Romidepsin (FK228, Depsipeptide)

Catalog No.S3020 Synonyms: FR 901228, NSC 630176

Romidepsin (FK228, Depsipeptide) Chemical Structure

Molecular Weight(MW): 540.7

Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively.

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Cited by 73 Publications

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively.
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 Mmj4R4VtdCCYaXHibYxqfHliQYPzZZk> NHPudI4zNjVvMUWgcm0> NEP5elU4OiCq MmTwbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>? MXmyOVc6ODlyNx?=
U2932  NGGzV2hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3PQRVIvPS1zNTDuUS=> MonTO|IhcA>? M1j4Nolv\HWlZYOgZ5l1d3SxeHnjbZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzyqB? M37lSVI2PzlyOUC3
OCI-LY7 Mo\5R4VtdCCYaXHibYxqfHliQYPzZZk> NVn2dndlOi53LUG1JI5O M3e3TlczKGh? NYXreWM4cW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?= MljXNlU4QTB7MEe=
Farage M1rWV2NmdGxiVnnhZoltcXS7IFHzd4F6 NEjUOoUzNjVvMUWgcm0> Mn\zO|IhcA>? NH\PbFhqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi MXiyOVc6ODlyNx?=
LY7/EBV MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFfHOXgzNjVvMUWgcm0> MnHLO|IhcA>? MVfpcoR2[2W|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh MU[yOVc6ODlyNx?=
U2932/EBV M1X1NGNmdGxiVnnhZoltcXS7IFHzd4F6 NHfoNW8zNjVvMUWgcm0> NVT3U4plPzJiaB?= MYLpcoR2[2W|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh NWrDNnR6OjV5OUC5NFc>
HCT116 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPhOU02ODByIH7N MWSyOEBp M{n6TmROW09? MkTYbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy M2jhOlI2PDl{NUG1
ACH-2 NGniTnBHfW6ldHnvckBCe3OjeR?= MmPmNU06KG6P NV;0TGlyOjRiaB?= MlzubY5lfWOnczDITXYuOSCHbo[g[ZhxemW|c3nvci=> NILQd|AzPTF2OUS2Oy=>
MCF-10A NXfyeZlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwMUhCtVAvODFibl2= NUTtNYUxOjR7NUS4OVY>
MCF-7 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDWTWM2OD1zLkGwxtExNjJyIH7N MV:yOFk2PDh3Nh?=
SK-BR-3 NFz4WIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLEUY5KSzVyPUGuNFDDuTBwM{Wgcm0> MYSyOFk2PDh3Nh?=
MDA-MB-231 NVrEXFlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrxcFZKSzVyPUCuOljDuTBwMUSgcm0> MofKNlQ6PTR6NU[=
PC3 NHHLTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULRZmJWUUN3ME2xMlY2yrFyLkO1JI5O MXmyOFk2PDh3Nh?=
HCT116 M1G3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\hXWlEPTB;MT6wNOKyOC5yMDDuUS=> NHPJPIkzPDl3NEi1Oi=>
HCT116-p21-/- MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7hZVVKSzVyPUGuNlbDuTBwM{egcm0> NG\1SpQzPDl3NEi1Oi=>
S1 NVXFSGp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq3VWdYUUN3ME23MlY4yrFyLkK5JI5O NYTkUohkOjR7NUS4OVY>
SW620 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFK5O4xKSzVyPUCuPVPDuTBwMkmgcm0> Ml6wNlQ6PTR6NU[=
LOX-IMVI NF\FbolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\sTWM2OD1yLki3xtExNjB|IH7N M4G0SVI1QTV2OEW2
UACC-62 MmDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnkTWM2OD1yLkW2xtExNjF4IH7N M{O3O|I1QTV2OEW2
MDA-MB-435 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwOUFCtVAvODZibl2= M1fyZlI1QTV2OEW2
SF-295 NWC5OXlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml2zTWM2OD1yLki4xtExNjF3IH7N NGfaW3QzPDl3NEi1Oi=>
A549 M3zmXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj0TWM2OD1zLkK2xtExNjJ2IH7N NH\6WXMzPDl3NEi1Oi=>
H460 NYT4cWFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYH0O5ZsUUN3ME2yMlU5yrFyLkiwJI5O M4nRc|I1QTV2OEW2
EKVX M{DrZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M12xe2lEPTB;MT6zN:KyOC5|NDDuUS=> NYnad3pkOjR7NUS4OVY>
H146 NF3yW3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjrPHozUUN3ME2wMlIzyrFyLkC3JI5O NVO4ZmJiOjR7NUS4OVY>
H526 M{nrbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGW0[4VKSzVyPUCuNVXDuTBwMEOgcm0> NXvsZ2s{OjR7NUS4OVY>
HuT-78 NFPkTmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFwN{RCtVAvPDRibl2= M{n6PFI1QTV2OEW2
HA MoXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorQNE43OjVvMUDuUS=> NUfROIRnPDhiaB?= NGC4eIJqdmS3Y3XzJIEhe2mpbnnmbYNidnSueTDzeJJwdmencjDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiClbz30doVifGWmIIfpeIgh[m:{dHX6c41q[g>? NHrUVJYzPDd5MUWxNC=>
MS-275 NFPRSm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSwMlYzPS1zMH7N M3XZelQ5KGh? NIfmN5BqdmS3Y3XzJIEhe2mpbnnmbYNidnSueTDzeJJwdmencjDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiClbz30doVifGWmIIfpeIgh[m:{dHX6c41q[g>? NGLnPZIzPDd5MUWxNC=>
CD4 T MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV60PEBp NIqyW|dGSzVyPUSuOeKyOS5yIH7N MoHuNlQ4OjJ2NUS=
CD4 T MoLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHv[XVlPDhiaB?= MX\DR|UxRTFyN9MxNVI3KG6P MX[yOFczOjR3NB?=
CD4+ T MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\USWM2OD1|IH7N NELNVXYzPDR7NUGwOS=>
A549 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXu4UYNqOTEkgKOxNFDDqG6P NHXPVYQzPC9|Nj:0PEBp M1G0eYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh[2:wY3XueJJifGmxbj2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= Ml36NlQ1QDV5OUm=
JJN3 NIjtZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITR[GczPC92ODDo M{TaWWVEPTB:MfMAjY5OQyB2OPMAjYg> MmHZNlQxOzBzNUC=
OPM-2 NWP4bmhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PmWlI1NzR6IHi= MlL5SWM2OHN;MfMAjY5OQyB2OPMAjYg> NUTVTFZQOjRyM{CxOVA>
RPMI-8226 M4jvRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLXTmgzPC92ODDo MVfFR|Uxez1zLklihKlvVTtiNElihKlp MYeyOFA{ODF3MB?=
U266 M2HGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnpS3MzPC92ODDo Mnj4SWM2OHN;MUFihKlvVTtiNElihKlp MoHTNlQxOzBzNUC=
CA46 MlfJRZBweHSxc3nzJGF{e2G7 NWnMdYJUPiCq MVrpcoR2[2W|IHLseY51KGGyb4D0c5Nqew>? M3nXZlI{QTZ4MU[0
DG75 NW[2NZZkSXCxcITvd4l{KEG|c3H5 NE\uVHM3KGh? NXz2UVNzcW6mdXPld{BvdyCjcH;weI9{cXN? Mo\CNlM6PjZzNkS=
Ramos M{PCN2Fxd3C2b4Ppd{BCe3OjeR?= NHXYO2U3KGh? MlnwbY5lfWOnczDlfJRmdnOrdnWgZZBweHSxc3nz MYWyN|k3PjF4NB?=
ST486 NGX0bY1CeG:ydH;zbZMhSXO|YYm= MoDrOkBp MWnpcoR2[2W|IHX4eIVve2m4ZTDhdI9xfG:|aYO= M4HjVlI{QTZ4MU[0
HuT78 MUXBdI9xfG:|aYOgRZN{[Xl? MVOxM|ExNzFyMDDuUS=> MlzOOFghcA>? NV\IZm01cW6mdXPld{BieG:ydH;zbZMh[XRiMTDuUS=> NEW3OoszOzV|MkezNi=>
DpVp35 MW\BdI9xfG:|aYOgRZN{[Xl? M{TIdlEwOTBxMUCwJI5O NHTkSo81QCCq MmXYbY5lfWOnczDicJVvfCCjcH;weI9{cXN? MXuyN|U{Ojd|Mh?=
