Ricolinostat (ACY-1215)

For research use only.

Catalog No.S8001 Synonyms: Rocilinostat

44 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.

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Selleck's Ricolinostat (ACY-1215) has been cited by 44 publications

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Biological Activity

Description 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.
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 Formulation Activity Description PMID
A-172 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYixNOKhdk1? MWGyOE81QCCq Ml7nbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NX;Pco9ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOVA{PDBpPkK2NVUxOzRyPD;hQi=>
U87MG MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvHNVDDqG6P MVuyOE81QCCq MXrpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NUD2O4VjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOVA{PDBpPkK2NVUxOzRyPD;hQi=>
Hbl-1 NGPWUJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjUXHI1QCCq M4n5XmlEPTB;MT62JO69VQ>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
OCI-Ly10 M37WWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\JWXVTPDhiaB?= MlX1TWM2OD1yLkmg{txO MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Riva NEj6XI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fNXVQ5KGh? MYDJR|UxRTJwMjFOwG0> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Su-DHL2 M2T6UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED1c3M1QCCq NV3hVZVSUUN3ME2zMlMh|ryP M{Wwd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
OCI-Ly1 NWPqb2xlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfP[Gs1QCCq NUDEVFF[UUN3ME2yMlQh|ryP M1fRc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
OCI-Ly7 M1;Dd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7WOFghcA>? NV7xZW01UUN3ME2xMlIh|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Su-DHL4 MmDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXjOFghcA>? NFG2R|VKSzVyPUSuO{DPxE1? NE\vOWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Su-DHL6 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;lUYM2PDhiaB?= MYDJR|UxRTNwMjFOwG0> NELPWXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Hbl-2 MmTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDQRWJoPDhiaB?= Mn\XTWM2OD1zLkmg{txO Mni4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
Jeko-1 M33DVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XUWVQ5KGh? NUPnbYhxUUN3ME2xMlUh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Jvm-2 M1\4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTaOFghcA>? NUfjUYJlUUN3ME20MlAh|ryP MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Rec-1  NETxXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fYSFQ5KGh? MVzJR|UxRTJwMzFOwG0> MoLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
CCL-119 Mn\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUG0PEBp MkTQTWM2OD1zLkeg{txO NHfZ[oE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
H9 NGjpSIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLVOFghcA>? NHXJdohKSzVyPUGuNkDPxE1? M{ezWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
HH M4iyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XMTFQ5KGh? NGrEXZVKSzVyPUKuOUDPxE1? NIW3W5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Sup-T1 NFTSdmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDMNVAxPDhiaB?= M{XWWmlEPTB;MT62JO69VQ>? NHXnNlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
MM.1S MmHVSpVv[3Srb36gRZN{[Xl? MW[wMVXPxE1? NYrBTFBwPiCq M2O0U4lv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? MlnvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
MM.1S M{DyXWZ2dmO2aX;uJGF{e2G7 M4Dh[|AvOjVxMd88US=> MmPKNVghcA>? M4CwdYlv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? Mk\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
MM.1R NV;UUHB2TnWwY4Tpc44hSXO|YYm= MlTwNE4zPS9zzszN NXL0VIM4OThiaB?= MknMbY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? NYmycnN5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
