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MedKoo Cat#: 540190 | Name: H8 dihydrochloride
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Description:

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

H8 dihydrochloride is a PKA inhibitor that modulates Ca 2+ signaling.

Chemical Structure

H8 dihydrochloride
H8 dihydrochloride
CAS#113276-94-1

Theoretical Analysis

MedKoo Cat#: 540190

Name: H8 dihydrochloride

CAS#: 113276-94-1

Chemical Formula: C12H17Cl2N3O2S

Exact Mass: 0.0000

Molecular Weight: 338.25

Elemental Analysis: C, 42.61; H, 5.07; Cl, 20.96; N, 12.42; O, 9.46; S, 9.48

Price and Availability

Size Price Availability Quantity
10mg USD 295.00 2 Weeks
25mg USD 550.00 2 Weeks
50mg USD 950.00 2 Weeks
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Synonym
H8; H 8; H-8; H8 dihydrochloride; H8 2HCl; H8 HCl; Protein Kinase Inhibitor H-8
IUPAC/Chemical Name
N-(2-(methylamino)ethyl)isoquinoline-5-sulfonamide dihydrochloride
InChi Key
RJJLZYZEVNCZIW-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H15N3O2S.2ClH/c1-13-7-8-15-18(16,17)12-4-2-3-10-9-14-6-5-11(10)12;;/h2-6,9,13,15H,7-8H2,1H3;2*1H
SMILES Code
O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC)=O.[H]Cl.[H]Cl
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).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
A potent, nonspecific kinase inhibitor.
In vitro activity:
H-8 was the most active of the inhibitors in this series and inhibited more markedly cyclic nucleotide dependent protein kinases, than other kinases, while the derivative with the sulfonylpiperazine residue (H-7) was the most potent in inhibiting protein kinase C. Reference: Biochemistry. 1984 Oct 9;23(21):5036-41. https://pubmed.ncbi.nlm.nih.gov/6238627/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 20.0 59.13
DMSO 20.0 59.13
PBS (pH 7.2) 10.0 29.56
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 338.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Hidaka H, Inagaki M, Kawamoto S, Sasaki Y. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984 Oct 9;23(21):5036-41. doi: 10.1021/bi00316a032. PMID: 6238627.
In vitro protocol:
1. Hidaka H, Inagaki M, Kawamoto S, Sasaki Y. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984 Oct 9;23(21):5036-41. doi: 10.1021/bi00316a032. PMID: 6238627.
In vivo protocol:
TBD
1: Niisato N, Ito Y, Marunaka Y. Effects of PKA inhibitors, H-compounds, on epithelial Na+ channels via PKA-independent mechanisms. Life Sci. 1999;65(10):PL109-14. PubMed PMID: 10499877. 2: Kraus D, Jäger A, Abuduwali N, Deschner J, Lossdörfer S. Intermittent PTH(1-34) signals through protein kinase A to regulate osteoprotegerin production in human periodontal ligament cells in vitro. Clin Oral Investig. 2012 Apr;16(2):611-8. doi: 10.1007/s00784-011-0541-z. Epub 2011 Mar 29. PubMed PMID: 22186940. 3: De Jonge HR, Tilly BC, Hogema BM, Pfau DJ, Kelley CA, Kelley MH, Melita AM, Morris MT, Viola RM, Forrest JN Jr. cGMP inhibition of type 3 phosphodiesterase is the major mechanism by which C-type natriuretic peptide activates CFTR in the shark rectal gland. Am J Physiol Cell Physiol. 2014 Feb 15;306(4):C343-53. doi: 10.1152/ajpcell.00326.2013. Epub 2013 Nov 20. PubMed PMID: 24259420; PubMed Central PMCID: PMC3919979. 4: Hirai H, Ikeuchi Y, Okada Y. The contribution of PKA to the excitatory mechanism of adenosine in guinea pig superior colliculus slices. Neurosci Lett. 1994 Nov 21;182(1):33-6. PubMed PMID: 7891883. 5: Murakami K, Arai T. [A selective inhibitor of cAMP-dependent protein kinase isolated from an alkalophilic strain of Bacillus species]. Nihon Saikingaku Zasshi. 