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BRD0705
- Optical Purity: 100% e.e.
- Soluble in DMSO
- MF: C20H23N3O
- MW: 321.42
Description
BRD0705 is a first-in-class, paralog selective GSK3α inhibitor with an IC50 value of 0.066 μM. BRD0705 induces differentiation, reduces transcriptional programs associated with stemness, and impairs colony formation in AML cell lines and primary patient samples without affecting normal hematopoietic cell growth.
Importantly, BRD0705 does not induce β-catenin stabilization or nuclear translocation at concentrations efficacious in multiple mouse models of AML, resulting in impaired leukemia initiation and prolonged survival.
Key Features
- First-in-class selective GSK3α inhibitor
- IC50: 0.066 μM
- Induces differentiation in AML models
- Reduces stemness-associated transcriptional programs
- Impairs colony formation in AML cell lines and primary patient samples
- Does not induce β-catenin stabilization at efficacious concentrations
Applications
- Acute myeloid leukemia (AML) research
- GSK3α signaling studies
- Cancer stemness and differentiation research
- Hematopoietic cell biology
- Leukemia initiation and survival studies
The negative control BRD5648 is available as Axon 3153. The racemic mixture of both enantiomers is available as Axon 3154.
More Information
| Parent CAS No. | 2056261-41-5 |
|---|---|
| Chemical Name | (S)-4-Ethyl-7,7-dimethyl-4-phenyl-6,7,8,9-tetrahydro-2H-pyrazolo[3,4-b]quinolin-5(4H)-one |
| SMILES | C12=NNC=C1[C@](CC)(C1C=CC=CC=1)C1C(=O)CC(C)(C)CC=1N2 |&1:5,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C20H23N3O/c1-4-20(13-8-6-5-7-9-13)14-12-21-23-18(14)22-15-10-19(2,3)11-16(24)17(15)20/h5-9,12H,4,10-11H2,1-3H3,(H2,21,22,23)/t20-/m0/s1 |
| InChiKey | NCKLQXXBRWCYMA-FQEVSTJZSA-N |
| CID | 136980453 |
| Short Description | GSK3α inhibitor |
References
- FF Wagner et al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431).
- L Benajiba et al. Identification of a first in class GSK3-alpha selective inhibitor as a new differentiation therapy for AML. Blood, 2015, 126(23), 870.
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