目录号
产品名
应用
产品描述
文献引用
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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。 - Myricitrin 是 myricetin 的 3-O-rhamnoside。Myricitrin 被一些甲虫种类用于它们的交流系统。
- Ayumi Yamamoto, .et al. , Nutrients, 2022, Mar 4;14(5):1078 PMID: 35268053
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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
- LDN193189 HCl 是 LDN193189 的盐酸盐。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。
- Andreea Manole, .et al. , Cell Rep, 2023, Dec 26;42(12):113466 PMID: 38039131
- Brandon J.Peiffer, .et al. , Cell Chem Biol, 2019, 26, 1-10 PMID: 30827938
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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。 -
p32-kinase activator
D-erythro-鞘氨醇（红鞘氨醇）是一种非常有效的p32-激酶激活剂，其EC50为8μM，并且能够抑制蛋白激酶C（PKC）。D-erythro-鞘氨醇（红鞘氨醇）也是PP2A的激活剂。 -
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
- Ingenol mebutate 是一种存在于植物大豆草(Euphorbia peplus) 树液中的物质，它是细胞死亡的诱导剂。
- Yao-Yu Hsieh, .et al. , Toxicol Appl Pharmacol, 2022, Aug 15;449 PMID: 35724704
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PKC activator
(-)-Indolactam V 是一种蛋白激酶C激活剂，它强烈地将来源于人类胚胎干细胞的确定性内胚层引导成胰腺内胚层。- Manuel Mendoza, .et al. , Tetrahedron, 2019, May
- alpha-淀粉样前体蛋白调节剂是一种细胞渗透性的苯并内酯衍生的PKC激活剂（对PKCα的Ki = 11.9 nM），即使在100 nM的浓度下，也能有效增强人类成纤维细胞中淀粉样前体蛋白（APP）的非淀粉样α-加工。
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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）。
