An inhibitor of PKG, PKA, MLCK, and PKC
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HA-1004

Item No. 45680

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[(aminoiminomethyl)amino]ethyl]-5-isoquinolinesulfonamide
CAS Number
91742-10-8
Molecular Formula
C12H15N5O2S
Formula Weight
293.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/mlPBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml
SMILES
O=S(NCCNC(N)=N)(C1=CC=CC2=C1C=CN=C2)=O
InChi Code
InChI=1S/C12H15N5O2S/c13-12(14)16-6-7-17-20(18,19)11-3-1-2-9-8-15-5-4-10(9)11/h1-5,8,17H,6-7H2,(H4,13,14,16)
InChi Key
MZNDNBFMSVMUCX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $209

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    5 mg

    $627

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    10 mg

    $941

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    Product Description

    HA-1004 is an inhibitor of PKG, PKA, myosin light-chain kinase (MLCK), and PKC (Kis = 1.3, 2.3, 70 and 18 µM, respectively, in cell-free assays).1 It induces relaxation of isolated rabbit aortic strips precontracted with histamine (Item No. 33828), serotonin (Item No. 14332), A23187 (Item No. 11016), angiotensin II (Item No. 17150), or prostaglandin F2α (Item No. 16010; EC50s = 0.32-0.63 µM), as well as phenylephrine (Item Nos. 18619 | 17205) with or without calcium (EC50s = 2.3 and 0.5 µM, respectively). HA-1004 also inhibits histamine-induced bronchoconstriction in guinea pigs without affecting blood pressure when administered intratracheally at a dose of 0.1 mg per animal.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hidaka, H., Inagaki, M., Kawamoto, S., et al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry 23(21), 5036-5041 (1984).

    2. Chapman, R.W., Tozzi, S., and Kreutner, W. Antibronchoconstrictor activity of the intracellular calcium antagonist HA 1004 in guinea pigs. Pharmacology 37(3), 187-194 (1988).