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Romidepsin (FK228, depsipeptide)Cat. No.: A8173

CAS No.: 128517-07-7

Formula: C24H36N4O6S2

M.Wt: 540.7

Synonyms: Istodax, Antibiotic FR 901228, FK228, FR

901228, FK-228,Romidepsin

Target: DNA Damage/DNA Repair

Pathway: HDAC

Storage: Store at -20°C

In Vitro

27.035mg/mL in DMSO, 35.27 mg/mL in EtOH with ultrasonic,insoluble in H2O

Preparing

Stock Solutions

Mass

1mg 5mg 10mgSolvent

Concentration

1 mM 1.8495 mL 9.2473 mL 18.4945 mL

5 mM 0.3699 mL 1.8495 mL 3.6989 mL

10 mM 0.1849 mL 0.9247 mL 1.8495 mL

Please refer to the solubility information to select the appropriate solvent.

Shortsummary HDAC1/HDAC2 inhibitor,potent and selective

IC₅₀ & Target 36 nM (HDAC1), 47 nM (HDAC2)

In Vitro

Cell Viability Assay

Cell Line: Human NB cell ( SMS-KCNR, SK-N-BE2, SH-SY5Y, SK-N-AS, L A1-15N,

SH-SHEP and IMR32 lines)

Preparation method The solubility of this compound in DMSO is >10 mM. General tips for obtaining

a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or

shake it in the ultrasonic bath for a while.Stock solution can be stored below

-20°C for several months.

Product Name: Romidepsin (FK228, depsipeptide)Revision Date: 01/10/2020

Product Data Sheet

Solvent & Solubility

Biological Activity

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Romidepsin (FKKKKKKKKKKKK2222222222222222222222228, ddepsipeptide)Cat. No.: A81777777777733333333333

CAS No.: 121222122221212121211212212128585858588585858585851717171711717171717177177------0700000000000 -7

Formula: C2CC2C2C2C2CCC2C2C2C2C2CC24H36N4O6S2

M.Wt: 540.7

Synonyms: Istodax, Antibiotic FR 9012288, FK228, FR

901228, FK-228,Romidepsin

Target: DNA Damage/DNA Repair

Pathway: HDAC

Storage: Store at -20°C

In Vitro

27.035mg/mL in DMSO, 35.27 mg/mL in EtOH with ultrasonic,insoluble in H2O

Preparing

Stock Solutions

Mass

1mg 5mg 10mgSolvent

Concentration

1 mM 1.8495 mL 9.2473 mL 18.4945 mL

5 mM 0.3699 mL 1.84444444959595959595955959595 mmmmmmmmmmmLLLLLLLLL 3.6989 mL

10 mM 0.1849 mL 0.0.0.0.0.0.0.0.0.0 9292929292922222929222292929299222444474747474747474744744474774474 mmL 1.8495 mL

PlPlPlPlPlPlPlPlPlP eaeaeeaeaeaeaeeaseseseseseseseseseseeesee rrrrrrrrrrrrefeeeeee er to the solubility information to select the appropriate ssssssssssssssssolololololololololololololooo veveveveveeeveveeeveveveevevevev ntntntntntntntntnntntn ...

Shortsummary HDAC1/HDAC2 inhibitor,potent and selective

IC₅₀ & Target 36 nM (HDAC1), 47 nM (HDAC2)

In Vitro

Cell Viabibibibibibibibibibiililiililililililllil tytytytytytytytytytytyy AAAAAAAAAAAAsssssssssssssssssssssssssayaaaaaaaa

CeCeCeCeCeeCeCeeCeellllllllllllllllllll LiLiLiLiLiLiLiLiLiLiL neneneneneeeeeeneeeneneeneneee:::::::::::::: Human NB cell ( SMS-KCNR, SKKKKKKKKKK-------NNNNNNNNNNNNN-BEBEBEBEBEBEBEBEBEBEBEE2,2,2,2,2,2,2,2,2,2,2, SSSSSSSSSSSSSH-SY5Y, SK-N-AS, L A1-15N,

SH-SHEP and IMR32 lines)

Preparation method The solubility of this compound in DMSO is >10 mM. General tips for obtaining

a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or

shake it in the ultrasonic bath for a while.Stock solution can be stored below

-20°C for several months.

Product Name: Romidepsin (FK228, depsipeptide)p ( , p p pRevision Date: 01/10/ 02020

etProduct Data Shee

Solvent &&&&& SSSSSSooooollllluuuuuuubbbbbbiiiiiiillllliiity

Biological Activity

2 | www.apexbt.com

Reacting conditions: 72h; IC50 ranged from 1–6.5 ng/ml

Applications: Romidepsin (0.5–30 ng/mL) resulted in a dose-dependent decrease in cell

viability of all NB cell lines as measured by the MTT or MTS assay. The

romidepsin IC50 ranged from 1–6.5 ng/ml in different NB cell lines.

