CAS 99873-43-5|Droxinostat

Introduction：Basic information about CAS 99873-43-5|Droxinostat, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Droxinostat BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles2
6. Synonyms

Common Name	Droxinostat
CAS Number	99873-43-5	Molecular Weight	243.68700
Density	1.252 g/cm3	Boiling Point	/
Molecular Formula	C₁₁H₁₄ClNO₃	Melting Point	/
MSDS	ChineseUSA	Flash Point	/
Symbol	GHS05, GHS07	Signal Word	Danger

Names

Name	4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide
Synonym	More Synonyms

Droxinostat BiologicalActivity

Description	Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.IC50 Value: 16.9 μM(HDAC3); 2.47 μM(HDAC6); 1.46 μM(HDAC8)Target: HDAC3/6/8in vitro: Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). the direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat selective inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively, without inhibiting other HDAC members (IC50 > 20 μM). In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis.in vivo: In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.
Related Catalog	Research Areas >>Cancer
Target	HDAC8:1.46 μM (IC50) HDAC6:2.47 μM (IC50) HDAC3:16.9 μM (IC50)
References	[1]. Liu J, et al. Droxinostat, a Histone Deacetylase Inhibitor, Induces Apoptosis in Hepatocellular Carcinoma Cell Lines via Activation of the Mitochondrial Pathway and Downregulation of FLIP. Transl Oncol. 2016 Feb;9(1):70-8. [2]. Wood TE et al. Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther. 2010 Jan;9(1):246-56. [3]. MMcCourt C, Maxwell P, Mazzucchelli R, Montironi R, Scarpelli M, Salto-Tellez M, O'Sullivan JM, Longley DB, Waugh DJ.,Elevation of c-FLIP in Castrate-Resistant Prostate Cancer Antagonizes Therapeutic Response to Androgen Receptor-Targeted Therapy.,Clin Cancer Res. 2012 Jul 15;18(14):3822-33. Epub 2012 May 23 [4]. Bijangi-Vishehsaraei K, Saadatzadeh MR, Huang S, Murphy MP, Safa AR.,4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide (CMH) targets mRNA of the c-FLIP variants and induces apoptosis in MCF-7 human breast cancer cells.,Mol Cell Biochem. 2010 Sep;342(1-2):133-42. Epub 2010 May 6. [5]. Wood TE, Dalili S, Simpson CD, Sukhai MA, Hurren R, Anyiwe K, Mao X, Suarez Saiz F, Gronda M, Eberhard Y, MacLean N, Ketela T, Reed JC, Moffat J, Minden MD, Batey RA, Schimmer AD.,Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands.,Mol Cancer Ther. 2010 Jan;9(1):246-56. Epub 2010 Jan 6.

Chemical & Physical Properties

Density	1.252 g/cm3
Molecular Formula	C₁₁H₁₄ClNO₃
Molecular Weight	243.68700
Exact Mass	243.06600
PSA	62.05000
LogP	3.15310
Appearance of Characters	white to off-white
InChIKey	JHSXDAWGLCZYSM-UHFFFAOYSA-N
SMILES	Cc1cc(Cl)ccc1OCCCC(=O)NO
Storage condition	2-8°C
Water Solubility	DMSO: ≥20mg/mL

Safety Information

Symbol	GHS05, GHS07
Signal Word	Danger
Hazard Statements	H302-H315-H318-H335
Precautionary Statements	P261-P280-P305 + P351 + P338
Hazard Codes	Xn
Risk Phrases	22-37/38-41
Safety Phrases	26-39
RIDADR	NONH for all modes of transport

Articles2

Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).

Bioorg. Med. Chem. 23 , 5151-5, (2015)

Two of the histone deacetylases, TbDAC1 and TbDAC3, have been reported to be essential genes in trypanosomes. Therefore, we tested the activity of a panel of human histone deacetylase inhibitors (HDAC...

Inhibition of Histone Deacetylases Permits Lipopolysaccharide-Mediated Secretion of Bioactive IL-1β via a Caspase-1-Independent Mechanism.

J. Immunol. 195 , 5421-31, (2015)

Histone deacetylase (HDAC) inhibitors (HDACi) are clinically approved anticancer drugs that have important immune-modulatory properties. We report the surprising finding that HDACi promote LPS-induced...

Synonyms

S1422_Selleck

cc-490

Droxinostat

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