Y27632 HCl
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MedKoo CAT#: 510272

CAS#: 129830-38-2 (2HCl)

Description: Y27632 is a selective ROCK inhibitor, which inhibits ET-1-induced increases in natriuretic peptide production, cell size, protein synthesis, and myofibrillar organization. Y27632 prevents dimethylnitrosamine-induced hepatic fibrosis in rats, increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium, affects initial heart myofibrillogenesis in cultured chick blastoderm, promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord.


Chemical Structure

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Y27632 HCl
CAS# 129830-38-2 (2HCl)

Theoretical Analysis

MedKoo Cat#: 510272
Name: Y27632 HCl
CAS#: 129830-38-2 (2HCl)
Chemical Formula: C14H23Cl2N3O
Exact Mass: 247.16846
Molecular Weight: 320.26
Elemental Analysis: C, 52.51; H, 7.24; Cl, 22.14; N, 13.12; O, 5.00

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 750.0 Ready to ship
200.0mg USD 1250.0 Ready to ship
500.0mg USD 2450.0 Ready to ship
1.0g USD 3450.0 Ready to ship
2.0g USD 5850.0 Ready to ship
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Related CAS #: 331752-47-7 (HCl hydrate)   129830-38-2 (2HCl)   146986-50-7 (free base)   138381-45-0 (racemate HCl)   310898-86-3 (recamte free base)    

Synonym: Y27632; Y-27632; Y 27632; Y27632 HCl; Y27632 dihydrochloride

IUPAC/Chemical Name: (1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride

InChi Key: IDDDVXIUIXWAGJ-LJDSMOQUSA-N

InChi Code: InChI=1S/C14H21N3O.2ClH/c1-10(15)11-2-4-12(5-3-11)14(18)17-13-6-8-16-9-7-13;;/h6-12H,2-5,15H2,1H3,(H,16,17,18);2*1H/t10-,11-,12-;;/m1../s1

SMILES Code: O=C([C@H]1CC[C@H]([C@H](N)C)CC1)NC2=CC=NC=C2.[H]Cl.[H]Cl

Appearance: white to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: Y-27632 dihydrochloride is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively.
In vitro activity: First this study treated HDFs with or without Y-27632 in the presence of 100 ng/ml IGFBP-5, a concentration close to what was found in the conditioned media after Y-27632 treatment. After 48 h, this study analyzed the senescence of HDFs by SA-β-gal staining and found that treatment with Y-27632 and/or IGFBP-5 significantly induced the senescence of HDFs (Figure 7A, 7B). In contrast, when HDFs were treated with Y-27632 with or without the knockdown of IGFBP-5 (siIGFBP-5), which was confirmed by RT-PCR analysis (Supplementary Figure 7A), the knockdown of IGFBP-5 significantly blocked the increased cellular senescence induced by Y-27632 (Figure 7C, 7D). These results suggest that the prolonged treatment of HDFs with Y-27632 increases cellular senescence probably by enhancing the expression and production of IGFBP-5. Reference: Aging (Albany NY). 2020 Aug 31; 12(16): 16621–16646. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7485707/
In vivo activity: In conclusion, this study demonstrated the role of the ROCK signaling pathway in the survival of mouse SGSCs. By inhibiting the ROCK signaling pathway through the chemical inhibitor Y-27632, dissociation-induced cell death of SGSCs was significantly reduced. In addition, ECM-based experiments revealed that the disruption of the cell–ECM interactions is associated with increased cell death of SGSCs. Reference: Molecules. 2021 May; 26(9): 2658. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8124333/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.51 123.37
DMF 20.0 62.45
Ethanol 8.5 26.54
PBS (pH 7.2) 10.0 31.22
Water 73.34 229.0

Preparing Stock Solutions

The following data is based on the product molecular weight 320.26 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Li X, Zhou Q, Wang S, Wang P, Li J, Xie Z, Liu C, Wen J, Wu X. Prolonged treatment with Y-27632 promotes the senescence of primary human dermal fibroblasts by increasing the expression of IGFBP-5 and transforming them into a CAF-like phenotype. Aging (Albany NY). 2020 Aug 25;12(16):16621-16646. doi: 10.18632/aging.103910. Epub 2020 Aug 25. PMID: 32843583; PMCID: PMC7485707. 2. Kim K, Min S, Kim D, Kim H, Roh S. A Rho Kinase (ROCK) Inhibitor, Y-27632, Inhibits the Dissociation-Induced Cell Death of Salivary Gland Stem Cells. Molecules. 2021 May 1;26(9):2658. doi: 10.3390/molecules26092658. PMID: 34062818; PMCID: PMC8124333.
In vitro protocol: 1. Li X, Zhou Q, Wang S, Wang P, Li J, Xie Z, Liu C, Wen J, Wu X. Prolonged treatment with Y-27632 promotes the senescence of primary human dermal fibroblasts by increasing the expression of IGFBP-5 and transforming them into a CAF-like phenotype. Aging (Albany NY). 2020 Aug 25;12(16):16621-16646. doi: 10.18632/aging.103910. Epub 2020 Aug 25. PMID: 32843583; PMCID: PMC7485707.
In vivo protocol: 1. Kim K, Min S, Kim D, Kim H, Roh S. A Rho Kinase (ROCK) Inhibitor, Y-27632, Inhibits the Dissociation-Induced Cell Death of Salivary Gland Stem Cells. Molecules. 2021 May 1;26(9):2658. doi: 10.3390/molecules26092658. PMID: 34062818; PMCID: PMC8124333.

