Romidepsin (FK228, Depsipeptide)

Name: Romidepsin (FK228, Depsipeptide)
Brand: Selleck Chemicals
SKU: S3020
Rating: 5 (140 reviews)

For research use only.

Catalog No.S3020 Synonyms: FR 901228, NSC 630176

140 publications

Romidepsin (FK228, Depsipeptide) Chemical Structure

CAS No. 128517-07-7

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.

Selleck's Romidepsin (FK228, Depsipeptide) has been cited by 140 publications

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

Nat Biotechnol, 2020, 10.1038/s41587-019-0388-4

PubMed: 31959954 ( click the link to review the publication )

Nature, 2017, 551(7679):247-250

PubMed: 29088702 ( click the link to review the publication )

Cancer Discov, 2017, 7(12):1450-1463

PubMed: 28963352 ( click the link to review the publication )

Cancers (Basel), 2021, 13(2)E259

PubMed: 33445642 ( click the link to review the publication )

Dev Dyn, 2021, 10.1002/dvdy.294

PubMed: 33410213 ( click the link to review the publication )

SLAS Discov, 2021, 2472555220983810

PubMed: 33427012 ( click the link to review the publication )

Nat Commun, 2020, 11(1):5775

PubMed: 33188175 ( click the link to review the publication )

EMBO Rep, 2020, 21:e50162

PubMed: 32314873 ( click the link to review the publication )

Int J Cancer, 2020, 10.1002/ijc.33046

PubMed: 32599665 ( click the link to review the publication )

PLoS Pathog, 2020, 16(2):e1008151

PubMed: 32109259 ( click the link to review the publication )

Cells, 2020, 10;9(6):E1447

PubMed: 32532133 ( click the link to review the publication )

J Immunol, 2020, 204(5):1242-1254

PubMed: 31988180 ( click the link to review the publication )

J Virol, 2020, 16;94(9) pii: e01845-19

PubMed: 32051267 ( click the link to review the publication )

Cancer Cell Int, 2020, 19;20:58

PubMed: 32099531 ( click the link to review the publication )

HIV Med, 2020, 21(11):747-757

PubMed: 33369029 ( click the link to review the publication )

Am J Transl Res, 2020, 12(10):6187-6203

PubMed: 33194023 ( click the link to review the publication )

Biochem Biophys Res Commun, 2020, 4;526(3):612-617

PubMed: 32247610 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00425-8

PubMed: 32886306 ( click the link to review the publication )

Blood Adv, 2020, 4(5):819-829

PubMed: 32126142 ( click the link to review the publication )

Sci Rep, 2020, 10(1):12864

PubMed: 32733053 ( click the link to review the publication )

Cancer Immunol Immunother, 2020, 10.1007/s00262-020-02653-1

PubMed: 32632663 ( click the link to review the publication )

Oncotarget, 2020, 11(37):3432-3442

PubMed: 32973968 ( click the link to review the publication )
Cancers (Basel), 2020, 12(12)E3589

PubMed: 33266275 ( click the link to review the publication )

Genes Chromosomes Cancer, 2020, 10.1002/gcc.22884

PubMed: 32614991 ( click the link to review the publication )

Front Immunol, 2020, 11:1746

PubMed: 33013828 ( click the link to review the publication )

Med Sci Monit, 2020, 26:e918528

PubMed: 31954012 ( click the link to review the publication )

PeerJ, 2020, 8:e10321

PubMed: 33282555 ( click the link to review the publication )

Epigenetics, 2020, 15(4):369-385

PubMed: 31533525 ( click the link to review the publication )

J Clin Invest, 2020, 135711

PubMed: 33270606 ( click the link to review the publication )

Nat Commun, 2019, 10(1):2189

PubMed: 31097698 ( click the link to review the publication )

J Thorac Oncol, 2019, 14(3):513-526

PubMed: 30521971 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432

PubMed: 30979734 ( click the link to review the publication )

Haematologica, 2019, 10.3324/haematol.2018.211110

PubMed: 30846494 ( click the link to review the publication )

Clin Infect Dis, 2019, 10.1093/cid/ciz108

PubMed: 30753360 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2152

PubMed: 31772119 ( click the link to review the publication )

Cell Rep, 2019, 29(9):2783-2795

PubMed: 31775045 ( click the link to review the publication )

Elife, 2019, 10.7554/eLife.44306

PubMed: 31050342 ( click the link to review the publication )

