Ricolinostat (ACY-1215)

Name: Ricolinostat (ACY-1215)
Brand: Selleck Chemicals
SKU: S8001
Rating: 5 (44 reviews)

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.

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

Science, 2020, 369(6510)eaas8995

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

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

PubMed: 33572814 ( 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 )

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, 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	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-
RPMI	M{PaTGNmdGxiVnnhZoltcXS7IFHzd4F6	NE\wfXoxNTkQvF2=	NX:0fFRwPDhiaB?=	Mo\h[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	NXvUe\|JbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
MM.1R	NVzvNVdbS2WubDDWbYFjcWyrdImgRZN{[Xl?	MY[wMVjPxE1?	M2\4bFQ5KGh?	NEXTNm5l\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	M17Te\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[yO\|YxLz5{MkK2Nlc3ODxxYU6=
LR5	NX7ydZJuS2WubDDWbYFjcWyrdImgRZN{[Xl?	NYDPNmh6OC16zszN	NUPyS\|RkPDhiaB?=	NIfxSYdl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	M{TkSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[yO\|YxLz5{MkK2Nlc3ODxxYU6=
OPM2	MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NVfuZpdbOC16zszN	NWX1em02PDhiaB?=	M1TIdoRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	Mnn3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO\|YxRC:jPh?=
Sf9	M{e2W2Z2dmO2aX;uJIF{e2G7		MnnmNVAhdWmwcx?=	NFTX[mZKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJIh2dWGwIILlZ49u[mmwYX70JG4ufGW{bXnuZYwhT1OWLYTh[4dm\CCKRFHDOkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy\|IIXzbY5oKE[WUzDhd{B{fWK\|dILheIUheHKnaX7jeYJifGWmIH\vdkAyOCCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCxdnXyJFMxKG2rboOsJGlEPTBiPTCwMlAxPDdizszNMi=>	MmfoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{izNlQoRjJ6MEO4N\|I1RC:jPh?=
Sf9	NVfpPJZVTnWwY4Tpc44h[XO\|YYm=		NFvKN20yPSCvaX7z	M4L0OWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBIW1RvdHHn[4VlKEiGQVO2JIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDz[lkh[2WubIOgeZNqdmdiQn;jMWx6ey1qQXOpMWFOSyCjczDzeYJ{fHKjdHWgdJJmcW6ldXLheIVlKG[xcjCxOUBucW6\|IH\vcIxwf2WmIHL5JJN2[nO2cnH0[UBi\GSrdHnvckBu\WG\|dYLl[EBi\nSncjC2NEBucW6\|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFAvODB7IN88UU4>	M2LCe\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUCwNVMxLz5{OUWwNFE{ODxxYU6=
Sf9	MlW4SpVv[3Srb36gZZN{[Xl?		Moq4NVUhdWmwcx?=	MVLJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIFOteIVzdWmwYXygTIl{NXSjZ3fl[EBJTEGFMz;OMZRmem2rbnHsJGdUXC22YXfn[YQhVkORUkKgLFM6PSC2bzC0PFkhemW\|aXT1[ZMqKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EB{\jliY3XscJMhfXOrbnegRo9kNUy7cz2oRYMqNUGPQzDhd{B{fWK\|dILheIUheHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIktKEmFNUCgQUAxNjB\|NzFOwG0v	NIGwRVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWwNFE{OCd-Mkm1NFAyOzB:L3G+
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Sf9	NF7JWFVHfW6ldHnvckBie3OjeR?=		NIS4NIsyOCCvaX7z	MonXTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDoeY1idiC{ZXPvcYJqdmGwdDDDMZRmem2rbnHsJGZNSUdvSHnzMZRi\2enZDDISGFEOSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJV{cW6pIF\UV{BieyC\|dXLzeJJifGVicILlbY5kfWKjdHXkJIZweiBzMDDtbY5{KG[xbHzve4VlKGK7IIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDveoVzKDNyIH3pcpMtKEmFNUCgQUAxNjB3ODFOwG0v	NEDLTlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECzPFMzPCd-MkiwN\|g{OjR:L3G+
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Sf9	M1PUWWZ2dmO2aX;uJIF{e2G7		M2nN[lE2KG2rboO=	NFLzZphKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGMufGW{bXnuZYwhTkyDRz;IbZMufGGpZ3XkJGhFSUNzIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CC\|ZkmgZ4VtdHNidYPpcochSm:lLVz5d{0pSWNrLVHNR{BieyC\|dXLzeJJifGVicILlbY5kfWKjdHXkJIZweiBzNTDtbY5{KG[xbHzve4VlKGK7IIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB4MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBie3NuIFnDOVAhRSByLkGg{txONg>?	MlqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MECxN\|AoRjJ7NUCwNVMxRC:jPh?=
BCP-ALL	MXzDfZRwfG:6aXPpeJkh[XO\|YYm=		MkfTO\|IhcHK\|	NVzJV4c3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkOSLVHMUEBk\WyuczDk[ZJqfmWmIH\yc40heGG2aXXueEAyKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5{OTFOwG0v	M4KzWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5\|MEO2OVg6OjxxYU6=
BCP-ALL	NFeyNnREgXSxdH;4bYNqfHliYYPzZZk>		NED0c3E4OiCqcoO=	MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCR3AuSUyOIHPlcIx{KGSncnn2[YQh\nKxbTDwZZRq\W62IESgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCwMlU1KM7:TT6=	MojJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
BCP-ALL	M{TGbWN6fG:2b4jpZ4l1gSCjc4PhfS=>		NHfvdlk4OiCqcoO=	MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCR3AuSUyOIHPlcIx{KGSncnn2[YQh\nKxbTDwZZRq\W62IEKgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCwMlU5KM7:TT6=	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
RPMI8226	NIDDZ2tEgXSxdH;4bYNqfHliYYPzZZk>		M1rYV\|czKGi{cx?=	M37LOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJRVUl6MkK2JINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkS2PEDPxE1w	MoDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEOwO\|goRjJ4NESzNFc5RC:jPh?=
SEM	MojLR5l1d3SxeHnjbZR6KGG\|c3H5		NIL0No84OiCqcoO=	M1X6U2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNGVSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFEvPjFizszNMi=>	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
SUP-B15	MoD3R5l1d3SxeHnjbZR6KGG\|c3H5		M{K0flczKGi{cx?=	MmLRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3VRNUJzNTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW\|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDFwOUKg{txONg>?	NGn1dHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
RPMI18226	NYTNe2FuS3m2b4TvfIlkcXS7IHHzd4F6		MlTzO\|IhcHK\|	MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSVG1KOTh{Mk[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSBzLkm3JO69VS5?	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
HL60	NXj2ZoVTS3m2b4TvfIlkcXS7IHHzd4F6		NI\kZm04OiCqcoO=	NF7zdldEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOi5\|NjFOwG0v	NEjEe3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
HL60	NXu4UZFwSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MYW0PEBpenN?	MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYX\0[ZIhPDhiaILzJIlvKHC{ZYPlcoNmKG:oIFrBT\|IhcW6qaXLpeI9zKEO\VD2zPFch[nliQ1PLMVgh[XO\|YYmsJGlEPTBiPTCyMlU1KM7:TT6=	NH\SWWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
K562	Mn;aRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NXTOUGR6PDhiaILz	MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYX\0[ZIhPDhiaILzJIlvKHC{ZYPlcoNmKG:oIFrBT\|IhcW6qaXLpeI9zKEO\VD2zPFch[nliQ1PLMVgh[XO\|YYmsJGlEPTBiPTCyMlU1KM7:TT6=	NXm1e4dnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFAyOTVpPkK5PVQxOTF3PD;hQi=>
HEL	MlXKRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M3vjVFQ5KGi{cx?=	NFG3TJlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjFUEBk\WyuczDh[pRmeiB2ODDodpMhcW5icILld4Vv[2Vib3[gTmFMOiCrbnjpZol1d3JiQ2nUMVM5PyCkeTDDR2suQCCjc4PhfUwhUUN3MDC9JFIvPTRizszNMi=>	MmHjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NECxNVUoRjJ7OUSwNVE2RC:jPh?=
KCL22	NG\1bHNEgXSxdH;4bYNqfHliYYPzZZk>		Mny1O\|IhcHK\|	NFqzbINEgXSxdH;4bYNqfHliYXfhbY5{fCCrbXH0bY5q[i2{ZYPpd5RidnRiaIXtZY4hU0OOMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB\|LkO4JO69VS5?	MmjGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|NkW4PVIoRjNyM{[1PFkzRC:jPh?=
U266	M4\oRmN6fG:2b4jpZ4l1gSCjc4PhfS=>		Mo\CO\|IhcHK\|	MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVNlY3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gN{42OiEQvF2u	NI\4Vow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
SUP-B15	M17KXmN6fG:2b4jpZ4l1gSCjc4PhfS=>		NV;sTlRRPzJiaILz	MmTIR5l1d3SxeHnjbZR6KGGpYXnud5QhcW2jdHnubYIuemW\|aYP0ZY51KGi3bXHuJHNWWC2EMUWgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB\|LkW0JO69VS5?	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB\|NkW4PVI9N2F-
KCL22	M1e1RmN6fG:2b4jpZ4l1gSCjc4PhfS=>		NGDucGY4OiCqcoO=	NH36SlNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMS0x{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW\|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDNwN{Wg{txONg>?	NWmwN4pIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlU5QTJpPkOwN\|Y2QDl{PD;hQi=>
HL60	NEfxcJlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MlzQOFghcHK\|	MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFSz24JIF{e2G7LDDJR\|UxKD1iMz63OUDPxE1w	NXTaeHlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFAyOTVpPkK5PVQxOTF3PD;hQi=>
K562	M{XMb2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		MWW0PEBpenN?	NWTDOHM3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDDR2suQCCjc4PhfUwhUUN3MDC9JFMvPzVizszNMi=>	M17vbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSwNVE2Lz5{OUm0NFEyPTxxYU6=
HEL	NX3GVYRsSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MWK0PEBpenN?	NXS2[3B3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDISWwh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT{05KGG\|c3H5MEBKSzVyIE2gN{44PSEQvF2u	NH\TTlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NFEyPSd-Mkm5OFAyOTV:L3G+
BCP-ALL	NIi2b5dEgXSxdH;4bYNqfHliYYPzZZk>		MorHO\|IhcHK\|	NVi4cJdbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkOSLVHMUEBk\WyuczDk[ZJqfmWmIH\yc40heGG2aXXueEA{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPC52NTFOwG0v	NHP1XYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
MV4-11	MlTwSpVv[3Srb36gZZN{[Xl?	NF;ZRY0yODByIH7N	MXq2JIhzew>?	MkjqTY5pcWKrdHnvckBw\iCKRFHDNU8zNzNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W\|c3XkJIF{KHWycnXneYxifGmxbjDv[kBpcXO2b37lJGg{KGGlZYT5cIF1cW:wIHH0JFExODBibl2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	MmTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NEOwO\|goRjJ4NESzNFc5RC:jPh?=
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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 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

In vivo Formulation Calculator (Clear solution)

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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.
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.

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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.
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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)