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Chemical Structure| 133053-19-7 Chemical Structure| 133053-19-7

Structure of Go 6983
CAS No.: 133053-19-7

Chemical Structure| 133053-19-7

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Go6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively and less potent to PKCζ and inactive to PKCμ.

Synonyms: Goe 6983; Go6983 Go-6983

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Product Details of Go 6983

CAS No. :133053-19-7
Formula : C26H26N4O3
M.W : 442.51
SMILES Code : O=C(C(C1=CN(CCCN(C)C)C2=C1C=C(OC)C=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O
Synonyms :
Goe 6983; Go6983 Go-6983
MDL No. :MFCD04040031
InChI Key :LLJJDLHGZUOMQP-UHFFFAOYSA-N
Pubchem ID :3499

Safety of Go 6983

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Go 6983

epigenetics
GPCR

Isoform Comparison

Biological Activity

Target
  • PKCβ

    PKCβ, IC50:7 nM

  • PKCγ

    PKCγ, IC50:6 nM

  • PKCζ

    PKCζ, IC50:60 nM

  • PKCα

    PKCα, IC50:7 nM

  • PKCδ

    PKCδ, IC50:10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
BT-474 cells 2 μM Gö6983 completely blocked PMA-induced down-regulation of P-Rex1 protein expression and suppressed PMA inhibition of BT-474 cell growth. PMC4887325
MCF-7 cells 2 μM Gö6983 completely blocked PMA-induced down-regulation of P-Rex1 protein expression and suppressed PMA inhibition of MCF-7 cell growth. PMC4887325
Primary mouse hepatocytes 10 μM 2 h To investigate the protective effect of Go 6983 against APAP-induced cytotoxicity. Results showed that Go 6983 protected hepatocytes from APAP-induced necrosis through a JNK-independent pathway. PMC3997165
HepG2 cells 10 μM 6 h To investigate the effect of Go 6983 on MG132-induced LDLR transcription increase, it was found that Go 6983 completely abolished the increase in LDLR transcription induced by short-term treatment with MG132 (0-6 h). PMC4125719
SH-SY5Y cells 1 μM 10 min Go 6983 completely blocked CCh-induced MARCKS phosphorylation and reduced the stimulation of ERK1/2 phosphorylation by CCh, indicating that PKC plays an important role in the anti-apoptotic effect of CCh. PMC5055140
Rat hippocampal CA1 region slices 10 µM 60 min To investigate the effect of Go 6983 on DHPG-induced long-term depression (LTD), results showed that Go 6983 had no effect on basal synaptic transmission or DHPG-induced LTD. PMC1572644
Rat hepatocytes 10 μM 1 h To investigate the effect of Go 6983 on the activity of PKCD/p38 and PKCD/JNK signaling pathways, the results showed that Go 6983 significantly inhibited the phosphorylation of PKCD, thereby inhibiting the phosphorylation of p38 and JNK. PMC6528867
COS-7 cells 2.5 µM 1 h Go 6983 potently blocked rapid PKD catalytic activation in response to bombesin, but the inhibitory effect was significantly diminished at later times (45 min), indicating that PKD activation proceeds through early PKC-dependent and late PKC-independent mechanisms. PMC2442337
Retinal venules 10 μM 30 min To evaluate the role of PKC in ET-1-induced constriction of retinal venules, results showed that Go 6983 did not significantly affect basal tone or ET-1-induced constriction. PMC8576499

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Long-Evans rats Alcohol withdrawal model Intra-LHb infusion 5 ng/200 nl/side Single injection Go-6983 alleviates anxiety- and depression-like behaviors associated with alcohol withdrawal by inhibiting PKC-γ and downregulating βCaMKII-AMPAR signaling PMC10516930

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.30mL

2.26mL

1.13mL

22.60mL

4.52mL

2.26mL

 

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