Romidepsin (FK228, Depsipeptide)

Catalog No.S3020 Synonyms: FR 901228, NSC 630176

For research use only.

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.

Romidepsin (FK228, Depsipeptide) Chemical Structure

CAS No. 128517-07-7

Selleck's Romidepsin (FK228, Depsipeptide) has been cited by 178 publications

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Biological Activity

Description 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.
Targets
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
36 nM 47 nM
In vitro

Unlike TSA, the active form redFK of Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively. Romidepsin is 17-23 times weaker than redFK in inhibiting these HDACs with IC50 of 36 nM, 47 nM, 510 nM, and 14 μM, respectively. Romidepsin treatment in HeLa cells induces histone acetylation and p21 expression with EC50 of 3.0 nM, more strongly than redFK with EC50 of 11 nM due to the instability of redFK. [1] In addition to G2/M arrest, Romidepsin treatment causes cyclin D1 downregulation and a p53-independent p21 induction, leading to inhibition of CDK and dephosphorylation of Rb resulting in growth arrest in the early G1 phase. [2] Romidepsin is 100 times more potent than TSA and 1,000,000 times more potent than butyrate in inhibiting the proliferation of the A549 cells. [3] Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 of 5.92 nM, 8.36 nM, and 6.95 nM, respectively. [5] Romidepsin promotes apoptosis in chronic lymphocytic leukemia (CLL) cells at a concentration corresponding to that at which H3 and H4 acetylation and HDAC inhibition occurs, selectively involving activation of caspase 8 and effector caspase 3, as well as down-regulation of c-FLIP protein. [6] In 11 of 13 (85%) renal cell carcinoma cell lines and in 16 of 37 (43%) other cancer cell lines, Romidepsin treatment up-regulates tumor death receptors, and potentiates natural killer (NK)-mediated tumor killing. [7] Romidepsin exhibits concentration-dependent cytotoxicity against a panel of mantle cell lymphoma (MCL) cell lines. [9]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SU-DHL4 M171SmNmdGxiVnnhZoltcXS7IFHzd4F6 M3PqR|IvPS1zNTDuUS=> MYC3NkBp NHizc5ZqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi NXXEXWV4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PVA6ODdpPkK1O|kxQTB5PD;hQi=>
U2932  MmDlR4VtdCCYaXHibYxqfHliQYPzZZk> M1zsXFIvPS1zNTDuUS=> MkTaO|IhcA>? MXfpcoR2[2W|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh NVmxT3RvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PVA6ODdpPkK1O|kxQTB5PD;hQi=>
OCI-LY7 M{fSUGNmdGxiVnnhZoltcXS7IFHzd4F6 NUHkU|ZiOi53LUG1JI5O MWq3NkBp MlXvbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>? NWjkb3pbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PVA6ODdpPkK1O|kxQTB5PD;hQi=>
Farage M3rPcWNmdGxiVnnhZoltcXS7IFHzd4F6 M1\WelIvPS1zNTDuUS=> MUe3NkBp NWHtbI13cW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?= NF;3RpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe5NFkxPyd-MkW3PVA6ODd:L3G+
LY7/EBV NH;HWFJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFPJR2ozNjVvMUWgcm0> M4W3fFczKGh? MoHXbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd7MEmwO{c,OjV5OUC5NFc9N2F-
U2932/EBV MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVKyMlUuOTVibl2= NHvKeZk4OiCq NYrEU4lscW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?= Mo\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5OUC5NFcoRjJ3N{mwPVA4RC:jPh?=
HCT116 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PkNlUuPTByMDDuUS=> M4nwbVI1KGh? M37ke2ROW09? MnfqbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy NFfoU5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS5NlUyPSd-MkW0PVI2OTV:L3G+
ACH-2 MnvoSpVv[3Srb36gRZN{[Xl? MlXjNU06KG6P MoKxNlQhcA>? NIjIbpRqdmS3Y3XzJGhKXi1zIFXuekBmgHC{ZYPzbY9v NFiwOZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUG0PVQ3Pyd-MkWxOFk1Pjd:L3G+
MCF-10A Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMUhCtVAvODFibl2= NXTzVnBtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
