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Raf inhibitor
索拉非尼酯（Nexavar）是一种新型小分子抑制剂，能够抑制多种酪氨酸蛋白激酶（VEGFR 和 PDGFR）以及 RAF/MEK/ERK 信号通路，对 Raf-1、野生型 BRAF 和 V599E 突变型 BRAF 的半抑制浓度（IC50）分别为 6、22、38 nM。- Arda Kipcak, .et al. , Mol Biol Rep, 2024, Jul 13;51(1):799 PMID: 39001931
- 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
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MEK1/2 inhibitor
AS703026 是一种新型、选择性、口服生物利用度的 MEK1/2 抑制剂，它能抑制 MM 细胞的生长和存活，以及细胞因子诱导的破骨细胞分化。 -
MEK Inhibitor
AZD8330 是一种新型、选择性的、非ATP竞争性的 MEK 1/2 抑制剂，其 IC50 为 7 nM。目前处于 第一阶段 临床试验。- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
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p38 MAPK inhibitor
Doramapimod（BIRB 796）是一种小分子抑制剂，针对 p38 MAPK 进行抑制，后者在调节促炎细胞因子的产生中起着关键作用。- Vincent de Laat, .et al. , Nat Commun, 2024, Oct 2;15(1):8540 PMID: 39358362
- 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
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MEK inhibitor
BIX 02189 是一种选择性的双重 MEK5 和 ERK5（或 BMK1）激酶抑制剂，其 IC50 值分别为 MEK5 1.5 nM、ERK5 59 nM、TGFbR1 580 nM 以及其他密切相关激酶 >6200 nM。- 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
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MEK1/2 inhibitor
PD184352（CI-1040）是一种ATP非竞争性的MEK1/2抑制剂，在细胞测试中的IC50为17 nM，对MEK1/2的选择性比MEK5高出100倍。目前处于临床试验第二阶段。- 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
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VEGFR inhibitor
Regorafenib（BAY 73-4506）是一种多激酶抑制剂，其IC50分别为17、40和69 nM的c-KIT、VEGFR2、B-Raf。Regorafenib（BAY 73-4506）是一种口服生物可用的多激酶抑制剂，针对肿瘤及其血管系统。- 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
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MEK inhibitor
PD0325901 是一种 MEK 抑制剂，并且与 ATP 非竞争性，对激活的 MEK1 和 MEK2 的 Kiapp 为 1 nM。- 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
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MEK inhibitor
AZD6244（Selumetinib），也被称为Selumetinib、ARRY142886、AZD-6244和ARRY-142886，是一种MEK 1/2 抑制剂，其GI50值在14到50纳摩尔之间。- Chia-Chi Chang, .et al. , Oncotarget, 2016, Jun 7; 7(23): 35270-35283 PMID: 27150057
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B-Raf inhibitor
GDC-0879 是一种特异性的 B-Raf 激酶抑制剂，针对 B-Raf (V600E)（IC50：0.13 nM）。- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
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p38 MAPK inhibitor
LY2228820 是一种新型且强效的 p38MAPK 抑制剂，具有强大的抗炎活性。 -
EphB4 inhibitor
NVP-BHG712 是一种选择性的 EphB4 激酶 抑制剂，在体外对 EphB4 的选择性优于40多种其他激酶，包括 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
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MEK Inhibitor
PD98059 是一个同等效力的芳香烃受体拮抗剂和丝裂原活化蛋白激酶激酶抑制剂。- 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
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Raf inhibitor
PLX4032（Vemurafenib），也被称为 RG7204、Vemurafenib、R7204；RO5185426。PLX4032 是一种 B-raf 抑制剂，其 IC50 为 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
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RAF/VEGFR Inhibitor
RAF265（CHIR-265）是一种口服、高度选择性的RAF和VEGFR激酶抑制剂，用于控制或正常化VEGFR-2，并同时抑制B-raf和c-Raf突变以预防癌症。 -
RAF/VEGFR Inhibitor
Raf265衍生物是Raf265的一个衍生物，它是一种口服的、高度选择性的RAF和VEGFR激酶抑制剂，其IC50值为5至10微摩尔。 -
p38 MAPK Inhibitor
SB202190 是一种高度选择性、高效且能渗透细胞的 p38 MAP激酶 抑制剂。- 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
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p38 MAPK inhibitor
SB 203580 是一种特异性抑制剂，针对 p38α 和 p38β，能够抑制下游的 MAPKAP kinase-2 和 heat shock protein 27 的激活。- Jung Hyun Kang, .et al. , Food Sci Biotechnol, 2024, 33: 3629-3637
