MAPK
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Catalog No.
Product Name
Application
Product Information
Product Citation
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FAK inhibitor
NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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VEGFR inhibitor
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. , Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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multi-targeted receptor tyrosine kinases inhibitor
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT. -
VEGFR/FGFR/EGFR inhibitor?€?
SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). -
c-Kit, PDGFR, VEGFR inhibitor
Toceranib is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.- Masaya Igase, .et al. , Can J Vet Res, 2016, Jan; 80(1): 21-31 PMID: 26733729
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VEGFR Antagonist
Buflomedil is a vasoactive agent used to treat peripheral vascular disease. - Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Adi Jacob Berger, .et al. , Nat Cancer, 2021, 2, 1055-1070 PMID: 35121883
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Tzeng SF, .et al. , FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Yuki Kawasaki, .et al. , Sci Rep, 2016, 6: 31502 PMID: 27531070
- Tetsuya Saita, .et al. , Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026
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ALK inhibitor
AP26113 is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. [1][2] AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. [3] -
VEGFR Inhibitor
ZM 323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR). -
CSF-1R inhibitor
GW2580 is a small-molecule, ATP-competitive inhibitor of cFMS kinase.- Ravikanth Maddipati, .et al. , bioRxiv, 2021, February 01
- Liu M, .et al. , Nat Immunol, 2019, Jan 21 PMID: 30664738
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FLT3 inhibitor
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. - (-)-Gallocatechin possesses free radical scavenging ability. It inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells.
- (-)-Catechin gallate is an antioxidant constituent of green tea. At uM concentrations, inhibits VEGF-induced tyrosine phosphorylation.
- MS Islam ,etc. Effect of UV Irradiation on the Nutritional Quality and Cytotoxicity of Apple Juice. Journal of Agricultural and Food Chemistry, 2016, 64(41), 7812-7822.
- MS Islam ,etc. UV-C irradiation as an alternative disinfection technique: Study of its effect on polyphenols and antioxidant activity of apple juice. Innovative Food Science & Emerging Technologies, 2016, 34, 344-351.
- Picropodophyllin (AXL1717) is the first targeted oral small-molecule IGF-1 receptor inhibitor with no effect on the insulin receptor.
- Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
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Src tyrosine kinase inhibitor
Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck. -
TGF-β/ALK5 inhibitor
A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7- Yomogi Shiota Sato, .et al. , Biomed Pharmacother, 2023, Sep;165:115079 PMID: 37413906
- Yomogi Sato, .et al. , Biomed Pharmacother, 2023, Jun;162:114651 PMID: 37030135
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Anna Nakanishi, .et al. , Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Amira Abugomaa, .et al. , Biomed Pharmacother, 2022, Oct;154:113597 PMID: 36030590
- Isamu Ogawa, .et al. , Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Mohamed Elbadawy, .et al. , Authorea, 2020, October 20
- Daichi Onozato, .et al. , Biol Pharm Bull, 2020, 43(7), 1088-1095
- Amira Abugomaa, .et al. , Sci Rep, 2020, Jun 10;10(1):9393 PMID: 32523078
- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
- Kondo S, .et al. , Biol Open, 2020, Jan 9;9(1) PMID: 31919043
- Onozato D, .et al. , Drug Metab Dispos, 2018, Nov;46(11):1572-1580 PMID: 29615438
- Usui T, .et al. , Curr Protoc Toxicol, 2018, Feb 21;75:22.6.1-22.6.7 PMID: 29512123
- Kondo S, .et al. , Inflamm Res, 2018, Dec;67(11-12):975-984 PMID: 30317465
- Onozato D, .et al. , Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Tatsuya Usui, .et al. , Cancer Sci, 2017, Dec; 108(12): 2383-2392 PMID: 29024204
- Tatsuya Usui, .et al. , Physiol Rep, 2017, Jun; 5(12): e13318 PMID: 28642339
- Tatsuya Usui, .et al. , Stem Cells Int, 2016, 2016: 7053872 PMID: 28119740
- MLR 1023 is a selective allosteric activator of Lyn kinase (EC50 = 63 nM)
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ABL/c-KIT dual kinase inhibitor
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor. -
VEGFR Inhibitor
SU 5416 is an inhibitor of vascular endothelial growth factor receptor (VEGFR) that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET.- Ayaka Kojima, .et al. , Xenobiotica, 2022, Jul;52(7):669-675 PMID: 36251932
- Guangyan Zhang, .et al. , Cardiovasc Drugs Ther, 2022, Feb 14 PMID: 35157168
- Michel R. Corboz, .et al. , Eur J Pharmacol, 2022, 916: 174484 PMID: 34508752
- Avner Adini, .et al. , Am J Respir Cell Mol Biol, 2020, Jul 14 PMID: 32663413
- Yin Kang, .et al. , Am J Physiol Heart Circ Physiol, 2020, Apr 1;318(4):H853-H866 PMID: 32108526
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CSF-1R Inhibitor
GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1. -
multi-targeted tyrosine kinase inhibitor
Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively. -
c-Met inhibitor
c-met-IN-1 (compound 16) is a potent and selective c-Met inhibitor, with IC50 of 1.1 nM, with antitumor activity. -
Eph receptor inhibitor
ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor. -
EGFR inhibitor
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. -
c-MET inhibitor
LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).- Ji-Eun Kim, .et al. , Immunity, 2022, Dec 13;55(12):2300-2317 PMID: 36473468
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PKC inhibitor
PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity. -
CSF1R inhibitor
JNJ-28312141 is an orally active CSF1R inhibitor (Colony-stimulating factor-1 receptor, CRF1R) and also a FLT3 inhibitor. CSF1R is expressed by many tumors and is a growth factor for macrophages and mediates osteoclast differentiation. JNJ-28312141 represents a new agent with potential therapeutic activity in acute myeloid leukemia and in settings where CSF-1-dependent macrophages and osteoclasts contribute to tumor growth and skeletal events. -
VEGFR inhibitor
NVP-BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation. -
JAK2/FLT3 inhibitor
Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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Src Inhibitor
PP1 is a potent inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl -
ALK2 inhibitor
DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).- Teresa Rayon, .et al. , Science, 2020, Sep 18;369(6510):eaba7667 PMID: 32943498