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AKT 抑制剂
MK-2206 2HCl 是一种高度选择性的 Akt1/2/3 抑制剂,其 IC50 分别为 8 nM/12 nM/65 nM。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Yi-Ru Pan, .et al. , Int J Biol Sci, 2023, May 21;19(9):2772-2786 PMID: 37324940
- Giorgio Caratti, .et al. , EMBO Rep, 2023, Feb 6;24(2):e55363 PMID: 36520372
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Ali Nasrollahzadeh, .et al. , Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Rona Aviram, .et al. , PLoS Biol, 2021, Dec 30;19(12):e3001492 PMID: 34968386
- Cristina Rosell??-Busquets, .et al. , Front Mol Neurosci, 2020, 13: 56 PMID: 32317932
- Dai-Chi Liu, .et al. , eNeuro, 2020, Mar 27;7(2):ENEURO.0438-19.2020 PMID: 32161037
- Nishihama K, .et al. , Metabolism, 2018, May;82:88-99 PMID: 29366755
- J Wei, .et al. , bioRxiv, 2018, 2018
- Joo Sang Lee, .et al. , Nat Commun, 2018, 9: 2546 PMID: 29959327
- Wan-Ting Hu, .et al. , Am J Cancer Res, 2018, 8(9): 1739-1751 PMID: 30323967
- Angela M. Gocher, .et al. , J Biol Chem, 2017, Aug 25; 292(34): 14188-14204 PMID: 28634229
- Kusuyama J, .et al. , Biochem J, 2017, Oct 5;474(20):3421-3437 PMID: 28887384
- Pi-Lin Sung, .et al. , Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Mikaël M. Martino, .et al. , Nat Commun, 2016, 7: 11051 PMID: 27001940
- Dominik Schulz, .et al. , Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
- Jewett KA, .et al. , J Neurochem., 2015, Oct;135(2):226-33 PMID: 26250624
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GSK-3 抑制剂
CHIR99021 是一种氨基嘧啶衍生物,能够抑制 GSK3α 和 GSK3β,其 IC50 值分别为 10 nM 和 6.7 nM。- Peilin Li, .et al. , Ecotoxicol Environ Saf, 2024, Dec:288:117330 PMID: 39571255
- Peilin Li, .et al. , Stem Cell Res Ther, 2024, Aug 26;15(1):269 PMID: 39183353
- Andreea Manole, .et al. , Cell Rep, 2023, Dec 26;42(12):113466 PMID: 38039131
- Claudia Z Han, .et al. , Immunity, 2023, Sep 12;56(9):2152-2171 PMID: 37582369
- Eric Lian, .et al. , STAR Protoc, 2023, May 22;4(2):102314 PMID: 37220001
- Tomoki Murata, .et al. , Int Immunol, 2023, Apr 13 PMID: 37052267
- Shunsuke Murakami, .et al. , Regen Ther, 2022, Nov 25;21:574-583 PMID: 36475025
- Adam Pietrobon, .et al. , Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Takayuki Miyoshi, .et al. , J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Tomoki Kamatani, .et al. , Inflamm Regen, 2022, Feb 2;42(1):4 PMID: 35105370
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Otsuka R, .et al. , Sci Rep, 2020, Jan 14;10(1):224 PMID: 31937817
- Yu Huang, .et al. , Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
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Gamma secretase 抑制剂
DAPT (GSI-IX) 是一种 γ-分泌酶 抑制剂,它能在人类原代神经细胞培养中降低 Aβ40 和 Aβ42 的水平,其 IC50 值分别为针对总 Aβ 的 115 nM 和针对 Aβ42 的 200 nM。- Kubra Telli, .et al. , Turkish Journal of Biochemistry, 2023, February 6
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
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Gamma-secretase 抑制剂
RO4929097 是一种口服生物利用度高的小分子伽马分泌酶(GS)抑制剂,其 IC50 为 4 nM。- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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p38 MAPK 抑制剂
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 抑制剂
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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TGF-beta/Smad 抑制剂
SB 431542 是一种强效且特异性的转化生长因子-β超家族类型 I ALK 受体 ALK4、ALK5 和 ALK7 的抑制剂。- Sebastian Held, .et al. , Cell Rep, 2025, Jan 28;44(1):115107 PMID: 39709600
- Yuri Nagaoka, .et al. , Arch Biochem Biophys, 2024, Jan:751:109824 PMID: 37984759
- Huong Pham, .et al. , Biotechnol Bioprocess Eng, 2020, ID: 222137835
- Tamara Chamberlin, .et al. , FASEB J, 2020, Jun;34(6):8611-8624 PMID: 32359100
- Satoshi Endo, .et al. , Nutr Res, 2019, 4 November
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Gamma-secretase 抑制剂
Semagacestat(LY450139)是一种针对Aβ42、Aβ40和Aβ38的γ-分泌酶抑制剂,其IC50分别为10.9 nM、12.1 nM和12.0 nM。Semagacestat还能抑制Notch信号传导,其IC50为14.1 nM。- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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HDAC 抑制剂
Valproic acid sodium salt (Sodium Valproate) 是一种 HDAC 抑制剂,其 IC50 在 0.5 至 2 mM 范围内,同时抑制 HDAC1(IC50,400 μM),并诱导 HDAC2 的蛋白酶体降解。 -
HDAC 抑制剂
Trichostatin A(TSA)抑制 HDACs 1, 3, 4, 6 和 10,其 IC50 值约为 20 nM。- Thibaud Reyser, .et al. , Pharmaceutics, 2023, Oct 10;15(10):2440 PMID: 37896200
- Goudreault M, .et al. , Research Square, 2021, 22 Nov
- Hiroyuki Imuta, .et al. , Heart Vessels, 2020, Jul 16 PMID: 32676696
- M??ndez-Blanco C, .et al. , Cancers (Basel), 2019, Dec 9;11(12). pii: E1984 PMID: 31835431
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PARP 抑制剂
XAV 939 是一种 TNKS 抑制剂(对于 TNKS1 和 TNKS2 的 IC50 值分别为 0.011 和 0.004 微米)。- Shizu Aikawa, .et al. , EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- Mikaël M. Martino, .et al. , Nat Commun, 2016, 7: 11051 PMID: 27001940
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ROCK 抑制剂
Y-27632 是一种 Rho-Associated Coil Kinase (ROCK) 抑制剂,能够提高人类胚胎干细胞(hESCs)的克隆效率。- Peilin Li, .et al. , Ecotoxicol Environ Saf, 2024, Dec:288:117330 PMID: 39571255
- Takaaki Fujimura, .et al. , NPJ Precis Oncol, 2024, Nov 17;8(1):264 PMID: 39551860
- Ayumi Horikawa, .et al. , In Vitro Cell Dev Biol Anim, 2024, Nov 15 PMID: 39546193
- Giovanni Tosi, .et al. , Nat Commun, 2024, Sep 18;15(1):8214 PMID: 39294175
- Christina Zarouchlioti, .et al. , EBioMedicine, 2024, Oct:108:105328 PMID: 39278108
- Kyunghyun Park, .et al. , Advanced Therapeutics, 2024, 7(6)
- Maude Hamilton, .et al. , Biol Open, 2024, Jan 15; 13(1): bio059919 PMID: 38252116
- Oliver Podmanicky, .et al. , Hum Mol Genet, 2024, Mar 1; 33(5): 435-447 PMID: 37975900
- Masayuki Fukumoto, .et al. , PLoS One, 2024, Dec 5;19(12):e0313312 PMID: 39636897
- Johannes Robert Fleischer, .et al. , Mol Cancer, 2023, Jan 24;22(1):17 PMID: 36691028
- Vignesh Jayarajan, .et al. , Cells, 2023, Jan 17;12(3):346 PMID: 36766688
- Giulia Bastianello, .et al. , Cell Rep, 2023, Dec 26;42(12):113555 PMID: 38088930
- Charlotte Phelps, .et al. , Sci Rep, 2023, Oct 23;13(1):18062 PMID: 37872186
- Mathilde Meyenberg, .et al. , Sci Rep, 2023, Aug 26;13(1):13964 PMID: 37633982
- Yu-Ting Wu, .et al. , J Biomed Sci, 2023, Aug 21;30(1):70 PMID: 37605213
- Heming Ning, .et al. , In Vitro Cell Dev Biol Anim, 2023, Jun;59(6):410-419 PMID: 37405627
- Eric Lian, .et al. , STAR Protoc, 2023, May 22;4(2):102314 PMID: 37220001
- Stephanie T Pohl, .et al. , Methods Mol Biol, 2023, 2584:371-387 PMID: 36495461
- Charlotte Phelps, .et al. , Am J Physiol Cell Physiol, 2023, Mar 1;324(3):C787-C797 PMID: 36689673
- Shunsuke Murakami, .et al. , Regen Ther, 2022, Nov 25;21:574-583 PMID: 36475025
- Sergio Pedraza-Arevalo, .et al. , STAR Protoc, 2022, Aug 30;3(3):101656 PMID: 36092820
- Ji-Hyun Lee, .et al. , Cell Stem Cell, 2022, May 5; 29(5): 826-839 PMID: 35523142
- Adam Pietrobon, .et al. , Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Sarkawt Hamad, .et al. , Stem Cell Res Ther, 2022, Jun 11;13(1):251 PMID: 35690874
- Stasia Krishtul, .et al. , Polym Adv Technol, 2022, 33( 11): 3842-3852
- Peter T Ruane, .et al. , Hum Reprod, 2022, Apr 1;37(4):777-792 PMID: 35079788
- Takayuki Miyoshi, .et al. , J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Ana-Maria Cujba, .et al. , Cell Rep, 2022, Mar 1;38(9):110425 PMID: 35235779
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Antigoni Gogolou, .et al. , Curr Protoc, 2021, Jun;1(6):e137 PMID: 34102038
- Tiago De Oliveira, .et al. , Cancers (Basel), 2021, Mar 2;S2451-9456(21)00095-7 PMID: 33671096
- Denise Muller, .et al. , BMC Med, 2021, Nov 16;19(1):300 PMID: 34781947
- Ayumi Horikawa, .et al. , PloS one, 2021, Jul 12;16(7):e0254373 PMID: 34252142
- Hayato Mizuta, .et al. , Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Scott Bell, .et al. , Stem Cell Reports, 2021, Jul 13;16(7):1749-1762 PMID: 34214487
- Shenyang Li, .et al. , J Cell Mol Med, 2020, Dec 20;25(2):1207-1220 PMID: 33342057
- Takao FUCHIGAMI, .et al. , J Appl Oral Sci, 2020, 28: e20190558 PMID: 32348439
- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
- Yu Huang, .et al. , Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
- XinYan, .et al. , Stem Cell Res, 2019, May 17 PMID: 31141763
- Daniela F. Duarte Campos, .et al. , J Biomed Mater Res A, 2019, April 22 PMID: 31012205
- Scott Bell, .et al. , Am J Hum Genet, 2019, May 2;104(5):815-834 PMID: 31031012
- Ooi J, .et al. , Cell Rep, 2019, Feb 26;26(9):2494-2508 PMID: 30811996
- Scott Bell, .et al. , Stem Cell Reports, 2018, Jul 10; 11(1):183-196 PMID: 29937144
- Christina Zarouchlioti, .et al. , Am J Hum Genet, 2018, Apr 5; 102(4): 528-539 PMID: 29526280
- Ai Takemoto, .et al. , Sci Rep, 2017, 7: 42186 PMID: 28176852
- Scott Bell, .et al. , Stem Cells Transl Med, 2017, Mar; 6(3): 886-896 PMID: 28170165
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Wnt/beta-catenin 抑制剂
ICG-001 是一种特定的 Wnt/β-catenin 信号通路抑制剂,它抑制 β-catenin/环状AMP反应元件结合(CREB)蛋白转录(IC50=3 微米)。- Hong Gao, .et al. , Sci Rep, 2024, Oct 15;14(1):24182 PMID: 39406776
- Yun-Sheng Chen, .et al. , Research Square, 2024, August 16th
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Seonmin Choi, .et al. , Yonsei Med J, 2021, Nov;62(11):1042-1051 PMID: 34672138
- Jasper C.Munro, .et al. , Livest Sci, 2019, 229 (2019) 159-169
- Kim JH, .et al. , Cell Rep, 2019, May 14;27(7):2105-2118.e5 PMID: 31091449
- Yamaoka R, .et al. , J Surg Oncol, 2018, Sep;118(4):664-674 PMID: 30196535
- Aida Y, .et al. , In Vitro Cell Dev Biol Anim, 2018, Jun;54(6):468-476 PMID: 29785536
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CK2 抑制剂
CX-4945 是一种有效且选择性的口服生物利用度高的小分子抑制剂,专门针对 CK2,能够抑制人类脐静脉内皮细胞迁移、管状形成,并阻断 CK2-依赖的癌细胞中低氧诱导因子 1 alpha (HIF-1α) 的转录。- Michael Ohene-Nyako, .et al. , ASN Neuro, 2023, Jan-Dec;15:17590914231158218 PMID: 36890725
- Wenjie Huang, .et al. , Am J Pathol, 2023, May;193(5):567-578 PMID: 37080661
- Xixi Zhao, .et al. , Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
- Janeen H. Trembley, .et al. , Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
- Tianzhi Huang, .et al. , Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- M Afzal, .et al. , Molecular and Cellular Biochemistry, 2020, 470, pages131-143
- Zaman MS, .et al. , Biometals, 2019, Oct 3 PMID: 31583500
- Fukumoto Y, .et al. , Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
- Fukumoto Y, .et al. , Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
- ST Ribeiro, .et al. , Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
- Valentina Gandin, .et al. , Nat Commun, 2016, 7: 11127 PMID: 27040916
- Ampofo E, .et al. , Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
- Emmanuel Ampofo, .et al. , Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
- Emmanuel Ampofo, .et al. , Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
- A. Margarida Gomes, .et al. , Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792
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PI3K 抑制剂
Wortmannin 是一种强效、选择性、细胞渗透性和不可逆的磷脂酰肌醇3激酶(PI 3-kinase)抑制剂(IC50 = 2 - 4 nM),同时也强效抑制polo样激酶1(PLK1)(IC50 = 5.8 nM)。- Weili Chen, .et al. , Communications Biology, 2024, 7:488
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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γ-secretase 抑制剂
YO-01027 是一种二肽类 γ-分泌酶抑制剂,用作抗阿尔茨海默病药物。- Weijun Zhang, .et al. , Stem Cell Rev Rep, 2023, Jan 7 PMID: 36609902
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Gamma secretase 抑制剂
LY-411575 是一种选择性的、细胞渗透性的、小分子 伽玛分泌酶抑制剂。- Haiwen Yu, .et al. , Immunol Invest, 2023, Feb;52(2):241-255 PMID: 36562737
- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Zhang ZH, .et al. , APMIS, 2019, Jul 5 PMID: 31274210
- Bo Pang, .et al. , Biosci Rep, 2018, Dec 21; 38(6): BSR20181922 PMID: 30473538
- Shuo Li, .et al. , Int Immunopharmacol, 2018, Oct;63:129-136 PMID: 30086535
- Jiang BC, .et al. , Viral Immunol, 2017, Sep;30(7):522-532 PMID: 28410452
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ALK 抑制剂
LDN193189 是一种高效的小分子 BMP 抑制剂,能够抑制 BMP 类型 I 受体 ALK2(IC50:5 nM)、ALK3(IC50:30 nM)和 ALK6(TGFβ1/BMP 信号传导)以及随后的 SMAD 磷酸化。- Lei Wang, .et al. , Theriogenology, 2023, Feb;197:167-176 PMID: 36525856
- Trang Thi Huyen Dang, .et al. , Mol Cell Biochem, 2021, May;476(5):2085-2097 PMID: 33517521
- Shizu Aikawa, .et al. , EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- HIROTAKA SOMEYA, .et al. , Int J Mol Med, 2015, May; 35(5): 1169-1178 PMID: 25739055
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Akt 抑制剂
GDC-0068 是一种选择性的、ATP竞争性的、全面的Akt抑制剂,它针对Akt1、2和3,在无细胞试验中的IC50值分别为5、18和8 nM。 -
γ-secretase 抑制剂
PF-03084014 是一种可逆的、选择性的 γ-secretase 抑制剂,其 IC50 值为 6.2 nM。 -
GSK-3 抑制剂
Tideglusib 是一种 GSK-3 抑制剂,目前正在进行第二阶段临床试验,用于治疗 阿尔茨海默病 和 进行性核上性麻痹。- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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ALK5 抑制剂
RepSox(SJN 2511)是TGF-β类型I受体ALK5的选择性抑制剂(IC50值分别为ALK5自磷酸化和ALK5结合时为0.004和0.023 μM)。- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Xu H, .et al. , Cancer Lett, 2020, Mar 1;472:151-164 PMID: 31846689
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AMPK 抑制剂
BML-275 是一种可渗透细胞的吡唑并嘧啶化合物,已被证明是 AMP激活的蛋白激酶(AMPK) 和 脂肪酸合成酶 抑制剂。- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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TGF-β/ALK5 抑制剂
A83-01 是一种选择性抑制剂,针对转化生长因子-β型I受体ALK5、Nodal受体ALK4以及Nodal受体ALK7。- Masayuki Fukumoto, .et al. , PLoS One, 2024, Dec 5;19(12):e0313312 PMID: 39636897
- Raghda Shahin, .et al. , Drug Metabolism and Pharmacokinetics, 2024, 4 December
- Kyunghyun Park, .et al. , Advanced Therapeutics, 2024, 7(6)
- Yuko Nagashima, .et al. , Research Square, 2024, June 4th
- Shota Mizuno, .et al. , Biol Pharm Bull, 2024, 47(1):120-129 PMID: 38171772
- Andreea Manole, .et al. , Cell Rep, 2023, Dec 26;42(12):113466 PMID: 38039131
- Claudia Z Han, .et al. , Immunity, 2023, Sep 12;56(9):2152-2171 PMID: 37582369
- 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
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γ-secretase 抑制剂
BMS 299897 是一种口服活性强的 γ-分泌酶抑制剂(IC50 = 12 nM)。在体外抑制 Aβ40 和 Aβ42 的形成(IC50 值分别为 7.4 和 7.9 nM),并在体内减少大脑、血浆和脑脊液中的 Aβ。- Chao Liu, .et al. , Cell Death Differ, 2018, Apr; 25(4): 661-676 PMID: 29238071
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YAP 抑制剂
Verteporfin 是一种小分子,能够抑制 TEAD、YAP 关联以及 YAP 引起的肝脏过度生长。它还是一种强效的第二代光敏剂,源自卟啉。- Shruti Vig, .et al. , Cancer Drug Resist, 2024, Sep 21:7:35 PMID: 39403604
- Yu Ren, .et al. , Eur J Med Res, 2024, May 30;29(1):303 PMID: 38812041
- Po-Ju Lee, .et al. , J Exp Clin Cancer Res, 2022, Aug 20;41(1):254 PMID: 35986369
- Ling-Yan Liu, .et al. , Int J Mol Med, 2020, Dec;46(6):2235-2250 PMID: 33125123
- Wang Y, .et al. , Toxicol Appl Pharmacol, 2019, 2019 Dec 5;387:114852 PMID: 31812773
- Abe T, .et al. , Toxicol Sci, 2018, Oct 1;165(2):408-419 PMID: 29893953
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Wnt 抑制剂
IWR-1-endo 是一种强效的 Wnt 反应抑制剂,能够阻断基于细胞的 Wnt/β-catenin 通路报告响应,其 IC50 值为 180 nM。Wnt 蛋白绑定到细胞表面的受体上,启动信号级联,导致 β-catenin 激活基因转录。- Charles A.Herring, .et al. , Cell, 2022, Oct 27;S0092-8674(22)01258-2 PMID: 36318921
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GSK-3 抑制剂
LY2090314 是一种强效的糖原合成酶激酶-3(GSK-3)抑制剂,GSK-3 在许多途径中扮演重要角色,包括蛋白质合成的启动、细胞增殖、细胞分化和凋亡。- Yuki Shimizu, .et al. , NPJ Precis Oncol, 2022, Mar 17;6(1):16 PMID: 35301419
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Smoothened 抑制剂
PF-5274857 是一种新型的 Smo 拮抗剂,它能特异性地与 Smo 结合,其 K(i) 为 4.6 ± 1.1 nmol/L,并且能完全阻断细胞中下游基因 Gli1 的转录活性,其 IC(50) 为 2.7 ± 1.4 nmol/L。 -
PORCN 抑制剂
LGK974 是一种高效、选择性强且口服生物利用度高的Porcupine抑制剂(Wnt信号拮抗剂),在Wnt信号报告基因检测和Porcupine结合检测中的IC50值均小于1 nM。- Uxia Gurriaran-Rodriguez, .et al. , Sci Adv, 2024, Dec 13;10(50):eado5914 PMID: 39661666
- Sho Tsukamoto, .et al. , Development, 2023, Aug 1;150(15):dev201734 PMID: 37539462
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- A-Ri Cho, .et al. , Sci Rep, 2022, Apr 29;12(1):7013 PMID: 35487932
- Yang JM, .et al. , Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
- E Lemieux, .et al. , Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543
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GSK3 抑制剂
AZD1080 是一种新型的 GSK3 抑制剂,能够挽救啮齿动物大脑中的突触可塑性缺陷,并在人体中展示外周靶点参与。- Shengzhong Liu, .et al. , J Cell Biochem, 2019, 2019 PMID: 30887575