Belinostat (PXD101)

Name: Belinostat (PXD101)
Brand: Selleck Chemicals
SKU: S1085
Rating: 5 (80 reviews)

For research use only.

Catalog No.S1085 Synonyms: NSC726630, PX-105684

80 publications

CAS No. 414864-00-9

Belinostat (PXD101, NSC726630, PX-105684) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.

Selleck's Belinostat (PXD101) has been cited by 80 publications

Cell, 2020, S0092-8674(20)31394-5

PubMed: 33147445 ( click the link to review the publication )

Nat Biotechnol, 2020, 10.1038/s41587-019-0388-4

PubMed: 31959954 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2018, 173(6):1413-1425

PubMed: 29754815 ( click the link to review the publication )

Nat Biotechnol, 2011, 29(3):255-65

PubMed: 21258344 ( click the link to review the publication )

Nat Commun, 2021, 12(1):117

PubMed: 33402692 ( click the link to review the publication )

Cancer Res, 2021, canres.0955.2021

PubMed: 34551960 ( click the link to review the publication )

Cancers (Basel), 2021, 13(15)3821

PubMed: 34359722 ( click the link to review the publication )

Cancers (Basel), 2021, 13(15)3862

PubMed: 34359763 ( click the link to review the publication )

Mol Cancer Ther, 2021, molcanther.MCT-21-0066-A.2021

PubMed: 34552007 ( click the link to review the publication )

Int J Mol Sci, 2021, 22(9)4559

PubMed: 33925399 ( click the link to review the publication )

Transl Oncol, 2021, 14(10):101181

PubMed: 34298440 ( click the link to review the publication )

Hum Cell, 2021, 10.1007/s13577-021-00579-z

PubMed: 34304386 ( click the link to review the publication )

Oncotarget, 2021, 12(7):674-685

PubMed: 33868588 ( click the link to review the publication )

J Dermatol Sci, 2021, S0923-1811(21)00005-0

PubMed: 33531202 ( click the link to review the publication )

Nat Commun, 2020, 29;11(1):2086

PubMed: 32350249 ( click the link to review the publication )

EMBO Rep, 2020, 21:e50162

PubMed: 32314873 ( click the link to review the publication )

Cancers (Basel), 2020, 12(10)E2903

PubMed: 33050470 ( click the link to review the publication )

Cancer Sci, 2020, 111(1):112-126

PubMed: 31675763 ( click the link to review the publication )

Cancer Cell Int, 2020, 19;20:58

PubMed: 32099531 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00425-8

PubMed: 32886306 ( click the link to review the publication )

Toxicol Lett, 2020, S0378-4274(20)30494-X

PubMed: 33290829 ( click the link to review the publication )
Cancer Sci, 2020, 111(7):2374-2384

PubMed: 32391602 ( click the link to review the publication )

J Exp Clin Cancer Res, 2019, 38(1):84

PubMed: 30777099 ( click the link to review the publication )

Cancers (Basel), 2019, 11(5)E645

PubMed: 31083396 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2019, 10.1111/pcmr.12841

PubMed: 31663663 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(1):185-195

PubMed: 30301863 ( click the link to review the publication )

Aging (Albany NY), 2019, 11(21):9778-9793

PubMed: 31727867 ( click the link to review the publication )

Biomolecules, 2019, 9(5)

PubMed: 31083537 ( click the link to review the publication )

Mol Pharmacol, 2019, 95(3):324-334

PubMed: 30622215 ( click the link to review the publication )

J Oncol, 2019, 2019:6179573

PubMed: 31396278 ( click the link to review the publication )

Cancer Res, 2018, 78(20):5731-5740

PubMed: 30135193 ( click the link to review the publication )

Int J Cancer, 2018, 143(6):1388-1401

PubMed: 29633255 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(1):17-25

PubMed: 29079711 ( click the link to review the publication )

Biomed Pharmacother, 2018, 99:543-551

PubMed: 29902865 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2018, 350:43-51

PubMed: 29733868 ( click the link to review the publication )

JCI Insight, 2018, 3(22)125568

PubMed: 30429379 ( click the link to review the publication )

Curr Protoc Pharmacol, 2018, 81(1):e41

PubMed: 29927058 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(18):5573-5584

PubMed: 28611196 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(12):3139-3149

PubMed: 27986747 ( click the link to review the publication )

