Product Name:Tubastatin A HCl Revision Date: 01/10/2020 ... · 1 | Tubastatin A HCl Cat. No.: A8547...

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1 | www.apexbt.com Tubastatin A HCl Cat. No.: A8547 CAS No.: 1310693-92-5 Formula: C20H21N3O2·HCl M.Wt: 371.86 Synonyms: TSA HCl;Tubastatin A hydrochloride Target: DNA Damage/DNA Repair Pathway: HDAC Storage: Store at -20°C In Vitro ı18.6mg/mL in DMSO Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 2.6892 mL 13.4459 mL 26.8918 mL 5 mM 0.5378 mL 2.6892 mL 5.3784 mL 10 mM 0.2689 mL 1.3446 mL 2.6892 mL Please refer to the solubility information to select the appropriate solvent. Shortsummary HDAC6 inhibitor,potent and selective IC₅₀ & Target 15 nM (HDAC6), 854 nM (HDAC8) In Vitro Cell Viability Assay Cell Line: HaCaT cells Preparation method˖ The solubility of this compound in DMSO is > 18.6 mg/mL. 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. Reacting conditions: 10 μM; 10 hrs Applications: In HaCaT cells, Tubastatin A HCl selectively inhibited HDAC6, preventing Product Name: Tubastatin A HCl Revision Date: 01/10/2020 Product Data Sheet Solvent & Solubility Biological Activity 1 | www.apexbt.com T ubastatin A HC C C C C C C C C C C Cl l l l l l l l l l l Cat. No.: A854 4 4 4 4 4 4 4 4 7 7 7 7 7 7 7 7 7 7 7 CAS No.: 13 13 3 3 13 3 3 3 13 13 13 13 1 13 13 3 13 1310 10 10 10 10 10 10 10 10 069 69 69 69 69 69 69 69 69 69 9 69 93 3 3 3 3 3 3 3 3 3 3 3 3 - 92 - 5 Formula: C2 C C2 C2 C2 C2 C C C2 C2 C2 C2 C2 C C20H21N3O2·HCl M.Wt: 371.86 Synonyms: TSA HCl;Tubastatin A hydroch hloride T arget: DNA Damage/DNA Repair Pathway: HDAC Storage: Store at - 20°C In Vitro ı ı ı ı ı ı ı ı ı ı ı ı ı ı ı 18.6mg/mL in DMSO Preparing Stock Solutions Mass 1mg 5mg 10mg Solvent Concentration 1 mM 2.6892 mL 13.4459 mL 26.8918 mL 5 mM 0.5378 mL 2.6892 mL 5.3784 mL 1 0 mM 0.2689 mL 1.34 4 4 4 4 4 4 4 4 446 46 46 46 46 46 46 6 46 46 46 46 4 m m m m m m m m m m mL L L L L L L L L L 2.6892 mL Plea a a a a a a a ase se s se se se se se se e e se e e e e r r r r r r r r r ref ef ef ef ef ef ef ef f e e e e ef e ef e er er er er er er er er er er t t t t t t t t t t to o o o o o o o o o o t t th t t t e solubility information to select the appropriate solvent nt nt t nt t t t nt t. Shortsummary HDAC6 inhibitor,potent and selective IC ₅₀ & Target 15 nM (HDAC6), 854 nM (HDAC8) In Vitro Cell Viability Assay Cell Line: e: e: e: e: e: e: e e e HaCaT cells Pr Pr Pr Pr r Pr Pr Pr Pr Pr P P ep ep ep ep ep ep e ep ep ep ep epar ar a ar ar ar ar ar ar a at at a at at t t t at at t t t at a at t t at ati i i i i io io io i i io io io io io io io o o o o ion n n n n n n n n n n n n method ˖ The solubility of this compound in D D D D D D D D D D D D D D D D DMS MS S S MS S S S MS MS MS MS MS MS MS MS MS MSO O O O O O O O O O O O is is is is is is is is is is is is s > > 18.6 mg/mL. General tips for obtaining a higher concentration: Pl P Pl Pl Pl Pl P Pl Pl Pl Pl P P ea ea ea ea ea ea ea ea ea a ea a ea ea ea ase se se se se se se s se se se se se s 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. Reacting conditions: 10 μM; 10 hrs Applications: In HaCaT cells, Tubastatin A HCl selectively inhibited HDAC6, preventing Product Name : Tubastatin A HCl Revision Date: 0 1 / 1 0 / 0 20 20 et Product Data Shee Solvent & Solu u u u u ub b b b b bi i i i i il l l l l l l l li i i it t t t t t t ty y y y y y y y y y Biologica a a al l l l l l A A A A A A Activity

