A ROCK1 and ROCK2 inhibitor
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TC-S 7001

Item No. 19129

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-N4-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,4-pyrimidinediamine
CAS Number
867017-68-3
Synonyms
  • Azaindole 1
Molecular Formula
C18H13ClF2N6O
Formula Weight
402.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleEthanol: Soluble
λmax
225, 266, 305, 311 nm
SMILES
ClC1=NC(N)=NC(NC2=CC(F)=C(OC3=CC=NC4=C3C(C)=CN4)C(F)=C2)=C1
InChi Code
InChI=1S/C18H13ClF2N6O/c1-8-7-24-17-15(8)12(2-3-23-17)28-16-10(20)4-9(5-11(16)21)25-14-6-13(19)26-18(22)27-14/h2-7H,1H3,(H,23,24)(H3,22,25,26,27)
InChi Key
NRSGWEVTVGZDFC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $129

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    1 mg

    $205

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    5 mg

    $574

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    Product Description

    TC-S 7001 is an inhibitor of Rho-associated kinase (ROCK; IC50s = 0.6 and 1.1 nM, respectively, for human ROCK1 and ROCK2).1 It is selective for ROCK over myosin light-chain kinase (MLCK) and zipper-interacting protein kinase (ZIP-kinase; IC50s = 7,400 and 4,100 nM, respectively), as well as 110 kinases in a panel at 1-10 µM, but does inhibit TRK and FLT3 (IC50s = 252 and 303 nM, respectively). TC-S 7001 reduces ROCK2-induced phosphorylation of human myosin-binding subunit (MBS) when used at a concentration of 3 nM and decreases ROCK2 autophosphorylation. It inhibits contraction of isolated rabbit saphenous artery induced by phenylephrine (IC50 = 65 nM) and decreases blood pressure in normotensive and hypertensive rats when administered at doses of 3 and 10 mg/kg. TC-S 7001 also decreases right ventricular systolic pressure and total pulmonary resistance in a rat model of monocrotaline-induced pulmonary hypertension when administered at a dose of 10 mg/kg per day.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kast, R., Schirok, H., Figueroa-Pérez, S., et al. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br. J. Pharmacol. 152(7), 1070-1080 (2007).

    2. Dahal, B.K., Kosanovic, D., Pamarthi, P.K., et al. Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension. Eur. Respir. J. 36(4), 808-818 (2010).