A3008-10mg | Y-27632 dihydrochloride [129830-38-2] Clinisciences

Y-27632 dihydrochloride is a small-molecule inhibitor of Rho-associated protein kinase p160ROCK with the IC50 of 140 nM. Y-27632 suppresses the kinase activity of both ROCK-1 and ROCK-2 in vitro, and this compound inhibits the kinases by binding to the catalytic site of ROCK-1 and ROCK-2. Thus Y-27632 function on Rho-mediated stress fiber formation, the G1-S phase progression and cytokinesis.

References

1. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. T Ishizaki, M Uehata, I Tamechika, J Keel Molecular Pharmacology 2000

2. A ROCK inhibitor permits survival of dissociated human embryonic stem cells K Watanabe, M Ueno, D Kamiya, A Nishiyama. Nature Biotechnology. 2007

1. Jessica E. Young, et al. "Differential effects of SORL1 deficiency on the endo-lysosomal network in human neurons and microglia." Philos Trans R Soc Lond B Biol Sci. 2024 Apr 8;379(1899):20220389. PMID: 38368935
2. Jose M de Hoyos-Vega, Xi Yu, et al. "Modeling Gut Neuro-Epithelial Connections in a Novel Microfluidic Device." Microsyst Nanoeng. 2023 Nov 14:9:144. PMID: 38025883
3. Yinju Liu, Jinlong Tan, et al. "A Strainer-Based Platform for the Collection and Immunolabeling of Porcine Epidemic Diarrhea Virus-Infected Porcine Intestinal Organoid." Int J Mol Sci. 2023 Oct 27;24(21):15671. PMID: 37958655
4. Rashmi Chandra, Arpine Sokratian, et al. "Gut mucosal cells transfer α-synuclein to the vagus nerve." bioRxiv. 2023 Aug 14;2023.08.14.553305. PMID: 37645945
5. Niamh McNamee, Mariadelva Catalano, et al. "An extensive study of potential inhibitors of extracellular vesicles release in triple-negative breast cancer." BMC Cancer. 2023 Jul 13;23(1):654. PMID: 37442985
6. Peiyan Ni, Chuqing Zhou, et al. "YBX1‐Mediated DNA Methylation‐DependentSHANK3Expression in PBMCs and Developing Cortical Interneurons in Schizophrenia." Adv Sci (Weinh). 2023 Jul;10(20):e2300455. PMID: 37211699
7. Peiyan Ni, Chuqing Zhou, et al. "Generation and characterization of human-derived iPSC lines from two cousins with schizophrenia and bipolar disorder and their unaffected cousin." Stem Cell Res. 2022 Aug;63:102832. PMID: 35700633
8. Ciaran A Shaughnessy, Pamela L Zeitlin, et al. "Net benefit of ivacaftor during prolonged tezacaftor/elexacaftor exposure in vitro." J Cyst Fibros. 2022 Mar 2;S1569-1993(22)00043-1. PMID: 35248469
9. Peiyan Ni, Huiyao Wang, et al. "Generation and characterization of human-derived iPSC lines from one pair of dizygotic twins discordant for schizophrenia." Stem Cell Res. 2022 Apr;60:102710. PMID: 35182860
10. XiangRong Luo, JianTao She, et al. "Establishment and characterization of organoids from a patient with adenomyoepithelioma of the breast." Bioengineered. 2021 Dec;12(2):11578-11585. PMID: 34874791
11. Changchun Shao, Xue Yang, et al. "The stemness of hepatocytes is maintained by high levels of lipopolysaccharide via YAP1 activation." Stem Cell Res Ther. 2021 Jun 10;12(1):342. PMID: 34112239
12. Chien-Liang Liu, Shih-Ping Cheng, et al. "Quinolinate Phosphoribosyltransferase Promotes Invasiveness of Breast Cancer Through Myosin Light Chain Phosphorylation." Front Endocrinol (Lausanne). 2021 Feb 4;11:621944. PMID: 33613454
13. Tanmoy Mondal, Gururaj N Shivange, et al. "Unexpected PD‐L1 immune evasion mechanism in TNBC, ovarian, and other solid tumors by DR5 agonist antibodies." EMBO Mol Med. 2021 Mar 5;13(3):e12716. PMID: 33587338
