂（对于JNK1/2/3，IC50 = 1.54/1.99/0.75 nM）；也绑定到IRAK1，PIK3C3，PIP5K3和PIP4K2C。了解更多

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AEG 3482

Catalog No. A11281
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JNK 抑制剂

AEG 3482是Jun激酶（JNK）依赖性细胞凋亡的小分子抑制剂。了解更多

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IQ 3

Catalog No. A16036
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JNK3 抑制剂

IQ 3是一种选择性JNK3抑制剂（JNK3，JNK1和JNK2的Kd值分别为66、240和290 nM）。抑制THP1-Blue细胞中的NF-kB/AP1转录活性（IC50 = 1.4μM）。在体外也抑制TNF-α和IL-6的产生。了解更多

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SU 3327

Catalog No. A16039
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JNK 抑制剂

SU 3327是JNK（c-Jun N-末端激酶）（IC50 = 0.7uM）的选择性抑制剂。显示SU 3327抑制JNK和JIP之间的蛋白质-蛋白质相互作用（IC50 = 239 nM）。了解更多

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JIP-1 (153-163)

Catalog No. A16041
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JNK 抑制剂

JIP-1 (153-163)是c-Jun N末端激酶（JNK）的肽抑制剂，基于JNK相互作用蛋白1（JIP-1）的153-163残基。以微摩尔范围的亲和力与JNK结合，并最小程度地抑制p38和ERK。了解更多

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TCS JNK 6o

Catalog No. A16054
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JNK 抑制剂

TCS JNK 6o是一种ATP竞争性选择性c-Jun N末端激酶（JNK）抑制剂。了解更多

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DTP3

Catalog No. A16059
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JNK 抑制剂

DTP3是选择性GADD45β/ MKK7抑制剂，可抑制癌症选择性NF-kB生存途径。了解更多

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AS601245

Catalog No. A21502
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cell-permeable JNK Inhibitor

AS601245 is a cell-permeable JNK Inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. 了解更多

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TCS JNK 5a

Catalog No. A11969
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JNK 抑制剂 IX

TCS JNK 5a是JNK2和JNK3的高度选择性抑制剂（对于JNK3，JNK2，JNK1和p38β，pIC50值分别为6.7、6.5，<5.0和<4.8）。了解更多

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IQ-1S

Catalog No. A16062
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JNK3 抑制剂

IQ-1S是一种选择性JNK3抑制剂，对于JNK1、2和3的IC50值分别为390、360和87 nM。了解更多

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SR 3576

Catalog No. A16020
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JNK3 抑制剂

SR 3576是一种高效的选择性JNK3抑制剂（IC50 = 7 nM）；表现出比p38高2800倍的选择性。了解更多

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c-JUN peptide

Catalog No. A16045
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JNK 抑制剂

c-JUN peptide是包含人c-Jun的JNK结合（δ）域的33-57位残基的肽。了解更多

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SR 11302

Catalog No. A14950
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AP-1 transcription factor 抑制剂

SR 11302，活化蛋白1（AP-1）转录因子活性的抑制剂，在体内表现出抗肿瘤作用。了解更多

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PNRI-299

Catalog No. A16305
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AP-1 transcription 抑制剂

PNRI-299是一种选择性AP-1转录抑制剂，IC50为20 uM，不影响NF-κB转录（最高200μM）或硫氧还蛋白（最高200μM）。了解更多

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PLX4032 (Vemurafenib)

Catalog No. A10739
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Raf 抑制剂

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。了解更多

Product Citations (11)

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- Lee YJ, .et al. Overexpression of Dock180 and Elmo1 in melanoma is associated with cell survival and migration, Research Square, 2022, April 27th
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Guixin Zhu, .et al. TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination, Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Kudo K, .et al. Cell surface CD63 increased by up-regulated polylactosamine modification sensitizes human melanoma cells to the BRAF inhibitor PLX4032, FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. miR-550a-3-5p acts as a tumor suppressor and reverses BRAF inhibitor resistance through the direct targeting of YAP, Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy, Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. Inhibition of Oncogenic BRAF Activity by Indole-3-Carbinol Disrupts Microphthalmia-Associated Transcription Factor Expression and Arrests Melanoma Cell Proliferation, Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- 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
- Toshinori Sueda, .et al. BRAFV600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells, Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells, Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739
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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。了解更多

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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Dabrafenib (GSK2118436A)

Catalog No. A11381
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Raf 抑制剂

Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。了解更多

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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
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Chenyang He, .et al. Detection of Dabrafenib using Optical Fibre Long Period Grating Sensor Modified with Surface Imprinted Polymers for Dose Detection and Prevention of Cancer Resistance, Clinical and Translational Biophotonics, 2020, TTh3B.2
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- 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
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NVP-BHG712

Catalog No. A10661
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EphB4 抑制剂

NVP-BHG712是EphB4激酶的选择性抑制剂，在体外对EphB4的选择性超过40多种其他激酶（包括FGFR3）。了解更多

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- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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LGX 818 (Encorafenib)

Catalog No. A13226
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Selective B-RAF 抑制剂

LGX 818 (Encorafenib)是一种Raf激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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- 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
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TAK-632

Catalog No. A13323
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pan-RAF 抑制剂

