Ricolinostat (ACY-1215)

Name: Ricolinostat (ACY-1215)
Brand: Selleck Chemicals
SKU: S8001
Rating: 5 (49 reviews)

For research use only.

Catalog No.S8001 Synonyms: Rocilinostat

49 publications

Ricolinostat (ACY-1215) Chemical Structure

CAS No. 1316214-52-4

Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2.

Selleck's Ricolinostat (ACY-1215) has been cited by 49 publications

Science, 2020, 369(6510)eaas8995

PubMed: 32943500 ( click the link to review the publication )

Elife, 2021, 10e63810

PubMed: 33835029 ( click the link to review the publication )

J Inflamm Res, 2021, 14:1473-1485

PubMed: 33883923 ( click the link to review the publication )

Int J Mol Sci, 2021, 22(3)1341

PubMed: 33572814 ( click the link to review the publication )

Breast Cancer Res Treat, 2021, 186(1):37-51

PubMed: 33452951 ( click the link to review the publication )

Cancers (Basel), 2020, 12(12)E3734

PubMed: 33322608 ( click the link to review the publication )

Front Cell Dev Biol, 2020, 8:689

PubMed: 32984302 ( click the link to review the publication )

Cancer Immunol Immunother, 2020, 20

PubMed: 32435850 ( click the link to review the publication )

Int J Biol Sci, 2020, 16(14):2595-2611

PubMed: 32792859 ( click the link to review the publication )

Am J Physiol Renal Physiol, 2020, 319(6):F1003-F1014

PubMed: 33103445 ( click the link to review the publication )

Oncol Lett, 2020, 20(1):533-540

PubMed: 32565979 ( click the link to review the publication )

BMC Pharmacol Toxicol, 2020, 21(1):21

PubMed: 32178737 ( click the link to review the publication )

Histol Histopathol, 2020, 18237

PubMed: 32572875 ( click the link to review the publication )

Front Cell Dev Biol, 2020, 8:610

PubMed: 32754596 ( click the link to review the publication )

J Immunother Cancer, 2019, 7(1):33

PubMed: 30728070 ( click the link to review the publication )

Cancer Res, 2019, 79(21):5482-5489

PubMed: 31311810 ( click the link to review the publication )

J Neurochem, 2019, 10.1111/jnc.14849

PubMed: 31390677 ( click the link to review the publication )

Front Pharmacol, 2019, 10:653

PubMed: 31244662 ( click the link to review the publication )

Biomed Pharmacother, 2019, 117:109166

PubMed: 31255993 ( click the link to review the publication )

Ann Transl Med, 2019, 7(1):2

PubMed: 30788349 ( click the link to review the publication )

Int J Oncol, 2019, 55(2):499-512

PubMed: 31268156 ( click the link to review the publication )

Life Sci, 2019, 238:116976

PubMed: 31634464 ( click the link to review the publication )

Neurochem Res, 2019, 44(11):2460-2469

PubMed: 31571096 ( click the link to review the publication )

ACS Omega, 2019, 4(22):19895-19904

PubMed: 31788622 ( click the link to review the publication )
Nucl Med Biol, 2019, 74-75:1-11

PubMed: 31421440 ( click the link to review the publication )

Anticancer Res, 2019, 39(12):6731-6741

PubMed: 31810938 ( click the link to review the publication )

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

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

J Pathol, 2018, 246(2):141-153

PubMed: 29876933 ( click the link to review the publication )

Cell Death Dis, 2018,

PubMed: 30050135 ( click the link to review the publication )

Int J Mol Sci, 2018, 19(8)

PubMed: 30081552 ( click the link to review the publication )

J Biol Chem, 2018, 293(6):1976-1993

PubMed: 29259132 ( click the link to review the publication )

Int J Oncol, 2018, 53(2):844-854

PubMed: 29749542 ( click the link to review the publication )

Br J Cancer, 2018, 119(10):1278-1287

PubMed: 30318510 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(6):1280-1290

PubMed: 29483217 ( click the link to review the publication )

Biochem Pharmacol, 2018, 155:316-325

PubMed: 30028995 ( click the link to review the publication )

Biomed Pharmacother, 2018, 97:818-824

PubMed: 29112935 ( click the link to review the publication )

Nat Cell Biol, 2017, 19(8):962-973

PubMed: 28737768 ( click the link to review the publication )

Oncogene, 2017, 10.1038/onc.2016.495

PubMed: 28114281 ( click the link to review the publication )

ACS Chem Biol, 2017, 12(8):2139-2148

PubMed: 28628306 ( click the link to review the publication )

Int J Parasitol Drugs Drug Resist, 2017, 7(1):51-60

PubMed: 28110187 ( click the link to review the publication )

J Periodontol, 2017, 88(1):e12-e23

PubMed: 27562218 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(15):4280-4289

PubMed: 28270494 ( click the link to review the publication )

Drug Des Devel Ther, 2017, 11:1369-1382

PubMed: 28496307 ( click the link to review the publication )

Oncotarget, 2017, 8(61):103797-103814

PubMed: 29262601 ( click the link to review the publication )

Oncotarget, 2016, 7(7):7715-31

PubMed: 26735339 ( click the link to review the publication )

Nat Commun, 2015, 3;6:10091

PubMed: 26631872 ( click the link to review the publication )

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

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

Tumour Biol, 2015, 36(12):9661-5

PubMed: 26150340 ( click the link to review the publication )
Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0481

PubMed: 25552369 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description

Features

Induced less cytotoxicity in PHA-stimulated PBMCs from 4 healthy donors compared with the pan-HDAC inhibitor SAHA.

Targets

HDAC6 ^[1] (Cell-free assay)	HDAC2 ^[1] (Cell-free assay)	HDAC3 ^[1] (Cell-free assay)	HDAC1 ^[1] (Cell-free assay)	HDAC8 ^[1] (Cell-free assay)
4.7 nM	48 nM	51 nM	58 nM	100 nM

In vitro

ACY-1215 is a hydroxamic acid derivative. ACY-1215 is 12-, 10-, and 11-fold less active against HDAC1, HDAC2, and HDAC3 (class I HDACs), respectively. ACY-1215 has minimal activity (IC50 > 1μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1μM). The IC50 values for ACY-1215 for T-cell toxicity is 2.5μM. ACY-1215 overcomes tumor cell growth and survival conferred by BMSCs and cytokines in the BM milieu. ACY-1215 in combination with bortezomib induces synergistic anti-MM activity. ACY-1215 induces potent acetylation of α-tubulin at very low doses and triggers acetylation of lysine on histone H3 and histone H4 only at higher doses, confirming its specific inhibitory effect on HDAC6 activity. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
A-172	MmCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2DNOFExyqCwTR?=	NF;v[YgzPC92ODDo	MV\pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5	M3nkTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUWwN\|QxLz5{NkG1NFM1ODxxYU6=
U87MG	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFLDPIgyOMLibl2=	Mnn6NlQwPDhiaB?=	M1P0NolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk>	NVXuSWNURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOVA{PDBpPkK2NVUxOzRyPD;hQi=>
Hbl-1	MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MVi0PEBp	NGTKNlBKSzVyPUGuOkDPxE1?	NIHVeYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
OCI-Ly10	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Ml[1OFghcA>?	MkezTWM2OD1yLkmg{txO	M4\TXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Riva	NX;tXm52T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		Ml7TOFghcA>?	MVTJR\|UxRTJwMjFOwG0>	MlKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO\|AoRjJ4MUG2NlcxRC:jPh?=
Su-DHL2	M1vsTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NX7KV2h7PDhiaB?=	M3rtfGlEPTB;Mz6zJO69VQ>?	Mn2xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO\|AoRjJ4MUG2NlcxRC:jPh?=
OCI-Ly1	NVjtOnZUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NUjme\|lkPDhiaB?=	NHHUT5dKSzVyPUKuOEDPxE1?	Mlj2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO\|AoRjJ4MUG2NlcxRC:jPh?=
OCI-Ly7	M{LsNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MXe0PEBp	NGLxcI9KSzVyPUGuNkDPxE1?	NV[0WVN1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Su-DHL4	M33BOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MXi0PEBp	MmPhTWM2OD12Lkeg{txO	NXf2[29KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Su-DHL6	NH3RTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkO3OFghcA>?	MkHQTWM2OD1\|LkKg{txO	NEnlNow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Hbl-2	MoHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MnzpOFghcA>?	NXez[IZCUUN3ME2xMlkh\|ryP	M2nyNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Jeko-1	NH76cm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MljFOFghcA>?	MmXjTWM2OD1zLkWg{txO	NU\6UnlPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Jvm-2	MmnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M1;6W\|Q5KGh?	MYjJR\|UxRTRwMDFOwG0>	M1vQVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Rec-1	NHGwfmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mmf6OFghcA>?	NILz[4NKSzVyPUKuN{DPxE1?	NX70fYR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
CCL-119	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mn3WOFghcA>?	MUjJR\|UxRTFwNzFOwG0>	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO\|A9N2F-
H9	MkjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M1jzW\|Q5KGh?	MoDVTWM2OD1zLkKg{txO	NHzRUG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
HH	NHjiNHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NWH2T3NXPDhiaB?=	NIfFe4VKSzVyPUKuOUDPxE1?	NHS0VYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Sup-T1	NHfwWFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NGfEdms1QCCq	NIfJeHVKSzVyPUGuOkDPxE1?	Mke3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO\|AoRjJ4MUG2NlcxRC:jPh?=
MM.1S	MmLNSpVv[3Srb36gRZN{[Xl?	NUfnVJo4OC13zszN	Mn\lOkBp	NWDsOlFQcW6lcnXhd4V{KGGlZYT5cIF1\WRizsGteJVjfWyrbh?=	NWrVOmN5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
MM.1S	NIL3NGRHfW6ldHnvckBCe3OjeR?=	NUnnfWNFOC5{NT:x{txO	NXvQUXpPOThiaB?=	M1jEb4lv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5?	NWe3W3RbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
MM.1R	MX;GeY5kfGmxbjDBd5NigQ>?	NFL2fYUxNjJ3L{JOwG0>	MkXCNVghcA>?	MoLHbY5kemWjc3XzJIFk\XS7bHH0[YQh\|rFvdIXieYxqdg>?	MmHnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO\|YxRC:jPh?=
RPMI8226	NXTSe2d{TnWwY4Tpc44hSXO\|YYm=	MViwMlI2NzIQvF2=	NWPBd3VVOThiaB?=	MoXqbY5kemWjc3XzJIFk\XS7bHH0[YQh\|rFvdIXieYxqdg>?	MnnuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO\|YxRC:jPh?=
MM.1S	M1zaTWNmdGxiVnnhZoltcXS7IFHzd4F6	MXGwMVjPxE1?	Mnj2OFghcA>?	Ml6z[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	M4P2WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[yO\|YxLz5{MkK2Nlc3ODxxYU6=
OPM1	MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	MWqwMVjPxE1?	NFfuSXM1QCCq	NUfpUFVu\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	NHywU5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
RPMI	MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NX[zdo5sOC16zszN	NXm1WoNMPDhiaB?=	MVrk[YNz\WG\|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	NVfXT4J3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
MM.1R	MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NYHxPG1vOC16zszN	MmG1OFghcA>?	MYDk[YNz\WG\|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	NVX5W\|NzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
LR5	MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	M1zuOVAuQM7:TR?=	NXy5bYpuPDhiaB?=	NX\uZoFk\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
OPM2	NV:2[G1DS2WubDDWbYFjcWyrdImgRZN{[Xl?	MmTiNE05\|ryP	MWm0PEBp	MUjk[YNz\WG\|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	NFH1SJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
Sf9	M{jHZWZ2dmO2aX;uJIF{e2G7		NX;Tbo1IOTBibXnudy=>	MWLJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIHj1cYFvKHKnY3;tZolv[W62IF6teIVzdWmwYXygS3NVNXSjZ3fl[EBJTEGFNjDlfJBz\XO\|ZXSgbY4hW2Z7IHPlcIx{KHW\|aX7nJGZVWyCjczDzeYJ{fHKjdHWgdJJmcW6ldXLheIVlKG[xcjCxNEBucW6\|IH\vcIxwf2WmIHL5JJN2[nO2cnH0[UBi\GSrdHnvckBu\WG\|dYLl[EBwfmW{IEOwJI1qdnNuIFnDOVAhRSByLkCwOFch\|ryPLh?=	MmPDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{izNlQoRjJ6MEO4N\|I1RC:jPh?=
Sf9	M{GxVGZ2dmO2aX;uJIF{e2G7		MmfkNVUhdWmwcx?=	NVjTNpBIUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBPNXSncn3pcoFtKEeVVD30ZYdo\WRiSFTBR\|Yh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnQSClZXzsd{B2e2mwZzDCc4MuVHm\|LTjBZ{kuSU2FIHHzJJN2[nO2cnH0[UBxemWrbnP1ZoF1\WRiZn;yJFE2KG2rboOg[o9tdG:5ZXSgZpkhe3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFYxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwJF0hOC5yMEmg{txONg>?	NUWwdYw1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NFAyOzBpPkK5OVAxOTNyPD;hQi=>
Sf9	NH36[WdHfW6ldHnvckBie3OjeR?=		MY[xOUBucW6\|	NVq2Olh7UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBENXSncn3pcoFtKEircz30ZYdo\WRiSFTBR\|MwVi22ZYLtbY5idCCJU2SteIFo\2WmIF7DU3IzKCh\|OUWgeI8hPDh7IILld4llfWW\|KTDlfJBz\XO\|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRic3[5JINmdGy\|IIXzbY5oKEKxYz3MfZMuMEGlKT3BUWMh[XNic4Xid5Rz[XSnIIDy[Ylv[3WkYYTl[EBnd3JiMUWgcYlveyCob3zsc5dm\CCkeTDzeYJ{fHKjdHWgZYRlcXSrLDDJR\|UxKD1iMD6wN\|ch\|ryPLh?=	M17vPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUCwNVMxLz5{OUWwNFE{ODxxYU6=
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Sf9	NHzVcJNHfW6ldHnvckBie3OjeR?=		NF63fGMyPSCvaX7z	MXjJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIFOteIVzdWmwYXygSmxCTy:KaYOteIFo\2WmIFjERWMyKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EB{\jliY3XscJMhfXOrbnegRo9kNUy7cz2oRYMqNUGPQzDhd{B{fWK\|dILheIUheHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkA3OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDhd5MtKEmFNUCgQUAxNjFizszNMi=>	M{PBV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUCwNVMxLz5{OUWwNFE{ODxxYU6=
BCP-ALL	NV7je4Z7S3m2b4TvfIlkcXS7IHHzd4F6		NHH3O3o4OiCqcoO=	MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCR3AuSUyOIHPlcIx{KGSncnn2[YQh\nKxbTDwZZRq\W62IEGgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCwMlI6KM7:TT6=	NWfTdIR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN\|Y2QDl{PD;hQi=>
BCP-ALL	MlT5R5l1d3SxeHnjbZR6KGG\|c3H5		M{PzVVczKGi{cx?=	M2Pj[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJEWC2DTFygZ4VtdHNiZHXybZZm\CCocn;tJJBifGmnboSgOEBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPTRizszNMi=>	M3LPbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5\|MEO2OVg6OjxxYU6=
BCP-ALL	MmTQR5l1d3SxeHnjbZR6KGG\|c3H5		MnnMO\|IhcHK\|	MoPNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmNRNUGOTDDj[YxteyCmZYLpeoVlKG[{b32gdIF1cWWwdDCyJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gNE42QCEQvF2u	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
RPMI8226	NIXB[pFEgXSxdH;4bYNqfHliYYPzZZk>		MXS3NkBpenN?	MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOS52Nkig{txONg>?	M2fqSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NESzNFc5Lz5{NkS0N\|A4QDxxYU6=
SEM	M4jITGN6fG:2b4jpZ4l1gSCjc4PhfS=>		MmX4O\|IhcHK\|	M{GzU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNGVSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFEvPjFizszNMi=>	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
SUP-B15	M1nuPGN6fG:2b4jpZ4l1gSCjc4PhfS=>		NWnIWXIzPzJiaILz	MlvJR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3VRNUJzNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW\|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDFwOUKg{txONg>?	M4rjVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5\|MEO2OVg6OjxxYU6=
RPMI18226	MX;DfZRwfG:6aXPpeJkh[XO\|YYm=		M1\VUlczKGi{cx?=	NF;JTJBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTWE2LMUiyNlYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCxMlk4KM7:TT6=	MmHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
HL60	Moq3R5l1d3SxeHnjbZR6KGG\|c3H5		NHHJRoQ4OiCqcoO=	M1zkdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAzNjN4IN88UU4>	NWjUWnIxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN\|Y2QDl{PD;hQi=>
HL60	M2XxPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NFzwbFc1QCCqcoO=	M{fYZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB2ODDodpMhcW5icILld4Vv[2Vib3[gTmFMOiCrbnjpZol1d3JiQ2nUMVM5PyCkeTDDR2suQCCjc4PhfUwhUUN3MDC9JFIvPTRizszNMi=>	NY[3OZdtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFAyOTVpPkK5PVQxOTF3PD;hQi=>
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HEL	M1nqfmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NX3NXXVHPDhiaILz	MmLPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKRVygZ4VtdHNiYX\0[ZIhPDhiaILzJIlvKHC{ZYPlcoNmKG:oIFrBT\|IhcW6qaXLpeI9zKEO\VD2zPFch[nliQ1PLMVgh[XO\|YYmsJGlEPTBiPTCyMlU1KM7:TT6=	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MEGxOUc,Ojl7NECxNVU9N2F-
KCL22	NVXMeZc3S3m2b4TvfIlkcXS7IHHzd4F6		M4jaRVczKGi{cx?=	NEe2S5BEgXSxdH;4bYNqfHliYXfhbY5{fCCrbXH0bY5q[i2{ZYPpd5RidnRiaIXtZY4hU0OOMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB\|LkO4JO69VS5?	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
U266	M3;kSmN6fG:2b4jpZ4l1gSCjc4PhfS=>		NELBT\|Q4OiCqcoO=	NX3oOlhqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTJ4NjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW\|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDNwNUKg{txONg>?	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
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KCL22	M1;PVmN6fG:2b4jpZ4l1gSCjc4PhfS=>		MnT4O\|IhcHK\|	NEHITYlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMS0x{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW\|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDNwN{Wg{txONg>?	MkDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
HL60	NVPybIk4SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NWHF[pVTPDhiaILz	NVS3ZYI{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDDR2suQCCjc4PhfUwhUUN3MDC9JFMvPzVizszNMi=>	M2fNPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwNVE2Lz5{OUm0NFEyPTxxYU6=
K562	MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MXi0PEBpenN?	Ml3CRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNNU[yJINmdGy\|IHHmeIVzKDR6IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OCB;IEOuO\|Uh\|ryPLh?=	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MEGxOUc,Ojl7NECxNVU9N2F-
HEL	Mn;pRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NH7FWmw1QCCqcoO=	MlXsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKRVygZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR\|UxKD1iMz63OUDPxE1w	M2TZbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwNVE2Lz5{OUm0NFEyPTxxYU6=
BCP-ALL	M1TyNGN6fG:2b4jpZ4l1gSCjc4PhfS=>		NXTZTploPzJiaILz	M2DmOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJEWC2DTFygZ4VtdHNiZHXybZZm\CCocn;tJJBifGmnboSgN{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQvPDVizszNMi=>	MlLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
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SH-SY5Y	NXr6fIR2TnWwY4Tpc44h[XO\|YYm=	MljHNE4yKHSxIEGgeW0>	MX2yOEBpenN?	NHn6XWJKdmirYnn0bY9vKG:oIFjERWM3KGmwIHj1cYFvKFOKLWPZOXkh[2WubIOgZZN{\XO\|ZXSgZZMhcW6lcnXhd4UhcW5iYXPleJlt[XSrb36gc4Yh[WyyaHGteJVjfWyrbjDheEAxNjFidH:gNUB2VSCjZoTldkAzPCCqcoOgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	MkLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMki2NVYoRjNyMEK4OlE3RC:jPh?=
SH-SY5Y	M4rQTGZ2dmO2aX;uJIF{e2G7	MV2wMlEhfG9iMTD1US=>	MWWyOEBpenN?	MVHJcohq[mm2aX;uJI9nKGOuYYPzJFEhUESDQzDpckBpfW2jbjDTTE1UYTW\IHPlcIx{KGG\|c3Xzd4VlKGG\|IHnuZ5Jm[XOnIHnuJIFk\XS7bHH0bY9vKG:oIHjpd5RwdmViSEOgZZQhOC5zIITvJFEhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	NFzI[ZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MECyPFYyPid-M{CwNlg3OTZ:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	Ac-α-tubulin / Ac-Histone H4 ; PubMed: 31015208 Blood Adv Ricolinostat promotes the accumulation of acetylated (Ac) α-tubulin. MM cells were treated with the indicated concentrations of ricolinostat for 24 hours. Protein expression was measured by immunoblotting. Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1; PubMed: 30050135 Cell Death Dis Western blot analysis of G2/M phase cell cycle regulatory-proteins for 48 h Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP; PubMed: 30050135 Cell Death Dis Western blot analysis of apoptosis regulatory-proteins for 48 h PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK; PubMed: 30050135 Cell Death Dis ACY-1215 treatment inhibited PI3K/AKT/mTOR and ERK signaling protein levels in ESCC EC109 and TE-1 cell lines for 48 h. Ac-β-catenin(K49) / p-β-catenin / β-catenin; PubMed: 25546293 ACS Chem Biol Time-course immunoblot analysis of human NPCs treated with an HDAC6 inhibitor. Human NPCs were treated with HDAC6 inhibitor ACY-1215 at 5 μM for the times points indicated and the lysates immunoblotted with antibodies against β-catenin, Ac-Lys49-β-catenin, phos-Ser45 and phos-Ser33, Ser37, and Thr41. β-actin is using shown as loading control.	31015208 30050135 25546293
Immunofluorescence	β-tubulin / β-catenin; PubMed: 25546293 ACS Chem Biol Immunofluorescence staining for β-catenin treated with HDAC6 inhibitor in human NPCs. Cells were treated with 5 μM ACY-1215 or DMSO for 18 h and imaged with anti-β-catenin antibody (green), anti-β-tubulin antibody (red), and Hoechst 33342 (blue). Scale bar, 20 μm. Quantification of β-catenin levels at the membrane represent two independent experiments with three fields of view each at 20× magnification. Error bars indicate standard deviation. and ** denote significance at p < 0.01 and p < 0.0001, respectively (unpaired t test).	25546293
Growth inhibition assay	Cell viability; PubMed: 31015208 Blood Adv Ricolinostat decreases MM cell viability. A panel of MM cell lines was treated with the indicated concentrations of ricolinostat for 72 hours. Cell viability was measured by MTT assay.	31015208

In vivo

ACY-1215 in combination with bortezomib triggered more significant anti-MM activity than either agent alone in suppressing tumor growth and prolonging survival in both plasmacytoma model and disseminated MM model without significant adverse effects. ACY-1215 is readily absorbed by tumor tissue. Moreover, the drug does not accumulate in tumor tissue, as evidenced by the parallel decline of acetylated α-tubulin in blood cells and tumor tissue by 24 hours after dose. ^[1]

Protocol

Kinase Assay: ^[1]	- Collapse HDAC enzymatic assays: ACY-1215 is dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated.
Cell Research: [1]	- Collapse Cell lines: MM cell lines, patient MM cells, and PBMCs Concentrations: ~8 μM Incubation Time: 48 hours Method: PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of ACY-1215. DNA synthesis is measured by tritiated thymidine uptake. CD4⁺T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3 × 10⁴cells/well) are incubated in 96-well culture plates with medium and different concentrations of ACY-1215, bortezomib, and/or recombinant IL-6 (10 ng/mL) or insulin-like growth factor-1 (IGF-1; 50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured. (Only for Reference)
Animal Research: ^[1]	- Collapse Animal Models: MM xenograft SCID mouse model Dosages: 50 mg/kg Administration: ip (Only for Reference)

References

[1] Santo L, et al. Blood, 2012, 119(11), 2579-2589.

Solubility (25°C)

In vitro	DMSO	86 mg/mL (198.38 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.	5mg/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 Ricolinostat (ACY-1215) SDF

Molecular Weight	433.5
Formula	C₂₄H₂₇N₅O₃
CAS No.	1316214-52-4
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	Rocilinostat
Smiles	C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO

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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.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02632071	Completed	Drug: ACY-1215\|Drug: Nab-paclitaxel	Metastatic Breast Cancer\|Breast Carcinoma	Columbia University\|Acetylon Pharmaceuticals Incorporated\|National Cancer Institute (NCI)	March 1 2016	Phase 1
NCT01583283	Active not recruiting	Drug: ACY-1215\|Drug: lenalidomide\|Drug: Dexamethasone	Multiple Myeloma	Celgene	July 12 2012	Phase 1\|Phase 2
NCT01323751	Completed	Drug: ACY-1215	Multiple Myeloma	Celgene\|The Leukemia and Lymphoma Society	July 2011	Phase 1\|Phase 2

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

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Frequently Asked Questions

Question 1:
What would you suggest to obtain a clear solution?
Answer:
S8001 ACY-1215 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 5 mg/ml clearly while it in 1% DMSO/30% polyethylene glycol/1% Tween 80 at 30 mg/ml is a suspension for oral administration. Please note that the precipitation will go out from the clear solution after stayed for about half an hour, So it is recommended to prepare the solution just before use.

HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

Pan HDAC Inhibitor

Panobinostat (LBH589) : Pan-HDAC inhibitor, 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

LMK-235 ^New

LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
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.
RGFP966

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
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.

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Ricolinostat (ACY-1215)