J Hematol Oncol, 2019, 12(1):30

PubMed: 30885250 ( click the link to review the publication )

Mol Ther, 2019, 27(5):1039-1050

PubMed: 30852137 ( click the link to review the publication )

Cancers (Basel), 2019, 11(5)E645

PubMed: 31083396 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)E1871

PubMed: 31769432 ( click the link to review the publication )

PLoS Pathog, 2019, 15(8):e1007991

PubMed: 31425551 ( click the link to review the publication )

Acta Pharm Sin B, 2019, 9(5):937-951

PubMed: 31649844 ( click the link to review the publication )

Front Immunol, 2019, 9:3162

PubMed: 30723480 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(5):900-908

PubMed: 30824609 ( click the link to review the publication )

Oncologist, 2019, 24(8):e740-e748

PubMed: 30696721 ( click the link to review the publication )
Mol Neurobiol, 2019, 10.1007/s12035-019-1565-7

PubMed: 30963442 ( click the link to review the publication )

AIDS, 2019, 33(2):199-209

PubMed: 30562171 ( click the link to review the publication )

Pharmacol Res, 2019, 142:192-204

PubMed: 30807866 ( click the link to review the publication )

Arthritis Res Ther, 2019, 21(1):50

PubMed: 30728075 ( click the link to review the publication )

Apoptosis, 2019, 24(5-6):404-413

PubMed: 30997620 ( click the link to review the publication )

J Biol Chem, 2019, 294(14):5576-5589

PubMed: 30745362 ( click the link to review the publication )

Exp Cell Res, 2019, 375(2):106-112

PubMed: 30579954 ( click the link to review the publication )

BMC Cancer, 2019, 19(1):79

PubMed: 30651077 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 510(2):278-283

PubMed: 30686534 ( click the link to review the publication )

ACS Omega, 2019, 4(22):19895-19904

PubMed: 31788622 ( click the link to review the publication )

Virus Res, 2019, 269:197631

PubMed: 31136823 ( click the link to review the publication )

Oncotarget, 2019, 10(55):5671-5679

PubMed: 31620242 ( click the link to review the publication )

J Nanobiotechnology, 2019, 17(1):69

PubMed: 31113488 ( click the link to review the publication )

J Virus Erad, 2019, 5(3):133-137

PubMed: 31700655 ( click the link to review the publication )

Blood, 2018, 131(4):397-407

PubMed: 29141948 ( click the link to review the publication )

J Clin Invest, 2018, 128(10):4413-4428

PubMed: 30148456 ( click the link to review the publication )

Nat Commun, 2018, 9(1):2024

PubMed: 29789628 ( click the link to review the publication )

Haematologica, 2018, 103(4):679-687

PubMed: 29305415 ( click the link to review the publication )

Int J Cancer, 2018, 143(6):1388-1401

PubMed: 29633255 ( click the link to review the publication )

MBio, 2018, 9(6)

PubMed: 30425153 ( click the link to review the publication )

Clin Epigenetics, 2018, 10:01

PubMed: 29312470 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(12):2767-2779

PubMed: 30232145 ( click the link to review the publication )

Cell Prolif, 2018, 51(3):e12447

PubMed: 29484736 ( click the link to review the publication )

J Virol, 2018, 92(13)

PubMed: 29643247 ( click the link to review the publication )
J Virol, 2018, 92(6)

PubMed: 29298886 ( click the link to review the publication )

Sci Rep, 2018, 8(1):1400

PubMed: 29362442 ( click the link to review the publication )

Stem Cells Int, 2018, 2018:2379546

PubMed: 29731773 ( click the link to review the publication )

Stem Cells Dev, 2018, 27(17):1215-1225

PubMed: 30032710 ( click the link to review the publication )

Cancers (Basel), 2018, 10(12)E505

PubMed: 30544928 ( click the link to review the publication )

Curr Protoc Pharmacol, 2018, 81(1):e41

PubMed: 29927058 ( click the link to review the publication )

Genome Res, 2018, 10.1101/gr.227272.117

PubMed: 29429976 ( click the link to review the publication )

Nat Neurosci, 2018, 21(4):564-575

PubMed: 29531362 ( click the link to review the publication )

JCI Insight, 2018, 3(22)125568

PubMed: 30429379 ( click the link to review the publication )

Nat Commun, 2017, 8(1):403

PubMed: 28864822 ( click the link to review the publication )

Nat Commun, 2017, 8(1):939

PubMed: 29038521 ( click the link to review the publication )

Genes Dev, 2017, 31(17):1770-1783

PubMed: 28982760 ( click the link to review the publication )

Cancer Immunol Res, 2017, 5(7):604-616

PubMed: 28615266 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(12):3084-3096

PubMed: 27993968 ( click the link to review the publication )

Arch Toxicol, 2017, 91(5):2191-2208

PubMed: 27807597 ( click the link to review the publication )

Cancer Discov, 2017, 7(12):1450-1463

PubMed: 28963352 ( click the link to review the publication )

FEBS J, 2017, 284(23):4035-4050

PubMed: 28985013 ( click the link to review the publication )

Biochem Pharmacol, 2017, 127:90-100

PubMed: 28012958 ( click the link to review the publication )

Int J Mol Sci, 2017, 18(5)

PubMed: 28481295 ( click the link to review the publication )

J Pharmacol Exp Ther, 2017, 363(2):211-220

PubMed: 28860353 ( click the link to review the publication )

Acta Pharmacol Sin, 2017, 38(4):551-560

PubMed: 28112184 ( click the link to review the publication )

Int J Parasitol Drugs Drug Resist, 2017, 7(1):42-50

PubMed: 28107750 ( click the link to review the publication )

JCI Insight, 2017, 2(1):e85811

PubMed: 28097226 ( click the link to review the publication )

Oncotarget, 2017, 8(4):6319-6329

PubMed: 28030834 ( click the link to review the publication )
JCI Insight, 2017, 2(6):e90196

PubMed: 28352655 ( click the link to review the publication )

Oncotarget, 2017, 9(3):3908-3921

PubMed: 29423093 ( click the link to review the publication )

Oncotarget, 2017, 8(30-:48737-48754

PubMed: 28467787 ( click the link to review the publication )

Ann Oncol, 2016, 27(3):508-13

PubMed: 26658891 ( click the link to review the publication )

EMBO Mol Med, 2016, 8(2):117-38

PubMed: 26681773 ( click the link to review the publication )

Clin Cancer Res, 2016, 22(16):4119-32

PubMed: 26964571 ( click the link to review the publication )

Kidney Int, 2016, 89(2):317-26

PubMed: 26509586 ( click the link to review the publication )

EBioMedicine, 2016, 8:217-229

PubMed: 27428432 ( click the link to review the publication )

PLoS Pathog, 2016, 12(4):e1005545

PubMed: 27082643 ( click the link to review the publication )

J Virol, 2016, 90(20):9018-28

PubMed: 27466424 ( click the link to review the publication )

Sci Rep, 2016, 6:30749

PubMed: 27480951 ( click the link to review the publication )

Int J Neuropsychopharmacol, 2016, 10.1093/ijnp/pyw035

PubMed: 27207921 ( click the link to review the publication )

Int J Oncol, 2016, 49(6):2453-2463

PubMed: 27748897 ( click the link to review the publication )

Am J Physiol Heart Circ Physiol, 2016, 311(5):H1139-H1149

PubMed: 27638876 ( click the link to review the publication )

Oncol Rep, 2016, 36(4):1875-85

PubMed: 27509880 ( click the link to review the publication )

Biochem Biophys Res Commun, 2016, 474(1):71-75

PubMed: 27091426 ( click the link to review the publication )

Leuk Res, 2016, 47:100-8

PubMed: 27294334 ( click the link to review the publication )

Target Oncol, 2016, 11(6):783-798

PubMed: 27250763 ( click the link to review the publication )

Oncotarget, 2016, 10.18632/oncotarget.8379

PubMed: 27028869 ( click the link to review the publication )

Oncotarget, 2016, 7(4):4454-67

PubMed: 26683357 ( click the link to review the publication )

Nat Commun, 2015, 3;6:10091

PubMed: 26631872 ( click the link to review the publication )

Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-1561

PubMed: ( click the link to review the publication )

Leukemia, 2015, 29(3):556-66

PubMed: 25118879 ( click the link to review the publication )

Clin Cancer Res, 2015, 21(7):1628-38

PubMed: 25623213 ( click the link to review the publication )
Blood Cancer J, 2015, 5:e357

PubMed: 26473529 ( click the link to review the publication )

Endocr Relat Cancer, 2015, 22(5):777-92

PubMed: 26206775 ( click the link to review the publication )

Epigenetics, 2015, 10.1080/15592294.2015.1039216

PubMed: 25923331 ( click the link to review the publication )

Antimicrob Agents Chemother, 2015, 59(7):3984-94

PubMed: 25896701 ( click the link to review the publication )

Sci Rep, 2015, 5:16445

PubMed: 26563568 ( click the link to review the publication )

J Biol Chem, 2015, 290(39):23725-37

PubMed: 26269591 ( click the link to review the publication )

J Biol Chem, 2015, 290(8):5028-40

PubMed: 25540204 ( click the link to review the publication )

J Biol Chem, 2015, 290(8):5028-40

PubMed: ( click the link to review the publication )

Int J Parasitol Drugs Drug Resist, 2015, 5(3):117-26

PubMed: 26199860 ( click the link to review the publication )

PLoS One, 2015, 10(12):e0145994

PubMed: 26717578 ( click the link to review the publication )

Tumour Biol, 2015, 36(7):5485-95

PubMed: 26036758 ( click the link to review the publication )

Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384

PubMed: 25355930 ( click the link to review the publication )

Diabetes, 2014, 63(9):2924-34

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PLoS Pathog, 2014, 10(8):e1004287

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Cell Death Dis, 2014, 5:e1134

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Mol Cell Biol, 2014, 34(7):1280-9

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J Chem Inf Model, 2014, 10.1002/ijc.28924

PubMed: 24771510 ( click the link to review the publication )

J Neurosci, 2013, 33(17):7535-47

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Mol Cancer Ther, 2013, 12(8):1591-604

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Br J Haematol, 2013, 162(4):559-62

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Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description

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	M2rWV2NmdGxiVnnhZoltcXS7IFHzd4F6	NYDZN4lIOi53LUG1JI5O	MoHVO\|IhcA>?		MV;pcoR2[2W\|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh	M4OzTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{mwPVA4Lz5{NUe5NFkxPzxxYU6=
U2932	M3K0O2NmdGxiVnnhZoltcXS7IFHzd4F6	MV[yMlUuOTVibl2=	M1rM[VczKGh?		MmXjbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>?	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd7MEmwO{c,OjV5OUC5NFc9N2F-
OCI-LY7	NYDmOFI1S2WubDDWbYFjcWyrdImgRZN{[Xl?	NX;oVGx2Oi53LUG1JI5O	MXK3NkBp		MYrpcoR2[2W\|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh	M3;id\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{mwPVA4Lz5{NUe5NFkxPzxxYU6=
Farage	MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NUW1e41ROi53LUG1JI5O	M4f5TFczKGh?		MXrpcoR2[2W\|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd7MEmwO{c,OjV5OUC5NFc9N2F-
LY7/EBV	MnXqR4VtdCCYaXHibYxqfHliQYPzZZk>	Mnv1Nk42NTF3IH7N	MWm3NkBp		NYGwfW5ScW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?=	NFHMWYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe5NFkxPyd-MkW3PVA6ODd:L3G+
U2932/EBV	Mk[0R4VtdCCYaXHibYxqfHliQYPzZZk>	M{HJOFIvPS1zNTDuUS=>	M1LPSlczKGh?		NH\BZYZqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi	M4fiOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{mwPVA4Lz5{NUe5NFkxPzxxYU6=
HCT116	M3\jNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHHLXFA2NTVyMECgcm0>	M4LrUVI1KGh?	M4jEfGROW09?	MnznbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR7MkWxOUc,OjV2OUK1NVU9N2F-
ACH-2	M4nw[mZ2dmO2aX;uJGF{e2G7	MXKxMVkhdk1?	M2C5XVI1KGh?		MmP2bY5lfWOnczDITXYuOSCHbo[g[ZhxemW\|c3nvci=>	NUTo[ZFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxOFk1PjdpPkK1NVQ6PDZ5PD;hQi=>
MCF-10A	M1yzcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NWTkcWdWUUN3ME2wMlE4yrFyLkCxJI5O	NGrnXG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm1OFg2Pid-MkS5OVQ5PTZ:L3G+
MCF-7	NXKycIxJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M3HXfGlEPTB;MT6xNOKyOC5{MDDuUS=>	NXmzcnJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OVQ5PTZpPkK0PVU1QDV4PD;hQi=>
SK-BR-3	NGjjcoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NVHUe4czUUN3ME2xMlAxyrFyLkO1JI5O	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
MDA-MB-231	MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NYOzR\|V{UUN3ME2wMlY5yrFyLkG0JI5O	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl3NEi1Okc,OjR7NUS4OVY9N2F-
PC3	M3vGUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M{XkOmlEPTB;MT62OeKyOC5\|NTDuUS=>	M361V\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
HCT116	Ml;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVPqT5BQUUN3ME2xMlAxyrFyLkCwJI5O	M4DFW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
HCT116-p21-/-	NUXUdVFbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M1PTeGlEPTB;MT6yOuKyOC5\|NzDuUS=>	M{GyTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUW0PFU3Lz5{NEm1OFg2PjxxYU6=
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HLF	M1\seGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MYO3NkBpenN?		NGPJO4ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMSkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygS2k2OCB;IECuNFA1QDlizszNMi=>	M17PPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{OxN\|M1Lz5{NkOzNVM{PDxxYU6=
WI38	MmXaRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MljXO\|IhcHK\|		M{jYWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iV1mzPEBk\WyuczDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygS2k2OCB;IECuNFA2OzlizszNMi=>	M{nNeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{OxN\|M1Lz5{NkOzNVM{PDxxYU6=
U937	Mki1SpVv[3Srb36gZZN{[Xl?		M{PieVI1KGi{cx?=		MVHJcohq[mm2aX;uJI9nKEiGQVO2JIlvKGi3bXHuJHU6OzdiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIFteGijLYT1ZoltcW5iYXPleJlt[XSrb36gZZQhPSCwTTD0c{A2KHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	NXn6[IRIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zN\|E{OzRpPkK2N\|MyOzN2PD;hQi=>
HCT116	NFzGSIdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MVW3NkBpenN?		MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSClb4XseIVzKGOxdX70[ZIhdWW2aH;kMEBKSzVyIE2gNE4xOjhizszNMi=>	NGDNRmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkS4NVY2QSd-Mk[0PFE3PTl:L3G+
IGROV1/Pt1	NXzYdlMxSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NYTGeWk5PzJiaILz		MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNU9RfDFiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ492dHSncjDjc5VvfGW{IH3leIhw\CxiSVO1NEA:KDBwMEig{txONg>?	MonxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2OEG2OVkoRjJ4NEixOlU6RC:jPh?=
IGROV1	NV7CTmVSSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MXm3NkBpenN?		NXO3NZMzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ492dHSncjDjc5VvfGW{IH3leIhw\CxiSVO1NEA:KDBwMkKg{txONg>?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjR6MU[1PUc,OjZ2OEG2OVk9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p21 / Cyclin D1; PubMed: 19682393 J Mol Signal 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 Blood Cancer J 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 Blood Cancer J 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 Blood Cancer J 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 Gynecol Oncol 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 Cancer Sci 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 Gynecol Oncol 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 Oncotarget A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells. Cleaved caspase-3; PubMed: 22531354 J Ovarian Res 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]	- Collapse 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]	- Collapse 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]	- Collapse 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. (Only for Reference)

References

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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 Download Romidepsin (FK228, Depsipeptide) SDF

Molecular Weight	540.7
Formula	C₂₄H₃₆N₄O₆S₂
CAS No.	128517-07-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	FR 901228, NSC 630176
Smiles	CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C

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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.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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The Serial Dilution Calculator Equation

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Computed Result

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03770000	Active not 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\|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

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.

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HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

Pan HDAC Inhibitor

Panobinostat (LBH589) : Pan-HDAC inhibitor, IC50=5 nM.
Most Potent HDAC Inhibitor

Quisinostat (JNJ-26481585) : HDAC1, IC50=0.11 nM; HDAC2, IC50=0.33 nM.
FDA-approved HDAC Inhibitor

Vorinostat (SAHA, MK0683) : Approved by FDA against cutaneous T cell lymphoma.
Newest HDAC Inhibitor

RG2833 (RGFP109) ^New : Brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.

Related HDAC Products

LMK-235 ^New

LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.
CAY10603 ^New

CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
Domatinostat (4SC-202) ^New

Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
Panobinostat (LBH589)

Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Vorinostat (SAHA)

Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Entinostat (MS-275)

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Trichostatin A (TSA)

Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
RGFP966

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Tubastatin A

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Mocetinostat (MGCD0103)

Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.

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Romidepsin (FK228, Depsipeptide)