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1: Yang CY, Liu Y, Lu Z, Ren R, Gong H. Effects of Y27632 on aqueous humor outflow facility with changes in hydrodynamic pattern and morphology in human eyes. Invest Ophthalmol Vis Sci. 2013 Aug 28;54(8):5859-70. doi: 10.1167/iovs.12-10930. PubMed PMID: 23920374; PubMed Central PMCID: PMC3757907.

2: Gandham VD, Maddala RL, Rao V, Jin JY, Epstein DL, Hall RP, Zhang JY. Effects of Y27632 on keratinocyte procurement and wound healing. Clin Exp Dermatol. 2013 Oct;38(7):782-6. doi: 10.1111/ced.12067. Epub 2013 May 16. PubMed PMID: 23675999; PubMed Central PMCID: PMC3748215.

3: Yu Z, Liu M, Fu P, Xie M, Wang W, Luo X. ROCK inhibition with Y27632 promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord. Neurochem Int. 2012 Dec;61(7):1114-20. doi: 10.1016/j.neuint.2012.08.003. Epub 2012 Aug 19. PubMed PMID: 22929997.

4: Huang HP, Wang CJ, Tsai JP, Wu SW, Hung TW, Lian JD, Chang HR. Y27632 attenuates the aristolochic acid-promoted invasion and migration of human urothelial cancer TSGH cells in vitro and inhibits the growth of xenografts in vivo. Nephrol Dial Transplant. 2012 Feb;27(2):565-75. doi: 10.1093/ndt/gfr366. Epub 2011 Jul 28. PubMed PMID: 21799205.

5: Lu Z, Zhang Y, Freddo TF, Gong H. Similar hydrodynamic and morphological changes in the aqueous humor outflow pathway after washout and Y27632 treatment in monkey eyes. Exp Eye Res. 2011 Oct;93(4):397-404. doi: 10.1016/j.exer.2011.05.012. Epub 2011 Jun 6. PubMed PMID: 21669200; PubMed Central PMCID: PMC3197945.

6: van Beuge MM, Prakash J, Lacombe M, Post E, Reker-Smit C, Beljaars L, Poelstra K. Increased liver uptake and reduced hepatic stellate cell activation with a cell-specific conjugate of the Rho-kinase inhibitor Y27632. Pharm Res. 2011 Aug;28(8):2045-54. doi: 10.1007/s11095-011-0430-9. Epub 2011 Mar 26. PubMed PMID: 21442374; PubMed Central PMCID: PMC3130909.

7: Balestrieri ML, Giovane A, Milone L, Felice F, Fiorito C, Crudele V, Esposito A, Rossiello R, Minucci PB, Farzati B, Servillo L, Napoli C. Modification of the detrimental effect of TNF-α on human endothelial progenitor cells by fasudil and Y27632. J Biochem Mol Toxicol. 2010 Nov-Dec;24(6):351-60. doi: 10.1002/jbt.20345. PubMed PMID: 20665603.

8: Sivasubramaniyan K, Pal R, Totey S, Bhat VS, Totey S. Rho kinase inhibitor y27632 alters the balance between pluripotency and early differentiation events in human embryonic stem cells. Curr Stem Cell Res Ther. 2010 Mar;5(1):2-12. PubMed PMID: 19951253.

9: Hampson L, He XT, Oliver AW, Hadfield JA, Kemp T, Butler J, McGown A, Kitchener HC, Hampson IN. Analogues of Y27632 increase gap junction communication and suppress the formation of transformed NIH3T3 colonies. Br J Cancer. 2009 Sep 1;101(5):829-39. doi: 10.1038/sj.bjc.6605208. PubMed PMID: 19707205; PubMed Central PMCID: PMC2736836.

10: Freitas MR, Eto M, Kirkbride JA, Schott C, Sassard J, Stoclet JC. Y27632, a Rho-activated kinase inhibitor, normalizes dysregulation in alpha1-adrenergic receptor-induced contraction of Lyon hypertensive rat artery smooth muscle. Fundam Clin Pharmacol. 2009 Apr;23(2):169-78. doi: 10.1111/j.1472-8206.2008.00658.x. Epub 2009 Mar 9. PubMed PMID: 19298234; PubMed Central PMCID: PMC2878275.



Additional Information

 Related CAS#
 CAS#129830-38-2 ( Y27632 2HCl);
CAS3146986-50-7 ( Y27632 free base)