Art. -Nr.: HY-10225

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Belinostat

(Synonyms: PXD101; PX105684)

38 Cited Publications

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Based on 38 publication(s) in Google Scholar

Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC₅₀ of 27 nM in HeLa cell extracts.

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Reinheit: 99.94%
CAS. Nr.: 866323-14-0
Formel: C₁₅H₁₄N₂O₄S
Molecular Weight:318.35

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Belinostat Chemical Structure

CAS. Nr.: 866323-14-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (38)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC₅₀ of 27 nM in HeLa cell extracts.

IC₅₀ & Target^[1]^[2]

HDAC6

82 nM (IC₅₀)

HDAC

27 nM (IC₅₀, Hela cell)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
143B	GI₅₀	3.3 μM Compound: 54; PDX-101	Antiproliferative activity against human 143B cells Antiproliferative activity against human 143B cells	[PMID: 37875056]
A2780	IC₅₀	0.67 μM Compound: PXD101	Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
A549	GI₅₀	0.78 μM Compound: PXD101	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay Antiproliferative activity against human A549 cells after 48 hrs by SRB assay	[PMID: 27344487]
A549	GI₅₀	0.23 μM Compound: 3; PXD101	Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
A549	IC₅₀	0.077 μM Compound: 2	Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
ASPC1	GI₅₀	0.65 μM Compound: 3; PXD101	Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
COLO 205	IC₅₀	0.7 μM Compound: PXD101	Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
HCT-116	IC₅₀	0.6 μM Compound: PXD101	Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
HCT-116	IC₅₀	160 nM Compound: 2, PXD101	Antiproliferative activity against human HCT116 cells assessed as growth inhibition Antiproliferative activity against human HCT116 cells assessed as growth inhibition	[PMID: 21650221]
HCT-116	IC₅₀	0.16 μM Compound: 2, PXD-101	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 21742496]
HCT-116	GI₅₀	0.13 μM Compound: PXD101	Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay	[PMID: 27344487]
HEK293	IC₅₀	15 nM Compound: PXD101	Inhibition of HDAC6 in HEK293 cells Inhibition of HDAC6 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	18 nM Compound: PXD101	Inhibition of HDAC1 in HEK293 cells Inhibition of HDAC1 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	46 nM Compound: PXD101	Inhibition of HDAC3 in HEK293 cells Inhibition of HDAC3 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	1.4 μM Compound: 33	Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay	[PMID: 28241112]
HEK293	IC₅₀	1420 nM Compound: Belinostat	Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay	[PMID: 30245402]
HEL	IC₅₀	0.1 μM Compound: PXD101	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay Antiproliferative activity against human HEL cells after 48 hrs by MTT assay	[PMID: 29533873]
HEL	IC₅₀	<0.78125 μM Compound: PXD101	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay Antiproliferative activity against human HEL cells after 48 hrs by MTT assay	[PMID: 30879863]
HeLa	IC₅₀	28 nM Compound: 17a, PXD101	Inhibition of HDAC from human HeLa cells Inhibition of HDAC from human HeLa cells	[PMID: 18247554]
HeLa	IC₅₀	27 nM Compound: PXD101	Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay	[PMID: 23639537]
HeLa	IC₅₀	26.4 nM Compound: 8, PXD101	Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay	[PMID: 25113875]
HeLa	IC₅₀	81 nM Compound: 3; PXD101	Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay	[PMID: 28395150]
HeLa	IC₅₀	0.087 μM Compound: 2	Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
HeLa	IC₅₀	0.51 μM Compound: PXD101	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 29533873]
HeLa	IC₅₀	0.087 μM Compound: PXD101	Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay	[PMID: 30879863]
HeLa	IC₅₀	1.07 μM Compound: PXD101	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 30879863]
HeLa	IC₅₀	189 nM Compound: PXD101	Inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay Inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay	[PMID: 31400937]
HeLa	IC₅₀	10 nM Compound: 25; PXD-101	Inhibition of HDAC in human HeLa cell extracts Inhibition of HDAC in human HeLa cell extracts	[PMID: 31536895]
HL-60	GI₅₀	1.09 μM Compound: PXD101	Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay	[PMID: 27344487]
HOS	GI₅₀	3.3 μM Compound: 54; PDX-101	Antiproliferative activity against human HOS cells Antiproliferative activity against human HOS cells	[PMID: 37875056]
HT-29	IC₅₀	0.86 μM Compound: PXD101	Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 30879863]
Huh-7	CC₅₀	0.68 μM Compound: 7, PXD101	Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay	[PMID: 25490700]
