Y-33075
Based on 14 publication(s) in Google Scholar
Y-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.44%
- CAS. Nr.: 199433-58-4
- Formel: C16H16N4O
- Molecular Weight:280.33
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Y-33075
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
Biologische Aktivität
Beschreibung
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. Nr. 199433-58-4
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Appearance Solid
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Molecular Weight 280.33
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Formel C16H16N4O
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Color White to off-white
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SMILES
O=C(NC1=C2C(NC=C2)=NC=C1)C3=CC=C(C=C3)[C@H](N)C
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Synonyms
Y-39983 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
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 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 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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Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (178.36 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (8.92 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 (8.92 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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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.
Reinheit & Dokumentation
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Data Sheet (288 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)
Verweise
[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.5672 mL | 17.8361 mL | 35.6721 mL | 89.1803 mL |
| 5 mM | 0.7134 mL | 3.5672 mL | 7.1344 mL | 17.8361 mL | |
| 10 mM | 0.3567 mL | 1.7836 mL | 3.5672 mL | 8.9180 mL | |
| 15 mM | 0.2378 mL | 1.1891 mL | 2.3781 mL | 5.9454 mL | |
| 20 mM | 0.1784 mL | 0.8918 mL | 1.7836 mL | 4.4590 mL | |
| 25 mM | 0.1427 mL | 0.7134 mL | 1.4269 mL | 3.5672 mL | |
| 30 mM | 0.1189 mL | 0.5945 mL | 1.1891 mL | 2.9727 mL | |
| 40 mM | 0.0892 mL | 0.4459 mL | 0.8918 mL | 2.2295 mL | |
| 50 mM | 0.0713 mL | 0.3567 mL | 0.7134 mL | 1.7836 mL | |
| 60 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
| 80 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL | |
| 100 mM | 0.0357 mL | 0.1784 mL | 0.3567 mL | 0.8918 mL |
Y-33075 Related Classifications
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