HA-1004
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526339

CAS#: 91742-10-8

Description: HA-1004 is an inhibitor of PKA, cGKI, PKC, MYLK, and calcium channel protein.


Price and Availability

Size
Price

10mg
USD 190
Size
Price

20mg
USD 350
Size
Price

50mg
USD 650

HA-1004, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526339
Name: HA-1004
CAS#: 91742-10-8
Chemical Formula: C12H17Cl2N5O2S
Exact Mass: 365.048
Molecular Weight: 366.261
Elemental Analysis: C, 39.35; H, 4.68; Cl, 19.36; N, 19.12; O, 8.74; S, 8.75


Synonym: HA-1004

IUPAC/Chemical Name: N-(2-Guanidinoethyl)-5-isoquinolinesulfonamide Dihydrochloride

InChi Key: PMTUBVLLVFJRLK-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H15N5O2S.2ClH/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);2*1H

SMILES Code: O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC(N)=N)=O.[H]Cl.[H]Cl


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Almela P, García-Carmona JA, Martínez-Laorden E, Milanés MV, Laorden ML. Crosstalk between G protein-coupled receptors (GPCRs) and tyrosine kinase receptor (TXR) in the heart after morphine withdrawal. Front Pharmacol. 2013 Dec 27;4:164. doi: 10.3389/fphar.2013.00164. eCollection 2013. PubMed PMID: 24409147; PubMed Central PMCID: PMC3873507.

2: Villarruel EQ, Borda E, Sterin-Borda L, Orman B. Lidocaine-induced apoptosis of gingival fibroblasts: participation of cAMP and PKC activity. Cell Biol Int. 2011 Aug;35(8):783-8. doi: 10.1042/CBI20100200. PubMed PMID: 21047305.

3: Almela P, Atucha NM, Milanés MV, Laorden ML. Cross-talk between protein kinase A and mitogen-activated protein kinases signalling in the adaptive changes observed during morphine withdrawal in the heart. J Pharmacol Exp Ther. 2009 Sep;330(3):771-82. doi: 10.1124/jpet.109.154583. Epub 2009 Jun 30. PubMed PMID: 19567779.

4: Varga F, Rumpler M, Spitzer S, Karlic H, Klaushofer K. Osteocalcin attenuates T3- and increases vitamin D3-induced expression of MMP-13 in mouse osteoblasts. Endocr J. 2009;56(3):441-50. Epub 2009 Feb 18. PubMed PMID: 19225217.

5: Almela P, Victoria Milanés M, Luisa Laorden M. Tyrosine hydroxylase phosphorylation after naloxone-induced morphine withdrawal in the left ventricle. Basic Res Cardiol. 2009 Jul;104(4):366-76. doi: 10.1007/s00395-008-0768-2. Epub 2008 Dec 22. PubMed PMID: 19104749.

6: Almela P, Milanés M, Laorden M. The PKs PKA and ERK 1/2 are involved in phosphorylation of TH at Serine 40 and 31 during morphine withdrawal in rat hearts. Br J Pharmacol. 2008 Sep;155(1):73-83. doi: 10.1038/bjp.2008.224. Epub 2008 Jun 9. PubMed PMID: 18536752; PubMed Central PMCID: PMC2527841.

7: Almela P, Cerezo M, González-Cuello A, Milanés MV, Laorden ML. Differential involvement of 3', 5'-cyclic adenosine monophosphate-dependent protein kinase in regulation of Fos and tyrosine hydroxylase expression in the heart after naloxone induced morphine withdrawal. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):293-303. Epub 2006 Nov 25. PubMed PMID: 17216288.

8: Schach C, Xu M, Platoshyn O, Keller SH, Yuan JX. Thiol oxidation causes pulmonary vasodilation by activating K+ channels and inhibiting store-operated Ca2+ channels. Am J Physiol Lung Cell Mol Physiol. 2007 Mar;292(3):L685-98. Epub 2006 Nov 10. PubMed PMID: 17098807.

9: Ghosh M, Gharami K, Paul S, Das S. Thyroid hormone-induced morphological differentiation and maturation of astrocytes involves activation of protein kinase A and ERK signalling pathway. Eur J Neurosci. 2005 Oct;22(7):1609-17. PubMed PMID: 16197501.

10: Broccardo CJ, Billings RE, Andersen ME, Hanneman WH. Probing the control elements of the CYP1A1 switching module in H4IIE hepatoma cells. Toxicol Sci. 2005 Nov;88(1):82-94. Epub 2005 Aug 4. PubMed PMID: 16081525.

11: Kochel I, Rapak A, Ziolo E, Strzadala L. Nur77 nuclear import and its NBRE-binding activity in thymic lymphoma cells are regulated by different mechanisms sensitive to FK506 or HA1004. Biochem Biophys Res Commun. 2005 Sep 9;334(4):1102-6. PubMed PMID: 16051191.

12: Kubo T, Hagiwara Y. Protein kinase C activation-induced increases of neural activity are enhanced in the hypothalamus of spontaneously hypertensive rats. Brain Res. 2005 Feb 8;1033(2):157-63. PubMed PMID: 15694920.

13: Benavides M, Laorden ML, Milanés MV. Involvement of 3',5'-cyclic adenosine monophosphate-dependent protein kinase in regulation of Fos expression and tyrosine hydroxylase levels during morphine withdrawal in the hypothalamic paraventricular nucleus and medulla oblongata catecholaminergic cell groups. J Neurochem. 2005 Jan;92(2):246-54. PubMed PMID: 15663473.

14: Shen KZ, Johnson SW. Group II metabotropic glutamate receptor modulation of excitatory transmission in rat subthalamic nucleus. J Physiol. 2003 Dec 1;553(Pt 2):489-96. Epub 2003 Sep 18. PubMed PMID: 14500768; PubMed Central PMCID: PMC2343573.

15: Wainszelbaum MJ, Belaunzarán ML, Lammel EM, Florin-Christensen M, Florin-Christensen J, Isola EL. Free fatty acids induce cell differentiation to infective forms in Trypanosoma cruzi. Biochem J. 2003 Nov 1;375(Pt 3):705-12. PubMed PMID: 12887332; PubMed Central PMCID: PMC1223715.

16: Miyoshi K, Kawakami N, Horio S, Fukui H. Inhibition of histamine H1 receptor downregulation by KT5823, a protein kinase G inhibitor. Methods Find Exp Clin Pharmacol. 2003 Jun;25(5):343-7. PubMed PMID: 12851655.

17: Kalas W, Matuszyk J, Ziolo E, Strzadala L. FK506 restores sensitivity of thymic lymphomas to calcium-mediated apoptosis and the inducible expression of Fas ligand. Anticancer Res. 2003 Mar-Apr;23(2B):1613-7. PubMed PMID: 12820430.

18: Martínez MD, Milanés MV, Laorden ML. Implication of the signal transduction pathways in the enhancement of noradrenaline turnover induced by morphine withdrawal in the heart. Eur J Pharmacol. 2003 Jun 20;471(2):113-9. PubMed PMID: 12818698.

19: Cerezo M, Laorden ML, Milanés MV. Inhibition of protein kinase C but not protein kinase A attenuates morphine withdrawal excitation of rat hypothalamus-pituitary-adrenal axis. Eur J Pharmacol. 2002 Sep 27;452(1):57-66. PubMed PMID: 12323385.

20: Matuszyk J, Cebrat M, Kalas W, Strzadala L. HA1004, an inhibitor of serine/threonine protein kinases, restores the sensitivity of thymic lymphomas to Ca2+-mediated apoptosis through a protein kinase A-independent mechanism. Int Immunopharmacol. 2002 Mar;2(4):435-42. PubMed PMID: 11962723.