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HomeProduct name listCB-839

CB-839

Synonym(s):GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem;

CB-839 Structural

What is CB-839?

Description

CB-839 (14393999-58-2)?is a potent (IC50?= 24 nM), selective and orally bioavailable inhibitor of glutaminase (KGA and GAC).1?CB-839 displayed an antiproliferative effect in the triple-negative breast cancer cell line, HCC-1806, but no activity in the estrogen receptor-positive cell line T47D.? CB-839 was able to cause proliferation arrest and apoptosis in acute myeloid leukemia cells without causing cytotoxicity against normal human CD34(+) progenitors.2? Aspartate-glutamate carrier 1 (AGC1) inhibition can synergize with CB-839 to limit tumor growth.3

The Uses of CB-839

CB-839 performs an antileukemic activity. It Inhibits GLS1 genes and reduces oxidative phosphorylation leading to leukamic cell proliferation arrest and apoptosis.

Storage

Store at -20°C

References

1) Gross?et al. (2014),?Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer; Mol. Cancer Ther.,13?890 2) Jacque?et al. (2015),?Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition; Blood,?126?1346 3) Alkan?et al.?(2018)?Cytosolic Aspartate Availability Determines Cell Survival When Glutamine is Limiting; Cell Metabolism?28?1

Properties of CB-839

Melting point: 186- 189° C
Density  1.430±0.06 g/cm3(Predicted)
storage temp.  +2C to +8C
solubility  Soluble in DMSO.
form  Yellow solid
pka 8.25±0.50(Predicted)
color  Pale yellow
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.

Safety information for CB-839

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for CB-839

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