Morphological examination by light microscopy revealed that all of the NB cell

lines treated with romidepsin had a dose-dependent decrease in cell number

and extensive change in morphology to rounded, denser and non-adherent

cells.

In Vivo

Animal experiment

Animal models: Normal and nude mice

Dosage form: 1.0-10kg/mL; i.v.; the tail injection

Applications: Clolon 38 and Colon 26 were implanted sc and M5076 and Meth A were

implanted id in mice on Day 0. When the drug were given beginning on Day 1.

romidepsin markedly inhibited the growth of Colon 38 and M5076, but not

Colon26 or Meth A. In addition, when the drug were given beginning on Day 4,

or on 7 or 8, romidepsin potently inhibited the growth of Colon 38, M5076 and

Meth A, and its activities against M5076 and Meth A were potent than when it

was given beginning on Day 1.

Other notes: Please test the solubility of all compounds indoor, and the actual solubility may

slightly differ with the theoretical value. This is caused by an experimental

system error and it is normal.

1. Kim SR, Lewis JM, et al. "BET inhibition in advanced cutaneous T cell lymphoma is synergistically potentiated by BCL2 inhibition or

HDAC inhibition." Oncotarget. 2018 Jun 26;9(49):29193-29207.PMID:30018745

2. Nakano Y, Kelly MC, et al. "Defects in the Alternative Splicing-Dependent Regulation of REST Cause Deafness." Cell. 2018 Jul

26;174(3):536-548.e21.PMID:29961578

3. Ho CF, Bon CP, et al. "Expression of DHA-Metabolizing Enzyme Alox15 is Regulated by Selective Histone Acetylation in

Neuroblastoma Cells." Neurochem Res. 2017 Dec 12.PMID:29235036

4. Tarasenko N, Chekroun-Setti H, et al. "COMPARISON OF THE ANTICANCER PROPERTIES OF A NOVEL VALPROIC ACID

PRODRUG TO LEADING HISTONE

DEACETYLASE INHIBITORS." J Cell Biochem. 2017 Nov 14.PMID:29135083

5. Bagnall NH, Hines BM, et al."Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia

cuprina." Int J Parasitol Drugs Drug Resist. 2017

Apr;7(1):51-60.PMID:28110187

See more customer validations on www.apexbt.com.

[1] Panicker J, Li Z, McMahon C, et al. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma

Product Citations

References

2 | www.apexbt.com

Reacting conditions: 72h; IC50 ranged from 1–6.5 ng/ml

Applications: Romidepsin (0.5–30 ng/mL) resulted in a dose-dependent decrease in cell

viability of all NB cell lines as measured by the MTT or MTS assay. The

romidepsin IC50 ranged from 1–6.5 ng/ml in different NB cell lines.

Morphological examination by light microscopy revealededededdedededededed that all of the NB cell

lines treated with romidepsin had a dose-dependdddddddddddeneneenenenenneneneee t ttttt ttttt dededededededededededecrcrcrcrcrcrcrcrcrcrcrrrccreaeeeeeeeeee se in cell number

and extensive change in morphology to rororoororoororoororounununununuunununununu dededdedeeeeededeeddededeeeeeeeedddd,dd,dddd,d,d,d,d,d,dd,d,d,d, dddddddddddddddenser and non-adherent

cells.

In Vivo

AAAAAAAAAnAAAAAA imal experiment

Animal models: Normal and nude mice

Dosage form: 1.0-10kg/mL; i.v.; the tail injection

Applications: Clolon 38 and Colon 26 were implanted sc and M5076 and Meth A were

implanted id in mice on Day 0. When the drug were given beginning on Day 1.

romidepsin markedly inhibited the growth of Colon 38 and M5076, but not

Colon26 or Meth A. In addition, when the drug were givenennenennenenene bbbbbbbbbbbegeeeeeeeee inning on Day 4,

or on 7 or 8, romidepsin potently inhibited the growowoooooooo thththththhhthththththttth ooooooooooof f ff f f fff fff CoCoCoCoCoCoCoCoCoCoCoCoololololololololololoon 38, M5076 and

Meth A, and its activities against M5076 aandndndnddndndndnddnd MMMMMMMMMMetetetetetetetetteetth h h h hh h hhhh AA A AA A AA A AAA A AAA wwwwewww re potent than when it

was given beginning on Day 1.

Other notes: Please test the solubility of all compounddddds indoor, and the actual solubility may

slightly differ with the theoretical value. This is caused by an experimental

system error and it is normal.

1. Kim SR, Lewis JM, et al. "BET inhnhnhnhnhhnhnhhnhnhn ibibibibibibibibbibibi ititititititittttioioioioioioioiooonnnnnn in advanced cutaneous T cell lymphoma is synergistically potttttttttenenenenenenenennenntititittititittittiatatatatatatataatatatedededededededededededdd bbbbbbbbbbbbbby BCL2 inhi r bition or

HDAC inhibition." Oncotarggetetetetetetetett. 200202020202000202020202022020018181818181818181818 JJJJJJJJJJJununununununuununununu 26;9(49):29193-29207.PMID:30018745

2. Nakano Y, Kelly MC,C,C,C,CC,CC,,, eeeeeeeeeeetttttttttt alalalalalalalaalaal.. "D"D"D"D"DDDDDD"D"D"DDDDD"DD"Deefefefeefefeeefe ects in the Alternative Splicing-Dependent Regulation ooooooooooff ff f f ff f f ff f f REREREREREREREREREEER STSTSTSTSTSTSTSTSSTSTT CCCCCCCCCCCCCCCCaaaauaaaaa se Deafness." Cell. 2018 Jul

26;174(3):536-548.8.8.8.8.8.8.8.8.8.88.88 e2e2e2e2e2e2e2e2e2e2e2e2ee2e 1.1.1.1.1.1.1.11111111 PMPMPMPMPMPMPMPMPMPMMMMIDIDIDIIIDIIDIDIDIDIDD:29961578

3. Ho CF, Bon CPCPCPCPCPCPCPCPCPCPCPCPPPCPP,,,,,,,,,,, eeeeeeeteeeee al. "Expression of DHA-Metabolizing Enzyme Alox15 is Regulated by Selective Histone Acetylation in

Neuroblastoma Cells." Neurochem Res. 2017 Dec 12.PMID:29235036

4. Tarasenko N, Chekroun-Setti H, et al. "COMPARISON OF THE ANTICANCER PROPERTIES OF A NOVEL VALPROIC ACID

PRODRUG TO LEADING HISTONE

DEACETYLASE INHIBITORS." J Cell Biochem. 2017 Nov 14.PMID:29135083

5. Bagnall NH, Hines BM, et al."Insecticidal activities of histone deacetylase inhibitors against a dipteraan n nnnnn n nnnn papapapapapapapapapapp rararrarararararaarasisisiiisississ te of sheep, Lucilia

cuprina." Int J Parasitol Drugs Drugugggggggggg RRRRRRRRRRReseseseseseseseesese ist. 2017

AApr;7(1):51-60.PMID:28110111187878777787788

See more customeeeeeeeer r r r r rrrrrrr vavavavavavavavavavavaliliilililililililidadadadaadadadadadadadadaddadaddaddd tititititititititttitititt ons on www.apexbt.com.

[1] Panicker J, Li Z, McMahon C, et al. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma

Product Citations

References

3 | www.apexbt.com

tumor cells[J]. Cell Cycle, 2010, 9(9): 1830-1838.

[2] Ueda H1, Manda T, Matsumoto S, Mukumoto S, Nishigaki F, Kawamura I, Shimomura K. FR901228, a novel antitumor bicyclic

depsipeptide produced by Chromobacterium violaceum No. 968. III. Antitumor activities on experimental tumors in mice. J Antibiot

(Tokyo). 1994 Mar;47(3):315-23.

FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.Specific storage and handling information for each product is indicated on the product datasheet. Most APExBIO products are stable

under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage

temperature. Shortterm storage of many products are stable in the short-term at temperatures that differ from that required for

long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt

of the product, follow the storage recommendations on the product data sheet.

APExBIO Technologywww.apexbt.com

7505 Fannin street, Suite 410, Houston, TX 77054. Tel: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: info@apexbt.com

Caution

3 | www.apexbt.com

tumor cells[J]. Cell Cycle, 2010, 9(9): 1830-1838.

[2] Ueda H1, Manda T, Matsumoto S, Mukumoto S, Nishigaki F, Kawamura I, Shimomura K. FR901228, a novel antitumor bicyclic

depsipeptide produced by Chromobacterium violaceum No. 968. III. Antitumor activities on experimental tumors in mice. J Antibiot

(Tokyo). 1994 Mar;47(3):315-23.

FOR RESEARCH PURPRPPPPPPPPPPOSOSOSOSOSOSOSOSOSOSO ESESESESESESESESESESESSS OOOOOOOOOOOONLN Y.NOT FOR HUMAN,NN,N,,N,NNNNN,, VVVVVVVVVVVVVETETETETETETETETETTEETTETE EREREREREREREREREREREERERERINI ARY DIAGNOSTIC OR THERAPEUTTIC USE.Specific storage and hhhhhhandling information for each product is indicatted on the product datasheet. Most APExBEE IO ble products are stab

under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storageed at a temperature that differs from the recommended storag

temperature. Shortterm storage of many products are stable in the sshort-term at temperatures that differ from that required for

long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt e

of the product, follow the storage recommendations on the product ddata sheet.

APExBIO Teechnologywww.apexbt.comxbt com

7505 Fannin street, Suite 410, Houston, TX 77054.Tel: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: info@apexbt.com

Caution