TAK-632是一种有效的泛RAF抑制剂，具有良好的体外活性（BRAF（V600E）IC50，2.4 nM; BRAF（wt），8.3 nM; CRAF，1.4 nM; pMEK（A375）IC50，12 nM; pMEK（HMVII ），49 nM。了解更多

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- Yosi Shamay, .et al. Quantitative Self-Assembly Prediction Yields Targeted Nanomedicines, Nat Mater, 2018, Apr; 17(4): 361-368 PMID: 29403054
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B-Raf-inhibitor 1

Catalog No. A14122
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B-Raf 抑制剂

B-Raf inhibitor 1是有效的选择性B-Raf抑制剂，对A375增殖和A375 p-ERK的细胞IC50分别为0.31 uM和2 nM。了解更多

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CEP-32496 hydrochloride

Catalog No. A15040
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Raf 抑制剂

CEP-32496 hydrochloride是野生型BRAF，V600E突变型BRAF和c-Raf的高效抑制剂，Kd值分别为14 nM，36 nM和39 nM。了解更多

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Dabrafenib Mesylate

Catalog No. A15059
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Raf 抑制剂

Dabrafenib Mesylate是一种新颖，有效和选择性的Raf激酶抑制剂，能够抑制野生型B-Raf，B-RafV600E和c-Raf的激酶活性，IC50值分别为3.2、0.8和5.0 nM。了解更多

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PLX7904

Catalog No. A15855
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Raf 抑制剂

PLX7904是有效的选择性悖论突破性RAF抑制剂。它能够有效抑制突变型BRAF黑色素瘤细胞中ERK1/2的激活，但不能过度激活突变型RAS表达细胞中的ERK1/2。了解更多

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ML 786 dihydrochloride

Catalog No. A11211
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Raf 抑制剂

ML 786 dihydrochloride是一种有效的Raf激酶抑制剂（B-RafV600E，C-Raf和野生型B-Raf的IC50值分别为2.1、2.5和4.2 nM）。了解更多

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HG6-64-1

Catalog No. A16022
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B-Raf 抑制剂

HG6-64-1是有效的选择性B-Raf和突变B-Raf抑制剂；更多信息可以在专利WO 2011090738中找到。了解更多

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LUT014

Catalog No. A19449
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B-Raf inhibitor

LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 . 了解更多

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RAF mutant-IN-1

Catalog No. A19011
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Raf nhibitor

RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF340D/Y341D, B-RAFV600E and B-RAFWT, respectively. 了解更多

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Belvarafenib

Catalog No. A13177
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pan RAF inhibitor

Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. 了解更多

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Regorafenib Hydrochloride

Catalog No. A11546
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VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor

Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. 了解更多

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LY3009120

Catalog No. A16603
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pan RAF inhibitor

LY3009120 is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively. 了解更多

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B-Raf IN 1

Catalog No. A21055
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B-Raf kinase inhibitor

B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM. 了解更多

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B-Raf inhibitor 1 dihydrochloride

Catalog No. A21834
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Raf kinase inhibitor

B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively. 了解更多

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Lifirafenib

Catalog No. A20988
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Raf/EGFR inhibitor

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively. 了解更多

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PLX-4720

Catalog No. A10002
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Raf 抑制剂

PLX-4720是一种有效的，选择性的B-RafV600E抑制剂，无细胞试验中IC50为13 nM，同样有效地作用于c-Raf-1(Y340D和Y341D突变型)，作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。了解更多

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RAF265 (CHIR-265)

Catalog No. A10773
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RAF/VEGFR 抑制剂

RAF265 (CHIR-265)是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，可控制或正常化VEGFR-2，同时抑制B-raf和c-Raf突变以预防癌症。了解更多

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GDC-0879

Catalog No. A10420
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B-Raf 抑制剂

GDC-0879是B-Raf激酶的特异性抑制剂，靶向B-Raf (V600E) (IC50: 0.13 nM)。了解更多

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AZ628

Catalog No. A11063
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Raf 抑制剂

AZ628是一种RAF抑制剂，IC50值：BRAF V600E和野生型CRAF约为30 nM，野生型BRAF约为100 nM。了解更多

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SB590885

Catalog No. A10829
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B-Raf 抑制剂

SB590885是B-Raf激酶的选择性小分子抑制剂，B-Raf和c-Raf的Ki app值分别为0.16和1.72 nM。了解更多

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ZM 336372

Catalog No. A11077
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C-Raf 抑制剂

ZM 336372是有效的ATP Raf-1体外竞争性抑制剂 (IC50 = 70 nM)。了解更多

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Raf265 derivative

Catalog No. A10774
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RAF/VEGFR 抑制剂

Raf265 derivative是Raf265的衍生物，Raf265是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，IC50为5至10μM。了解更多

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GW 5074

Catalog No. A11436
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Raf-1 抑制剂

GW 5074是一种强效、选择性和细胞渗透性的c-Raf1激酶抑制剂。了解更多

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MLN2480 (BIIB-024)

Catalog No. A11240
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pan-Raf 抑制剂

MLN2480 (BIIB-024)是一种口服的Raf激酶抑制剂。了解更多

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PF-04880594

Catalog No. A12739
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RAF 抑制剂

PF-04880594是RAF抑制剂，BRAF/BRAFV599E和c-RAF的IC50值分别为0.19 nM/0.13 nM和0.39 nM。了解更多

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