1989 Nov;44(6):789-96. Japanese. PubMed PMID: 2621791. 6: Yonemaru M, Kasuga I, Kusumoto H, Kiyokawa H, Kuwabara S, Ichinose Y, Toyama K. Protein kinase inhibitor attenuates an increase in endothelial monolayer permeability induced by tumour necrosis factor-alpha. Respirology. 1997 Mar;2(1):63-9. PubMed PMID: 9424406. 7: Santhosh KT, Elkhateeb O, Nolette N, Outbih O, Halayko AJ, Dakshinamurti S. Milrinone attenuates thromboxane receptor-mediated hyperresponsiveness in hypoxic pulmonary arterial myocytes. Br J Pharmacol. 2011 Jul;163(6):1223-36. doi: 10.1111/j.1476-5381.2011.01306.x. PubMed PMID: 21385177; PubMed Central PMCID: PMC3144536. 8: Wolf M, Jäger A, Abuduwali N, Götz W, Lossdörfer S. Continuous PTH modulates alkaline phosphatase activity in human PDL cells via protein kinase C dependent pathways in vitro. Ann Anat. 2013 Oct;195(5):455-60. doi: 10.1016/j.aanat.2013.04.006. Epub 2013 May 13. PubMed PMID: 23742978. 9: Jarvis BW, Qureshi N. Inhibition of lipopolysaccharide-induced transcription factor Sp1 binding by spectrally pure diphosphoryl lipid A from Rhodobacter sphaeroides, protein kinase inhibitor H-8, and dexamethasone. Infect Immun. 1997 May;65(5):1640-3. PubMed PMID: 9125541; PubMed Central PMCID: PMC175189. 10: Gillette MA, Dacheux RF. Protein kinase modulation of GABAA currents in rabbit retinal rod bipolar cells. J Neurophysiol. 1996 Nov;76(5):3070-86. PubMed PMID: 8930256. 11: Xiao Gh, Falkner KC, Xie Y, Lindahl RG, Prough RA. cAMP-dependent negative regulation of rat aldehyde dehydrogenase class 3 gene expression. J Biol Chem. 1997 Feb 7;272(6):3238-45. PubMed PMID: 9013560. 12: Zhang W, Han XY, Wong SM, Takeuchi H. Effects of inhibitors for intracellular signal transduction systems on the inward current produced by GABA in a snail neuron. Gen Pharmacol. 1998 Feb;30(2):221-5. PubMed PMID: 9502177. 13: Maggi CA, Santicioli P, Giuliani S. Protein kinase A inhibitors selectively inhibit the tonic contraction of the guinea pig ureter to high potassium. Gen Pharmacol. 1996 Mar;27(2):341-8. PubMed PMID: 8919654. 14: Selvaraj NG, Prasad R, Goldstein JL, Rao MC. Evidence for the presence of cGMP-dependent protein kinase-II in human distal colon and in T84, the colonic cell line. Biochim Biophys Acta. 2000 Oct 20;1498(1):32-43. PubMed PMID: 11042348. 15: Wang H, Ye Y, Zhu M, Cho C. Increased interleukin-8 expression by cigarette smoke extract in endothelial cells. Environ Toxicol Pharmacol. 2000 Dec;9(1-2):19-23. PubMed PMID: 11137464. 16: Motoyashiki T, Morita T, Ueki H. Involvement of the rapid increase in cAMP content in the vanadate-stimulated release of lipoprotein lipase activity from rat fat pads. Biol Pharm Bull. 1996 Nov;19(11):1412-6. PubMed PMID: 8951155. 17: Poueymirou WT, Schultz RM. Regulation of mouse preimplantation development: inhibition of synthesis of proteins in the two-cell embryo that require transcription by inhibitors of cAMP-dependent protein kinase. Dev Biol. 1989 Jun;133(2):588-99. PubMed PMID: 2543602. 18: Lee YS, Chuong CM. Activation of protein kinase A is a pivotal step involved in both BMP-2- and cyclic AMP-induced chondrogenesis. J Cell Physiol. 1997 Feb;170(2):153-65. PubMed PMID: 9009144. 19: Gwosdow AR, O'Connell NA, Abou-Samra AB. Interleukin-1 increases protein kinase A activity by a cAMP-independent mechanism in AtT-20 cells. Am J Physiol. 1994 Jan;266(1 Pt 1):E79-84. PubMed PMID: 7508195. 20: Chen CC, Chiu KT, Sun YT, Chen WC. Role of the cyclic AMP-protein kinase A pathway in lipopolysaccharide-induced nitric oxide synthase expression in RAW 264.7 macrophages. Involvement of cyclooxygenase-2. J Biol Chem. 1999 Oct 29;274(44):31559-64. PubMed PMID: 10531359.