Y-33075 dihydrochloride
Based on 14 publication(s) in Google Scholar
Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
For research use only. We do not sell to patients.
- Purity : 98.81%
- CAS No.: 173897-44-4
- Formula: C16H18Cl2N4O
- Molecular Weight:353.25
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Y-33075 dihydrochloride
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Cell. 2018 Jul 26;174(3):636-648.e18. [Abstract]
- Nat Commun. 2020 Jan 3;11(1):88. [Abstract]
- J Adv Res. 2024 Sep:63:117-128. [Abstract]
- Adv Sci (Weinh). 2022 May;9(13):e2104682. [Abstract]
- Cell Death Dis. 2024 Dec 26;15(12):932. [Abstract]
- Acta Neuropathol Commun. 2024 Sep 14;12(1):150. [Abstract]
- Cells. 2024 Nov 18;13(22):1907. [Abstract]
- Stem Cell Reports. 2020 Jan 14;14(1):49-59. [Abstract]
- J Cell Physiol. 2021 Dec;236(12):8226-8238. [Abstract]
- Neurotox Res. 2013 Apr;23(3):238-48. [Abstract]
- PLoS One. 2023 Jan 31;18(1):e0270288. [Abstract]
- bioRxiv. 2025 June 03.
- Patent. US20170349879A1.
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
Biological Activity
Description
IC50 & Target
[1]|
ROCK 3.6 nM (IC50) |
PKC 420 nM (IC50) |
CaMKII 810 nM (IC50) |
In Vitro
Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII more potently than Y-27632, and the IC50s of Y-27632 and Y-33075 for PKC are 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII are 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-33075 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII is 236 and 225 times those for ROCK, respectively[1]. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983[2]. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions. Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 173897-44-4
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Appearance Solid
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Molecular Weight 353.25
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Formula C16H18Cl2N4O
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Color White to gray
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SMILES
O=C(C1=CC=C([C@@H](C)N)C=C1)NC2=C3C(NC=C3)=NC=C2.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (14)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Cell
2018 Jul 26;174(3):636-648.e18. PMID: 30017246 -
Nat Commun
2020 Jan 3;11(1):88. PMID: 31900402 -
J Adv Res
Leucine zipper protein 1 attenuates pressure overload-induced cardiac hypertrophy through inhibiting Stat3 signaling. [Abstract]2024 Sep:63:117-128. PMID: 37806546 -
Adv Sci (Weinh)
Pharmacological Perturbation of Mechanical Contractility Enables Robust Transdifferentiation of Human Fibroblasts into Neurons. [Abstract]2022 May;9(13):e2104682. PMID: 35240008 -
Cell Death Dis
TRIM59/RBPJ positive feedback circuit confers gemcitabine resistance in pancreatic cancer by activating the Notch signaling pathway. [Abstract]2024 Dec 26;15(12):932. PMID: 39725730 -
Acta Neuropathol Commun
Evaluation of Rho kinase inhibitor effects on neuroprotection and neuroinflammation in an ex-vivo retinal explant model. [Abstract]2024 Sep 14;12(1):150. PMID: 39300576 -
Cells
Thrombospondin 1 Mediates Autophagy Upon Inhibition of the Rho-Associated Protein Kinase Inhibitor. [Abstract]2024 Nov 18;13(22):1907. PMID: 39594655 -
Stem Cell Reports
iPSC-Derived Platelets Depleted of HLA Class I Are Inert to Anti-HLA Class I and Natural Killer Cell Immunity. [Abstract]2020 Jan 14;14(1):49-59. PMID: 31883921 -
J Cell Physiol
2021 Dec;236(12):8226-8238. PMID: 34180057 -
Neurotox Res
The Rho-kinase (ROCK) inhibitor Y-27632 protects against excitotoxicity-induced neuronal death in vivo and in vitro. [Abstract]2013 Apr;23(3):238-48. PMID: 22810835
Y-33075 dihydrochloride purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2013 Apr;23(3):238-48. [Abstract]
Effect of Y39983 on glutamate-treated HT22 cell viability.
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PLoS One
The non-selective Rho-kinase inhibitors Y-27632 and Y-33075 decrease contraction but increase migration in murine and human hepatic stellate cells. [Abstract]2023 Jan 31;18(1):e0270288. PMID: 36719899
Y-33075 dihydrochloride purchased from MedChemExpress. Usage Cited in: PLoS One. 2023 Jan 31;18(1):e0270288. [Abstract]
Y-27632 (10, 100 nM and 10, 100 µM; 24 h) decreases phosphorylation of MLC starting at a concentration of 100 nM in HSCs.
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Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (283.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (141.54 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (283.09 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hideki Tokushige, et al. Effects of Topical Administration of Y-39983, a Selective Rho-Associated Protein Kinase Inhibitor, on Ocular Tissues in Rabbits and Monkeys Invest. Ophthalmol. Vis. Sci. July 2007 vol. 48no. 7 3216-3222 [Content Brief]
[2]. Tokushige H, et al. Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats. Curr Eye Res. 2011 Oct;36(10):964-70. [Content Brief]
[3]. Watabe H, et al. Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries.Jpn J Ophthalmol. 2011 Jul;55(4):411-7. Epub 2011 Jun 11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.8309 mL | 14.1543 mL | 28.3086 mL | 70.7714 mL |
| 5 mM | 0.5662 mL | 2.8309 mL | 5.6617 mL | 14.1543 mL | |
| 10 mM | 0.2831 mL | 1.4154 mL | 2.8309 mL | 7.0771 mL | |
| 15 mM | 0.1887 mL | 0.9436 mL | 1.8872 mL | 4.7181 mL | |
| 20 mM | 0.1415 mL | 0.7077 mL | 1.4154 mL | 3.5386 mL | |
| 25 mM | 0.1132 mL | 0.5662 mL | 1.1323 mL | 2.8309 mL | |
| 30 mM | 0.0944 mL | 0.4718 mL | 0.9436 mL | 2.3590 mL | |
| 40 mM | 0.0708 mL | 0.3539 mL | 0.7077 mL | 1.7693 mL | |
| 50 mM | 0.0566 mL | 0.2831 mL | 0.5662 mL | 1.4154 mL | |
| 60 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 1.1795 mL | |
| 80 mM | 0.0354 mL | 0.1769 mL | 0.3539 mL | 0.8846 mL | |
| 100 mM | 0.0283 mL | 0.1415 mL | 0.2831 mL | 0.7077 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Y-33075 dihydrochloride Related Classifications
HY-10069 Related Classifications
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