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Go 6983 - 10mM in DMSO, high purity , CAS No.133053-19-7(DMSO), Inhibitor of protein kinase C alpha;Inhibitor of protein kinase C beta;Inhibitor of protein kinase C delta;Inhibitor of protein kinase C gamma;Inhibitor of protein kinase C zeta

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Item Number
G408092
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G408092-1ml
1ml
Available within 8-12 weeks(?)
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$253.90

PKC Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms GOE 6983, Gö 6983 | 1H-Pyrrole-2,5-dione, 3-[1-[3-(dimethylamino)propyl]-5-methoxy-1H-indol-3-yl]-4-(1H-indol-3-yl)-
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms Go 6983 (GOE 6983, Gö 6983) 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; less potent to PKCζ and inactive to PKCμ.
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of protein kinase C alpha;Inhibitor of protein kinase C beta;Inhibitor of protein kinase C delta;Inhibitor of protein kinase C gamma;Inhibitor of protein kinase C zeta
Product Description

Information

Go 6983 Go 6983 (GOE 6983, Gö 6983) 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; less potent to PKCζ and inactive to PKCμ.
In vitro

Go 6983 (300 μM) suppresses PKCμ auto-phosphorylation by 20% reduction in NIH3T3 transfected with PKCμ. In hearts reperfused with PMNs and Gö 6983 (100 nM), left ventricular developed pressure (LVDP) and the rate of LVDP recoveres to 89% and 74% of baseline values, respectively, significantly higher than PMNs alone. Gö 6983 (100 nM) significantly reduces PMNs adherence to the endothelium and infiltration into the myocardium compared with Ischemia followed by reperfusion (I/R)+ PMN hearts, and significantly inhibits superoxide release from PMNs by 90%. Gö 6983 attenuates post-I/R cardiac contractile dysfunction in the presence of PMNs, which may be related in part to decreased superoxide production. Gö 6983 significantly inhibits antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. Go 6983 inhibited intracellular Ca(2+) accumulation in human vascular tissue, suggesting a mechanism for its vasodilator properties. Go-6983 (1 μM) combined with Ro-31-8425 (390 nM) slightly inhibits Angiotensin II–induced PLD2 activity in PGSMCs. Go 6983 is isoform-specific PKC inhibitor that target the ATP binding site. Go 6983 inhibits ΔPfPKB activity with an IC50 of 1 μM. In Go 6983 (5 μM)-treated cells, the number of rings in the following cycle is markedly less compared with the control cultures. Go 6983 (5 μM) treatment results in an almost 60% decrease in formation of new rings in P. falciparum cultures.

In vivo

Go6983 (22.0 μg/mouse, i.v.) strongly inhibits tumor metastasis by 51.2 % in a mouse pulmonary B16BL6 tumor model.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥96%

Product Properties

ALogP 3.54
hba_count 3
HBD Count 2
Rotatable Bond 7

Associated Targets(Human)

PRKCZ Tchem Protein kinase C zeta type (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKCD Tclin Protein kinase C delta type (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKCB Tchem Protein kinase C beta type (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKCG Tchem Protein kinase C gamma type (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKCA Tchem Protein kinase C alpha type (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles COC1=CC=C2[N](CCCN(C)C)C=C(C2=C1)C3=C(C(=O)NC3=O)C4=C[NH]C5=C4C=CC=C5
Molecular Weight 442.51
Reaxy-Rn 8592990
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8592990&ln=

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility 59
DMSO(mM) Max Solubility 133.33
Water(mg / mL) Max Solubility <1

Solution Calculators

Reviews

Customer Reviews

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