Arch Toxicol, 2017, 91(2):839-864

PubMed: 27188386 ( click the link to review the publication )

Arch Toxicol, 2017, 91(1):365-391

PubMed: 27015953 ( click the link to review the publication )

Mol Oncol, 2017, 11(8):965-980

PubMed: 28397399 ( click the link to review the publication )

Lung Cancer, 2017, 103:58-65

PubMed: 28024697 ( click the link to review the publication )

Front Cell Neurosci, 2017, 11:315

PubMed: 29114207 ( click the link to review the publication )

Int J Parasitol Drugs Drug Resist, 2017, 7(1):42-50

PubMed: 28107750 ( click the link to review the publication )
Oncotarget, 2017, 8(44):77254-77267

PubMed: 29100385 ( click the link to review the publication )

JCI Insight, 2017, 2(6):e90196

PubMed: 28352655 ( click the link to review the publication )

EMBO Mol Med, 2016, 8(2):117-38

PubMed: 26681773 ( click the link to review the publication )

Cancer Res, 2016, 76(11):3319-31

PubMed: 26988986 ( click the link to review the publication )

Oncoimmunology, 2016,

PubMed: 27471639 ( click the link to review the publication )

Sci Rep, 2016, 6:38407

PubMed: 27910927 ( click the link to review the publication )

Biomed Pharmacother, 2016, 79:62-70

PubMed: 27044813 ( click the link to review the publication )

Oncol Res, 2016, 24(5):327-335

PubMed: 27712589 ( click the link to review the publication )

J Med Chem, 2015, 58(2):785-800

PubMed: 25490700 ( click the link to review the publication )

J Med Chem, 2015, 58(2):785-800

PubMed: ( click the link to review the publication )

Arch Toxicol, 2015, 89(9):1599-618

PubMed: 26272509 ( click the link to review the publication )

Endocr Relat Cancer, 2015, 22(5):777-92

PubMed: 26206775 ( click the link to review the publication )

J Cell Mol Med, 2015, 10.1111/jcmm.12550

PubMed: 25864732 ( click the link to review the publication )

J Biol Chem, 2015, 290(8):5028-40

PubMed: 25540204 ( click the link to review the publication )

J Biol Chem, 2015, 290(8):5028-40

PubMed: ( click the link to review the publication )

Int J Parasitol Drugs Drug Resist, 2015, 5(3):117-26

PubMed: 26199860 ( click the link to review the publication )

Biomed Rep, 2015, 3(6):797-801

PubMed: 26623018 ( click the link to review the publication )

Biochem Biophys Res Commun, 2015, 456(1):156-61

PubMed: 25446119 ( click the link to review the publication )

Biochem Bioph Res Co, 2015, 456(1):156-61

PubMed: ( click the link to review the publication )

Oncotarget, 2015, 6(18):15814-27

PubMed: 26158412 ( click the link to review the publication )

Cancer Immunol Res, 2015, 3(12):1375-85

PubMed: 26297712 ( click the link to review the publication )

Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384

PubMed: 25355930 ( click the link to review the publication )

Mol Carcinog, 2014, 53(9):722-35

PubMed: 23475695 ( click the link to review the publication )

PLoS One, 2014, 9(3):e92919

PubMed: 24651853 ( click the link to review the publication )
Anticancer Drugs, 2014, 25(8):938-49

PubMed: 24800886 ( click the link to review the publication )

Curr Pharm Desigh, 2014, 20(11):1874-80

PubMed: 23888956 ( click the link to review the publication )

Cell Rep, 2013, 5(6):1679-89

PubMed: 24360956 ( click the link to review the publication )

Gene Ther, 2013, 20(7):770-8

PubMed: 23282955 ( click the link to review the publication )

PLoS One, 2013, 8(10):e77684

PubMed: 24155971 ( click the link to review the publication )

J Thromb Thrombolysis, 2013, 35(2):185-92

PubMed: 23229086 ( click the link to review the publication )

Breast Cancer Res Treat, 2012, 131(3):777-89

PubMed: 21452019 ( click the link to review the publication )

Mol Med, 2011, 17(5-6):466-72

PubMed: 21424110 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description

Features

Lead compound of Topotarget.

Targets

HDAC ^[1]
(Cell-free assay)

27 nM

In vitro

Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780 cells. Belinostat could induce apoptosis through PARP cleavage and acetylation of histones H3/H4. ^[1] Belinostat inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase and increase in G2-M phase. ^[2] The growth inhibitory activity of belinostat on cell lines is not strongly influenced by the multidrug-resistant phenotype, whereas the activity of docetaxel is clearly affected. Belinostat could enhance the growth inhibitory activity of docetaxel or carboplatin in OVCAR-3 and A2780 cells. Belinostat also shows enhanced tubulin acetylation in ovarian cancer cell lines. ^[3] A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HCT116	NYPLZ405TnWwY4Tpc44hSXO\|YYm=	MljtNE46yqEQvF5CpC=>	M1zSfFI1KGh?		MmfT[I94di2{ZXf1cIF1eyCWUzDwdo91\WmwIHzleoVteyCjZoTldkA3yqCqIHnuZ5Vj[XSrb36=	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzF{NEW5OEc,OTdzMkS1PVQ9N2F-
HCT116	M1HZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NGPaNY01QCCq		MlXySWM2OD1yLkK4JO69VQ>?	NFXFfoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{GyOFU6PCd-MUexNlQ2QTR:L3G+
Granta-519	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFHNRlUzPCCq		NGfBfJpKSzVyPUW2MlMh\|ryP	NVnQe4ZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCwOlgxQDBpPkKwNFY5ODhyPD;hQi=>
Jeko-1	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M3robVI1KGh?		NF3SZlVKSzVyPUCuNkDPxE1?	NUSz[4JYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCwOlgxQDBpPkKwNFY5ODhyPD;hQi=>
HBL-2	MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NF\HcY0zPCCq		NWfBW\|BiUUN3ME2wMlQh\|ryP	NYrSNnh7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCwOlgxQDBpPkKwNFY5ODhyPD;hQi=>
Panc-1	MVrBdI9xfG:\|aYOgRZN{[Xl?	NH3yc4oyODBxNUCwM\|ExODBibl2=	MmLkOFghcA>?		Mlz4bY5lfWOnczDkc5NmKGSncHXu[IVvfCCjcH;weI9{cXN?	NUK5O\|JuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
AsPC-1	M2\WN2Fxd3C2b4Ppd{BCe3OjeR?=	MnfHNVAxNzVyMD:xNFAxKG6P	MX60PEBp		MmXIbY5lfWOnczDkc5NmKGSncHXu[IVvfCCjcH;weI9{cXN?	NVPoVFVHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
T3M4	MV;BdI9xfG:\|aYOgRZN{[Xl?	M3XkNFExOC93MECvNVAxOCCwTR?=	MY[0PEBp		MVLpcoR2[2W\|IHTvd4Uh\GWyZX7k[Y51KGGyb4D0c5Nqew>?	NHi0TGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[4NVY6QCd-MkK2PFE3QTh:L3G+
Panc-1	Moe1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MViwMVgxOCCwTR?=	Mn3uOFghcA>?		NF;SOYtqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI>	MmS3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OEG2PVgoRjJ{NkixOlk5RC:jPh?=
AsPC-1	Mlr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlfENE05ODBibl2=	MnO4OFghcA>?		MWDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=	NYjMNYJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
T3M4	MoXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M17pVFAuQDByIH7N	MneyOFghcA>?		MnXJbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy	NVqwWm43RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PFE3QThpPkKyOlgyPjl6PD;hQi=>
MiaPaCa2	M{LrVWZ2dmO2aX;uJGF{e2G7	Ml23NU8yOCEQvF2=	NGXE[G8zPCCq		M3nIeolv\HWlZYOgJIdzd3e2aDDhdpJme3SnZDDpckBIOi:P	MlXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ\|NEe1Olk2RC:jPh?=
AsPc1	NWTBXpRmTnWwY4Tpc44hSXO\|YYm=	MYexM\|ExKM7:TR?=	MYGyOEBp		NGLMZppqdmS3Y3XzJEBoem:5dHigZZJz\XO2ZXSgbY4hTzJxTR?=	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc0403	MUHBdI9xfG:\|aYOgRZN{[Xl?	M17jfFEh\|ryP	M17pcFI1KGh?		MY\pcoR2[2W\|IHHwc5B1d3Orcx?=	NGHiT4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O\|U3QTV:L3G+
Panc1005	M4fESGFxd3C2b4Ppd{BCe3OjeR?=	MlLUNUDPxE1?	NHHySmgzPCCq		NVWxS25[cW6mdXPld{BieG:ydH;zbZM>	MlLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ\|NEe1Olk2RC:jPh?=
Panc0327	NUXoe5FISXCxcITvd4l{KEG\|c3H5	NFzhW\|cyKM7:TR?=	M1jzS\|I1KGh?		M1zOT4lv\HWlZYOgZZBweHSxc3nz	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NU[5OUc,OjN2N{W2PVU9N2F-
Panc0203	MoHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NFP3dIU1QCCq		MW\FR\|UxRTJ{LkKg{txO	M2THOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
PL45	NWLTVJhpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NYfs[ZJDPDhiaB?=		NHzBd29GSzVyPUKwMlgh\|ryP	NXjCbXNTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O\|U3QTVpPkKzOFc2Pjl3PD;hQi=>
Panc1005	NXSzVWZvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M4\mT\|Q5KGh?		MVXFR\|UxRTFwMTFOwG0>	NHPYSW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O\|U3QTV:L3G+
Panc0403	NX[zdHRwT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MmjvOFghcA>?		M33F[WVEPTB;MT6xJO69VQ>?	M1PkelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEe1Olk2Lz5{M{S3OVY6PTxxYU6=
BxPc3	NWXkfHloT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MV20PEBp		M4fLcGVEPTB;MT6wJO69VQ>?	MkDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2N{W2PVUoRjJ\|NEe1Olk2RC:jPh?=
MiaPaCa2	NFzHdXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mn3VOFghcA>?		M{fkXGVEPTB;MD63JO69VQ>?	NFvYSpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O\|U3QTV:L3G+
Panc0327	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M2HtSVQ5KGh?		MUTFR\|UxRTBwNTFOwG0>	NYHFT\|F4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0O\|U3QTVpPkKzOFc2Pjl3PD;hQi=>
AsPc1	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M17hR\|Q5KGh?		MmjTSWM2OD1yLkOg{txO	NGXHNZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3OVY6PSd-MkO0O\|U3QTV:L3G+
PC9	NI\0cXdHfW6ldHnvckBCe3OjeR?=	NFn5TIgxNjVxMT:yJO69VQ>?	MnHDOEBp	MUHEUXNQ	NF\RU\|VqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S	NGnK[Jc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WxOVc2Oid-MkO1NVU4PTJ:L3G+
H1650	MVTGeY5kfGmxbjDBd5NigQ>?	MWKwMlUwOS9{IN88US=>	M1TqZ\|QhcA>?	NUfMNpcxTE2VTx?=	NWX2NWtncW6qaXLpeJMhfGinIHzleoVteyCxZjDBb5QhMHBvQXv0LUBidmRiRVfGVi=>	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzVzNUe1Nkc,OjN3MUW3OVI9N2F-
H460	M{HhSGZ2dmO2aX;uJGF{e2G7	MUmwMlUwOS9{IN88US=>	MUG0JIg>	NV7ueotnTE2VTx?=	NUnTU5R2cW6qaXLpeJMhfGinIHzleoVteyCxZjDBb5QhMHBvQXv0LUBidmRiRVfGVi=>	Mnz2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ\|NUG1O\|UzRC:jPh?=
PC9	MUXGeY5kfGmxbjDBd5NigQ>?	M2X3b\|UxOMLibl2=	MUCyOOKhcA>?	NGfrfmpFVVOR	NIjJcmJl\WO{ZXHz[ZMhTUeIUjDlfJBz\XO\|aX;u	MnfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3MUW3OVIoRjJ\|NUG1O\|UzRC:jPh?=
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HCT116	M2fUUGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MXe0PEBpenN?		NY\6NGJqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOFghcHK\|IHL5JHNTSiCjc4PhfUwhT0l3MDC9JFAvOTNizszNMi=>	M1HMNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{S0OFg4Lz5{N{O0OFQ5PzxxYU6=