MCF-7 NVyzRXFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFX6fZFKSzVyPUGuNVDDuTBwMkCgcm0> NEPIV2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
SK-BR-3 M1XpNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi0XWZKSzVyPUGuNFDDuTBwM{Wgcm0> NXzxelJ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
MDA-MB-231 Mnu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz1eYEzUUN3ME2wMlY5yrFyLkG0JI5O NELNSXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
PC3 MmPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHK[lFKSzVyPUGuOlXDuTBwM{Wgcm0> NUizelJCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
HCT116 Mlj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jtWGlEPTB;MT6wNOKyOC5yMDDuUS=> M{DaXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
HCT116-p21-/- MlizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTFwMkdCtVAvOzdibl2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
S1 M2q5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7IVItPUUN3ME23MlY4yrFyLkK5JI5O NVv3e3p[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
SW620 NHTwPWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXVdlZKSzVyPUCuPVPDuTBwMkmgcm0> Mn[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUS4OVYoRjJ2OUW0PFU3RC:jPh?=
LOX-IMVI NFTHUpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13hfmlEPTB;MD64O:KyOC5yMzDuUS=> MmqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUS4OVYoRjJ2OUW0PFU3RC:jPh?=
UACC-62 M3\4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXW3U4t6UUN3ME2wMlU3yrFyLkG2JI5O NUXRN5pWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
MDA-MB-435 NEfnNm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLkTWM2OD1yLkmwxtExNjB4IH7N NELhZZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
SF-295 MoizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHuTWM2OD1yLki4xtExNjF3IH7N NFHzTnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
A549 M2fhS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIj1W4hKSzVyPUGuNlbDuTBwMkSgcm0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
H460 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[5TW1nUUN3ME2yMlU5yrFyLkiwJI5O MoTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUS4OVYoRjJ2OUW0PFU3RC:jPh?=
EKVX M3PjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LGW2lEPTB;MT6zN:KyOC5|NDDuUS=> NG\XXIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
H146 M{\zdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHVfYxKSzVyPUCuNlLDuTBwMEegcm0> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
H526 NIrCTpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXGNXJIUUN3ME2wMlE2yrFyLkCzJI5O MmX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUS4OVYoRjJ2OUW0PFU3RC:jPh?=
HuT-78 NX\0[WhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fZZ2lEPTB;MT63N:KyOC52NDDuUS=> NXv4UGNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
HA NES1W5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nFe|AvPjJ3LUGwcm0> MXi0PEBp M3X5UIlv\HWlZYOgZUB{cWewaX\pZ4FvfGy7IIP0do9v\2W{IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGOxLYTy[YF1\WRid3n0bEBjd3K2ZYrvcYlj NX7J[mo{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|E2OTBpPkK0O|cyPTFyPD;hQi=>
MS-275 MmjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\aNE43OjVvMUDuUS=> M2naRVQ5KGh? NXWySXRNcW6mdXPld{BiKHOrZ37p[olk[W62bImgd5Rzd26pZYKgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iY3:teJJm[XSnZDD3bZRpKGKxcoTlfo9ucWJ? Mn:2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{G1NVAoRjJ2N{exOVExRC:jPh?=
CD4 T MmLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf0T3c1QCCq MlXWSWM2OD12LkZCtVEvOCCwTR?= M3;iNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{KyOFU1Lz5{NEeyNlQ2PDxxYU6=
CD4 T MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrUNWs1QCCq NYS2bFc1S0N3ME2xNFfDuTF{NjDuUS=> NEPPRWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEeyNlQ2PCd-MkS3NlI1PTR:L3G+
CD4+ T MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID0PYVGSzVyPUOgcm0> NV7zfpdGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVUyODVpPkK0OFk2OTB3PD;hQi=>
A549 NHXObnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rjOlEx6oDVMUCwxsBvVQ>? MWGyOE8{Pi92ODDo MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJINwdmOnboTyZZRqd25vIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? NGn5SFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES4OVc6QSd-MkS0PFU4QTl:L3G+
JJN3 NFvtTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nod|I1NzR6IHi= MYHFR|UxRDIkgJnuUVshPDkkgJno MlTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyM{CxOVAoRjJ2MEOwNVUxRC:jPh?=
OPM-2 MnrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\lOVZ3OjRxNEigbC=> M17IfWVEPTC|PUJihKlvVTtiNElihKlp Mn;FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyM{CxOVAoRjJ2MEOwNVUxRC:jPh?=
RPMI-8226 NXHMbI5VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnUWFYzPC92ODDo MlTiSWM2OHN;MT645qCKdk19IES45qCKcA>? M4LFWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEOwNVUxLz5{NECzNFE2ODxxYU6=
U266 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3p[|MzPC92ODDo NYLHZm1mTUN3MIO9NVDjiImwTUugOFjjiImq M1juO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEOwNVUxLz5{NECzNFE2ODxxYU6=
CA46 MnvvRZBweHSxc3nzJGF{e2G7 MWm2JIg> NXfISnJicW6mdXPld{BjdHWwdDDhdI9xfG:|aYO= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4NkG2OEc,OjN7Nk[xOlQ9N2F-
DG75 M2CzSGFxd3C2b4Ppd{BCe3OjeR?= NWDZSlYyPiCq MnzpbY5lfWOnczDuc{BieG:ydH;zbZM> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl4NkG2OEc,OjN7Nk[xOlQ9N2F-
Ramos NYTFfVNDSXCxcITvd4l{KEG|c3H5 M{HWWVYhcA>? NI\J[FdqdmS3Y3XzJIV5fGWwc3n2[UBieG:ydH;zbZM> MkSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[xOlQoRjJ|OU[2NVY1RC:jPh?=
ST486 NFi0b2RCeG:ydH;zbZMhSXO|YYm= MlfVOkBp Ml:xbY5lfWOnczDlfJRmdnOrdnWgZZBweHSxc3nz NW\KfIZPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OlYyPjRpPkKzPVY3OTZ2PD;hQi=>
HuT78 MXrBdI9xfG:|aYOgRZN{[Xl? NGjyZo4yNzFyL{GwNEBvVQ>? MnLHOFghcA>? NWnndYs4cW6mdXPld{BieG:ydH;zbZMh[XRiMTDuUS=> NX\lc5NmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1N|I4OzJpPkKzOVMzPzN{PD;hQi=>
DpVp35 NFK3UJRCeG:ydH;zbZMhSXO|YYm= Mnf2NU8yOC9zMECgcm0> NFmwWHA1QCCq NVvlZ3o3cW6mdXPld{BjdHWwdDDhdI9xfG:|aYO= M3XsOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUOyO|MzLz5{M{WzNlc{OjxxYU6=
DpVp50 NIHQeZpCeG:ydH;zbZMhSXO|YYm= MnqyNU8yOC9zMECgcm0> M3TCZ|Q5KGh? MWPpcoR2[2W|IHLseY51KGGyb4D0c5Nqew>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV|MkezNkc,OjN3M{K3N|I9N2F-
DpP75  NV[zT4ttSXCxcITvd4l{KEG|c3H5 MonQNU8yOC9zMECgcm0> NILMXGk1QCCq NFS5Z4hqdmS3Y3XzJIJtfW62IHHwc5B1d3Orcx?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV|MkezNkc,OjN3M{K3N|I9N2F-
SKOV-3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknrNgKBmzJybl2= Mnf0O|IhcA>? MoDxSG1UVw>? MUny[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGGub37lJIFv\CClb33ibY5m\CC5aYToJINqe3CuYYTpci=> M3nmXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEGwN|Q5Lz5{M{CxNFM1QDxxYU6=
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OVCAR-8  M2jjfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjhN5lFOeLCk{Kwcm0> M2TCcFczKGh? Mo\ySG1UVw>? NHyzd5dz\WS3Y3XzJINmdGxidnnhZoltcXS7IHHsc45mKGGwZDDjc41jcW6nZDD3bZRpKGOrc4DsZZRqdg>? MmTOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUCzOFgoRjJ|MEGwN|Q5RC:jPh?=
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697  MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfDcW9nUUN3MPMAjV3jiIl{LkZCpI5O MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV|OEKxOkc,OjF3M{iyNVY9N2F-
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THJ-16T M3izW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrQeJoyKG6P MXiyOEBp MkHKbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NF;kcWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEixNFU3QCd-MkC4NVA2Pjh:L3G+
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B104  NEHQWHBHfW6ldHnvckBCe3OjeR?= MU[yJI5O MWqyOE81QC95MjDo NET2[mxqdmO{ZXHz[ZMhfGinIIP1doZi[2ViZYjwdoV{e2mxbjDv[kBETDJywrC= Mn3GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OE[1NFUoRjJyNki2OVA2RC:jPh?=
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HCT116 NI\MSIJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MoTWOFghcHK| NE\ETHhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC0PEBpenNiaX6gdJJme2WwY3Wgc4YhTFSWIHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF2N{[xNkc,OjVzNEe2NVI9N2F-
MOLT4 NHXiXmxCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NH;kVHk4OiCqcoO= NUTxZoVTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{Bi\nSncjC3NkBpenNiYomgR2NMQCCjc4PhfUwhT0l3MDC9JFAvODB{ME[g{txONg>? NF3aSIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkOzNVM{PCd-Mk[zN|E{OzR:L3G+
DU145 NUXJW2RzSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGT0OmU4OiCqcoO= M2fZTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRGWxOFUh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT|gh[XO|YYmsJGdKPTBiPTCwMlAxOjV3IN88UU4> NYTqbFVlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zN|E{OzRpPkK2N|MyOzN2PD;hQi=>
U937 MYPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MYK3NkBpenN? NESxSoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGW5N|ch[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT|gh[XO|YYmsJGdKPTBiPTCwMlAxOzRzIN88UU4> M{i3fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{OxN|M1Lz5{NkOzNVM{PDxxYU6=
HLF MlLLRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MV[3NkBpenN? NXLhbVN1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUGYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT|gh[XO|YYmsJGdKPTBiPTCwMlAxPDh7IN88UU4> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN|MUOzOEc,OjZ|M{GzN|Q9N2F-
WI38 MVrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1zXRlczKGi{cx?= MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFeLM{igZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFfJOVAhRSByLkCwOVM6KM7:TT6= M4rG[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{OxN|M1Lz5{NkOzNVM{PDxxYU6=
U937 NETtR2dHfW6ldHnvckBie3OjeR?= NVPUUWNXOjRiaILz MUfJcohq[mm2aX;uJI9nKEiGQVO2JIlvKGi3bXHuJHU6OzdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIFteGijLYT1ZoltcW5iYXPleJlt[XSrb36gZZQhPSCwTTD0c{A2KHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NVSyRoVKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zN|E{OzRpPkK2N|MyOzN2PD;hQi=>
HCT116 MmPsRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NFXncmw4OiCqcoO= NYfHfVhySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ492dHSncjDjc5VvfGW{IH3leIhw\CxiSVO1NEA:KDBwMEK4JO69VS5? NWO5SHQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0PFE3PTlpPkK2OFgyPjV7PD;hQi=>
IGROV1/Pt1 NUfmb2VRSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGHlT5k4OiCqcoO= MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNU9RfDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ492dHSncjDjc5VvfGW{IH3leIhw\CxiSVO1NEA:KDBwMEig{txONg>? M3S1[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEixOlU6Lz5{NkS4NVY2QTxxYU6=
IGROV1 M1LCVmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MV:3NkBpenN? MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSClb4XseIVzKGOxdX70[ZIhdWW2aH;kMEBKSzVyIE2gNE4zOiEQvF2u MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR6MU[1PUc,OjZ2OEG2OVk9N2F-
Assay
Methods Test Index PMID
Western blot p21 / Cyclin D1 ; AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) ; HDAC3 / HDAC4 / HDAC6 / HDAC2 ; γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP ; Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac ; pAKT(S473) / pAKT(T308) / AKT 19682393 26473529 27444036 25492515
Growth inhibition assay Cell viability 27444036
Immunofluorescence SS18/TLE1 ; Cleaved caspase-3 27120803 22531354
In vivo Romidepsin treatment potently inhibits the neovascularization of chick embryo and that of adult mice in the Matrigel plug assay. [4]Administration of Romidepsin at 0.1-1 mg/kg twice a week significantly prolongs the survival of mice bearing U-937 lymphoma, with median survival times of 30.5 (0.56 mg/kg) and 33 days (0.32 mg/kg), respectively (vs. 20 days in control mice). [5]

Protocol (from reference)

Kinase Assay:

[1]

  • HDAC-inhibitory activity:

    For the enzyme assay, 10 μL of [3H]acetyl-labeled histones (25,000 cpm/10 μg) are added to 90 μL of the HDAC enzyme fraction extracted from 293T cells overexpressing HDAC1 or HDAC2 in the presence of increasing concentrations of Romidepsin, and the mixture is incubated at 37 °C for 15 minutes. The enzyme reaction is linear for at least 1 hour. The reaction is stopped by the addition of 10 μL of concentrated HCl. The released [3H]acetic acid is extracted with 1 mL of ethylacetate, and 0.9 mL of the solvent layer is taken into 5 mL of aqueous counting scintillant II solution for determination of radioactivity. The IC50 values are determined from at least three independent dose-response curves.

Cell Research:

[3]

  • Cell lines: HL60, Jurkat, A549, and MCF-7
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to various concentrations of Romidepsin for 72 hours in 96-well plates. 20 μL of 5 mg/mL MTT solution in PBS is added to each well for 4 hours. After removal of the medium, 170 μL of DMSO is added to each well to dissolve the formazan crystals. The absorbance at 540 nm is determined. In addition, cells are incubated with trypan blue, and the numbers of blue (dead) cells and transparent (live) cells are counted in a hemocytometer. For cell cycle analysis, cells are incubated for 30 minutes in propidium iodide staining solution containing 0.05 mg/mL propidium iodide, 1 mM EDTA, 0.1% Triton X-100, and 1 mg/mL RNase A in PBS. The suspension is then passed through a nylon mesh filter and analyzed on a Becton Dickinson FACScan.

Animal Research:

[5]

  • Animal Models: Male scid mice inoculated i.p. with U-937 cells
  • Dosages: ~1 mg/kg once or twice a week
  • Administration: Treated i.p.

Solubility (25°C)

In vitro

DMSO 10 mg/mL
(18.49 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+5%Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 540.7
Formula

C24H36N4O6S2

CAS No. 128517-07-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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
%DMSO %

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03770000 Completed Drug: Tenalisib|Drug: Romidepsin T Cell Lymphoma Rhizen Pharmaceuticals SA March 12 2019 Phase 1|Phase 2
NCT02616965 Recruiting Drug: Romidepsin|Drug: Brentuximab vedotin Cutaneous T-cell Lymphoma (CTCL) Fox Chase Cancer Center|Seagen Inc.|Celgene Corporation February 22 2017 Phase 1
NCT02616874 Completed Drug: MVA.HIVconsv vaccine|Drug: Romidepsin HIV IrsiCaixa|Germans Trias i Pujol Hospital|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint February 2016 Phase 1
NCT03141203 Active not recruiting Drug: Romidepsin|Drug: Carfilzomib Peripheral T Cell Lymphoma University of Birmingham|Bloodwise|Celgene|Amgen July 13 2015 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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