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XX-650-23

Catalog No. T24212   CAS 117739-40-9
Synonyms: XX65023, XX 650 23

XX-650-23 is a small molecule CREB inhibitor that blocks the critical interaction between CREB and its required coactivator, CBP (CREB-binding protein), inducing apoptosis and cell cycle arrest in AML cells, and can be used in the study of acute myelogenous leukaemia (AML).

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XX-650-23 Chemical Structure
XX-650-23, CAS 117739-40-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 39.00
5 mg In stock $ 93.00
10 mg In stock $ 148.00
25 mg In stock $ 297.00
50 mg In stock $ 497.00
100 mg In stock $ 693.00
500 mg In stock $ 1,450.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 97.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description XX-650-23 is a small molecule CREB inhibitor that blocks the critical interaction between CREB and its required coactivator, CBP (CREB-binding protein), inducing apoptosis and cell cycle arrest in AML cells, and can be used in the study of acute myelogenous leukaemia (AML).
Targets&IC50 AML:870 nM-2.3 μM
In vitro During split Renilla luciferase complementation analysis, XX-650-23 exhibited an IC50 of 3.20 ± 0.43 μM in inhibiting the interaction between CREB and CBP [1]. Following treatment with XX-650-23 (100 pM - 10 μM) for 48 hours, four AML cell lines showed IC50 values ranging from 870 nM to 2.3 μM, defined as a 50% reduction in viable cell count compared to DMSO-treated cells, indicating the inhibition of AML growth by XX-650-23 [1].
In vivo XX-650-23 (2.3 mg/kg, intravenous injection) extends the survival of AML mouse model (NSG mice) and exhibits no toxicity[1].
Synonyms XX65023, XX 650 23
Molecular Weight 288.3
Formula C18H12N2O2
CAS No. 117739-40-9

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (277.49 mM), Sonication is recommended.

TargetMolReferences and Literature

1. B Mitton, et al. Small molecule inhibition of cAMP response element binding protein in human acute myeloid leukemia cells. Leukemia. 2016 Dec;30(12):2302-2311. 2. François S, Sen N, Mitton B, Xiao X, Sakamoto KM, Arvin A. Varicella-Zoster Virus Activates CREB, and Inhibition of the pCREB-p300/CBP Interaction Inhibits Viral Replication In Vitro and Skin Pathogenesis In Vivo. J Virol. 2016 Sep 12;90(19):8686-97. doi: 10.1128/JVI.00920-16. Print 2016 Oct 1. PubMed PMID: 27440893; PubMed Central PMCID: PMC5021407. 3. Mitton B, Chae HD, Hsu K, Dutta R, Aldana-Masangkay G, Ferrari R, Davis K, Tiu BC, Kaul A, Lacayo N, Dahl G, Xie F, Li BX, Breese MR, Landaw EM, Nolan G, Pellegrini M, Romanov S, Xiao X, Sakamoto KM. Small molecule inhibition of cAMP response element binding protein in human acute myeloid leukemia cells. Leukemia. 2016 Dec;30(12):2302-2311. doi: 10.1038/leu.2016.139. Epub 2016 May 23. PubMed PMID: 27211267; PubMed Central PMCID: PMC5143163.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library

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Keywords

XX-650-23 117739-40-9 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain XX65023 XX 650 23 inhibitor inhibit

 

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