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AKT Inhibitor
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.- 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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DNMT inhibitor
Azacitidine is a chemical analogue of the cytosine nucleoside used in DNA and RNA that is mainly used in the treatment of myelodysplastic syndrome (MDS). -
GSK-3 Inhibitor
CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.- 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 inhibitor
DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.- 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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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
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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.- 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 inhibitor
SB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I ALK receptors ALK4, ALK5, and ALK7 .- 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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HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
RAR agonist
Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors). -
HDAC Inhibitor
Trichostatin A (TSA) inhibits the HDACs 1, 3, 4, 6 and 10 with IC50 values around 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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ROCK Inhibitor
Y-27632 is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hESCs).- 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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PI3K inhibitor
Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 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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Gamma secretase inhibitor
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
- 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 inhibitor
LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.- 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 Inhibitor
GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays - LDN193189 HCl is the hydrochloride salt of LDN193189. LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
- 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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Hedgehog signaling activator
Purmorphamine is a 2,6,9-trisubstituted purine that promotes the differentiation of both human and mouse mesenchymal progenitor cells into osteoblasts.- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
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ALK5 inhibitor
RepSox (SJN 2511) is a selective inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively).- 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
- Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
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AMPK inhibitor
BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and fatty acid synthase inhibitor.- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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TGF-β/ALK5 inhibitor
A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor 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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Wnt inhibitor
IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription.- Charles A.Herring, .et al. , Cell, 2022, Oct 27;S0092-8674(22)01258-2 PMID: 36318921
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BMP inhibitor
Dorsomorphin, also known as BML-275, is a selective small molecule inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling.- Kameshima S, .et al. , Apoptosis, 2019, Feb 8 PMID: 30737648
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HDAC inhibitor
Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
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ROCK-I/ROCK-II inhibitor
Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.- Sara B Linker, .et al. , Curr Biol, 2022, Nov 21;32(22):4797-4807 PMID: 36228612
- Renata Santos, .et al. , STAR Protoc, 2022, Mar 17;3(2):101261 PMID: 35313707
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pan-Akt inhibitor
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA. -
BMP type I receptor inhibitor
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50??500 nM). -
BMP signaling inhibitor
LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.