An inhibitor of ROCK2
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Alternative(s)
36216Y-33075 (hydrochloride)
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Y-33075

Item No. 35108

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(1R)-1-aminoethyl]-N-1H-pyrrolo[2,3-b]pyridin-4-yl-benzamide
CAS Number
199433-58-4
Synonyms
  • RKI-983
  • SNJ-1656
  • Y-39983
Molecular Formula
C16H16N4O
Formula Weight
280.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
O=C(C1=CC=C(C=C1)[C@H](N)C)NC2=C3C(NC=C3)=NC=C2
InChi Code
InChI=1S/C16H16N4O/c1-10(17)11-2-4-12(5-3-11)16(21)20-14-7-9-19-15-13(14)6-8-18-15/h2-10H,17H2,1H3,(H2,18,19,20,21)/t10-/m1/s1
InChi Key
JTVBXQAYBIJXRP-SNVBAGLBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $86

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    Product Description

    Y-33075 is an inhibitor of Rho-associated kinase 2 (ROCK2; IC50 = 3.6 nM).1 It is selective for ROCK2 over PKC and calcium/calmodulin-dependent protein kinase II (CaMKII; IC50s = 420 and 810 nM, respectively). Topical application of Y-33075 (0.05% v/v) reduces intraocular pressure in rabbit and cynomolgus monkeys. Y-33075 (10 and 100 µM) increases axonal regeneration at the crush site in a cat model of surgically-induced optic nerve damage.2 It also inhibits demyelination and reduces the incidence of relapse episodes in a mouse model of chronic relapsing experimental autoimmune encephalomyelitis (EAE).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tokushige, H., Inatani, M., Nemoto, S., 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. 48(7), 3216-3222 (2007).

    2. Sagawa, H., Terasaki, H., Nakamura, M., et al. A novel ROCK inhibitor, Y-39983, promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult cats. Exp. Neurol. 205(1), 230-240 (2007).

    3. Gao, C., Huang, L., Long, Y., et al. Y-39983, a selective Rho-kinase inhibitor, attenuates experimental autoimmune encephalomyelitis via inhibition of demyelination. Neuroimmunomodulation 20(6), 334-340 (2013).