DpVp50 MlHLRZBweHSxc3nzJGF{e2G7 NUnkUHRJOS9zMD:xNFAhdk1? NGfweWg1QCCq Mmq4bY5lfWOnczDicJVvfCCjcH;weI9{cXN? M{ezT|I{PTN{N{Oy
DpP75  NEm5SnlCeG:ydH;zbZMhSXO|YYm= NX7xfYJLOS9zMD:xNFAhdk1? M{e3XlQ5KGh? MUDpcoR2[2W|IHLseY51KGGyb4D0c5Nqew>? MUWyN|U{Ojd|Mh?=
SKOV-3 NWq1TpN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3RSZAy6oDVMkDuUS=> M3X6W|czKGh? M1\FemROW09? NUi5dFR3emWmdXPld{Bk\WyuII\pZYJqdGm2eTDhcI9v\SCjbnSgZ49u[mmwZXSge4l1cCClaYPwcIF1cW5? M4fENFI{ODFyM{S4
Brca1 WT MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPCNgKBmzJybl2= MlHnO|IhcA>? NE[wUJlFVVOR NXWzUm5RemWmdXPld{Bk\WyuII\pZYJqdGm2eTDhcI9v\SCjbnSgZ49u[mmwZXSge4l1cCClaYPwcIF1cW5? M2m3PVI{ODFyM{S4
Brca1 Null NF\SbpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2x5qCUOjCwTR?= Mm[zO|IhcA>? MUXEUXNQ MlHhdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjbH;u[UBidmRiY3;tZolv\WRid3n0bEBkcXOybHH0bY4> NYW0PYNDOjNyMUCzOFg>
OVCAR-8  M{\1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TlTFHjiJN{MH7N MoC0O|IhcA>? MnS1SG1UVw>? MVjy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGGub37lJIFv\CClb33ibY5m\CC5aYToJINqe3CuYYTpci=> NHTWXpAzOzBzMEO0PC=>
NCI/ADR-RES NUm2eY06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj4NgKBmzJybl2= M4DpdlczKGh? MV\EUXNQ MmPGdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjbH;u[UBidmRiY3;tZolv\WRid3n0bEBkcXOybHH0bY4> MVqyN|AyODN2OB?=
HCT116 MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C3TFUhdk1vNUCg{txO NXr6fVJ7OjRiaB?= M1PSbGROW09? NIXtSmtqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? M3;tV|IzQTJ2OUW4
RKO NXvSNItkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWS1JI5ONTVyIN88US=> MUeyOEBp NUP3Z5BqTE2VTx?= MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NHLldY8zOjl{NEm1PC=>
CO115 NUHRbYxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LlcFUhdk1vNUCg{txO NGrSd5IzPCCq M1TtR2ROW09? NXnXeIFHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MoHWNlI6OjR7NUi=
HFS MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[1JI5O M{HjXFI1NzR6L{eyJIg> NH\BcYVqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lMYRmeGWwZHXueIx6 M3fyflIzOTB4Mkiy
LNCaP MlXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ztZVUhdk1? MXKyOE81QC95MjDo MmiwbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZT3k[ZBmdmSnboTsfS=> NVzCWJJYOjJzME[yPFI>
A549 MnjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrIVog2KG6P M2jDTVI1NzR6L{eyJIg> M4WxdIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWt[IVx\W6mZX70cJk> NVqwSmZWOjJzME[yPFI>
697  Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ToOmlEPTEkgJm95qCKOi53wrDuUS=> MYiyNVU{QDJzNh?=
697-R NWXUNW9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzrNHNKSzVy4pEJQgKBkThwNtMgcm3DqA>? M{nBU|IyPTN6MkG2
HUT78 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3joT2lEPTB;MTDuUS=> MXuyNVE6QDV2NR?=
THJ-16T NXK4T4R2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3MNUBvVQ>? NITNNFEzPCCq NGnEeXlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NYLOV|U6OjB6MUC1Olg>
