BIO - Moligand™, 10mM in DMSO , Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta, CAS No.667463-62-9, Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta

CAS: 667463-62-9 Cat. No.: B407765 Molecular Weight: 356.17 EC Number: 636-292-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052 | 2H-Indol-2-one, 6-bromo-3-[(3E)-1,3-dihydro-3-(hydroxyimino)-2H-indol-2-ylidene]-1,3-dihydro-, (3Z)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor ofGSK-3withIC50of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAKinhibitor with IC50 of 30 nM forT
In vitro

BIO (6-bromoindirubin-3\'-oxime) is a specific inhibitor of glycogen synthase kinase-3 (GSK-3), with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5. BIO interacts within the ATP binding pocket of these kinases, reduces β-catenin phosphorylation on a GSK-3-specific site in cellular models, closely mimicks Wnt signaling in Xenopus embryos. In human and mouse embryonic stem cells, BIO maintains the undifferentiated phenotype and sustains expression of the pluripotent state-specific transcription factors Oct-3/4, Rex-1 and Nanog. BIO-mediated Wnt activation is functionally reversible, as withdrawal of the compound leads to normal multidifferentiation programs in both human and mouse embryonic stem cells. BIO promotes proliferation in mammalian cardiomyocytes. 6BIO is also a pan-JAK inhibitor, with IC50 values of 0.03, 1.5, 8.0, 0.5 μM for TYK2, JAK1, JAK2 and JAK3. BIO selectively inhibits phosphorylation of STAT3 and induces apoptosis of human melanoma cells.

In vivo

BIO suppresses melanoma tumor growth in a mouse xenograft model.
Cell Data

cell lines：

Concentrations：~10 μM

Incubation Time：12 or 24 h

Powder Purity:≥99%

Specifications

Synonyms

GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052 | 2H-Indol-2-one, 6-bromo-3-[(3E)-1, 3-dihydro-3-(hydroxyimino)-2H-indol-2-ylidene]-1, 3-dihydro-, (3Z)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3\'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 3

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta

Names and Identifiers

• Isomeric SMILES: C1=CC=C2C(=C1)C(=C(N2)C3=C(NC4=C3C=CC(=C4)Br)O)N=O
• WGK Germany: 3
• Molecular Weight: 356.17
• Reaxy-Rn: 23724350
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23724350&ln=

Associated Targets(Human)

CDK1 Tchem Cyclin-dependent kinase 1 (1 Activities)

Discover Target: CDK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK5 Tchem Cyclin-dependent-like kinase 5 (1 Activities)

Discover Target: CDK5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta (0 Activities)

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha (0 Activities)

Discover Target: GSK3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 44 mg/mL (197.98 mM)
• Melt Point(°C): 300 °C