14. Leqian Yu, Yulei Wei, et al. "Derivation of Intermediate Pluripotent Stem Cells Amenable to Primordial Germ Cell Specification." Cell Stem Cell. 2021 Mar 4;28(3):550-567.e12. PMID: 33271070
15. Priscilla Cheung, Jordi Xiol, et al. "Regenerative Reprogramming of the Intestinal Stem Cell State via Hippo Signaling Suppresses Metastatic Colorectal Cancer." Cell Stem Cell. 2020 Oct 1;27(4):590-604.e9. PMID: 32730753
16. Nathan D. Jackson, Jamie L. Everman, et al. "Single-Cell and Population Transcriptomics Reveal Pan-epithelial Remodeling in Type 2-High Asthma." Cell Reports;Volume 32, Issue 1, 7 July 2020, 107872. PMID: 32640237
17. Zhao Y, Ge X, et al. "Inhibition of ROCK signaling pathway accelerates enteric neural crest cell-based therapy after transplantation in a rat hypoganglionic model." Neurogastroenterol Motil. 2020;e13895. PMID: 32515097
18. Andrew S. Riching, Etienne Danis, et al. "Suppression of canonical TGF-β signaling enables GATA4 to interact with H3K27me3 demethylase JMJD3 to promote cardiomyogenesis." bioRxiv. 2020 February 12.
19. Miller AJ, Yu Q, et al. "In Vitro and In Vivo Development of the Human Airway at Single-Cell Resolution." Dev Cell. 2020;S1534-5807(20)30065-4. PMID: 32109386
20. Allison Knupp, Swati Mishra, et al. "Depletion of the AD risk gene SORL1 selectively impairs neuronal endosomal traffic independent of amyloidogenic APP processing." bioRxiv. 2020 January 06.
21. Jennifer E. Speer, Yuli Wang, et al. "Evaluation of human primary intestinal monolayers for drug metabolizing capabilities." Journal of Biological Engineering volume 13, Article number: 82 (2019)
22. Selvaraj S, Mondragon-Gonzalez R, et al. "Screening identifies small molecules that enhance the maturation of human pluripotent stem cell-derived myotubes." Elife. 2019 Nov 11;8. pii: e47970. PMID: 31710288
23. Tonnessen-Murray CA, Frey WD, et al. "Chemotherapy-induced senescent cancer cells engulf other cells to enhance their survival." J Cell Biol. 2019 Sep 17. pii: jcb.201904051. PMID: 31530580
24. Rachit Neupane. "BMI1 is a context-dependent tumor suppressor that is a barrier to dedifferentiation in non-small cell lung adenocarcinoma." Massachusetts Institute of Technology. 2019.
25. Sagi I, De Pinho JC, et al. "Distinct Imprinting Signatures and Biased Differentiation of Human Androgenetic and Parthenogenetic Embryonic Stem Cells." Cell Stem Cell. 2019 Sep 5;25(3):419-432.e9. PMID: 31491396
26. Samuel S. Hinman, Yuli Wang, et al. "Photopatterned Membranes and Chemical Gradients Enable Scalable Phenotypic Organization of Primary Human Colon Epithelial Models." chemrxiv.org. 2019.
27. Matthew DiSalvo, Nicole M. Smiddy, et al. "Automated sensing and splitting of stem cell colonies on microraft arrays." APL Bioengineering. 29 August 2019.
28. Cheng CW, Biton M, et al. "Ketone Body Signaling Mediates Intestinal Stem Cell Homeostasis and Adaptation to Diet." Cell. 2019 Aug 22;178(5):1115-1131.e15. PMID: 31442404
29. Alfajaro MM, Kim JY, et al. "Dual Recognition of Sialic Acid and αGal Epitopes by the VP8* Domains of the Bovine Rotavirus G6P[5] WC3 and of Its Mono-reassortant G4P[5] RotaTeq Vaccine Strains." J Virol. 2019 Jun 26. pii: JVI.00941-19. PMID: 31243129
30. Ni P, Noh H, et al. "Large-Scale Generation and Characterization of Homogeneous Populations of Migratory Cortical Interneurons from Human Pluripotent Stem Cells." Mol Ther Methods Clin Dev. 2019 Apr 8;13:414-430. PMID: 31061832
31. Speer JE, Gunasekara DB, et al. "Molecular transport through primary human small intestinal monolayers by culture on a collagen scaffold with a gradient of chemical cross-linking." J Biol Eng. 2019 Apr 27;13:36. PMID: 31061676