RPMI8226  NX3CZ|BUTnWwY4Tpc44hSXO|YYm= M3HJZVAvOjVxMd88US=> MX:xPEBp NH7KXYtqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
MM.1S NV3oeohNS2WubDDWbYFjcWyrdImgRZN{[Xl? MYewMVjPxE1? MUm0PEBp M3vnboRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF3xfYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
OPM1 NVvFRYhXS2WubDDWbYFjcWyrdImgRZN{[Xl? NWW0N3h3OC16zszN MoPzOFghcA>? MlW4[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
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HL60 NEfxcJlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MlzQOFghcHK| MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR|UxKD1iMz63OUDPxE1w NXTaeHlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFAyOTVpPkK5PVQxOTF3PD;hQi=>
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OHS-50 NVXGOmt7eUiWUzDhd5NigQ>? Mmf1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M1[2cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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MG 63 (6-TG R) M3j3cJFJXFNiYYPzZZk> M2rNWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= NIPTfYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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HL60 NGXjOnpHfW6ldHnvckBie3OjeR?= MVKwMlEhfG9iMUCgeW0> NGXlNmUzPCCqcoO= NXnsflZPUW6qaXLpeIlwdiCxZjDISGFEPiCrbjDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGGlZYT5cE1idHCqYTD0eYJ2dGmwIHX4dJJme3Orb36gZZQhOC5zIITvJFExKHWPIHHmeIVzKDJ2IHjyd{BjgSCrbX31co9jdG:2IHHzd4F6 MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
SEM MXnGeY5kfGmxbjDhd5NigQ>? NXPZXJZHOC5zIITvJFExKHWP M13FdFI1KGi{cx?= MlfvTY5pcWKrdHnvckBw\iCKRFHDOkBqdiCqdX3hckBUTU1iY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZYNmfHmuLXHsdIhiKHS3YoXsbY4h\XiycnXzd4lwdiCjdDCwMlEhfG9iMUCgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5Qh[XO|YYm= NV\JTXRJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN|Y2QDl{PD;hQi=>
SUP-B15 NHfGU3BHfW6ldHnvckBie3OjeR?= NWnGT3p4OC5zIITvJFExKHWP NVi1N|hOOjRiaILz MmfQTY5pcWKrdHnvckBw\iCKRFHDOkBqdiCrbXH0bY5q[i2{ZYPpd5RidnRiaIXtZY4hW1WSLVKxOUBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCjY3X0fYwu[WyyaHGgeJVjfWyrbjDlfJBz\XO|aX;uJIF1KDBwMTD0c{AyOCC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdDDhd5NigQ>? M3PsblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
HL60 MV;GeY5kfGmxbjDhd5NigQ>? MXqwMlEhfG9iMUCgeW0> MlPMNlQhcHK| NF76XVRKdmirYnn0bY9vKG:oIFjERWM3KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[WOndInsMYhqe3SxbnWgTFMh\XiycnXzd4lwdiCjdDCwMlEhfG9iMUCgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5Qh[XO|YYm= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
SEM Mo\lSpVv[3Srb36gZZN{[Xl? M1fGb|AvOSC2bzCxNEB2VQ>? NHTHVIszPCCqcoO= NGTmUVZKdmirYnn0bY9vKG:oIFjERWM3KGmwIHj1cYFvKFOHTTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBi[2W2eXytbIl{fG:wZTDIN{BmgHC{ZYPzbY9vKGG2IECuNUB1dyBzMDD1UUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveEBie3OjeR?= NYLDSWYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN|Y2QDl{PD;hQi=>
SUP-B15 NWSxSm1wTnWwY4Tpc44h[XO|YYm= M2eyNVAvOSC2bzCxNEB2VQ>? Mlv1NlQhcHK| MVLJcohq[mm2aX;uJI9nKEiGQVO2JIlvKGmvYYTpcoljNXKnc3nzeIFvfCCqdX3hckBUXVBvQkG1JINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGGlZYT5cE1pcXO2b37lJGg{KGW6cILld5Nqd25iYYSgNE4yKHSxIEGwJJVOKGGodHXyJFI1KGi{czDifUBqdW23bn;icI91KGG|c3H5 MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
HL60 MXnGeY5kfGmxbjDhd5NigQ>? NHf1PGwxNjFidH:gNVAhfU1? M1jpXVI1KGi{cx?= NEDPVHdKdmirYnn0bY9vKG:oIFjERWM3KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2ynYY\l[EBRSVKSIHX4dJJme3Orb36gZZQhOC5zIITvJFExKHWPIHHmeIVzKDJ2IHjyd{BjgSCrbX31co9jdG:2IHHzd4F6 MnG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
SEM NWr5Z4pTTnWwY4Tpc44h[XO|YYm= M1SxWVAvOSC2bzCxNEB2VQ>? Ml2wNlQhcHK| NYrPfos6UW6qaXLpeIlwdiCxZjDISGFEPiCrbjDoeY1idiCVRV2gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[2ynYY\l[EBRSVKSIHX4dJJme3Orb36gZZQhOC5zIITvJFExKHWPIHHmeIVzKDJ2IHjyd{BjgSCrbX31co9jdG:2IHHzd4F6 M1LjeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
SUP-B15 MYHGeY5kfGmxbjDhd5NigQ>? MkCwNE4yKHSxIEGwJJVO MlHnNlQhcHK| NWPMc|J4UW6qaXLpeIlwdiCxZjDISGFEPiCrbjDpcYF1cW6rYj3y[ZNqe3SjboSgbJVu[W5iU2XQMWIyPSClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjcIVifmWmIGDBVnAh\XiycnXzd4lwdiCjdDCwMlEhfG9iMUCgeW0h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3Lsc5Qh[XO|YYm= M3HFSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
SEM M3noNmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MYGyOEB1dyB5MjDodpM> NX\zd|ZISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSW0h[2WubIOgZZQhUUN3MDD0c{AzKHSrbXXzJGlEPTBiYX\0[ZIhOjRidH:gO|IhcHK|IHL5JJRzgXCjbjDlfINtfXOrb36gcYV1cG:m MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
HEL Mm\RR4VtdCCleXPs[UBie3OjeR?= NIfUOpMyKHSxIEGwJJVO M3fWdVQ5KGi{cx?= MWnD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDISWwh[2WubIOgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIHH0JGcyKHCqYYPlJIF1KDFidH:gNVAhfU1iYX\0[ZIhPDhiaILzJJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZoF{\WRiZnzve{BkgXSxbXX0dpk> Ml3FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NECxNVUoRjJ7OUSwNVE2RC:jPh?=
SEM MmjtSpVv[3Srb36gZZN{[Xl? MmfMNVghcHK| MUnJcohq[mm2aX;uJI9nKEiGQVO2JIlvKGi3bXHuJHNGVSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDh[4dz\XOxbXWgZYNkfW23bHH0bY9vKGG2IFnDOVAh[W[2ZYKgNVghcHK|IHL5JIZtfW:{ZYPj[Y5k\SCvaXPyc5Nkd3CrYzDt[ZRpd2R? NWfJUoZLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN|Y2QDl{PD;hQi=>
SEM M3eyXGZ2dmO2aX;uJIF{e2G7 M2j5c|EvPiC3TR?= M{HETFE5KGi{cx?= NYrtTWc6UW6qaXLpeIlwdiCxZjDISGFEPiCrbjDoeY1idiCVRV2gZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[WepcnXzc41mKGGlY4XteYxifGmxbjDheEAyNjZidV2gZYZ1\XJiMUigbJJ{KGK7IF\BR3Mh[W6jbInzbZM> MljUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
SH-SY5Y M3rxPGZ2dmO2aX;uJIF{e2G7 NFnLVFUxNjFidH:gNUB2VQ>? NGfB[FczPCCqcoO= MYTJcohq[mm2aX;uJI9nKEiGQVO2JIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[WOndInsZZRqd25ib3[gZYxxcGFvdIXieYxqdiCjdDCwMlEhfG9iMTD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MmrtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMki2NVYoRjNyMEK4OlE3RC:jPh?=
SH-SY5Y MYDGeY5kfGmxbjDhd5NigQ>? MnHyNE4yKHSxIEGgeW0> MUiyOEBpenN? NHnCXYxKdmirYnn0bY9vKG:oIHPsZZN{KDFiSFTBR{BqdiCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFMh[XRiMD6xJJRwKDFidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MnL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMki2NVYoRjNyMEK4OlE3RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Ac-α-tubulin / Ac-Histone H4 ; 

PubMed: 31015208     


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     


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     


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     


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     


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     


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     


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]

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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]

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  • 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]

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  • Animal Models: MM xenograft SCID mouse model
  • Dosages: 50 mg/kg
  • Administration: ip
    (Only for Reference)

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

Molecular Weight 433.5
Formula

C24H27N5O3

CAS No. 1316214-52-4
Storage powder
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

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 Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

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)

  • Mass
    Concentration
    Volume
    Molecular Weight

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

Dilution Calculator

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 )

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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

Mass Concentration Volume Molecular Weight

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.

  • * Indicates a Required Field

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID