General Information of Drug (ID: DMOQJZC)

Drug Name
Bisindolylmaleimide-I Drug Info
Synonyms
Bisindolylmaleimide i; bisindolylmaleimide i; 133052-90-1; GF 109203X; GF109203X; Go 6850; GF-109203X; RBT205 INHIBITOR; Go-6850; UNII-L79H6N0V6C; 6850; Bisindolylmaleimide I (GF 109203X); CHEMBL7463; 3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE; 3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione; L79H6N0V6C; QMGUOJYZJKLOLH-UHFFFAOYSA-N; 2-[1-(3-dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl)maleimide; GF-109203; Go6850
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
2396
CAS Number
CAS 133052-90-1
TTD Drug ID
DMOQJZC
VARIDT Drug ID
DR00622

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Bacterial Lethal factor (Bact lef) TTIQSC1 LEF_BACAN Inhibitor [2]
Checkpoint kinase-1 (CHK1) TTTU902 CHK1_HUMAN Inhibitor [3]
Cyclin-dependent kinase 1 (CDK1) TTH6V3D CDK1_HUMAN Inhibitor [4]
Extracellular signal-regulated kinase 2 (ERK2) TT4TQBX MK01_HUMAN Inhibitor [3]
G2/mitotic-specific cyclin B1 (CCNB1) TT9P6OW CCNB1_HUMAN Inhibitor [4]
Glycogen synthase kinase-3 beta (GSK-3B) TTRSMW9 GSK3B_HUMAN Inhibitor [3]
LCK tyrosine protein kinase (LCK) TT860QF LCK_HUMAN Inhibitor [3]
MAP kinase p38 (MAPK12) TTYT93M MK12_HUMAN Inhibitor [3]
PKC-delta messenger RNA (PRKCD mRNA) TT7A1BO KPCD_HUMAN Inhibitor [5]
PKC-epsilon messenger RNA (PRKCE mRNA) TT57MT2 KPCE_HUMAN Inhibitor [5]
Protein kinase C (PRKC) TTYVX59 NOUNIPROTAC Inhibitor [6]
Protein kinase C gamma (PRKCG) TTRFOXJ KPCG_HUMAN Inhibitor [5]
Protein kinase C zeta (PRKCZ) TTUWGRA KPCZ_HUMAN Inhibitor [7]
RAC-alpha serine/threonine-protein kinase (AKT1) TTWTSCV AKT1_HUMAN Inhibitor [3]
Rho-associated protein kinase 1 (ROCK1) TTZN7RP ROCK1_HUMAN Inhibitor [3]
Serine/threonine-protein kinase Sgk1 (SGK1) TTTV8EJ SGK1_HUMAN Inhibitor [3]
Stress-activated protein kinase 2a (p38 alpha) TTQBR95 MK14_HUMAN Inhibitor [3]
Stress-activated protein kinase 2b (p38 beta) TT73U6C MK11_HUMAN Inhibitor [3]
Stress-activated protein kinase JNK1 (JNK1) TT0K6EO MK08_HUMAN Inhibitor [3]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
RAC-alpha serine/threonine-protein kinase (AKT1) DTT AKT1 7.399 7.276 7.816 6.959
Protein kinase C zeta (PRKCZ) DTT PRKCZ 3.935 6.204 5.503 7.245
Checkpoint kinase-1 (CHK1) DTT CHEK1 4.267 4.629 3.739 5.322
Glycogen synthase kinase-3 beta (GSK-3B) DTT GSK3B 6.506 6.618 6.514 6.885
Protein kinase C gamma (PRKCG) DTT PRKCG 2.104 0.848 0.678 1.848
Stress-activated protein kinase 2a (p38 alpha) DTT MAPK14 7.103 6.87 6.74 6.306
Cyclin-dependent kinase 1 (CDK1) DTT CDK1 2.036 5.914 4.781 5.914
LCK tyrosine protein kinase (LCK) DTT LCK 5.2 4.443 4.53 6.325
Stress-activated protein kinase 2b (p38 beta) DTT MAPK11 3.907 2.485 3.655 2.945
Extracellular signal-regulated kinase 2 (ERK2) DTT MAPK1 5.848 6.896 7.236 6.465
Stress-activated protein kinase JNK1 (JNK1) DTT MAPK8 2.667 5.044 5.196 2.644
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Discovery agent
ICD Disease Classification N.A.
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Glycogen synthase kinase-3 beta (GSK-3B) DTT GSK3B 1.26E-01 -0.23 -0.77
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

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: 5193).
2 Amiodarone and bepridil inhibit anthrax toxin entry into host cells. Antimicrob Agents Chemother. 2007 Jul;51(7):2403-11.
3 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
4 Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure. Bioorg Med Chem Lett. 1998 May 5;8(9):1019-22.
5 Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2... J Biol Chem. 2007 Nov 9;282(45):33052-63.
6 Protein kinase epsilon dampens the secretory response of model intestinal epithelia during ischemia. Surgery. 2001 Aug;130(2):310-8.
7 Protein kinase C zeta isoform is critical for proliferation in human glioblastoma cell lines. J Neurooncol. 2000 Apr;47(2):109-15.