32. Ni P, Noh H, et al."iPSC-derived homogeneous populations of developing schizophrenia cortical interneurons have compromised mitochondrial function." Mol Psychiatry. 2019 Apr 24. PMID: 31019265
33. Dakhama A, Al Mubarak R, et al. "Tollip Inhibits ST2 Signaling in Airway Epithelial Cells Exposed to Type 2 Cytokines and Rhinovirus." J Innate Immun. 2019 Mar 29:1-13. PMID: 30928973
34. Grun D, Adhikary G, et al. "NRP-1 interacts with GIPC1 and SYX to activate p38 MAPK signaling and cancer stem cell survival." Mol Carcinog. 2018 Nov 19. PMID: 30456845
35. Alyssa J. Miller, Quanhui Yu, et al. "Basal stem cell fate specification is mediated by SMAD signaling in the developing human lung."bioRxiv. 2018 November 4.
36. Wang Y, Li Y, et al. "The cerebral cavernous malformation disease causing gene KRIT1 participates in intestinal epithelial barrier maintenance and regulation." FASEB J. 2018 Sep 25:fj201800343R. PMID: 30252535
37. Everman JL, Rios C, Seibold MA. "Utilization of Air-Liquid Interface Cultures as an In Vitro Model to Assess Primary Airway Epithelial Cell Responses to the Type 2 Cytokine Interleukin-13." Methods Mol Biol. 2018;1799:419-432. PMID: 29956168
38. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
39. Mihaylova MM, Cheng CW, et al. "Fasting Activates Fatty Acid Oxidation to Enhance Intestinal Stem Cell Function during Homeostasis and Aging." Cell Stem Cell. 2018 May 3;22(5):769-778. PMID: 29727683
40. Wang Y, Kim R, et al. "Formation of Human Colonic Crypt Array by Application of Chemical Gradients Across a Shaped Epithelial Monolayer." Cell Mol Gastroenterol Hepatol. 2017 Nov 3;5(2):113-130. PMID: 29693040
41. Lin L, Li M, et al. "FPPS mediates TGF-β1-induced non-small cell lung cancer cell invasion and the EMT process via the RhoA/Rock1 pathway." Biochem Biophys Res Commun. 2018 Feb 5;496(2):536-541. PMID: 29337059
42. Roper J, Tammela T, et al."Colonoscopy-based colorectal cancer modeling in mice with CRISPR-Cas9 genome editing and organoid transplantation." Nat Protoc. 2018 Feb;13(2):217-234. PMID: 29300388
43. Miller AJ, Hill DR, et al. "In Vitro Induction and In Vivo Engraftment of Lung Bud Tip Progenitor Cells Derived from Human Pluripotent Stem Cells." Stem Cell Reports.2017 Dec 12. pii: S2213-6711(17)30519-2. PMID: 29249664
44. Wang Y, DiSalvo M, et al. "Self-renewing Monolayer of Primary Colonic or Rectal Epithelial Cells." Cell Mol Gastroenterol Hepatol. 2017 Mar 6;4(1):165-182.e7. PMID: 29204504
45. Schwartz DM, Pehlivaner Kara MO, et al. "Spray Delivery of Intestinal Organoids to Reconstitute Epithelium on Decellularized Native Extracellular Matrix. Tissue Eng Part C Methods." 2017 Jul 29. PMID: 28756760
46. Roper J, Tammela T, et al. "In vivo genome editing and organoid transplantation models of colorectal cancer and metastasis." Nat Biotechnol. 2017 Jun;35(6):569-576. PMID: 28459449
47. Alyssa J. Miller, Briana R. Dye, et al. "Integrated growth factor signaling promotes lung epithelial progenitor cell expansion and maintenance in mice and humans." bioRxiv, 2017: 108845.
48. Reynolds SD, Rios C, et al. "Airway Progenitor Clone Formation is Enhanced by Y-27632-dependent Changes in the Transcriptome." Am J Respir Cell Mol Biol. 2016 May 4. PMID: 27144410
49. Yagyu, Shigeki, et al. "An Inducible Caspase-9 Suicide Gene to Improve the Safety of Therapy Using Human Induced Pluripotent Stem Cells." Molecular Therapy (2015). PMID: 26022733