MOLT4	NV3hVmhZSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3fwOVQ5KGi{cx?=		MlPmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPT1zUOEBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR\|UxKD1iMD6xOEDPxE1w	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV\|M{i3N{c,Ojl3M{O4O\|M9N2F-
HCT116	M37oUWFvfGmycn;sbYZmemG2aY\lJIF{e2G7				NI\UWVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdixiSVO1NEA:KDBwMU[g{txONg>?	M4rpZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNkWwNlIyLz5{MU[1NFIzOTxxYU6=
HCT116	NE\2ZppCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=				M2XL[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzMEBKSzVyIE2gNE4yPiEQvF2u	NILpbVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe0NlQ6Pid-MkG3OFI1QTZ:L3G+
SK-N-BE(2)	MnLqRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M2\FT\|Q5KGi{cx?=		NVXsVGdmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1PNUKHKEKpJINmdGy\|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkOxJO69VS5?	NVXvSZI6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1N\|M5PzNpPkK5OVM{QDd\|PD;hQi=>
PC3	MmKzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MknrOFghcHK\|		MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCJSUWwJF0hOC5\|OTFOwG0v	NIGyO4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O0OFQ5Pyd-MkezOFQ1QDd:L3G+
PC3	NHjWS5hCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NGnERo86PiCqcoO=		M{TlXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy\|IHHmeIVzKDl4IHjyd{BjgSClZXzseIl1\XJiOU[gZZN{[XluIFnDOVAhRSByLkS1JO69VS5?	M3;NOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNkO0OFMxLz5{MU[zOFQ{ODxxYU6=
H1299	NHHvWYRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=				MlfhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKMUK5PUBk\WyuczygTWM2OCB;IECuOFYh\|ryPLh?=	MlfsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF4NUCyNlEoRjJzNkWwNlIyRC:jPh?=
HeLa	NH7tUndCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NVPYdlRSPDhiaILz		MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwNUGg{txONg>?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV\|M{i3N{c,Ojl3M{O4O\|M9N2F-
HCT116	MlmwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NV7TeVFVQTZiaILz		NUDUPIpbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JINmdGy2aYTldkA6PiCjc4PhfUwhUUN3MDC9JFAvPiEQvF2u	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ\|NESzNEc,OjF4M{S0N\|A9N2F-
A2780	MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MV65OkBpenN?		M2LwZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IHPlcIx1cXSncjC5OkBie3OjeTygTWM2OCB;IECuOlch\|ryPLh?=	M1PrdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNkO0OFMxLz5{MU[zOFQ{ODxxYU6=
HuH7	NEDqeHREgXSxdH;4bYNqfHliYYPzZZk>		NIfkZ2Q{KGSjeYO=		MoDhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVJPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxidnnhZoltcXS7IHHmeIVzKDNiZHH5d{BjgSCFZXzsWIl1\XJiOU[gZZN{[XluIFPDOVAhRSByLk[4JO69VS5?	M1\3dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEmwO\|AxLz5{NUS5NFcxODxxYU6=
COLO205	MV\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M3n2e\|k3KGi{cx?=		M2\HNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU\|IxPSClZXzsd{Bi\nSncjC5OkBpenNiYomgZ4VtdHSrdHXyJFk3KGG\|c3H5MEBKSzVyIE2gNE44KM7:TT6=	NWHB[4Y6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2N\|Q1OzBpPkKxOlM1PDNyPD;hQi=>
