CAY10603 Chemical Properties

Density 

1.231±0.06 g/cm3(Predicted)

storage temp. 

+2C to +8C

solubility 

≥22.35 mg/mL in DMSO; insoluble in EtOH; ≥24.85 mg/mL in H2O

form 

Beige to light brown solid

pka

9.47±0.20(Predicted)

color 

White to light yellow

CAY10603 Usage And Synthesis

Description

Histone deacetylase 6 (HDAC6) is a class II HDAC that represses transcription by removing acetyl groups from histones. In addition, HDAC6 deacetylases tubulin, which is important in regulating microtubule stability and function. CAY10603 is a potent and selective inhibitor of HDAC6 (IC₅₀ = 0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively). Also, CAY10603 prevents the growth of several pancreatic cancer cell lines (IC₅₀ = 0.1-1 μM). The HDAC6 inhibitor is more active in inhibiting cell growth than the broad spectrum HDAC inhibitor suberoylanilide hydroxamic acid (SAHA).

Uses

HDAC6 Inhibitor is an inhibitor of HDAC6.

Definition

ChEBI: N-[4-[3-[[[7-(hydroxyamino)-7-oxoheptyl]amino]-oxomethyl]-5-isoxazolyl]phenyl]carbamic acid tert-butyl ester is a carbamate ester.

General Description

A cell-permeable, active site Zn²⁺-targeting phenylisoxazolo-hydroxamate that acts a potent and highly selective HDAC6 inhibitor (IC₅₀ = 0.002, 0.42, 90.7, 252, 271 and 6851 nM against HDAC-6, -3, -10, -2, -1 and -8, respectively). Shown to be more potent than SAHA in inhibiting the proliferation of a panel of pancreatic cancer cell lines (IC₅₀<1.0 μM).

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