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

General Information of Drug (ID: DMWZJG6)

Drug Name

K00248 Drug Info

Synonyms

PKCbeta Inhibitor; 257879-35-9; K00248; CHEMBL366266; 3-(1-(3-Imidazol-1-ylpropyl)-1H-indol-3-yl)-4-anilino-1H-pyrrole-2,5-dione; PKC Inhibitor; AC1O4WCS; SCHEMBL7841474; GTPL6025; CHEBI:94140; CTK8F0351; DTXSID20423555; HMS3229K09; BDBM50153461; IN1136; CCG-206785; RT-015068; J-016132; BRD-K89687904-001-01-8; 3-anilino-4-[1-(3-imidazol-1-ylpropyl)indol-3-yl]pyrrole-2,5-dione; 3-[1-[3-(1H-Imidazole-1-yl)propyl]-1H-indole-3-yl]-4-anilino-1H-pyrrole-2,5-dione

Indication

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

Cross-matching ID

PubChem CID: 6419755
ChEBI ID: CHEBI:94140
CAS Number: CAS 257879-35-9
TTD Drug ID: DMWZJG6

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Protein kinase C beta (PRKCB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[3]
RUBOXISTAURIN HYDROCHLORIDE	DMQOCD8	Lymphoma	2A80-2A86	Phase 3	[4]
Sotrastaurin acetate	DME53YS	Renal transplantation	NE84	Phase 2	[5]
LY333531	DMGMC8H	Solid tumour/cancer	2A00-2F9Z	Phase 2	[6]
MS-553	DM7ER9J	Chronic lymphocytic leukaemia	2A82.0	Phase 1	[7]
Linetastine	DMF8B62	Rhinitis	FA20	Discontinued in Phase 2	[8]
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[9]
RO-320432	DMFZ1YW	N. A.	N. A.	Terminated	[10]
LY-317644	DMM20PI	N. A.	N. A.	Terminated	[11]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[12]
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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
Protein kinase C beta (PRKCB)	TTYPXQF	KPCB_HUMAN	Inhibitor	[2]

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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: 6025).
2	Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.
3	The oral protein-kinase C beta inhibitor enzastaurin (LY317615) suppresses signalling through the AKT pathway, inhibits proliferation and induces apoptosis in multiple myeloma cell lines. Leuk Lymphoma. 2008 Jul;49(7):1374-83.
4	Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-9.
5	Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
6	Protein kinase C beta inhibition attenuates the progression of experimental diabetic nephropathy in the presence of continued hypertension. Diabetes. 2003 Feb;52(2):512-8.
7	ClinicalTrials.gov (NCT03492125) A Study Of The Selective PKC-beta Inhibitor MS- 553. U.S. National Institutes of Health.
8	Potential new medical therapies for diabetic retinopathy: protein kinase C inhibitors. Am J Ophthalmol. 2002 May;133(5):693-8.
9	Evaluation of differential hypoxic cytotoxicity and electrochemical studies of nitro 5-deazaflavins, Bioorg. Med. Chem. Lett. 5(18):2155-2160 (1995).
10	Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain, Bioorg. Med. Chem. Lett. 4(11):1303-1308 (1994).
11	Synthesis of bisindolylmaleimide macrocycles, Bioorg. Med. Chem. Lett. 5(18):2093-2096 (1995).
12	Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.