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PKC inhibitor
Chelerythrine 影响 PKC 从细胞质到质膜的转移。已显示可阻止神经突生长。以浓度和时间依赖的方式诱导凋亡。 -
PKC inhibitor
Bryostatin 1 是从海洋苔藓动物 Bugula neritina 中分离出的一种大环内酯，它调节蛋白激酶 C（PKC）的活性。Bryostatin 1 引发 PKC 的快速激活和自磷酸化，导致 PKC 酶转移到膜上。 -
PKCβ inhibitor
LY317615（Enzastaurin）是一种强效且选择性的PKCβ抑制剂，具有抗增殖活性（IC50约为6 nM）。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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ROCK inhibitor
Fasudil HCl 是一种环核苷酸依赖性蛋白激酶抑制剂和Rho相关激酶抑制剂（IC50 = 10.7 μM）。- Jiwan Choi, .et al. , Stem Cell Res Ther, 2024, Jul 29;15(1):229 PMID: 39075621
- Patrick D Lyden, .et al. , Sci Transl Med, 2023, Sep 20;15(714):eadg8656 PMID: 37729432
- Seongjun So, .et al. , Int J Mol Sci, 2022, Dec 31;24(1):701 PMID: 36614165
- Chengyu Xiang, .et al. , J Cardiovasc Transl Res, 2022, May 12 PMID: 35551627
- Yeonmi Lee, .et al. , Commun Biol, 2022, Jan 25;5(1):95 PMID: 35079104
- Jiwan Choi, .et al. , Stem Cell Res Ther, 2021, Nov 12;12(1):569
- Jee Myung Yang, .et al. , Exp Mol Med, 2021, Apr;53(4):631-642 PMID: 33828232
- Jooyoung Lee, .et al. , Cells, 2020, Jun; 9(6): 1521 PMID: 32580448
- Kumar M, .et al. , Behav Brain Res, 2018, Oct 1;351:4-16 PMID: 29807069
- Wei J, .et al. , Shock, 2018, Dec;50(6):706-713 PMID: 29283979
- Hofni A, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2017, Aug;390(8):801-811 PMID: 28493050
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ROCK Inhibitor
GSK429286A 是一种细胞渗透性、选择性的小分子抑制剂，专门针对 Rho-associated, coiled-coil containing protein kinase (ROCK)。 -
PDE4 inhibitor
Hesperetin，一种选择性的磷酸二酯酶（PDE）4抑制剂，存在于传统中药陈皮中。Hesperetin 是一种柑橘类黄酮，已被报道可降低血浆胆固醇。Hesperetin 在剂量依赖性的方式下减少 Hep-G2 细胞中 ACAT-2 mRNA 的转录，并减少 ApoB 蛋白的合成。它也是一种潜在的类癌综合症癌症治疗方法。 -
MAO-B inhibitor
槲皮素能够抑制多种酶系统，包括酪氨酸蛋白激酶、磷脂酶A2、磷酸二酯酶、线粒体ATP酶、PI 3-激酶和蛋白激酶C。 -
TGF-beta/Smad inhibitor
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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PKC inhibitor
Staurosporine 是一种天然产物，最初于 1977 年从细菌 Streptomyces staurosporeus 中分离出来。Staurosporine 的主要生物活性是通过阻止 ATP 与激酶结合来抑制 蛋白激酶。这是通过 Staurosporine 对激酶上的 ATP 结合位点具有更强的亲和力来实现的。- Lisa M Kim, .et al. , Cancer Res, 2022, Sep 2;82(17):3045-3057 PMID: 35792658
- Jacobs CL, .et al. , Nat Methods, 2018, Jul;15(7):523-526 PMID: 29967496
- Birte Plitzko, .et al. , J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
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ROCK Inhibitor
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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TGF-βR Inhibitor
LY2157299 是一种口服活性的转化生长因子β受体（TGF-βR）激酶抑制剂。- Yuri Nagaoka, .et al. , Arch Biochem Biophys, 2024, Jan:751:109824 PMID: 37984759
- Eunji Jang, .et al. , Exp Mol Med, 2023, May;55(5):974-986 PMID: 37121972
- Satoshi Endo, .et al. , Nutr Res, 2019, 4 November
- Oguri G, .et al. , Am J Physiol Heart Circ Physiol., 2014, 307(9):H1339-52 PMID: 25172898
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Akt inhibitor
A-674563 是一种 B/Akt 抑制剂，其 IC50 为 14 nM，同时也显示出对 PKA 和 CDK2 的抑制活性，其 IC50 分别为 16 nM 和 46 nM。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Kobayashi T, .et al. , Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. , Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. , Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
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TβRI/II kinase inhibitor
LY2109761，一种新型的转化生长因子β受体I型和II型双重抑制剂，作为抑制胰腺癌转移的治疗方法。- Yimei Wei, .et al. , Int J Rheum Dis, 2024, May;27(5):e15164 PMID: 38706209
- Yan Yang, .et al. , J Thorac Dis, 2024, Feb 29;16(2):1128-1140 PMID: 38505034
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Uto T, .et al. , J Allergy Clin Immunol, 2018, Jun;141(6):2156-2167.e9 PMID: 29477579
- Jared M. Fischer, .et al. , Proc Natl Acad Sci U S A, 2016, Oct 25; 113(43): 12192-12197 PMID: 27791005
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ALK inhibitor
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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ALK5 inhibitor
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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PKA inhibitor
H 89 二盐酸盐是一种细胞渗透性、选择性、可逆的、与ATP竞争的、强效的蛋白激酶抑制剂。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Guo Q, .et al. , Biomed Pharmacother, 2020, Mar;123:109812 PMID: 31945696
- Y Kaibori, .et al. , the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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PKC inhibitor
Verbascoside，从马缨丹（Lantana camara）中提取，作为PKC的ATP竞争性抑制剂，具有25 μM的IC50值，并具有抗肿瘤、抗炎和抗神经痛活性。 -
ROCK inhibitor
GSK 269962 是一种强效的 Rho 激酶（ROCK）抑制剂（对重组人类 ROCK1 和 ROCK2 的 IC50 值分别为 1.6 和 4 nM）。- Praneeth Siripurapu, .et al. , J Biol Chem, 2017, Oct 20; 292(42): 17482-17495 PMID: 28864771
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TGF-β/ALK5 inhibitor
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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PKC inhibitor
Ruboxistaurin（LY333531）是一种强效、选择性的蛋白激酶C同工酶抑制剂，针对PKC β I（IC50=4.7 nM）和PKC β II（IC50=5.9 nM）具有抑制作用。 -
PKC inhibitor
PKC 412 是一种广谱蛋白激酶抑制剂。它能抑制常规的 PKC 同型体 α/β/γ，PDFRβ，VEGFR2，Syk，Flk-1，Flt3，Cdk1/B，PKA，c-Kit，c-Fgr，c-Src，VEGFR1 和 EGFR。展示出强大的抗肿瘤活性。 -
ROCK inhibitor
SR 3677 二盐酸盐是一种强效且选择性的Rho激酶抑制剂（IC50值分别为ROCK-II的3 nM和ROCK-I的56 nM）。 -
BMP inhibitor
DMH-1 是一种选择性抑制骨形态发生蛋白（BMP）ALK2 受体的抑制剂（IC50 = 108 nM）。- Teresa Rayon, .et al. , Science, 2020, Sep 18;369(6510):eaba7667 PMID: 32943498
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BMP receptor inhibitor
LDN-212854 是一种 ALK2-Biased BMP Type I Receptor Kinase Inhibitor。 -
δ-protein kinase C (δPKC) inhibitor
Delcasertib (KAI-9803) 是一种强效且选择性的 δ-蛋白激酶C (δPKC) 抑制剂。 -
TGF-β inhibitor
ITD-1 是一种新型且高度选择性的 TGFβ 通路抑制剂。ITD-1 分子将干细胞转化为心脏细胞。- M. C. Wilkes, .et al. , Nat Commun, 2020, 11: 3344 PMID: 32620751
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PKC inhibitor
GF 109203X 是一种强效且选择性的 蛋白激酶C 抑制剂，特别选择性地针对 α 和 β1 亚型（IC50 值分别为 0.0084、0.0180、0.210、0.132 和 5.8 μM，针对 α、β1、δ、ε 和 ζ 亚型）。相较于 MLCK、PKG 和 PKA 具有选择性（IC50 值分别为 0.6、4.6 和 33 μM）。在 5-HT3 受体上是一种强效拮抗剂（Ki = 29.5 nM）。 -
PKC inhibitor
Ro 31-8220 mesylate 是一种 PKC-抑制剂，它能够抑制由 PKC-激活剂 phorbol myristate acetate（PMA，IC50 = 1.35 x 10(-6) M）或 diacylglycerols（OAG, diC8）诱导的人类中性粒细胞（PMNs）的刺激性液体胞饮作用，抑制率达到95%。- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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PKA, PKG, Casein Kinase I and II inhibitor
A-3 Hydrochloride 是一种抑制剂，它可以抑制 PKA（cAMP-dependent protein kinase，Ki=4.3μM）和 cGMP-dependent protein kinase（Ki=3.8μM），PKC（protein kinase C，Ki=47μM），casein kinase I 和 II，以及 MLCK（myosin light chain kinase）（Ki=7.4μM）。 -
ROCK inhibitor
Glycyl-H 1152 2HCl 是一种选择性且高效的 ROCK 抑制剂（IC50 值分别为 0.0118、2.35、2.57、3.26、>10 和 >10 uM，针对 ROCKII、Aurora A、CAMKII、PKG、PKA 和 PKC）。 -
PKC inhibitor
GO6983 是一种强效的蛋白激酶C（PKC）抑制剂。它可以减少心肌缺血/再灌注损伤后的多形核白细胞粘附和浸润。- Kouki Kawakami, .et al. , Nat Commun, 2022, 13: 487 PMID: 35078997
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ALK4/ALK5 inhibitor
EW-7197 是一种高效、选择性强且口服生物利用度高的 TGF-β I 受体 ALK4/ALK5 抑制剂，其 IC50 分别为 13 nM 和 11 nM。- Bordignon P, .et al. , Cell Rep, 2019, Aug 27;28(9):2358-2372 PMID: 31461652
- Morita T, .et al. , Mol Cancer Res, 2018, May;16(5):880-893 PMID: 29330296
