Romidepsin

Catalog No.S3020 Synonyms: FK228, Depsipeptide, 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  Chemical Structure

CAS No. 128517-07-7

Selleck's Romidepsin has been cited by 184 publications

Purity & Quality Control

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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 NVvhUFdSS2WubDDWbYFjcWyrdImgRZN{[Xl? NVPlV4R[Oi53LUG1JI5O NHLNdIw4OiCq NUXEUZlbcW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?= MoXJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5OUC5NFcoRjJ3N{mwPVA4RC:jPh?=
U2932  NU[5fJVFS2WubDDWbYFjcWyrdImgRZN{[Xl? MVSyMlUuOTVibl2= NILQe4s4OiCq NHG1[VVqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd7MEmwO{c,OjV5OUC5NFc9N2F-
OCI-LY7 NGfsZYdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYXqVlU6Oi53LUG1JI5O M1vMd|czKGh? NUjETJVYcW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?= M{PXXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{mwPVA4Lz5{NUe5NFkxPzxxYU6=
Farage Ml\yR4VtdCCYaXHibYxqfHliQYPzZZk> NUPabGF3Oi53LUG1JI5O NX35SoVWPzJiaB?= MnjSbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>? NVjycnZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PVA6ODdpPkK1O|kxQTB5PD;hQi=>
LY7/EBV M2T3dGNmdGxiVnnhZoltcXS7IFHzd4F6 M4\aTFIvPS1zNTDuUS=> MoDFO|IhcA>? MUjpcoR2[2W|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh NYn6eWxzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3PVA6ODdpPkK1O|kxQTB5PD;hQi=>
U2932/EBV NUG3UYV2S2WubDDWbYFjcWyrdImgRZN{[Xl? NXr4WXZPOi53LUG1JI5O NYe3W49EPzJiaB?= NGHSN2VqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd7MEmwO{c,OjV5OUC5NFc9N2F-
HCT116 M1;rbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjCOU02ODByIH7N M4Tv[VI1KGh? MlrVSG1UVw>? M1juXIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR7MkWxOUc,OjV2OUK1NVU9N2F-
ACH-2 MlG4SpVv[3Srb36gRZN{[Xl? NGDP[2UyNTlibl2= M{HnUVI1KGh? M2jze4lv\HWlZYOgTGlXNTFiRX72JIV5eHKnc4Ppc44> NH\uPWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUG0PVQ3Pyd-MkWxOFk1Pjd:L3G+
MCF-10A NHW5T3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7qdllEUUN3ME2wMlE4yrFyLkCxJI5O M4S0b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
MCF-7 NISzeZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16wS2lEPTB;MT6xNOKyOC5{MDDuUS=> NHL3doU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
SK-BR-3 NYHXUGxET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnTU5dYUUN3ME2xMlAxyrFyLkO1JI5O M4PpflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
MDA-MB-231 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\5TWM2OD1yLk[4xtExNjF2IH7N MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
PC3 NHXNPWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\VNHR{UUN3ME2xMlY2yrFyLkO1JI5O NHHJN|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
HCT116 NFfNOHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jaZ2lEPTB;MT6wNOKyOC5yMDDuUS=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
HCT116-p21-/- NVf1WlQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M125RWlEPTB;MT6yOuKyOC5|NzDuUS=> M1fZ[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
S1 M4PSRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPXTWM2OD15Lk[3xtExNjJ7IH7N M2fZWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
SW620 NFnVW5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jXTWlEPTB;MD65N:KyOC5{OTDuUS=> NX2wTYxURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
LOX-IMVI M4DnOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTFTWM2OD1yLki3xtExNjB|IH7N M3TlclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
UACC-62 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;vTWM2OD1yLkW2xtExNjF4IH7N NYq0c2xNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
MDA-MB-435 MnjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYX4XmtyUUN3ME2wMlkxyrFyLkC2JI5O NHHSeGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
SF-295 NHvKU3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonDTWM2OD1yLki4xtExNjF3IH7N NF3kV|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
A549 Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLwTWM2OD1zLkK2xtExNjJ2IH7N M4S3ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
H460 NYPQeGpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfNSJJKSzVyPUKuOVjDuTBwOECgcm0> NIHJR3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
EKVX MnzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTFwM{RCtVAvOzRibl2= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
H146 MkTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXGZpVKSzVyPUCuNlLDuTBwMEegcm0> NFTkWZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
H526 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33jPWlEPTB;MD6xOeKyOC5yMzDuUS=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
HuT-78 MkjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfaT2twUUN3ME2xMlc{yrFyLkS0JI5O MnLUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NUS4OVYoRjJ2OUW0PFU3RC:jPh?=
HA MnXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;S[FAvPjJ3LUGwcm0> M3vmOVQ5KGh? MnHHbY5lfWOnczDhJJNq\26rZnnjZY51dHlic4Tyc45o\XJiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[29vdILlZZRm\CC5aYToJIJwenSnen;tbYI> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5MUWxNEc,OjR5N{G1NVA9N2F-
MS-275 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrBWGYxNjZ{NT2xNI5O MoDCOFghcA>? MYPpcoR2[2W|IHGgd4lodmmoaXPhcpRtgSC|dILvcodmeiCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBkdy22cnXheIVlKHerdHigZo9zfGW8b33pZi=> NHvlSoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3NVUyOCd-MkS3O|E2OTB:L3G+
CD4 T MnjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjpOFghcA>? NFi0WlZGSzVyPUSuOeKyOS5yIH7N NXz4O5ExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3NlI1PTRpPkK0O|IzPDV2PD;hQi=>
CD4 T NXH4NmxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fVdlQ5KGh? MUfDR|UxRTFyN9MxNVI3KG6P M{K2fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{KyOFU1Lz5{NEeyNlQ2PDxxYU6=
CD4+ T NUf4U5FCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfkNWNOTUN3ME2zJI5O NVWxWZBlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVUyODVpPkK0OFk2OTB3PD;hQi=>
A549 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEju[I4yOOLCk{GwNOKhdk1? MoTENlQwOzZxNEigbC=> NFvINo1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGOxbnPlcpRz[XSrb36tJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NIrEVpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES4OVc6QSd-MkS0PFU4QTl:L3G+
JJN3 M1XCVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TDSFI1NzR6IHi= NUm5PYYyTUN3MEyx5qCKdk19IES45qCKcA>? NXLuUJIyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwN|AyPTBpPkK0NFMxOTVyPD;hQi=>
OPM-2 NYi4WZBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTmb5IzPC92ODDo NXPGfJpCTUN3MIO9NgKBkW6POzC0PQKBkWh? MnTLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyM{CxOVAoRjJ2MEOwNVUxRC:jPh?=
RPMI-8226 NVrqO5Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOyOE81QCCq M3LoTmVEPTC|PUGuPQKBkW6POzC0PQKBkWh? M2jCPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEOwNVUxLz5{NECzNFE2ODxxYU6=
U266 NEK1SoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnn4NlQwPDhiaB?= M4XBNWVEPTC|PUGw5qCKdk19IES45qCKcA>? MkLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyM{CxOVAoRjJ2MEOwNVUxRC:jPh?=
CA46 MX3BdI9xfG:|aYOgRZN{[Xl? NFGwZ3U3KGh? MWrpcoR2[2W|IHLseY51KGGyb4D0c5Nqew>? MlXKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7Nk[xOlQoRjJ|OU[2NVY1RC:jPh?=
DG75 Mn24RZBweHSxc3nzJGF{e2G7 M{frZlYhcA>? MknNbY5lfWOnczDuc{BieG:ydH;zbZM> NFfHbmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlE3PCd-MkO5OlYyPjR:L3G+
Ramos NXPsVXhtSXCxcITvd4l{KEG|c3H5 NYnRWGV1PiCq MUjpcoR2[2W|IHX4eIVve2m4ZTDhdI9xfG:|aYO= NFfWcYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlE3PCd-MkO5OlYyPjR:L3G+
ST486 MWjBdI9xfG:|aYOgRZN{[Xl? NIDBWY43KGh? NYHhWnNLcW6mdXPld{BmgHSnboPpeoUh[XCxcITvd4l{ NGfkUlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m2OlE3PCd-MkO5OlYyPjR:L3G+
HuT78 NIf2XFZCeG:ydH;zbZMhSXO|YYm= NIq1UpkyNzFyL{GwNEBvVQ>? NILSTFE1QCCq MWjpcoR2[2W|IHHwc5B1d3OrczDheEAyKG6P M3TGflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUOyO|MzLz5{M{WzNlc{OjxxYU6=
DpVp35 MnzYRZBweHSxc3nzJGF{e2G7 Mny0NU8yOC9zMECgcm0> M1Hae|Q5KGh? NYntZ|B1cW6mdXPld{BjdHWwdDDhdI9xfG:|aYO= NYHTPWpzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1N|I4OzJpPkKzOVMzPzN{PD;hQi=>
DpVp50 MnzwRZBweHSxc3nzJGF{e2G7 NFXMV|YyNzFyL{GwNEBvVQ>? M1j1b|Q5KGh? NEHNO3VqdmS3Y3XzJIJtfW62IHHwc5B1d3Orcx?= NGCxcm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WzNlc{Oid-MkO1N|I4OzJ:L3G+
DpP75  NYLXfXdrSXCxcITvd4l{KEG|c3H5 NH;yco0yNzFyL{GwNEBvVQ>? NGfhPZk1QCCq NXrlc41jcW6mdXPld{BjdHWwdDDhdI9xfG:|aYO= MnPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3M{K3N|IoRjJ|NUOyO|MzRC:jPh?=
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HCT15 NE\YVIxEgXSxdH;4bYNqfHliYYPzZZk> NHrQRnFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzNTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTBiPTCwMlQ2KM7:TT6= M1PkeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUi5OFg3Lz5{NEW4PVQ5PjxxYU6=
mink Mv1Lu M1HUVWZ2dmO2aX;uJIF{e2G7 NFjpUI8zPCCqcoO= NGm1PVZKdmO{ZXHz[UBqdiCqdX3hckB4cWymIIT5dIUheDJzIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBucW6tIF32NWx2KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDwNlEheHKxbX;0[ZIh[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiMD6xJI1OKGSrdHjpc5RpemWrdH;sMEBGSzFyMECgQUAxNjBzNUeg{txONg>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl7N{W3PEc,OjR7OUe1O|g9N2F-
HCT116 NW\YdI17SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MojVOFghcHK| NHrGRVdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC0PEBpenNiaX6gdJJme2WwY3Wgc4YhTFSWIHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> M4HVNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUS3OlEzLz5{NUG0O|YyOjxxYU6=
MOLT4 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MV23NkBpenN? NXjMdnVXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{Bi\nSncjC3NkBpenNiYomgR2NMQCCjc4PhfUwhT0l3MDC9JFAvODB{ME[g{txONg>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN|MUOzOEc,OjZ|M{GzN|Q9N2F-
DU145 NEfKe3hCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Ml75O|IhcHK| MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESXMUS1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDHTVUxKD1iMD6wNFI2PSEQvF2u MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN|MUOzOEc,OjZ|M{GzN|Q9N2F-
U937 M2LBU2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NWe0WYdHPzJiaILz MnzsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOUO3JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDHTVUxKD1iMD6wNFM1OSEQvF2u Mn[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|M{GzN|QoRjJ4M{OxN|M1RC:jPh?=
HLF M{\DNGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXi3NkBpenN? NEXNV5NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMSkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygS2k2OCB;IECuNFA1QDlizszNMi=> MlexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|M{GzN|QoRjJ4M{OxN|M1RC:jPh?=
WI38 M{fSc2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVW2cGhHPzJiaILz M2q0SGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iV1mzPEBk\WyuczDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygS2k2OCB;IECuNFA2OzlizszNMi=> NH3tTpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkOzNVM{PCd-Mk[zN|E{OzR:L3G+
U937 NFzNRVlHfW6ldHnvckBie3OjeR?= NGTJbZgzPCCqcoO= MYjJcohq[mm2aX;uJI9nKEiGQVO2JIlvKGi3bXHuJHU6OzdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIFteGijLYT1ZoltcW5iYXPleJlt[XSrb36gZZQhPSCwTTD0c{A2KHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NXLpbW5WRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zN|E{OzRpPkK2N|MyOzN2PD;hQi=>
HCT116 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MUi3NkBpenN? NVHu[ldFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ492dHSncjDjc5VvfGW{IH3leIhw\CxiSVO1NEA:KDBwMEK4JO69VS5? NVX6XYhyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0PFE3PTlpPkK2OFgyPjV7PD;hQi=>
IGROV1/Pt1 NV3R[3ZDSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MkLDO|IhcHK| MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNU9RfDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ492dHSncjDjc5VvfGW{IH3leIhw\CxiSVO1NEA:KDBwMEig{txONg>? M4jzclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEixOlU6Lz5{NkS4NVY2QTxxYU6=
IGROV1 MnznRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3H6eFczKGi{cx?= MmTMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCLR2LPWlEh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3;1cJRmeiClb4XueIVzKG2ndHjv[EwhUUN3MDC9JFAvOjJizszNMi=> MUG8ZUB1[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

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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