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GSK690693 - 10mM in DMSO, high purity , CAS No.937174-76-0(DMSO), Protein kinase C (PKC) inhibitor

COA COA
In stock
Item Number
G409035
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Availability
 Price Qty
G409035-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$269.90
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Akt2 Selective Inhibitors

View related series
Compound libraries (12325)

Basic Description

Synonyms 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-((S)-piperidin-3-ylmethoxy)-1H-imidazo[4,5-c]pyridin-4-yl)-2-methylbut-3-yn-2-ol
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50
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 Protein kinase C (PKC) inhibitor
Product Description

Information

GSK690693 is a pan-Akt inhibitor targetingAkt1/2/3withIC50of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibitsAMPKandDAPK3from the CAMK family with IC50 of 50 nM and
In vitro

GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50 of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50 of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50 ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations >100 nM in both LNCaP and BT474 cells. Consistent with the role of AKT in cell survival, GSK690693 induces apoptosis in sensitive ALL cell lines.

In vivo

A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day. GSK690693 exhibits efficacy irrespective of the mechanism of Akt activation involved. GSK690693 is most effective in delaying tumor progression in Lck-MyrAkt2 mice expressing a membrane-bound, constitutively active form of Akt.
Cell Data

cell lines：Ba/F3 cells expressing wild-type or mutant human Kit, HMC1, HMC-1α155

Concentrations：Dissolved in DMSO, final concentrations ~30 μM

Incubation Time：72 hours

Powder Purity:≥98%

Product Properties

ALogP 1.839
hba_count 6
HBD Count 2
Rotatable Bond 7

Associated Targets(Human)

DCTPP1 Tchem dCTP pyrophosphatase 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PAK5 Tchem Serine/threonine-protein kinase PAK 5 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKX Tchem cAMP-dependent protein kinase catalytic subunit PRKX (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKAR2A Tchem cAMP-dependent protein kinase type II-alpha regulatory subunit (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKACB Tchem cAMP-dependent protein kinase catalytic subunit beta (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKG1 Tchem cGMP-dependent protein kinase 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKG2 Tchem cGMP-dependent protein kinase 2 (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)
PRKCE Tchem Protein kinase C epsilon type (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKCH Tchem Protein kinase C eta type (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AKT3 Tchem RAC-gamma serine/threonine-protein kinase (5 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AKT2 Tchem RAC-beta serine/threonine-protein kinase (6 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AKT1 Tchem RAC-alpha serine/threonine-protein kinase (10 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKAG2 Tchem 5'-AMP-activated protein kinase subunit gamma-2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PAK4 Tchem Serine/threonine-protein kinase PAK 4 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PAK6 Tchem Serine/threonine-protein kinase PAK 6 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKACA Tchem cAMP-dependent protein kinase catalytic subunit alpha (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRKCQ Tchem Protein kinase C theta type (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles CC[N]1C(=NC2=C1C(=CN=C2C#CC(C)(C)O)OCC3CCCNC3)C4=NON=C4N
Molecular Weight 425.48
Reaxy-Rn 15495142
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15495142&ln=

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

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

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 100 mg/mL (354.3 mM);    
DMSO(mg / mL) Max Solubility 39
DMSO(mM) Max Solubility 91.66
Water(mg / mL) Max Solubility <1

Solution Calculators

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