MAPK
-
Raf inhibitor
Sorafenib Tosylate (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. , Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. , J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. , Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. , J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. , Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. , J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
-
MEK1/2 inhibitor
AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that inhibits growth and survival of MM cells and cytokine-induced osteoclast differentiation. -
Anti-inflammatory agent
Asiatic acid is commonly used in wound healing. Asiatic acid has antioxidant, anti-inflammatory and neuroprotective properties. Asiatic acid derivative synthesis can be used as Anticancer agents; Glycogen phosphorylase inhibitors; Hepatoprotectants.
- Rakhi Mishra, .et al. , Indian J Res Homoeopathy, 2022, Sep 27
-
MEK Inhibitor
AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
-
p38 MAPK inhibitor
Doramapimod (BIRB 796) is a small molecule inhibitor of p38 MAPK,which plays a critical role in regulating the production of proinflammatory cytokines.- Ken Kobayashi, .et al. , Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Junsuke Uwada, .et al. , Biochem Pharmacol, 2020, Oct 22;182:114297 PMID: 33132165
- Perera LMB, .et al. , J Invest Dermatol, 2018, Nov 4. pii: S0022-202X(18)32791-X PMID: 30404019
-
MEK inhibitor
BIX 02189 is a selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Mitsunori Miyazaki, .et al. , FEBS Open Bio, 2017, Mar; 7(3): 424-433 PMID: 28286738
-
MEK1/2 inhibitor
PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.- Sachio Suzuki, .et al. , Cell Chem Biol, 2022, Sep 15;29(9):1446-1464 PMID: 35835118
- Masaru Yoshikawa, .et al. , J Am Chem Soc, 2021, May 5;143(17):6434-6446 PMID: 33890764
-
VEGFR inhibitor
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.- Hasan U, .et al. , Research Square, 2023, 13 Apr
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. , Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. , Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. , Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
-
MEK inhibitor
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.- Tadaaki Nakajima, .et al. , FEBS Open Bio, 2024, Jan;14(1):37-50 PMID: 37953493
- Jan Langkabel, .et al. , bioRxiv, 2021, January 25
- Ryan Clarke, .et al. , Mol Cell, 2021, Jan 21;81(2):226-238.e5 PMID: 33378644
- Tzeng SF, .et al. , FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fukumoto S, .et al. , Acta Histochem, 2018, Feb;120(2):142-150 PMID: 29397960
- Yoshiteru Yano, .et al. , Regenerative Therapy, 2016, 3 (2016) 1-6
-
MEK inhibitor
AZD6244 (Selumetinib) also known as Selumetinib, ARRY142886, AZD-6244 & ARRY-142886 is MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nm.- Chia-Chi Chang, .et al. , Oncotarget, 2016, Jun 7; 7(23): 35270-35283 PMID: 27150057
-
B-Raf inhibitor
GDC-0879 is a specific inhibitor of B-Raf kinase enzyme,targeting B-Raf (V600E) (IC50: 0.13 nM).- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
-
p38 MAPK inhibitor
LY2228820 is a novel and potent p38MAPK inhibitor with potent antiinflammatory activity. -
EphB4 inhibitor
NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- Y Kaibori, .et al. , the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
-
MEK Inhibitor
PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase.- Masayuki Harada, .et al. , Cell Cycle, 2024, Feb;23(3):308-327 PMID: 38461418
- Shota Mizuno, .et al. , Biol Pharm Bull, 2024, 47(1):120-129 PMID: 38171772
- Anna Nakanishi, .et al. , Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Isamu Ogawa, .et al. , Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Hanna Galganska, .et al. , Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Akinobu Nakamura, .et al. , ACS Chem Biol, 2020, Apr 17;15(4):1004-1015 PMID: 32162909
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Kwang Woon Kim, .et al. , Oncotarget, 2019, Sep 24; 10(54): 5645-5659 PMID: 31608140
- Tsai CC, .et al. , Biochim Biophys Acta Mol Cell Res, 2018, Oct 13. pii: S0167-4889(18)30452-X PMID: 30321617
- Kim MH, .et al. , Oncol Rep, 2018, Nov;40(5):2977-2987 PMID: 30226616
- Onozato D, .et al. , Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
-
Raf inhibitor
PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Lee YJ, .et al. , Research Square, 2022, April 27th
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Guixin Zhu, .et al. , Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Kudo K, .et al. , FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. , Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. , Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. , Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Toshinori Sueda, .et al. , Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. , Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739
-
RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
p38 MAPK Inhibitor
SB202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinase.- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Tsai CC, .et al. , Biochim Biophys Acta Mol Cell Res, 2018, Oct 13. pii: S0167-4889(18)30452-X PMID: 30321617
- Jia-Shiuan Tsai, .et al. , PLoS One, 2016, 11(1): e0147011 PMID: 26751215
-
p38 MAPK inhibitor
SB 203580 is a specific inhibitor of p38α and p38β which suppresses downstream activation of MAPKAP kinase-2 and heat shock protein 27.- Masayuki Harada, .et al. , Cell Cycle, 2024, Feb;23(3):308-327 PMID: 38461418
- Dan Mao, .et al. , J Oral Biosci, 2024, Mar;66(1):105-111 PMID: 38182046
- Lei Zhang, .et al. , Stem Cell Reports, 2022, Jun 14;17(6):1428-1441 PMID: 35561683
- Tomoyuki Hashimoto, .et al. , Ann Nucl Med, 2021, Aug 19 PMID: 34410619
- Y Zou, .et al. , BMC Cancer, 2019, Oct 15;19(1):949 PMID: 31615459
- Wei P, .et al. , Cell Death Dis, 2019, Sep 11;10(9):670 PMID: 31511493
- Uwada J, .et al. , Cell Signal, 2019, Nov;63:109358 PMID: 31295519
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Uwada J, .et al. , Cell Signal, 2017, Jul;35:188-196 PMID: 28412413
- ZHIQIANG ZHANG, .et al. , Mol Med Rep. , 2015, Jul;12(1):1499-505. PMID: 25815691
- Choe YJ, .et al. , Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
-
JNK inhibitor
SP600125 is a JNK inhibitor with IC50=40 nM for JNK-1 and JNK-2 and 90 nM for JNK-3.- Peiling Zhang, .et al. , Regen Biomater, 2023, Sep 7:10:rbad079 PMID: 38020237
- Tetsuya Kouno, .et al. , J Biol Chem, 2022, Jul;298(7):102056 PMID: 35605662
- Mark P Roberto, .et al. , Immunity, 2021, Aug 10;54(8):1807-1824.e14 PMID: 34380064
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Yuki Haga, .et al. , PLoS One, 2017, 12(3): e0174153 PMID: 28323861
- Jia-Shiuan Tsai, .et al. , PLoS One, 2016, 11(1): e0147011 PMID: 26751215
- Choe YJ, .et al. , Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
-
p38 MAPK inhibitor
Pexmetinib is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. -
MEK inhibitor
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.- Hanna Galganska, .et al. , Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. , Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
-
p38 MAPK inhibitor
VX-702 is an orally bioavailable inhibitor of p38 MAP kinase that inhibits platelet agonist induced p38 activation (IC50= 4 to 20 nM). -
p38 MAPK inhibitor
VX-745 is a small-molecule inhibitor of MAPK that is reported to be active against several isotypes of p38 MAPK, including p38α, p38βand p38γ . -
MEK Inhibitor
GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Meenu Kesarwani, .et al. , Blood Adv, 2024, Jun 11;8(11):2765-2776 PMID: 38531054
- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
- Tsung-Ming Chang, .et al. , Journal of Biomedical Science, 2022, 29:92
- Nao Yamagishi, .et al. , Biol Pharm Bull, 2022, 45(10):1553-1558 PMID: 36184515
- Hayato Mizuta, .et al. , Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Keisuke Yanagida, .et al. , Dev Cell, 2020, 52 (6), 779-793 PMID: 32059774
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Kanemaru Y, .et al. , Acta Neuropathol Commun, 2019, Jul 25;7(1):119 PMID: 31345255
- Chul Min Park, .et al. , Oncol Lett, 2018, Feb; 15(2): 1758-1762 PMID: 29434871
- Sumi T, .et al. , Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601
- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- 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
-
MEK Inhibitor
TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
-
p38 MAPK inhibitor
PH-797804 is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase.- Yuho Ito, .et al. , Biosci Biotechnol Biochem, 2015, 79(11):1794-801 PMID: 26057585
-
p38 MAPK inhibitor
SKF 86002 Dihydrochloride is inhibitor of p38 MAP kinase (IC50 = 0.1 - 1 uM). Potently inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 uM). -
Raf inhibitor
ML 786 dihydrochloride is a potent Raf kinase inhibitor (IC50 values are 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf respectively). -
p38 MAPK inhibitor
PD 169316 (PD169316) is a selective inhibitor of p38 MAPK.1 that inhibits p38 MAPK with an IC50 of 89 nM.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
-
ERK1/RasGAP Inhibitor
The activity of Pluripotin (SC-1) is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.- Mohammad Azhar, .et al. , Blood Adv, 2022, Aug 31 PMID: 36044389
-
pan-Raf inhibitor
MLN 2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials. -
MEK inhibitor
Refametinib is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. -
SAPKs/JNKs activator
Anisomycin is a pyrrolidine antibiotic, acts as an anti-fungal antibiotic which inhibits Protein Synthesis, also is a potent activator of SAPKs/JNKs.- Ken Kobayashi, .et al. , Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Li Li, .et al. , Cancer Cell Int, 2021, May 13;21(1):260 PMID: 33985519
-
MK2 Inhibitor
PF-3644022 is a potent and selective mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) inhibitor (Ki =3 nM). -
JNK inhibitor
AS 602801 is a novel, orally active, Jun Kinase Inhibitor.- Shuai Zhang, .et al. , J Cell Mol Med, 2021, Apr;25(8):4062-4072 PMID: 33609076
- Kuramoto K, .et al. , Anticancer Res, 2018, Sep;38(9):5093-5099 PMID: 30194154
-
p38 MAPK inhibitor
Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. -
JNK inhibitor
CC-401 is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity.- Jacob Insua‐Rodriguez, .et al. , EMBO Mol Med, 2018, Oct; 10(10): e9003 PMID: 30190333
-
Raf inhibitor
Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial.- Rana Can Baygin, .et al. , Sci Rep, 2024, Jan 2;14(1):286 PMID: 38167959
- Ali Talebi, .et al. , J Exp Clin Cancer Res, 2023, Apr 19;42(1):92 PMID: 37072838
- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Chenyang He, .et al. , Clinical and Translational Biophotonics, 2020, TTh3B.2
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358