HA-100 dihydrochlorideAn inhibitor of MYLK, PKA, and PKC

HA-100 dihydrochloride (CAS 84468-24-6)

HA-100 dihydrochloride | CAS 84468-24-6 is rated 5.0 out of 5 by 1.
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Synonym: 1-(5-Isoquinolinylsulfonyl)piperazine . 2HCl
Application: An inhibitor of MYLK, PKA, and PKC
CAS Number: 84468-24-6
Purity: ≥98%
Molecular Weight: 350.26
Molecular Formula: C13H15N3O2S•2HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 µM, respectively). It less effectively blocks the activity of myosin light chain kinase (IC50 = 240 µM).


References

1. Hagiwara, M., et al., 1987. Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives. Molecular pharmacology. 32(1): 7-12. PMID: 2955213
2. Gerard, C., et al., 1986. Role of protein kinases in stimulation of human polymorphonuclear leukocyte oxidative metabolism by various agonists. Differential effects of a novel protein kinase inhibitor. The Journal of clinical investigation. 77(1): 61-5. PMID: 3003155

Physical State :
Solid
Solubility :
Soluble in water (10 mg/ml), and DMSO (35 mg/ml).
Storage :
Store at 4° C
Boiling Point :
537.7° C at 760 mmHg (Predicted)
Refractive Index :
n20D ~1.64 (Predicted)
IC50 :
Plasmodium falciparum: IC50 = 4.3 µM; cAMP-dependent protein kinase : IC50 = 6 µM (human); Protein kinase C : IC50 = 12 µM (human); Protein kinase Pfmrk: IC50 >0.5 mM (Plasmodium falciparum)
Ki Data :
Adenosine A3-R: Ki= 25 µM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
TM0862600
PubChem CID :
13135529
MDL Number :
MFCD01310980
SMILES :
C1CN(CCN1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl.Cl

Download SDS (MSDS)

Certificate of Analysis

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HA-100 dihydrochloride  Product Citations

See how others have used HA-100 dihydrochloride. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 27 total

PMID: # 31419739  Wang, X.|Malinowski, AR.|Beckenbauer, J.|Siehler, J.|Blöchinger, A.|Meitinger, T.|Häring, HU.|Staiger, H.|Burtscher, I.|Lickert, H.| et al. 2019. Stem Cell Res. 39: 101531.

PMID: # 29681516  2018. Cell Stem Cell. 22: 698-712.e9.

PMID: # 29396371  Wang, X.|Sterr, M.|Burtscher, I.|Chen, S.|Hieronimus, A.|Machicao, F.|Staiger, H.|Häring, HU.|Lederer, G.|Meitinger, T.|Cernilogar, FM.|Schotta, G.|Irmler, M.|Beckers, J.|Hrabě de Angelis, M.|Ray, M.|Wright, CVE.|Bakhti, M.|Lickert, H.| et al. 2018. Mol Metab. 9: 57-68.

PMID: # 28287393  Zaritsky, A. et al. 2017. Elife. 6:

PMID: # 24677069  Liu, G. et al. 2014. Molecular neurobiology. 50: 673-84.

PMID: # 22132178  Mack, AA. et al. 2011. PLoS ONE. 6: e27956.

PMID: # 21390254  Yu, J. et al. 2011. PLoS ONE. 6: e17557.

PMID: # 2185457  Nucleic Acids Res. 18 Suppl: 2549-87.

PMID: # 3316711  J. Virol. 61: 4019-22.

PMID: # 3260631  J. Virol. 62: 2578-86.

Citations 1 to 10 of 27 total

Is there any other solubility information available?

Asked by: SCchem16
Thank you for your question. This chemical, HA-100 dihydrochloride (CAS 84468-24-6), is also soluble at ~0.5 mg/ml in 1:1 DMF:PBS (pH 7.2).
Answered by: Chemical Support 2
Date published: 2017-02-24
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Rated 5 out of 5 by from Gerard Gerard, et al. (PubMed ID 3003155) produced this compound [also known as 1-(5-Isoquinolinylsulfonyl)piperazine or C-I] in lab and characterized it by NMR, MS and IR. Gerard also investigated C-I in terms of its capability of inhibiting the response of human PMN's to PMA exposure. -SCBT Publication Review
Date published: 2015-07-18
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