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 52 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 MmDFR4VtdCCYaXHibYxqfHliQYPzZZk> M{LyeFIvPS1zNTDuUS=> NG\DXmM4OiCq NHrkeXZqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi MkXZNlU4QTB7MEe=
U2932  MnzjR4VtdCCYaXHibYxqfHliQYPzZZk> M4DzfFIvPS1zNTDuUS=> M1zERVczKGh? MXzpcoR2[2W|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh MVGyOVc6ODlyNx?=
OCI-LY7 M4LoVmNmdGxiVnnhZoltcXS7IFHzd4F6 MmO5Nk42NTF3IH7N NHr3Z2U4OiCq MoDIbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>? M2\ie|I2PzlyOUC3
Farage MoHvR4VtdCCYaXHibYxqfHliQYPzZZk> NX\T[ZBVOi53LUG1JI5O MXO3NkBp NEfxRo5qdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi NIHtcG0zPTd7MEmwOy=>
LY7/EBV M1XUdGNmdGxiVnnhZoltcXS7IFHzd4F6 M4rwOVIvPS1zNTDuUS=> NETtfog4OiCq Mk\KbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>? NXq0XpA5OjV5OUC5NFc>
U2932/EBV Mm\sR4VtdCCYaXHibYxqfHliQYPzZZk> MoXUNk42NTF3IH7N MWK3NkBp NGTMdnRqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi MlPENlU4QTB7MEe=
HCT116 M3f0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWW1MVUxODBibl2= MVGyOEBp MWHEUXNQ MnTabY5lfWOnczDj[YxtKGSnYYToJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy NEK4cIUzPTR7MkWxOS=>
ACH-2 NFTHb5ZHfW6ldHnvckBCe3OjeR?= MVmxMVkhdk1? M3HaOVI1KGh? NEHOSWdqdmS3Y3XzJGhKXi1zIFXuekBmgHC{ZYPzbY9v M4j3dlI2OTR7NE[3
MCF-10A NHTHcVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPoTWM2OD1yLkG3xtExNjBzIH7N M1W0PVI1QTV2OEW2
MCF-7 NG\acXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XuRmlEPTB;MT6xNOKyOC5{MDDuUS=> NXzhR4JGOjR7NUS4OVY>
SK-BR-3 M2\6Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXQTWM2OD1zLkCwxtExNjN3IH7N NXrsSokxOjR7NUS4OVY>
MDA-MB-231 MnTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjFcmZwUUN3ME2wMlY5yrFyLkG0JI5O MXSyOFk2PDh3Nh?=
PC3 NWTUSWJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXv[3ZKSzVyPUGuOlXDuTBwM{Wgcm0> M2C0Z|I1QTV2OEW2
HCT116 M3jpbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7WZpBKSzVyPUGuNFDDuTBwMECgcm0> NFOzUoMzPDl3NEi1Oi=>
HCT116-p21-/- M4\1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULmXIJMUUN3ME2xMlI3yrFyLkO3JI5O NVHKSY1HOjR7NUS4OVY>
S1 NUjQS|BjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTdwNkhCtVAvOjlibl2= NX3WZZlHOjR7NUS4OVY>
SW620 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7tR5k6UUN3ME2wMlk{yrFyLkK5JI5O NUW3[osyOjR7NUS4OVY>
LOX-IMVI M375Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3yyOmlEPTB;MD64O:KyOC5yMzDuUS=> MV2yOFk2PDh3Nh?=
UACC-62 MoTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwNUdCtVAvOTZibl2= NX3ofYxnOjR7NUS4OVY>
MDA-MB-435 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnIVXhKSzVyPUCuPVDDuTBwME[gcm0> MoPVNlQ6PTR6NU[=
SF-295 NEXycYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUm1WJF2UUN3ME2wMlg5yrFyLkG1JI5O NET0eXEzPDl3NEi1Oi=>
A549 NGTUeGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrpZoJKSzVyPUGuNlbDuTBwMkSgcm0> NEfqPWgzPDl3NEi1Oi=>
H460 NEGzN|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHSTWM2OD1{LkW4xtExNjhyIH7N M1HPXFI1QTV2OEW2
EKVX NWqyWoExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDhU2pKSzVyPUGuN|PDuTBwM{Sgcm0> NHnZc2wzPDl3NEi1Oi=>
H146 NUnaeIFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PBbmlEPTB;MD6yNuKyOC5yNzDuUS=> MY[yOFk2PDh3Nh?=
H526 NVfoU3JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\CfWlEPTB;MD6xOeKyOC5yMzDuUS=> MWWyOFk2PDh3Nh?=
HuT-78 M1fRNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7QOIJIUUN3ME2xMlc{yrFyLkS0JI5O NEflTGkzPDl3NEi1Oi=>
HA MlO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmO3NE43OjVvMUDuUS=> MnvBOFghcA>? MWrpcoR2[2W|IHGgd4lodmmoaXPhcpRtgSC|dILvcodmeiCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBkdy22cnXheIVlKHerdHigZo9zfGW8b33pZi=> M2fDT|I1PzdzNUGw
MS-275 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37Ve|AvPjJ3LUGwcm0> NFm0XG01QCCq MnPmbY5lfWOnczDhJJNq\26rZnnjZY51dHlic4Tyc45o\XJiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[29vdILlZZRm\CC5aYToJIJwenSnen;tbYI> NF7pT5IzPDd5MUWxNC=>
CD4 T MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUC0PEBp MnfJSWM2OD12LkZCtVEvOCCwTR?= MXmyOFczOjR3NB?=
CD4 T Mmm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPLU4dsPDhiaB?= M4DQT2NEPTB;MUC3xtEyOjZibl2= NHzXfoEzPDd{MkS1OC=>
CD4+ T Ml\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXMSWM2OD1|IH7N M2Ph[FI1PDl3MUC1
A549 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIi4dWsyOOLCk{GwNOKhdk1? M2P2b|I1NzN4L{S4JIg> NIO3T4lqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGOxbnPlcpRz[XSrb36tJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M3n6[FI1PDh3N{m5
JJN3 NX;3fIR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmyOE81QCCq MXnFR|UxRDIkgJnuUVshPDkkgJno M17LO|I1ODNyMUWw
OPM-2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfCUXAzPC92ODDo MUHFR|Uxez1z4pEJcm08KDR64pEJbC=> Ml22NlQxOzBzNUC=
RPMI-8226 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLlcIl1OjRxNEigbC=> MkPnSWM2OHN;MT645qCKdk19IES45qCKcA>? M2fCWlI1ODNyMUWw
U266 NVLFcpJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVqyW2h[OjRxNEigbC=> MX3FR|Uxez1zMPMAjY5OQyB2OPMAjYg> NFHCUngzPDB|MEG1NC=>
CA46 Mn7FRZBweHSxc3nzJGF{e2G7 NWrkTnpYPiCq NWXsfVM4cW6mdXPld{BjdHWwdDDhdI9xfG:|aYO= MkHLNlM6PjZzNkS=
DG75 MV7BdI9xfG:|aYOgRZN{[Xl? NVO4eHZiPiCq MVrpcoR2[2W|IH7vJIFxd3C2b4Ppdy=> MXeyN|k3PjF4NB?=
Ramos MX3BdI9xfG:|aYOgRZN{[Xl? M4PJPVYhcA>? M2DnXolv\HWlZYOg[Zh1\W6|aY\lJIFxd3C2b4Ppdy=> M1TRVVI{QTZ4MU[0
ST486 Mnu4RZBweHSxc3nzJGF{e2G7 NYLVR49CPiCq M2TpfIlv\HWlZYOg[Zh1\W6|aY\lJIFxd3C2b4Ppdy=> MWOyN|k3PjF4NB?=
HuT78 NF3VUJRCeG:ydH;zbZMhSXO|YYm= MlfiNU8yOC9zMECgcm0> NWnKTWxNPDhiaB?= NIHqSYFqdmS3Y3XzJIFxd3C2b4Ppd{BifCBzIH7N NU\wdYJmOjN3M{K3N|I>
DpVp35 NXrsUmhTSXCxcITvd4l{KEG|c3H5 M2PSRVEwOTBxMUCwJI5O MkfZOFghcA>? M1v1bIlv\HWlZYOgZox2dnRiYYDvdJRwe2m| MV:yN|U{Ojd|Mh?=
DpVp50 NXLTfm9LSXCxcITvd4l{KEG|c3H5 NXTsTGtVOS9zMD:xNFAhdk1? MWm0PEBp NHTkcYdqdmS3Y3XzJIJtfW62IHHwc5B1d3Orcx?= M{fJcVI{PTN{N{Oy
DpP75  MXfBdI9xfG:|aYOgRZN{[Xl? MlnwNU8yOC9zMECgcm0> M2jwXlQ5KGh? NF\i[nRqdmS3Y3XzJIJtfW62IHHwc5B1d3Orcx?= MWCyN|U{Ojd|Mh?=
SKOV-3 MoDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzpNgKBmzJybl2= NWjDVnlGPzJiaB?= MofkSG1UVw>? MmXjdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjbH;u[UBidmRiY3;tZolv\WRid3n0bEBkcXOybHH0bY4> MmXGNlMxOTB|NEi=
Brca1 WT MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vBTlHjiJN{MH7N Ml3ZO|IhcA>? M3:xU2ROW09? MV\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGGub37lJIFv\CClb33ibY5m\CC5aYToJINqe3CuYYTpci=> MUCyN|AyODN2OB?=
Brca1 Null NFXwSIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;FWFAy6oDVMkDuUS=> M3zx[FczKGh? MWnEUXNQ NVXrWWFNemWmdXPld{Bk\WyuII\pZYJqdGm2eTDhcI9v\SCjbnSgZ49u[mmwZXSge4l1cCClaYPwcIF1cW5? M3z1WVI{ODFyM{S4
OVCAR-8  NYX5OVJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7MNgKBmzJybl2= MUm3NkBp NHzZc|BFVVOR MVvy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGGub37lJIFv\CClb33ibY5m\CC5aYToJINqe3CuYYTpci=> MlHWNlMxOTB|NEi=
NCI/ADR-RES NV7QVIt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLLNgKBmzJybl2= NUS0PWJGPzJiaB?= MXHEUXNQ NHHzeXVz\WS3Y3XzJINmdGxidnnhZoltcXS7IHHsc45mKGGwZDDjc41jcW6nZDD3bZRpKGOrc4DsZZRqdg>? MorqNlMxOTB|NEi=
HCT116 MlLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HwRVUhdk1vNUCg{txO M{fLXlI1KGh? MVrEUXNQ NYXMbVZZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MUiyNlkzPDl3OB?=
RKO M3;K[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[1JI5ONTVyIN88US=> NWLTWXZxOjRiaB?= MXzEUXNQ MkXWbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NF3tXVUzOjl{NEm1PC=>
CO115 MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYntNVExPSCwTT21NEDPxE1? NEjUbpczPCCq NYnwbHRpTE2VTx?= NUD3SGJlcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? M4\4W|IzQTJ2OUW4
HFS Mn\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYS1JI5O MV:yOE81QC95MjDo MWnpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nLXTldIVv\GWwdHz5 Mk\LNlIyODZ{OEK=
LNCaP M1XD[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{SzSVUhdk1? NWD0b4dPOjRxNEivO|IhcA>? MV;pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nLXTldIVv\GWwdHz5 MXWyNlExPjJ6Mh?=
A549 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrLTVVPPSCwTR?= M1zO[|I1NzR6L{eyJIg> NEHkeY9qdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lMYRmeGWwZHXueIx6 MVSyNlExPjJ6Mh?=
697  M4i3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUOze5RCUUN3MPMAjV3jiIl{LkZCpI5O MoewNlE2Ozh{MU[=
697-R NGrIfnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;aZ2lEPTEkgJm95qCKQC54wrDuUeKh NEnTR5kzOTV|OEKxOi=>
HUT78 NX;HN3lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFibl2= M4ni[VIyOTl6NUS1
THJ-16T NGfrN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXQVJdPOSCwTR?= NX7i[VhWOjRiaB?= MlTvbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MVmyNFgyODV4OB?=
HCT116 NV3CVI9bTnWwY4Tpc44hSXO|YYm= NYm5XJBQOjBibl2= MkP0PEBp M3nido1w\HWuYYTld{B1emGwc3PybZB1KGyndnXsd{Bnd3JiaIXu[JJm\HNib3[g[4Vv\XNiaX6g[Yl1cGW{IHTpdoVkfGmxbh?= MoTpNlA4Ozl2NUS=
B104  M120WGZ2dmO2aX;uJGF{e2G7 NFu0UXIzKG6P NIHOcm8zPC92OD:3NkBp M3TMc4lv[3KnYYPld{B1cGVic4Xy[oFk\SCneIDy[ZN{cW:wIH;mJGNFOjEEoB?= M1;yclIxPjh4NUC1
HL-60  NF3ZWIpEgXSxdH;4bYNqfHliQYPzZZk> NXPQcGR5OS13MECgcm0> MVeyOEBp NUS1OHJ[cW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?= M{WydlIxPjJ2MU[z
HP100 MWTDfZRwfG:6aXPpeJkhSXO|YYm= M3TkcVEuPTByIH7N MYqyOEBp MWPpcoR2[2W|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh M33HU|IxPjJ2MU[z
HL-60  NX:1e21STnWwY4Tpc44hSXO|YYm= NFjJN|cyOCCwTR?= MkDyOE83NzF4IHi= NIrpTm1qdmS3Y3XzJJRp\SCpZX7ldoF1cW:wIH;mJIh6\HKxZ3XuJJBmem:6aXTlJIZzd21iNHi= M2j4cFIxPjJ2MU[z
HP100 NHPreXhHfW6ldHnvckBCe3OjeR?= NIHkNY8yOCCwTR?= MX60M|YwOTZiaB?= M1LOXYlv\HWlZYOgeIhmKGenbnXyZZRqd25ib3[gbJllem:pZX6gdIVzd3irZHWg[pJwdSB2aB?= NH63PYczODZ{NEG2Ny=>
HL-60  NVTaOXdnTnWwY4Tpc44hSXO|YYm= NUfUPVhLOTBvNUCwJI5O NUj4d5p[PCCq M3XCWoRm[3KnYYPld{B1cGViaHnzeI9v\SCmZXHj[ZR6dGG|ZTCoTGRCSyliYXP0bZZqfHoEoB?= NWXmTGxNOjB4MkSxOlM>
HP100 MYLGeY5kfGmxbjDBd5NigQ>? MV[xNE02ODBibl2= MlzjOEBp M2HIVYRm[3KnYYPld{B1cGViaHnzeI9v\SCmZXHj[ZR6dGG|ZTCoTGRCSyliYXP0bZZqfHoEoB?= NEfyeXczODZ{NEG2Ny=>
11z MWrLbY5ie2ViQYPzZZk> M{PX[|MuOTByIH7N MkfSdoVlfWOnczDISGFEKGWweontZZRq[yCjY4Tpeol1gSBqSVO1NOKhRSB4LkWgxtEhOC54IH7tc4wwVCl? MkD3NlA3ODVzNES=
SKOV-3 NHKwPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoK0OE85NzF4IH7N MUO0PEBp MWPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> M3rFOVIxPDB2NU[0
OVCAR-3 NVHRN5FIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWG0M|gwOTZibl2= NEH0[Ys1QCCq NGmzenlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NHq2R4czODRyNEW2OC=>
HBL-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1L1V|IuOTBibl2= NXTSSZJqOjRiaB?= NVnkc25SUUN3ME20MlMhdk1? NWDwRVFSOjByNkiwPFA>
Jeko-1 M1vSO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfnXYszNTVyIH7N NFfZU5gzPCCq NGnPU2tKSzVyPUGxJI5O M3vZclIxODZ6MEiw
Granta-519 MnThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljsOU01OCCwTR?= NW\uU4kzOjRiaB?= NUT2[JlLUUN3ME21PE42KG6P NHO4foIzODB4OEC4NC=>
L1236 MYPDfZRwfG:6aXPpeJkhSXO|YYm= NX3MNWxjOSCwTT2xNFAh|ryP NVrxOZlbPDhiaB?= MkPSSWM2OD1yLkC3JO69VQ>? M3LyTlE6OjN|NEew
L428 NVjDNHI{S3m2b4TvfIlkcXS7IFHzd4F6 MmDWNUBvVS1zMECg{txO MlPVOFghcA>? NHjYdpBGSzVyPUCuOFMh|ryP MYixPVI{OzR5MB?=
KM-H2 NYPreHFxS3m2b4TvfIlkcXS7IFHzd4F6 Mmn5NUBvVS1zMECg{txO M2TUUlQ5KGh? MYDFR|UxRTBwNUig{txO MWWxPVI{OzR5MB?=
L540Cy NHzBSnJEgXSxdH;4bYNqfHliQYPzZZk> MXKxJI5ONTFyMDFOwG0> MVy0PEBp NVfMb2hWTUN3ME2wMlE3KM7:TR?= MlOzNVkzOzN2N{C=
G401 NFnOc49HfW6ldHnvckBCe3OjeR?= M1fJZ|ExKG6P NEDS[lIzPC92OD:3NkBp MmDOSG1UVw>? MVLpcoNz\WG|ZYOgR2RMVjGFIHX4dJJme3Orb36= MofDNVkzOjF3OE[=
STM91-01 NGjSWFdHfW6ldHnvckBCe3OjeR?= MnnZNVAhdk1? M1XmN|I1NzR6L{eyJIg> Mo\aSG1UVw>? M4DyOIlv[3KnYYPld{BETEuQMVOg[ZhxemW|c3nvci=> M3H2fVE6OjJzNUi2
SJSC  NIfxXZlHfW6ldHnvckBCe3OjeR?= NV7ucZRyOTBibl2= MnvMNlQwPDhxN{KgbC=> NHXJd|NFVVOR M1WzUolv[3KnYYPld{BETEuQMVOg[ZhxemW|c3nvci=> NHLlWocyQTJ{MUW4Oi=>
BT16  NGm1bGZHfW6ldHnvckBCe3OjeR?= MoixNVAhdk1? Ml;0NlQwPDhxN{KgbC=> Mlq2SG1UVw>? MVLpcoNz\WG|ZYOgR2RMVjGFIHX4dJJme3Orb36= NYjnNVJGOTl{MkG1PFY>
NCI-H1299 MmqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTSTWM2OD12LkdCtVAvOiCwZz;tcC=> NVuwVJQ3OTlzN{m4PVA>
NCI-2882 NGnlfW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrrU5lRUUN3ME2xMlbDuTBwMESgcocwdWx? MVSxPVE4QTh7MB?=
HCC95 NULPSVJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJwNdMxNE4xPSCwZz;tcC=> MYexPVE4QTh7MB?=
NCI-H23 NVTPdG1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HuVmlEPTB;Mj65xtExNjJibnevcYw> MVWxPVE4QTh7MB?=
NCI-H157 NIXBbllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\JcFVbUUN3ME2xMlbDuTBwMEKgcocwdWx? MUmxPVE4QTh7MB?=
NCI-H460 NYjldXo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHwbZIzUUN3ME2yMlHDuTBwMEegcocwdWx? M3vTXFE6OTd7OEmw
NCI-H1975 MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTFwM9MxNE4xPCCwZz;tcC=> MmnaNVkyPzl6OUC=
NCI-H820 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLCTpJKSzVyPUKuOOKyOC5zIH7nM41t MX[xPVE4QTh7MB?=
NCI-H1650 M2jUeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\4c3FKSzVyPUSuPeKyOC5|IH7nM41t NI\hfpoyQTF5OUi5NC=>
DTC1 NVPYRmdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwNUGgcm0> MnTZNVg2PjZ{NE[=
KAO NX\iS|VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\2TWM2OD1yLkmxJI5O Ml3JNVg2PjZ{NE[=
SU-CCS-1 NFrn[2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7LdIJKSzVyPUCuPFkhdk1? MU[xPFU3PjJ2Nh?=
SYO-1 NHHvO3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XCeWlEPTB;MD62O{BvVQ>? NYq2[JE{OTh3Nk[yOFY>
FUJI M3TRW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjxUZE2UUN3ME2xMlMyKG6P M2XSdFE5PTZ4MkS2
SKNMC M4nUOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLZTWM2OD1zLkG3JI5O MmfYNVg2PjZ{NE[=
402-91 M{jkTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFwMk[gcm0> NH7iXFEyQDV4NkK0Oi=>
1765-92 M1i5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NECzR29KSzVyPUGuO|chdk1? NYXabHZbOTh3Nk[yOFY>
JN-DSRCT-1 MkDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke3TWM2OD1zLkK1JI5O NEnXXJAyQDV4NkK0Oi=>
NMS-2PC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwOEGgcm0> Mk\1NVg2PjZ{NE[=
HL60 NV3HbJR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXiclI3UUN3ME2xMlg3KG6P NV;CcmUzOTh3Nk[yOFY>
A549 NWXicHZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTNwMkSgcm0> Ml3oNVg2PjZ{NE[=
SW480 NGP6RW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnrTWM2OD1{Lk[5JI5O MVOxPFU3PjJ2Nh?=
MCF7 MkWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTNwNUWgcm0> M4S2NlE5PTZ4MkS2
PC-3 MlzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1K1N2lEPTB;Mj61NUBvVQ>? MV:xPFU3PjJ2Nh?=
MMRU MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnhO5JDUUN3ME2yMlU4KG6P NI\6cHgyQDV4NkK0Oi=>
Hs68 M4rlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfQUYZKSzVyPU6xNEBvVQ>? NWHDdnNwOTh3Nk[yOFY>
hMSC-001F M3vpN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fLUGlEPTB;PkGwJI5O NF7rVZYyQDV4NkK0Oi=>

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID