1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
  2. ROCK

Y-33075 dihydrochloride 

Cat. No.: HY-10069 Purity: 97.92%
Data Sheet SDS Handling Instructions

Y-33075 dihydrochloride is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632.

For research use only. We do not sell to patients.
Y-33075 dihydrochloride Chemical Structure

Y-33075 dihydrochloride Chemical Structure

CAS No. : 173897-44-4

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Other In-stock Forms of Y-33075 dihydrochloride:

Other Forms of Y-33075 dihydrochloride:

    Y-33075 dihydrochloride purchased from MCE. Usage Cited in: Neurotox Res. 2013 Apr;23(3):238-48.

    Effect of Y39983 on glutamate-treated HT22 cell viability.

    Y-33075 dihydrochloride purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    Y-33075 dihydrochloride purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Y-33075 dihydrochloride is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632.

    In Vitro

    In the examination of inhibition of PKC and CaMKII, the IC50s of Y-27632 and Y-39983 for PKC is 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-39983 for CaMKII is 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-39983 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-39983 for CaMKII is 236 and 225 times those for ROCK, respectively[1]. Y-39983 (10 μM) extends neurites in the RGCs compared with those in RGCs treated without Y-39983[2].

    In Vivo

    In rabbits and in monkeys, Y-39983 lowers IOP in a dose-dependent fashion[1]. An increase in regenerating axons of RGCs in 100 mM Y-39983-treated eyes is observed compared with saline-treated eyes. Y-39983 dose-dependently increases the number of RGCs with regenerating axons[2]. Both Y-27632 and Y-39983 induces a concentration-dependent relaxation in rabbit ciliary arteries precontracted with a high-potassium (high-K) solution. The amplitude of relaxation induced by Y-27632 and Y-39983 is not affected by either 100 μM N (G)-nitro-L: -arginine methyl ester (L: -NAME) or 10 μM indomethacin. In Ca2+-free solution, Y-27632 and Y-39983 significantly inhibits the transient contraction of ciliary arteries induced by 10 μM histamine. However, neither Y-27632 nor Y-39983 affects the elevation of [Ca2+](i) induced by high-K solution and histamine[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.8309 mL 14.1543 mL 28.3086 mL
    5 mM 0.5662 mL 2.8309 mL 5.6617 mL
    10 mM 0.2831 mL 1.4154 mL 2.8309 mL
    Please refer to the solubility information to select the appropriate solvent.
    Animal Administration
    [2]

    Y-33075 is formulated in saline.

    In brief, SD rats is anesthetized with an intraperitoneal injection of sodium pentobarbital (0.4 mg/kg body weight), and the optic nerve of one eye is transected 4 to 6 mm posterior to the eyeball, taking care to avoid injury to the ophthalmic artery. The anterior branch of the sciatic nerve is excised and sutured autologously to the optic nerve stump with nylon sutures. The other end of the graft is sutured to the temporalis muscle. A small piece (3 mm × 3 mm) of gelatin sponge soaked with 10 μM Y-39983 or saline as a control is implanted in the space behind the optic stump after optic nerve transection in intact animals. Five μL of 0.12 mM or 1.2 mM Y-39983 solution or saline is administered into the vitreous body to final concentrations of 10 μM or 100 μM, respectively. The concentrations of Y-39983 used is determined as 10 μM that is effective in the in vitro study on axonal regeneration of RGCs, and also as 100 μM in order to confirm the dose response of Y-39983. Six weeks after surgery, rats is anesthetized with an intraperitoneal injection of sodium pentobarbital (0.4 mg/kg body weight), and 4-Di-10ASP is embedded in the transplanted sciatic nerve to retrogradely label RGCs with axonal regeneration into the sciatic nerve. Three days after dye embedding, rats is euthanized and the eyes is enucleated for preparation of retinal flat-mounts. The posterior eyecup is then separated from the vitreous body and postfixed with 4% paraformaldehyde solution in phosphate buffer for around 1 hour at room temperature. Fluorescence micrographs of the labeled cells is imported using a fluorescence microscope connected to a computer. Labeled cells is counted using image analysis software. As a normal group, the subsequent procedure for retrograde labeling with 4-Di-10ASP is performed without grafting sciatic nerve and administering the test drug. Statistical analysis is performed using logarithmically transformed values due to differences in variance among the groups. The statistical significance of differences between the normal and saline groups and the saline and Y-39983 groups is examined by t-test (onesided) and William’s test (one-sided). Findings of p < 0.05 is considered significant. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    353.25

    Formula

    C₁₆H₁₈Cl₂N₄O

    CAS No.

    173897-44-4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO; 10 mM in H2O

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Y-33075 dihydrochloride
    Cat. No.:
    HY-10069
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