Hide ↑↑

Physical Appearance	A solid
Storage	Desiccate at 4°C or below
M.Wt	320.26
Cas No.	129830-38-2
Formula	C₁₄H₂₁N₃O·2HCl
Synonyms	y-27632, Y27632, Y-27632 dihydrochloride, Y 27632
Solubility	≥111.2 mg/mL in DMSO; ≥17.57 mg/mL in EtOH; ≥52.9 mg/mL in H2O
Chemical Name	4-[(1R)-1-aminoethyl]-N-pyridin-4-ylcyclohexane-1-carboxamide
SDF	Download SDF
Canonical SMILES	CC(C1CCC(CC1)C(=O)NC2=CC=NC=C2)N
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Cell experiment [1]:
Cell lines	Human (hu) and rat(r) prostatic smooth mus-cle cells (PSM)
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.
Reaction Conditions	24h and 48 h; 100 μM
Applications	After identifying prostatic smooth muscle cells and confirming the expression of Rho-kinase in these cells we investigated whether the Rho-kinase inhibitor Y-27632 affected the viability and proliferation of these cells. In serum-free medium huPSM and rPSM were made quiescent for 24 hours. Cell viability using neutral red and MTT assays was assessed 24 and 48 hours after stimulating the cells with 1% serum in the absence and presence of Y-27632 (0.01 to 100 μM). The results of these assays showed that the number of the cells increased between the 24- and 48-hour incubation periods after re-stimulation with 1% serum. However, in the presence of Y-27632 the increase in the number of live cells was less than in the control group. This effect was concentration dependent.
Animal experiment [2]:
Animal models	Adult Swiss male albino mice
Dosage form	0.1 mg/kg/day; intrapertoneal injection
Applications	The drug was tested by histopathological examination showed that Y-27632 administration to EAC-bearing mice diminished pathological structure, to 60–70% degree, toward to normal intact histological structure especially in pre-carcinoma inoculation regime. Respect to this, ROCK inhibition by Y-27632 decreased significantly tumor invasion and metastasis. Our immunohistochemistry results showed that ROCK2 was mainly inhibited by Y-27632 in pre-carcinoma, but not in post-carcinoma, groups.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1] Rees R W, Foxwell N A, Ralph D J, et al. Y-27632, a Rho-kinase inhibitor, inhibits proliferation and adrenergic contraction of prostatic smooth muscle cells[J]. The Journal of urology, 2003, 170(6): 2517-2522. [2] Isler D, Ozaslan M, Karagoz I D, et al. Antitumoral effect of a selective Rho-kinase inhibitor Y-27632 against Ehrlich ascites carcinoma in mice[J]. Pharmacological Reports, 2014, 66(1): 114-120.

Description	Y-27632 is a selective inhibitor of ROCK1 (p160ROCK) with Ki of 140 nM, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Targets	ROCK1	ROCK2
IC50	140 nM (K_i)	300 nM (K_i)

Purity = 99.54%

Y-27632 dihydrochloride [129830-38-2]

Referência A3008-10mg

Contactar o distribuidor local :

Marca : APExBIO Technology

Contactar o distribuidor local :

Background

Product Citation

Chemical Properties

Protocol

Biological Activity

Quality Control

Você também pode estar interessado nos seguintes produtos: