H-89 dihydrochloride CAS: 130964-39-5
MF: C20H20BrN3O2S•2HCl
MW: 519.28
A potent, cell-permeable and reversible inhibitor of PKA.

H-89 dihydrochloride (CAS 130964-39-5)

H-89 dihydrochloride | CAS 130964-39-5 is rated 5.0 out of 5 by 1.
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Synonym: N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide 2HCl
Application: A potent, cell-permeable and reversible inhibitor of PKA
CAS Number: 130964-39-5
Purity: >99%
Molecular Weight: 519.28
Molecular Formula: C20H20BrN3O2S•2HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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H-89, Dihydrochloride is a cell-permeable, non-selective, reversible, ATP-competitive, potent inhibitor of PKA (cyclic AMP-dependent protein kinase). PKA regulates glycogen, sugar and lipid metabolism and plays an important role in the cell cycle. H-89, once thought to be a selective PKA inhibitor, has been shown to also inhibit CaM kinase II, casein kinase I, Rsk-2 (MAPKAP-K1b), MSK1, MYLK (myosin light chain kinase), Akt1 (PKB α), PKC μ, Rock-2 (ROCK-II) and p70 S6 kinase α.


References

1. Chijiwa, T., et al. 1990. J. Biol. Chem. 265: 5267-5272. PMID: 2156866
2. Engh, R.A., et al. 1996. J. Biol. Chem. 271: 26157-26164. PMID: 8824261
3. Davies, S.P., et al. 2000. Biochem. J. 351: 95-105. PMID: 10998351
4. Chase, A., et al. 2010. J Mol Cell Cardiol. PMID: 20188735
5. Menegaz, D., et al. 2010. J Steroid Biochem Mol Biol. PMID: 20156558

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mg/ml), ethanol (2 mg/ml (gentle warming)), water (poorly soluble), and methanol.
Storage :
Store at -20° C
IC50 :
ROCK-II: IC50 = 270 nM; S6K1: IC50 = 80 ; MSK1: IC50 = 120 ; PKA: IC50 = 135 ; PKBα: IC50 = 2600 ; MAPKAP-K1b: IC50 = 2800
Ki Data :
protein kinase A: Ki= 48 nM; CaM kinase II: Ki= 29.7 µM; casein kinase I : Ki= 38.3 µM; myosin light chain kinase: Ki= 28.3 µM; protein kinase C: Ki= 31.7 µM
pK Values :
pKa: 10.40 (Predicted), pKb: 7.72 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5702541
MDL Number :
MFCD11045926
SMILES :
C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNC/C=C/C3=CC=C(C=C3)Br.Cl.Cl

Download SDS (MSDS)

Certificate of Analysis

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H-89 dihydrochloride  Product Citations

See how others have used H-89 dihydrochloride. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 35 total

PMID: # 31059522  Paul, P.|Ramachandran, S.|Xia, S.|Unruh, JR.|Conkright-Fincham, J.|Li, R.| et al. 2019. PLoS ONE. 14: e0216220.

PMID: # 30809021  Ferretti, AC.|Hidalgo, F.|Tonucci, FM.|Almada, E.|Pariani, A.|Larocca, MC.|Favre, C.| et al. 2019. Sci Rep. 9: 2815.

PMID: # 29491159  Riva, L.|Song, OR.|Prentoe, J.|Helle, F.|L'homme, L.|Gattolliat, CH.|Vandeputte, A.|Fénéant, L.|Belouzard, S.|Baumert, TF.|Asselah, T.|Bukh, J.|Brodin, P.|Cocquerel, L.|Rouillé, Y.|Dubuisson, J.| et al. 2018. J. Virol. 92:

PMID: # 29249556  Wu, HY. et al. 2018. J. Neuroimmunol. 316: 17-22.

PMID: # 29638041  Choi, M. et al. 2018. IUBMB Life. 70: 563-573.

PMID: # 28099152  Jelinic, P. et al. 2017. Oncotarget. 8: 13792-13804.

PMID: # 28379541  Aslani, F. et al. 2017. Mol. Hum. Reprod. 23: 370-380.

PMID: # 27431894  Choi, JH.|Kim, SW.|Yu, R.|Yun, JW.| et al. 2017. Eur J Nutr. 56: 2329-2341.

PMID: # 28327597  Li, TF. et al. 2017. Sci Rep. 7: 45056.

PMID: # 28036359  Estep, CM. et al. 2016. PLoS ONE. 11: e0169044.

Citations 1 to 10 of 35 total
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Rated 5 out of 5 by from Guan Guan, et. al. (PubMed ID 19136032) used H-89, a PKA inhibitor, to study the binding activity of CREB and DNA of HBECs promoted by VIP. -SCBT Publication Review
Date published: 2015-04-01
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