- 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
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JNK inhibitor
SP600125 是一种 JNK 抑制剂，对 JNK-1 和 JNK-2 的 IC50 为 40 nM，对 JNK-3 的 IC50 为 90 nM。- 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
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p38 MAPK inhibitor
Pexmetinib 是一种强效的细胞因子合成抑制剂，通过双重抑制 p38 丝裂原活化蛋白激酶（MAPK） 和 Tie2/Tek 受体酪氨酸激酶 来发挥作用。 -
MEK inhibitor
U0126-EtOH 是一种同时抑制 MEK1 和 MEK2 的抑制剂，其半抑制浓度（IC50）分别为 72 nM 和 58 nM。- Ji Wang, .et al. , Acta Pharmacol Sin, 2024, Nov 20 PMID: 39567750
- 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
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p38 MAPK inhibitor
VX-702 是一种口服生物可利用的 p38 MAP激酶 抑制剂，能够抑制血小板激动剂诱导的 p38 激活（IC50= 4 至 20 nM）。 -
p38 MAPK inhibitor
VX-745 是一种小分子抑制剂，针对 MAPK（丝裂原活化蛋白激酶）具有活性，据报道它能够抑制多种 p38 MAPK 异构体，包括 p38α、p38β 和 p38γ。 -
MEK Inhibitor
GSK1120212（JTP-74057）强烈抑制了MEK1和MEK2激酶的活性，而不是其他98种激酶的活性。- Song Han, .et al. , Neoplasia, 2025, Jan:59:101070 PMID: 39541736
- 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
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MEK Inhibitor
TAK-733 是一种口服生物利用度高的小分子抑制剂，针对 MEK1 和 MEK2（MEK1/2），具有潜在的抗肿瘤活性。- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
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p38 MAPK inhibitor
PH-797804 是一种 双芳基吡啶酮 抑制剂，针对 p38 丝裂原活化蛋白（MAP）激酶。- Yuho Ito, .et al. , Biosci Biotechnol Biochem, 2015, 79(11):1794-801 PMID: 26057585
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p38 MAPK inhibitor
SKF 86002 Dihydrochloride 是 p38 MAP 激酶的抑制剂（IC50 = 0.1 - 1 uM）。强效抑制人单核细胞中 LPS 诱导的 IL-1 和 TNF-α 生产（IC50 = 1 uM）。 -
Raf inhibitor
ML 786 二盐酸盐是一种强效的 Raf激酶抑制剂（IC50值分别为B-RafV600E、C-Raf和野生型B-Raf的2.1、2.5和4.2 nM）。 -
p38 MAPK inhibitor
PD 169316（PD169316）是一种选择性的 p38 MAPK 抑制剂，其对 p38 MAPK 的抑制作用的 IC50 为 89 nM。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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ERK1/RasGAP Inhibitor
Pluripotin（SC-1）的活性是通过同时抑制 RasGAP 和 ERK1 来介导的，其 Kd 值分别为 98 nM 和 212 nM。- Mohammad Azhar, .et al. , Blood Adv, 2022, Aug 31 PMID: 36044389
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MEK inhibitor
Refametinib 是一种强效的、非ATP竞争性的、高度选择性的 MEK1 和 MEK2 抑制剂，其半抑制浓度（IC50）分别为19 nM和47 nM。 -
JNK inhibitor
AS 602801 是一种新型、口服活性的 Jun Kinase 抑制剂。- 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
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p38 MAPK inhibitor
Skepinone-L 是一种选择性的 p38 丝裂原活化蛋白激酶 抑制剂。 -
JNK inhibitor
CC-401 是一种第二代 ATP 竞争性 anthrapyrazolone c-Jun N terminal kinase (JNK) 抑制剂，具有潜在的抗肿瘤活性。- Jacob Insua‐Rodriguez, .et al. , EMBO Mol Med, 2018, Oct; 10(10): e9003 PMID: 30190333
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Raf inhibitor
Dabrafenib 是一种强效且选择性的 B-RAF 蛋白激酶 抑制剂，针对携带 V600E 突变，目前处于临床试验阶段。- 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
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MEK1 inhibitor
Cobimetinib（GDC-0973，RG7420）是一种强效且高度选择性的 MEK1 抑制剂，其 IC50 为 4.2 nM，对 MEK1 的选择性超过 MEK2 的100倍以上，并且在针对100多种丝氨酸-苏氨酸和酪氨酸激酶的测试中未显示出显著抑制作用。- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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MEK1/2 inhibitor
MEK162 (ARRY-438162) 是一种强效、选择性的、非竞争性 ATP 抑制剂，针对 MEK1/2。- S Shahab, .et al. , J Neuropathol Exp Neurol, 2020, Jul 1;79(7):746-753
- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
- Alquezar C, .et al. , Eur Neuropsychopharmacol, 2015, Mar;25(3):386-403 PMID: 25624003
