Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM80QF9)

Drug Name

H-8 Drug Info

Synonyms

84478-11-5; Protein kinase inhibitor H-8; h-8; H-8 Protein kinase inhibitor; N-(2-(Methylamino)ethyl)-5-isoquinolinesulfonamide; N-[2-(METHYLAMINO)ETHYL]-5-ISOQUINOLINESULFONAMIDE; N-[2-(methylamino)ethyl]isoquinoline-5-sulfonamide; (5-Isoquinolylsulfonyl)[2-(methylamino)ethyl]amine; Lopac-M-9656; CHEMBL148333; CHEBI:43561; H8; N-(2-methylaminoethyl)isoquinoline-5-sulfonamide; (5-Isoquinolylsulfonyl)(2-(methylamino)ethyl)amine; 5-Isoquinolinesulfonamide, N-(2-(methylamino)ethyl)-; N-(2-(Methylamino)ethyl)isoquinoline- 5-s

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

Cross-matching ID

PubChem CID: 3540
ChEBI ID: CHEBI:43561
CAS Number: CAS 84478-11-5
TTD Drug ID: DM80QF9

Molecule-Related Drug Atlas

Molecule Type:

DTT

DOT

Drug Status:

Clinical Trial Drug(s)

Investigative Drug(s)

Approved Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Cyclic nucleotide-gated channel alpha-1 (CNGA1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
dequalinium	DMXM19W	Myelopathy	8B42	Clinical trial	[4]
L-(cis)-diltiazem	DMK07MI	Discovery agent	N.A.	Investigative	[5]
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Drug(s) Affected By DNA-directed RNA polymerase II subunit RPB1 (POLR2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selenium	DM25CGV	N. A.	N. A.	Approved	[6]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[7]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[3]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[8]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[9]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[10]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[11]
Deferasirox	DM6ETS0	Beta thalassemia	3A50.2	Approved	[12]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[13]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[14]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cyclic nucleotide-gated channel alpha-1 (CNGA1)	TTHIQMC	CNGA1_HUMAN	Blocker (channel blocker)	[2]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
DNA-directed RNA polymerase II subunit RPB1 (POLR2A)	OTHJQ1DZ	RPB1_HUMAN	Post-Translational Modifications	[3]

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References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2348).
2	Direct blockade of both cloned rat rod photoreceptor cyclic nucleotide-gated non-selective cation (CNG) channel alpha-subunit and native CNG channels from Xenopus rod outer segments by H-8, a non-specific cyclic nucleotide-dependent protein kinase inhibitor. Neurosci Lett. 1997 Sep 12;233(1):37-40.
3	Phosphorylation of the RNA polymerase II largest subunit during heat shock and inhibition of transcription in HeLa cells. J Cell Physiol. 1994 Mar;158(3):417-26. doi: 10.1002/jcp.1041580305.
4	Dequalinium: a novel, high-affinity blocker of CNGA1 channels. J Gen Physiol. 2003 Jan;121(1):37-47.
5	A new subunit of the cyclic nucleotide-gated cation channel in retinal rods. Nature. 1993 Apr 22;362(6422):764-7.
6	Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
7	Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
8	Quantitative phosphoproteomics reveal cellular responses from caffeine, coumarin and quercetin in treated HepG2 cells. Toxicol Appl Pharmacol. 2022 Aug 15;449:116110. doi: 10.1016/j.taap.2022.116110. Epub 2022 Jun 7.
9	Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells. Mol Cancer Ther. 2014 May;13(5):1142-54.
10	Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
11	Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
12	Iron chelators ICL670 and 311 inhibit HIV-1 transcription. Virology. 2007 Oct 25;367(2):324-33. doi: 10.1016/j.virol.2007.06.011. Epub 2007 Jul 13.
13	Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
14	Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.