A549	Mn[1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NIXVUXo1QCCqcoO=		NIOyOmZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGPSRkBie3OjeTygS2k2OCB;IECuO\|gh\|ryPLh?=	NYfSZXV4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezOFQ1QDdpPkK3N\|Q1PDh5PD;hQi=>
HL60	NIjOfpFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MYW0PEBpenN?		NVfyPWh[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO\|YYmsJGdKPTBiPTCxMlA6KM7:TT6=	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN2NES4O{c,Ojd\|NES0PFc9N2F-
K562	MU\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M323UlQ5KGi{cx?=		NVm2[lBVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCxMlEh\|ryPLh?=	NYXnfIFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1N\|M5PzNpPkK5OVM{QDd\|PD;hQi=>
PC3	M1jOcGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NEmyPGM1QCCqcoO=		NYjWflJLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR\|Mh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuN{DPxE1w	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV\|M{i3N{c,Ojl3M{O4O\|M9N2F-
NFF	MnLVR5l1d3SxeHnjbZR6KGG\|c3H5		NXm3NohGPzJiaILz		NVixRpdSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVk[IIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUAyNjRizszNMi=>	M4XWXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkSxNVEzLz5{OEK0NVEyOjxxYU6=
HEK293	NFnpW4NEgXSxdH;4bYNqfHliYYPzZZk>		NIXBSpY1QCCqcoO=		NWPSS5BvS3m2b4TvfIlkcXS7IHHnZYlve3RiSFXLNlk{KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDy[ZNignW{aX6gZZN{[XluIFnDOVAhRSBzLkSg{txONg>?	M2ixcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkSxNVEzLz5{OEK0NVEyOjxxYU6=
NFF	M{jpbGN6fG:2b4jpZ4l1gSCjc4PhfS=>		NYXBT2x5PzJiaILz		MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOSmYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEmFNUCgQUAyNjR{IN88UU4>	NELaXpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEK0OVQxOid-M{CyOFU1ODJ:L3G+
HEK293	MnXoR5l1d3SxeHnjbZR6KGG\|c3H5		NVPLTY1qPDhiaILz		NG\2ZWNEgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IILld4F7fXKrbjDkfYUh[mG\|ZXSgZZN{[XluIFnDOVAhRSBzLkSyJO69VS5?	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ2NUSwNkc,OzB{NEW0NFI9N2F-
RAW264.7	NV3oNG91SW62aT3pcoZt[W2vYYTvdpkh[XO\|YYm=		MYWxJIhz		Mo[0RY51cS2rbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hVFCVLYP0bY12dGG2ZXSgcY92e2ViUlHXNlY1NjdiY3XscJMh[XO\|ZYPz[YQh[XNic4XwdJJme3Orb36gc4Yhdmm2cnnjJI95cWSnIIDyc4R2[3Srb36gdJJmNWmwY4XiZZRm\CCob4KgNUBpeiCkZX\vdoUhVFCVIIP0bY12dGG2aX;uJIZweiB{NDDodpMh[nliR4Lp[ZN{KHKnYXflcpQh[mG\|ZXSgZZN{[XluIFnDOVAhRSB{LkKg{txONg>?	MlPiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUO4O\|UoRjJ3MUGzPFc2RC:jPh?=
RAW264.7	MYXBcpRqNWmwZnzhcY1ifG:{eTDhd5NigQ>?		MV:xJIhz		NG\0OHJCdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCOUGOtd5RqdXWuYYTl[EBud3W\|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW\|c3nvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh[mWob4LlJGxRWyC\|dHnteYxifGmxbjDmc5IhOjRiaILzJIJ6KEWOSWPBJI1mfGixZDygTWM2OCB;IESuO{DPxE1w	MoLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUO4O\|UoRjJ3MUGzPFc2RC:jPh?=
RAW264.7	Mn7pRY51cS2rbn\sZY1u[XSxcomgZZN{[Xl?		M1rieVEhcHJ?		MYLBcpRqNWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDpckBNWFNvc4TpcZVt[XSnZDDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyC\|dYDwdoV{e2mxbjDv[kBRT0V{IIDyc4R2[3Srb36gdJJmNWmwY4XiZZRm\CCob4KgNUBpeiCkZX\vdoUhVFCVIIP0bY12dGG2aX;uJIZweiB{NDDodpMh[nliZX76fY1mKGmvbYXuc4F{e2G7IH3leIhw\CxiSVO1NEA:KDhwMkig{txONg>?	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTFzM{i3OUc,OjVzMUO4O\|U9N2F-
Huh-luc/neo7	MkO3SpVv[3Srb36gZZN{[Xl?	NEOzTIIyKHWP	NIDqfpcyKHSxIEOgbJJ{		M{ftUGlvcGmkaYTpc44hd2ZiSFTBR{BkdGG\|czCxJIlvKGi3bXHuJGh2cC2udXOvcoVwPyClZXzsd{Bie3Onc4Pl[EBieyCqaYP0c45mKEh\|IHHj[ZR6dGG2aX;uJIF1KDFidV2gZYZ1\XJiMTD0c{A{KGi{czDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz	M4jFTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUO3NFE4Lz5{NUmzO\|AyPzxxYU6=
PC3	MkL0SpVv[3Srb36gZZN{[Xl?	MofFNE4{KHWP	MVS0PEBpenN?		NVi3UpVpUW6qaXLpeIlwdiCxZjDISGFEKGmwIHj1cYFvKFCFMzDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG\|ZTDpckBidW:3boSgc4Yh[WOndInsZZRm\CCqaYP0c45mKEh\|IHH0JFAvOyC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	NVzNT2pkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezOFQ1QDdpPkK3N\|Q1PDh5PD;hQi=>
HCT116	MkP5SpVv[3Srb36gZZN{[Xl?	NGrqboMxNjNidV2=	M{myWVQ5KGi{cx?=		MoTCTY5pcWKrdHnvckBw\iCKRFHDJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG\|ZTDpckBidW:3boSgc4Yh[WOndInsZZRm\CCqaYP0c45mKEh\|IHH0JFAvOyC3TTDh[pRmeiB2ODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	NETCNpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O0OFQ5Pyd-MkezOFQ1QDd:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-H2AX(Ser139) / KU70 / KU80 / RAD51 / RAD52 / ERCC1 ; PubMed: 24155971 PLoS One increasing doses of PXD101 enhanced degradation of KU70, KU80 and RAD51, and enhanced expression of p-H2AX (Ser139), RAD52 and ERCC1 in BHP7-13, WRO82-1 and 8505C. Acetyl Histone H3 / Acetyl Histone H4 / Acetyl tubulin; PubMed: 24155971 PLoS One PXD101 induced acetylation of histone H3 and histone H4 in a dose-dependent manner. PXD101 also increased acetylation of tubulin in BHP7-13, WRO82-1 and 8505C. p21 / p27 ; PubMed: 23982416 Cancer Biol Ther (A and B) The cell lines shown were treated with PXD101 for 0, 2, 4, 8, 24, 48, and 72 h. Whole cell extracts were generated and subjected to western blotting with antibodies against p21, p27, hsp90, α-tubulin, or GAPDH. PXD101-resistant cell lines are shown in (A, left) while PXD101-sensitive cell lines are shown in (B, right). SOS1 / SOS2; PubMed: 28397399 Mol Oncol (A) Cell lysates were harvested from lung SCC cells after treatment with increasing doses of belinostat (PXD101) (0.1, 0.2, 0.3, 1, 3 μm) to evaluate the changes in SOS1 and SOS2. PARP / p-ERK / p-p38 / p38 / p-BRAF / p-MEK / MEK ; PubMed: 28397399 Mol Oncol Cell lysates were harvested from lung SCC cells after treatment with increasing doses of belinostat (0.1, 0.2, 0.3, 1, 3 μm). Immunoblotting was performed to evaluate the changes in phosphorylated protein levels of the targets identified in 1D (ERK1/2, p38, B‐Raf, MEK1/2) as well as PARP. β‐Actin shown as loading control.	24155971 23982416 28397399
Growth inhibition assay	Cell viability; PubMed: 24155971 PLoS One Dose-response curves were obtained on day 4 from cells treated with a series of six 1:1 dilutions of PXD101. IC50; PubMed: 28397399 Mol Oncol Lung SCC cell lines and normal lung fibroblast cell lines were treated with belinostat (PXD101) for 72 h, and cell viability was determined with CellTiter assay. Data are represented as mean IC50 ± SD (n = 3).	24155971 28397399

In vivo

Belinostat indicates significant tumor growth delay in A2780 and A2780/cp70 xenograft at a dose of 10mg/kg with no effects on the body weight. ^[1] Belinostat also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. ^[2] Belinostat monotherapy induces dose-proportional antitumor effects with TGI of 47% at a dose of 100mg/kg in A2780 xenograft. The combination of Belinostat (100 mg/kg) with carboplatin (40 mg/kg) could delay tumor growth from 18.6 days to 22.5 days. ^[3] Combining with bortezomib, Belinostat results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft. ^[5]

Protocol

Kinase Assay:^[1]	- Collapse Histone Deacetylase Activity: Subconfluent cultures are harvested and washed twice in ice cold PBS and pelleted by centrifugation at 200 × g for 5 min. The cell pellet is resuspended in two volumes of lysis buffer [60 mM Tris buffer (pH 7.4) containing 30% glycerol and 450 mM NaCl] and lysed by three freeze (dry ice) thaw (30 °C water bath) cycles. Cell debris is removed by centrifugation at 1.2 × 10⁴ g for 5 min, and the supernatant is stored at −80 °C. Histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRK corresponding to the 20 NH2-terminal residues) is acetylated by a recombinant protein containing the hypoxanthine-aminopterin-thymidine domain of p300, using [³H]acetyl CoA as a source of acetate. H4 peptide (100 μg) is mixed with hypoxanthine-aminopterin-thymidine buffer (50 mM Tris HCl pH 8.0, 5% glycerol, 50 mM KCl, and 0.1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoethyl) benzenesulfonylfluoride, 1 × complete protease inhibitors, 50 μL of purified p300, and 1.85 m [³H]acetyl CoA (4.50Ci/mmol) in a final volume of 300 μL and incubated at 30 °C for 45 min. The p300 protein is removed by incubation with 20 μL of 50% Ni-agaroase beads for 1 hour at 4 °C and centrifugation. The supernatant is applied to a 2 mL Sephadex G15 column, and the flow through is collected. One milliliter of distilled H₂O is gently applied, and three drop fractions are collected; this is repeated until 4–5 mL of distilled H₂O has been added, and ∼40 fractions are collected. Three microliters of each fraction are diluted in 2 mL of scintillation fluid and counted in a scintillation counter to identify the fractions containing the labeled peptide. These fractions are pooled, and 1 μL of the combined sample is measured to assess the radioactivity in every peptide batch (3-7×10³ cpm/μL). 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 1.2× 10⁴ g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted.
Cell Research:^[1]	- Collapse Cell lines: A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852 Concentrations: 0.016 - 10 μM Incubation Time: 24 hours Method: Tumor cell lines are seeded in 5 mL of medium at a density of 8 × 10⁴ cells/25 cm2 flask and incubated for 48 hours. Cells are exposed to Belinostat (0.016 to 10 μM) for 24 hours. 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 0.5-2× 10³ 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 defined as the concentration of belinostat required to reduce the number of colonies to 50% of that of the control untreated cells. (Only for Reference)
Animal Research:^[1]	- Collapse Animal Models: A2780, A2780/cp70 and HCT116 cells are injected s.c. into the right flank of CD1 nu/nu mice. Dosages: ≤40 mg/kg Administration: Administered via i.p. (Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	64 mg/mL (201.03 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing.	10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Belinostat (PXD101) SDF

Molecular Weight	318.35
Formula	C₁₅H₁₄N₂O₄S
CAS No.	414864-00-9
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	NSC726630, PX-105684
Smiles	C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04703920	Recruiting	Drug: Talazoparib\|Drug: Belinostat	Metastatic Breast Cancer\|Metastatic Castration-resistant Prostate Cancer\|Metastatic Ovarian Carcinoma	University of Michigan Rogel Cancer Center\|Pfizer\|Acrotech Biopharma LLC	March 4 2021	Phase 1
NCT04315233	Recruiting	Drug: Ribociclib\|Drug: Belinostat	Metastatic Breast Cancer\|Recurrent Ovarian Carcinoma	University of Utah\|Novartis\|Acrotech Biopharma	October 29 2020	Phase 1
NCT03772925	Recruiting	Drug: Belinostat\|Drug: Pevonedistat	Recurrent Acute Myeloid Leukemia\|Recurrent Myelodysplastic Syndrome\|Refractory Acute Myeloid Leukemia\|Refractory Myelodysplastic Syndrome	National Cancer Institute (NCI)	February 28 2019	Phase 1
NCT02680795	Recruiting	Drug: Belinostat IV	Solid Tumors\|Hematological Malignancies	Acrotech Biopharma LLC\|Axis Clinicals Limited	March 2016	Phase 1
NCT02679131	Terminated	Drug: Belinostat	Relapsed/Refractory Solid Tumors/Hematological Malignancies	Acrotech Biopharma LLC\|Axis Clinicals Limited	March 2016	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Could you please give some suggestions for the use of Belinostat in vivo (i.p. injection)?
Answer:
For I.P. injection, S1085 Belinostat (PXD101) can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 10 mg/ml clearly. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water. Hope this information is useful to you.

HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

Selective HDAC Inhibitors

Rocilinostat (ACY-1215) : HDAC5-selective, IC50=5 nM.
Most Potent HDAC Inhibitor

Quisinostat (JNJ-26481585) : HDAC1, IC50=0.11 nM; HDAC2, IC50=0.33 nM.
FDA-approved HDAC Inhibitor

Vorinostat (SAHA, MK0683) : Approved by FDA against cutaneous T cell lymphoma.
Newest HDAC Inhibitor

RG2833 (RGFP109) ^New : Brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.

Related HDAC Products

CAY10603 ^New

CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
Domatinostat (4SC-202) ^New

Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
Panobinostat (LBH589)

Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Vorinostat (SAHA)

Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Entinostat (MS-275)

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Trichostatin A (TSA)

Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Romidepsin (FK228, Depsipeptide)

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.

Features:More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
Tubastatin A

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Mocetinostat (MGCD0103)

Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.

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Belinostat (PXD101)