Catalog Number
ACM136194779
Description
GO 6976, also known as PD-406976, is a potent inhibitor of neurotrophin-receptor intrinsic tyrosine kinase. Gö 6976 blocked neurotrophin-induced signaling and autophosphorylation of neurotrophin-specific tyrosine kinase (Trk) receptors, either Trk B in cortical neurons or Trk A in GT1-1-trk9 cells.
Synonyms
GO6976; GO-6976; GO 6976; PD406976; PD 406976; PD-406976
IUPAC Name
3-(13-methyl-5-oxo-6,7-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12(13H)-yl)propanenitrile
Molecular Formula
C24H18N4O
Canonical SMILES
N#CCCN(C1=C2C(CNC3=O)=C3C4=C1N(C)C5=C4C=CC=C5)C6=C2C=CC=C6
InChI
InChI=1S/C24H18N4O/c1-27-17-9-4-2-7-14(17)20-21-16(13-26-24(21)29)19-15-8-3-5-10-18(15)28(12-6-11-25)23(19)22(20)27/h2-5,7-10H,6,12-13H2,1H3,(H,26,29)
InChI Key
VWVYILCFSYNJHF-UHFFFAOYSA-N
Solubility
Soluble in DMSO, not in water
Appearance
White solid powder
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
Go6976 is a Protein Kinase C (PKC) inhibitor, with an IC50 of 20 nM.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 76.17; H, 4.79; N, 14.81; O, 4.23
HS Tariff Code
2934.99.9001
In Vitro Activity
In vitro experiments were conducted to explore the effect of Gö6976 on leukemia cells. The CCK-8 assay results showed that the optical density (OD) of K562 cells in the Gö6976 groups was decreased at 24, 48 and 72 h compared with that in the control group. To further explore whether Gö6976 affects the anti-CML effect of TKIs, imatinib was added for the study. At the same time, the proliferation of K562 cells in the groups treated with imatinib and Gö6976 was more inhibited than in the group treated with imatinib alone, and the difference was statistically significant. The above results indicate that Gö6976 has a significant inhibitory effect on the growth of K562 cells and can enhance the sensitivity of K562 cells to imatinib.
Reference: Hematology. 2021 Dec;26(1):543-551. https://pubmed.ncbi.nlm.nih.gov/34348586/
In Vivo Activity
To explore the effects of Gö6976 in the body, a mouse model of CML was created. Mice began to develop leukemic symptoms at approximately 3 weeks after injection of tumor cells. Compared with the control group, the mice in the Gö6976 group had significantly less weight loss 5 weeks after injection. The number of WBCs in the 2.5 mg/kg Gö6976 group was significantly decreased compared with that in the control group from the 3rd to the 5th weeks. At the fourth week, the CD45+ leukemia cells in the 2.5 mg/kg Gö6976 group were significantly fewer than those in the control group. The survival time of the mice in the 2.5 mg/kg Gö6976 group was significantly longer than that of the mice in the control group. In summary, Gö6976 can directly inhibit the progression of CML and effectively increase the survival rate of mice.
Reference: Hematology. 2021 Dec;26(1):543-551. https://pubmed.ncbi.nlm.nih.gov/34348586/
Shipping
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.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
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