Huh-7	EC₅₀	0.12 μM Compound: 7, PXD101	Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay	[PMID: 25490700]
Huh-7	CC₅₀	0.65 μM Compound: Belinostat	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 31201063]
Jurkat	IC₅₀	0.07 μM Compound: PXD101	Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay	[PMID: 29533873]
Jurkat	GI₅₀	0.11 μM Compound: 2	Growth inhibition of human Jurkat cells Growth inhibition of human Jurkat cells	[PMID: 37429084]
K562	IC₅₀	1.1 μM Compound: PXD101	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 29533873]
K562	IC₅₀	1.07 μM Compound: PXD101	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 30879863]
MCF7	IC₅₀	0.096 μM Compound: 2	Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
MDA-MB-231	GI₅₀	0.28 μM Compound: 3; PXD101	Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
MDA-MB-231	IC₅₀	0.062 μM Compound: 2	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
MOLT-4	IC₅₀	0.14 μM Compound: PXD101	Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay	[PMID: 29533873]
MOLT-4	GI₅₀	0.12 μM Compound: 2	Growth inhibition of human MOLT-4 cells measured after 24 hrs by MTT assay Growth inhibition of human MOLT-4 cells measured after 24 hrs by MTT assay	[PMID: 37429084]
NCI-H1299	IC₅₀	460 nM Compound: 2, PXD101	Antiproliferative activity against human H1299 cells Antiproliferative activity against human H1299 cells	[PMID: 21650221]
NCI-H23	IC₅₀	2.53 μM Compound: 54; PDX-101	Antiproliferative activity against human NCI-H23 cells incubated for 48 hrs by colorimetric method Antiproliferative activity against human NCI-H23 cells incubated for 48 hrs by colorimetric method	[PMID: 37875056]
NFF	IC₅₀	1.4 μM Compound: 33	Cytotoxicity against human NFF cells after 72 hrs by SRB assay Cytotoxicity against human NFF cells after 72 hrs by SRB assay	[PMID: 28241112]
NFF	IC₅₀	1420 nM Compound: Belinostat	Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay	[PMID: 30245402]
NFF	IC₅₀	2.37 μM Compound: Belinostat	Cytotoxicity against human NFF cells incubated for 72 hrs by SRB assay Cytotoxicity against human NFF cells incubated for 72 hrs by SRB assay	[PMID: 39208744]
PC-3	IC₅₀	0.45 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
PC-3	GI₅₀	0.39 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay	[PMID: 27344487]
PC-3	GI₅₀	0.31 μM Compound: 3; PXD101	Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
PC-3	IC₅₀	1.3 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 29533873]
PC-3	IC₅₀	1.32 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 30879863]
PC-3	IC₅₀	2.53 μM Compound: 54; PDX-101	Antiproliferative activity against human PC-3 cells incubated for 48 hrs by colorimetric method Antiproliferative activity against human PC-3 cells incubated for 48 hrs by colorimetric method	[PMID: 37875056]
RAW264.7	IC₅₀	2.2 μM Compound: 8, PXD101	Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of nitric oxide production pre-incubated for 1 hr before LPS stimulation for 24 hrs by Griess reagent based assay Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of nitric oxide production pre-incubated for 1 hr before LPS stimulation for 24 hrs by Griess reagent based assay	[PMID: 25113875]
RAW264.7	IC₅₀	4.7 μM Compound: 8, PXD101	Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method	[PMID: 25113875]
RAW264.7	IC₅₀	8.28 μM Compound: 8, PXD101	Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of PGE2 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by enzyme immunoassay method Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of PGE2 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by enzyme immunoassay method	[PMID: 25113875]
RAW264.7	IC₅₀	0.059 nM Compound: 8, PXD101	Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method	[PMID: 25113875]
RAW264.7	IC₅₀	0.059 x 10^-3 μM Compound: 8, PXD101	Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method	[PMID: 25113875]
SAOS-2	GI₅₀	3.3 μM Compound: 54; PDX-101	Antiproliferative activity against human SAOS-2 cells Antiproliferative activity against human SAOS-2 cells	[PMID: 37875056]
SW-620	IC₅₀	2.53 μM Compound: 54; PDX-101	Antiproliferative activity against human SW620 cells incubated for 48 hrs by colorimetric method Antiproliferative activity against human SW620 cells incubated for 48 hrs by colorimetric method	[PMID: 37875056]
THP-1	GI₅₀	0.075 μM Compound: 2	Growth inhibition of human THP-1 cells Growth inhibition of human THP-1 cells	[PMID: 37429084]
THP-1	IC₅₀	0.4 μM Compound: Belinostat	Inhibition of cell growth of human THP-1 cells Inhibition of cell growth of human THP-1 cells	[PMID: 38236416]
U-937	IC₅₀	0.4 μM Compound: PXD101	Antiproliferative activity against human U937 cells after 48 hrs by MTT assay Antiproliferative activity against human U937 cells after 48 hrs by MTT assay	[PMID: 30879863]

In Vitro

Belinostat (PXD101) induces a concentration-dependent (0.2-5 μM) increase in acetylation of histone H4 in tumor cell lines. Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC₅₀s in the range 0.2-3.4 μM as determined by a clonogenic assay and induces apoptosis. Belinostat inhibits the growth of a number of human tumor cell lines in vitro with IC₅₀s determined by a clonogenic assay in the range 0.2-3.4 μM^[1]. Belinostat (PXD101) is a potent histone deacetylase (HDAC) inhibitor, potently inhibits the enzymatic activity of purified recombinant HDAC6 (IC₅₀ of 82 nM)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Treatment of nude mice bearing human ovarian and colon tumor xenografts with Belinostat (10-40 mg/kg/day i.p.) daily for 7 days causes a significant dose-dependent growth delay with no obvious signs of toxicity to the mice. Growth delay is also observed for xenografts of cisplatin-resistant ovarian tumor cells. A marked increase in acetylation of H4 is detected in blood and tumor of mice 3 h after treatment with Belinostat (PXD101). The inhibition of growth of human tumor xenografts in mice, with no apparent toxicity^[1]. Belinostat (PXD101) displays single-agent antitumor activity on human A2780 ovarian cancer s.c. xenografts which is enhanced via combination therapy with Carboplatin^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 866323-14-0
Appearance Solid
Molecular Weight 318.35
Formel C₁₅H₁₄N₂O₄S
Color White to off-white
SMILES

O=S(NC1=CC=CC=C1)(C2=CC(/C=C/C(NO)=O)=CC=C2)=O
Synonyms

PXD101; PX105684
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (38)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyIFIn Vivo ImagingWB

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Journal Impact Factor

Signal Transduct Target Ther

The noncanonical function of liver-type phosphofructokinase potentiates the efficacy of HDAC inhibitors in cancer. [Abstract]

2025 Oct 14;10(1):341. PMID: 41083431

Belinostat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Oct 14;10(1):341. [Abstract]

Cell viability of TFK1 cells expressing either a negative control sgRNA (sgNC) or sgRNAs targeting PFKL (sgPFKL-1 and sgPFKL-2) following treatment with specified concentrations of belinostat, vorinostat, apicidin or HC-toxin for 72 hours.
Adv Mater

Dual Targeting of m7G tRNA Modification and Histone Acetylation using Carrier-Free Nano-Epidrugs to Evoke Osteosarcoma Chemosensitization. [Abstract]

2025 Oct 10:e05951. PMID: 41074238
Cancer Res

An In Vivo CRISPR Screen Identifies Stepwise Genetic Dependencies of Metastatic Progression. [Abstract]

2022 Feb 15;82(4):681-694. PMID: 34916221

Belinostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2022 Feb 15;82(4):681-694. [Abstract]

Plot showing the luminescence signal (ph/sec/cm2/sr) over time from NSG mice intracranially injected with either 2.0 × 105 MDA-MB-231-GFP-Luc cells and treated either with vehicle (l-arginine (100 mg/mL) in ddH2O) or 80 mg/kg Belinostat for five consecutive days a week, for a total of three cycles.

Belinostat purchased from MedChemExpress. Usage Cited in: Cancer Res. 2022 Feb 15;82(4):681-694. [Abstract]

Representative images of the bioluminescence signal measured from brains of NSG mice intracranially injected with either MDA-MB-231-GFP-Luc cells and treated either with vehicle [l-arginine (100 mg/mL) in ddH2O] or 80 mg/kg belinostat.
Nat Commun

Histone 4 lysine 5/12 acetylation enables developmental plasticity of Pristionchus mouth form. [Abstract]

2023 Apr 13;14(1):2095. PMID: 37055396
Nat Commun

Phenotype-driven precision oncology as a guide for clinical decisions one patient at a time. [Abstract]

2017 Sep 5;8(1):435. PMID: 28874669
J Exp Clin Cancer Res

Comparative analysis of response to treatments and molecular features of tumor-derived organoids versus cell lines and PDX derived from the same ovarian clear cell carcinoma. [Abstract]

2023 Oct 7;42(1):260. PMID: 37803448
Pharmacol Res

The histone deacetylase inhibitor belinostat ameliorates experimental autoimmune encephalomyelitis in mice by inhibiting TLR2/MyD88 and HDAC3/ NF-κB p65-mediated neuroinflammation. [Abstract]

2022 Feb:176:105969. PMID: 34758400
Cell Death Dis

Targeting HDAC/OAZ1 axis with a novel inhibitor effectively reverses cisplatin resistance in non-small cell lung cancer. [Abstract]

2019 May 24;10(6):400. PMID: 31127087
Cell Death Dis

Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. [Abstract]

2018 Jan 26;9(2):129. PMID: 29374157

Belinostat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]

Belinostat (PDX101: 5/10 μM). PXD101The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.
NPJ Breast Cancer

Epigenetically upregulating TROP2 and SLFN11 enhances therapeutic efficacy of TROP2 antibody drug conjugate sacitizumab govitecan. [Abstract]

2023 Aug 11;9(1):66. PMID: 37567892
Blood Adv

BH3 mimetic drugs overcome the microenvironment-induced resistance to crizotinib in ALK+ anaplastic large cell lymphoma. [Abstract]

2025 Jul 2:bloodadvances.2024015322. PMID: 40601898
Cell Rep

[Studies on ECMO. II. The effect of ECMO in respiratory failure and the trial of long-term ECMO; two experimental studies in dogs and goats]. [Abstract]

2022 Sep 20;40(12):111396. PMID: 3613050
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
JCI Insight

Methylation-induced suppression of YAP/TAZ confers sensitivity to HDAC inhibitors in high grade IDH mutant gliomas. [Abstract]

2025 Oct 9:e195385. PMID: 41066183
Mol Ther Nucleic Acids

2025 Dec 15.
Cells

HDAC Inhibition Induces Transient Phenotypic Inertia in Dormant OCCC Spheroids by Derepression of Cell Cycle Genes. [Abstract]

2026 Apr 10;15(8):673. PMID: 42041541
Commun Biol

CBX4 enhances acute monocytic leukemia development via HDAC-mediated suppression of Runx1. [Abstract]

2026 Jun 1. PMID: 42225948
Eur J Pharmacol

Identification of novel SIRT1 up-regulators using a cell-based high-throughput screening assay. [Abstract]

2025 Oct 15:1005:178066. PMID: 40818658
Pharmaceuticals (Basel)

Valproic Acid Prodrug Affects Selective Markers, Augments Doxorubicin Anticancer Activity and Attenuates Its Toxicity in a Murine Model of Aggressive Breast Cancer. [Abstract]

2021 Nov 30;14(12):1244. PMID: 34959644
Cancers (Basel)

Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]

2022 Mar 19;14(6):1575. PMID: 35326726
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Viruses

Identification of Combinations of Protein Kinase C Activators and Histone Deacetylase Inhibitors That Potently Reactivate Latent HIV. [Abstract]

2020 Jun 3;12(6):609. PMID: 32503121
Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Int Immunol

Generation of allo-antigen-specific induced Treg stabilized by vitamin C treatment and its application for prevention of acute graft versus host disease model. [Abstract]

2017 Dec 18;29(10):457-469. PMID: 29126272
Invest New Drugs

Molecular and cellular effects of a novel hydroxamate-based HDAC inhibitor - belinostat - in glioblastoma cell lines: a preliminary report. [Abstract]

2016 Oct;34(5):552-64. PMID: 27468826

Belinostat purchased from MedChemExpress. Usage Cited in: Invest New Drugs. 2016 Oct;34(5):552-64. [Abstract]

Phenotypic characteristics of LN-229 glioblastoma cells after 48 hours of treatment with Belinostat (Bel). Representative images are shown in the figure. Morphological changes induced by 0.5 and 2 μmol/L Bel treatment for 48 hours were assessed by phase contrast microscopy (100x magnification).
Saudi Med J

Investigation of the effect of belinostat on MCF-7 breast cancer stem cells via the Wnt, Notch, and Hedgehog signaling pathway. [Abstract]

2024 Feb;45(2):121-127. PMID: 38309728
bioRxiv

2026 Mar 14.
Res Sq

2025 Sep 23.
bioRxiv

2025 Aug 25.
Patent

US20250152731A1.
Patent

US20250161243A1.
Patent

US20220362183A1.
Annals of Medical Research

2021;28(5):941-5.
bioRxiv

2021 Jan 5.
Textbook of Personalized Medicine

2020 Dec 6.
Patent

US20200218874A1

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (314.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 25 mg/mL (78.53 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1412 mL

15.7060 mL

31.4120 mL

5 mM

0.6282 mL

3.1412 mL

6.2824 mL

10 mM

0.3141 mL

1.5706 mL

3.1412 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

For activity assays, the reaction is carried out in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] containing 2 μL of cell extract and, where used, 2 μL of Belinostat. The reaction is started by the addition of 2 μL of [³H]labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH₂-terminal residues). Samples are incubated at 37°C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12 M final concentrations, respectively). Released [³H]acetate is extracted into 750 μL of ethyl acetate, and samples are centrifuged at 12,000× g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

The human ovarian cell line A2780 and Cisplatin (A2780/cp70) and Doxorubicin (2780AD) resistant derivatives are grown in RPMI 1640 supplemented with glutamine (2 mM) and FCS (10%). The human colon (HCT116 and HT29), melanoma (HS852), prostate (PC3), lung (CALU-3), and breast (MCF7) cell lines are grown in RPMI 1640 and the rest in DMEM supplemented as above. The human non-small cell lung cancer cell line WIL is grown in DMEM supplemented as above. Drug sensitivity is determined by a clonogenic assay. Briefly, cells are plated in 5 mL of medium at a density of 8×10⁴ cells/25 cm² flask and allowed to attach and grow for 48 h. Cells are exposed to Belinostat (five concentrations from 0.016 to 10 μM) for 24 h. The medium is removed, and 1 mL of trypsin/EDTA is added to each flask. Once the cells have detached, 1 mL of medium is added, the cells are resuspended, and those from the control untreated flask are counted. Cells are diluted and plated into 6-cm Petri dishes (three per flask) at a density of 500-2000 cells/dish depending on the cell line. Cells from the drug-treated flasks are diluted and plated as for the control flasks. Dishes are incubated for 10-15 days at 37°C. Cells are washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC₅₀ (mean±SE of three experiments) defined as the concentration of drug required to reduce the number of colonies to 50% of that of the control untreated cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
For the human tumor xenograft studies, monolayer cultures are harvested with trypsin/EDTA (0.25%/1 mM in PBS) and resuspended in PBS. About 10⁷ cells are injected s.c. into the right flank of athymic nude mice (CD1 nu/nu mice). After 10-15 days when the mean tumor diameter is ≥0.5 cm, animals are randomized into groups of six for experiments. Belinostat is dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10% and is administered i.p. at the times specified. This formulation gives sufficient solubility for doses of ≤ 40 mg/kg. Mice are weighed daily, and tumor volumes are estimated by caliper measurements assuming spherical geometry (volume=d³×π/6).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Plumb JA, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histonedeacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8. [Content Brief]

[2]. Qian X, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006 Aug;5(8):2086-95. [Content Brief]

[3]. Chia S, et al. Phenotype-driven precision oncology as a guide for clinical decisions one patient at a time. Nat Commun. 2017 Sep 5;8(1):435. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	3.1412 mL	15.7060 mL	31.4120 mL	78.5299 mL
	5 mM	0.6282 mL	3.1412 mL	6.2824 mL	15.7060 mL
	10 mM	0.3141 mL	1.5706 mL	3.1412 mL	7.8530 mL
	15 mM	0.2094 mL	1.0471 mL	2.0941 mL	5.2353 mL
	20 mM	0.1571 mL	0.7853 mL	1.5706 mL	3.9265 mL
	25 mM	0.1256 mL	0.6282 mL	1.2565 mL	3.1412 mL
	30 mM	0.1047 mL	0.5235 mL	1.0471 mL	2.6177 mL
	40 mM	0.0785 mL	0.3926 mL	0.7853 mL	1.9632 mL
	50 mM	0.0628 mL	0.3141 mL	0.6282 mL	1.5706 mL
	60 mM	0.0524 mL	0.2618 mL	0.5235 mL	1.3088 mL
DMSO	80 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9816 mL
DMSO	100 mM	0.0314 mL	0.1571 mL	0.3141 mL	0.7853 mL

Keywords

Belinostat

38 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Belinostat

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Biologische Aktivität

Chemical Information

Publications (38)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Belinostat Related Classifications

HY-10225 Related Classifications