HCT116 MXfGeY5kfGmxbjDBd5NigQ>? NYH4OJI2OjBibl2= NGmwRVM5KGh? M{fqUY1w\HWuYYTld{B1emGwc3PybZB1KGyndnXsd{Bnd3JiaIXu[JJm\HNib3[g[4Vv\XNiaX6g[Yl1cGW{IHTpdoVkfGmxbh?= MWqyNFc{QTR3NB?=
B104  M2rMeWZ2dmO2aX;uJGF{e2G7 NFG4XmIzKG6P NFHUTWozPC92OD:3NkBp NWHXd|JkcW6lcnXhd4V{KHSqZTDzeZJn[WOnIHX4dJJme3Orb36gc4YhS0R{MNMg NXHaOoV6OjB4OE[1NFU>
HL-60  NIr2emxEgXSxdH;4bYNqfHliQYPzZZk> MYixMVUxOCCwTR?= M{PaT|I1KGh? M1q4b4lv\HWlZYOgZ5l1d3SxeHnjbZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzyqB? NILmZowzODZ{NEG2Ny=>
HP100 MWjDfZRwfG:6aXPpeJkhSXO|YYm= M{XhblEuPTByIH7N MlLFNlQhcA>? M1TKdYlv\HWlZYOgZ5l1d3SxeHnjbZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzyqB? NFXZeZczODZ{NEG2Ny=>
HL-60  NILw[oxHfW6ldHnvckBCe3OjeR?= NVqyeIxIOTBibl2= MY[0M|YwOTZiaB?= NXrpOVFKcW6mdXPld{B1cGViZ3Xu[ZJifGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[UBnem:vIETo M4jRflIxPjJ2MU[z
HP100 M1TufGZ2dmO2aX;uJGF{e2G7 M4LMO|ExKG6P M1Wy[VQwPi9zNjDo MlzHbY5lfWOnczD0bIUh\2WwZYLheIlwdiCxZjDofYRzd2enbjDw[ZJwgGmmZTDmdo9uKDSq Mn[3NlA3OjRzNkO=
HL-60  MoLRSpVv[3Srb36gRZN{[Xl? NVfvN3V7OTBvNUCwJI5O M13Sc|QhcA>? NUOz[FM6\GWlcnXhd4V{KHSqZTDobZN1d26nIHTlZYNmfHmuYYPlJEhJTEGFKTDhZ5Rqfmm2edMg NFnTdnkzODZ{NEG2Ny=>
HP100 MXTGeY5kfGmxbjDBd5NigQ>? MmnMNVAuPTByIH7N NVnkTpk4PCCq M1jITYRm[3KnYYPld{B1cGViaHnzeI9v\SCmZXHj[ZR6dGG|ZTCoTGRCSyliYXP0bZZqfHoEoB?= NFzudHkzODZ{NEG2Ny=>
11z NHz3VVZMcW6jc3WgRZN{[Xl? M2DhNFMuOTByIH7N NWS5bYF6emWmdXPld{BJTEGFIHXufplu[XSrYzDhZ5Rqfmm2eTCoTWM2OMLiPTC2MlUhyrFiMD62JI5ud2xxTDm= M4\yd|IxPjB3MUS0
SKOV-3 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF35dZA1NzhxMU[gcm0> NUf4OZE1PDhiaB?= NGHlOWxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NWTzfYpVOjB2MES1OlQ>
OVCAR-3 NYnvSop7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXDR41FPC96L{G2JI5O Mnv6OFghcA>? MX7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NIPF[3gzODRyNEW2OC=>
HBL-2 NWO0c3JVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULqdlhHOi1zMDDuUS=> MnjCNlQhcA>? MnHUTWM2OD12LkOgcm0> MWKyNFA3QDB6MB?=
Jeko-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PtSVIuPTBibl2= MVSyOEBp MXnJR|UxRTFzIH7N NULtWXY1OjByNkiwPFA>
Granta-519 NFTiWoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mom2OU01OCCwTR?= NGLkSW8zPCCq NEfwdXRKSzVyPUW4MlUhdk1? MnHDNlAxPjhyOEC=
L1236 NGTMUJdEgXSxdH;4bYNqfHliQYPzZZk> MnjVNUBvVS1zMECg{txO MXu0PEBp NVryTII1TUN3ME2wMlA4KM7:TR?= NIXL[nIyQTJ|M{S3NC=>
L428 NH7zWZNEgXSxdH;4bYNqfHliQYPzZZk> Mn;WNUBvVS1zMECg{txO MojJOFghcA>? MkP2SWM2OD1yLkSzJO69VQ>? NEL0R2cyQTJ|M{S3NC=>
KM-H2 NWnuT21oS3m2b4TvfIlkcXS7IFHzd4F6 NXrwS5E{OSCwTT2xNFAh|ryP NFLYb3E1QCCq M3LsS2VEPTB;MD61PEDPxE1? NWDMRXNmOTl{M{O0O|A>
L540Cy NF34O4FEgXSxdH;4bYNqfHliQYPzZZk> NFz1PY0yKG6PLUGwNEDPxE1? MoTaOFghcA>? MVnFR|UxRTBwMU[g{txO MoOyNVkzOzN2N{C=
G401 MVPGeY5kfGmxbjDBd5NigQ>? MonjNVAhdk1? MWCyOE81QC95MjDo NIjaTnpFVVOR M1Lreolv[3KnYYPld{BETEuQMVOg[ZhxemW|c3nvci=> MmnVNVkzOjF3OE[=
STM91-01 NIDre4lHfW6ldHnvckBCe3OjeR?= NYPV[41OOTBibl2= M37aW|I1NzR6L{eyJIg> NHy0Z3pFVVOR M4HRcYlv[3KnYYPld{BETEuQMVOg[ZhxemW|c3nvci=> M1:5UFE6OjJzNUi2
SJSC  M1TqUGZ2dmO2aX;uJGF{e2G7 M4nIfVExKG6P NXvOXZFnOjRxNEivO|IhcA>? M3vQ[mROW09? MUDpcoNz\WG|ZYOgR2RMVjGFIHX4dJJme3Orb36= MYKxPVIzOTV6Nh?=
BT16  M2rtdmZ2dmO2aX;uJGF{e2G7 NF34fpUyOCCwTR?= M1W2ZVI1NzR6L{eyJIg> NWrP[opUTE2VTx?= M4rWS4lv[3KnYYPld{BETEuQMVOg[ZhxemW|c3nvci=> M2exfVE6OjJzNUi2
NCI-H1299 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTRwNtMxNE4zKG6pL33s MlfwNVkyPzl6OUC=
NCI-2882 M4nrUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHUTWM2OD1zLkdCtVAvODRibnevcYw> M1\kd|E6OTd7OEmw
HCC95 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PVUGlEPTB;Mj61xtExNjB3IH7nM41t MkT6NVkyPzl6OUC=
NCI-H23 M{nP[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml64TWM2OD1{LkpCtVAvOiCwZz;tcC=> M{fOdlE6OTd7OEmw
NCI-H157 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37nXGlEPTB;MT62xtExNjB{IH7nM41t NIL6XlAyQTF5OUi5NC=>
NCI-H460 NUG1OWp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJwMdMxNE4xPyCwZz;tcC=> MmL0NVkyPzl6OUC=
NCI-H1975 M{j6fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XWUmlEPTB;MT6zxtExNjB2IH7nM41t NFTHfGIyQTF5OUi5NC=>
NCI-H820 NYO1ZlRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJwNNMxNE4yKG6pL33s NFLtTIcyQTF5OUi5NC=>
NCI-H1650 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTRwOdMxNE4{KG6pL33s NXK4WIxbOTlzN{m4PVA>
DTC1 NELZT2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHoWIRKSzVyPUCuOVEhdk1? NYrnTWdsOTh3Nk[yOFY>
KAO MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwOUGgcm0> MoK5NVg2PjZ{NE[=
SU-CCS-1 NIe2[JhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;WNJlqUUN3ME2wMlg6KG6P MoG0NVg2PjZ{NE[=
SYO-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17E[mlEPTB;MD62O{BvVQ>? NIq2ZYgyQDV4NkK0Oi=>
FUJI MmT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnDXnQ5UUN3ME2xMlMyKG6P NY\SZlhVOTh3Nk[yOFY>
SKNMC M3zsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFwMUegcm0> M1LpXFE5PTZ4MkS2
402-91 NFH0dY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7JdI93UUN3ME2xMlI3KG6P NVnaRmZpOTh3Nk[yOFY>
1765-92 M4\udGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PWcmlEPTB;MT63O{BvVQ>? Mn[5NVg2PjZ{NE[=
JN-DSRCT-1 MljaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFwMkWgcm0> Ml7yNVg2PjZ{NE[=
NMS-2PC M{GyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXMTWM2OD1yLkixJI5O MX[xPFU3PjJ2Nh?=
HL60 M4fJXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFwOE[gcm0> NIHURogyQDV4NkK0Oi=>
A549 M2PIe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TJT2lEPTB;Mz6yOEBvVQ>? NHm2c2oyQDV4NkK0Oi=>
SW480 M4LVbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{ftXWlEPTB;Mj62PUBvVQ>? NWrG[|RNOTh3Nk[yOFY>
MCF7 MorJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDIToRQUUN3ME2zMlU2KG6P MUOxPFU3PjJ2Nh?=
PC-3 NX7x[lVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\lRplKSzVyPUKuOVEhdk1? NIG1XFYyQDV4NkK0Oi=>
MMRU NEHTVHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfOTWM2OD1{LkW3JI5O NFW3eHEyQDV4NkK0Oi=>
Hs68 NGjiXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL3WZpKSzVyPU6xNEBvVQ>? NX;Pb|VlOTh3Nk[yOFY>
hMSC-001F Mm\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;DTWM2OD1-MUCgcm0> M3;l[FE5PTZ4MkS2

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p21 / Cyclin D1; 

PubMed: 19682393     


NIH 3T3 cells stably expressing the indicated proteins were treated with DMSO (Vehicle) or the indicated concentration of romidepsin for 24 h. Cell lysates were analyzed by western blotting with antibodies to cyclin D1, p21 and β-actin (loading control). Data shown are representative of at least two independent experiments.

AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27); 

PubMed: 26473529     


Effects of romidepsin (Rom) on the levels of acetylated proteins and related enzymes. Cells were exposed to romidepsin for 48 h and total cell extracts were analyzed by western blot.

HDAC3 / HDAC4 / HDAC6 / HDAC2; 

PubMed: 26473529     


Effects of romidepsin (Rom) on the levels of acetylated proteins and related enzymes. Cells were exposed to romidepsin for 48 h and total cell extracts were analyzed by western blot.

γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP; 

PubMed: 26473529     


Western blot analysis of proteins involved in DNA-damage response and apoptosis. Established cell lines were exposed to different concentrations of romidepsin (Rom) for 48 h and total cell extracts were analyzed.

Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac; 

PubMed: 27444036     


Western blot analysis of the effects of panobinostat (25 nM), vorinostat (5 µM) and romidepsin (10 nM) on expression of cyclin E1, E2F1, BRCA1, cleaved PARP and acetylated histone H3 in OVCAR-3 cells. Actin and histone H3 were loading controls. 

pAKT(S473) / pAKT(T308) / AKT; 

PubMed: 25492515     


Western blot analysis of phosphorylated AKT in PC3 cells. Cells were treated for 3 h with various concentrations of FK228. 

19682393 26473529 27444036 25492515
Growth inhibition assay
Cell viability; 

PubMed: 27444036     


Concentration-dependent effects of panobinostat and vorinostat in SRB viability assays in OVCAR-3 cells (72 h). Values are mean+SE of 3 independent experiments. 

27444036
Immunofluorescence
SS18/TLE1; 

PubMed: 27120803     


A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells.

Cleaved caspase-3; 

PubMed: 22531354     


TDP-B activates cleaved caspase-3 by immunofluorescence. Representative immunofluorescence staining for cleaved caspase 3 (green) in SKOV-3 ovarian cancer cells treated with 10 nM FK228, TDP-A or TDP-B after 24 h of exposure. The nuclei are stained with DAPI (blue).

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

Kinase Assay:

[1]

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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]

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  • 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.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: Male scid mice inoculated i.p. with U-937 cells
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: ~1 mg/kg once or twice a week
  • Administration: Treated i.p.
    (Only for Reference)

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

* 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 540.7
Formula

C24H36N4O6S2

CAS No. 128517-07-7
Storage powder
in solvent
Synonyms FR 901228, NSC 630176

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
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    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

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03770000 Recruiting 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|Seattle Genetics Inc.|Celgene Corporation February 22 2017 Phase 1
NCT02616874 Completed Drug: MVA.HIVconsv vaccine|Drug: Romidepsin HIV IrsiCaixa|Germans Trias i Pujol Hospital|Fundacio Lluita Contra la SIDA|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint February 2016 Phase 1
NCT03141203 Recruiting Drug: Romidepsin|Drug: Carfilzomib Peripheral T Cell Lymphoma University of Birmingham|Bloodwise|Celgene|Amgen July 13 2015 Phase 1|Phase 2
NCT02393794 Recruiting Drug: Romidepsin|Drug: Cisplatin|Drug: Nivolumab Triple-Negative Breast Cancer|Breast Cancer Priyanka Sharma|Celgene Corporation|Bristol-Myers Squibb|University of Kansas Medical Center July 17 2015 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID