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Chemical Structure| 130964-39-5 Chemical Structure| 130964-39-5

Structure of H-89 2HCl
CAS No.: 130964-39-5

Chemical Structure| 130964-39-5

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H-89 dihydrochloride proves to be a potent and selective inhibitor of protein kinase A (PKA), featuring an IC50 of 48 nM, and exhibits weak inhibition on PKG, PKC, and Casein Kinase.

Synonyms: H-89 (hydrochloride); Protein Kinase Inhibitor H-89; 5-Isoquinolinesulfonamide

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Product Details of H-89 2HCl

CAS No. :130964-39-5
Formula : C20H22BrCl2N3O2S
M.W : 519.28
SMILES Code : O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.[H]Cl.[H]Cl
Synonyms :
H-89 (hydrochloride); Protein Kinase Inhibitor H-89; 5-Isoquinolinesulfonamide
MDL No. :MFCD00214120
InChI Key :GELOGQJVGPIKAM-WTVBWJGASA-N
Pubchem ID :5702541

Safety of H-89 2HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of H-89 2HCl

epigenetics
DNA
Hedgehog

Isoform Comparison

Biological Activity

Target
  • PKA

    PKA, Ki:48 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
GluTag L-cells 10 μM 30 min inhibited PKA activity, thereby abrogating H-89-induced GLP-1 secretion Mol Nutr Food Res. 2020 Mar;64(6):e1900978.
Sf9 cells 60 µM 1 h H89 2HCl significantly inhibited PKA activity in Sf9 cells and reduced cell tolerance to permethrin. Int J Mol Sci. 2019 Sep 3;20(17):4300.
TF-1 cells 10 μM 1 h Inhibition of PKA activity to study its effect on CREB-1 phosphorylation. Results showed that H-89 significantly inhibited forskolin-induced nuclear accumulation of pCREB-1, indicating that PKA plays a central role in the cAMP-PKA-pCREB network. Biomed Pharmacother. 2011 Jul;65(4):293-7.
TF-1 cells 10 μM 15 h Study the effect of PKA inhibition on CCR5 transcription. Results showed that H-89 significantly inhibited forskolin-induced increase in CCR5 mRNA levels, indicating that PKA acts in concert with CREB to modulate cAMP-mediated CCR5 transcription. Biomed Pharmacother. 2011 Jul;65(4):293-7.
Human Umbilical Vein Endothelial Cells (HUVEC) 20 μM 30 min Inhibited PKA phosphorylation, thereby inhibiting eNOS Ser1177 phosphorylation Cells. 2019 Apr 27;8(5):388.
rat neocortical neurons 10 μM 40 min Inhibition of PKA activity, preventing PTX-induced hyperphosphorylation of Shank3 S1615 Elife. 2022 Apr 26;11:e74277.
COX-2 KO and control cells 10 µM 6 days To study the role of H-89 in COX-2 KO and control cells, it was found that H-89 attenuated the suppressing effect of PGE2 on adipocyte differentiation. Cells. 2022 Jun 2;11(11):1819.
bone marrow-derived macrophages (BMDMs) 20 μM 1 h To investigate whether db-cAMP-induced macrophage polarization is dependent on PKA.The results showed that pre-treatment with H89 inhibited db-cAMP-induced Arg-1 and CD206 expression and IL-10 levels, suggesting that PKA is involved in db-cAMP-induced macrophage polarization Cells. 2020 Jan 6;9(1):128.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Culex quinquefasciatus HAmCqG8 and MAmCqG6 resistant mosquito larvae Water treatment 6.25, 12.5, 25, 50 µM Single treatment, lasting 24 hours H89 2HCl significantly reduced the resistance of mosquito larvae to permethrin. Int J Mol Sci. 2019 Sep 3;20(17):4300.
BALB/c mice LPS-induced pleurisy model Intrapleural injection 4 mg/kg Single injection, lasting 30 hours To investigate the effect of db-cAMP on macrophage polarization in vivo, results showed that db-cAMP decreased the number of LPS-induced M1 macrophages and increased the expression of engulfment-related molecules AnxA1 and CD36. Cells. 2020 Jan 6;9(1):128.
Mice Acute brain slices Intraperitoneal or subcutaneous injections 5 mg/kg Single injection, lasting 30 minutes H-89 pretreatment prevented the increase in mEPSC frequency and dendritic spine density induced by Drd1 agonist Elife. 2015 Nov 9;4:e10111
Mice High-fat diet-induced MAFL model Intraperitoneal injection 1 mg/kg Once daily for 8 weeks To evaluate the effect of H-89 on MAFL formation, the results showed that H-89 significantly improved hepatic steatosis and reduced ALT activity, and decreased the nuclear level of mature SREBP1c. Cell Rep Med. 2024 Mar 19;5(3):101477

Protocol

Bio Calculators
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0.19mL

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1.93mL

0.96mL

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1.93mL

References

 

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