Transcript of Product Name:Tubastatin A HCl Revision Date: 01/10/2020 ... · 1 | Tubastatin A HCl Cat. No.: A8547...

  • 1 | www.apexbt.com

    Tubastatin A HClCat. No.: A8547

    CAS No.: 1310693-92-5

    Formula: C20H21N3O2·HCl

    M.Wt: 371.86

    Synonyms: TSA HCl;Tubastatin A hydrochloride

    Target: DNA Damage/DNA Repair

    Pathway: HDAC

    Storage: Store at -20°C

    In Vitro

    18.6mg/mL in DMSO

    Preparing

    Stock Solutions

    Mass

    1mg 5mg 10mgSolvent

    Concentration

    1 mM 2.6892 mL 13.4459 mL 26.8918 mL

    5 mM 0.5378 mL 2.6892 mL 5.3784 mL

    10 mM 0.2689 mL 1.3446 mL 2.6892 mL

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

    Shortsummary HDAC6 inhibitor,potent and selective

    IC₅₀ & Target 15 nM (HDAC6), 854 nM (HDAC8)

    In Vitro

    Cell Viability Assay

    Cell Line: HaCaT cells

    Preparation method The solubility of this compound in DMSO is > 18.6 mg/mL. 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.

    Reacting conditions: 10 μM; 10 hrs

    Applications: In HaCaT cells, Tubastatin A HCl selectively inhibited HDAC6, preventing

    Product Name: Tubastatin A HClRevision Date: 01/10/2020

    Product Data Sheet

    Solvent & Solubility

    Biological Activity

    1 | www.apexbt.com

    Tubastatin A HCCCCCCCCCCCClllllllllllCat. No.: A85444444444477777777777

    CAS No.: 13133313333131313131131331313101010101010101010069696969669696969696996993333333333333-92-5

    Formula: C2CC2C2C2C2CCC2C2C2C2C2CC20H21N3O2·HCl

    M.Wt: 371.86

    Synonyms: TSA HCl;Tubastatin A hydrochhloride

    Target: DNA Damage/DNA Repair

    Pathway: HDAC

    Storage: Store at -20°C

    In Vitro

    18.6mg/mL in DMSO

    Preparing

    Stock Solutions

    Mass

    1mg 5mg 10mgSolvent

    Concentration

    1 mM 2.6892 mL 13.4459 mL 26.8918 mL

    5 mM 0.5378 mL 2.6892 mL 5.3784 mL

    10 mM 0.2689 mL 1.34444444444464646464646466464646464 mmmmmmmmmmmLLLLLLLLLL 2.6892 mL

    Pleaaaaaaaaasesesseseseseseseeeseeeeese rrrrrrrrrrefefefefefefefeffeeeeefeefe erererererererererer ttttttttttto oooooooooo ttthttt e solubility information to select the appropriate solventntnttnttttntt.

    Shortsummary HDAC6 inhibitor,potent and selective

    IC₅₀ & Target 15 nM (HDAC6), 854 nM (HDAC8)

    In Vitro

    Cell Viability Assay

    Cell Line:e:e:e:e:e:e:eee HaCaT cells

    PrPrPrPrrPrPrPrPrPrPP epepepepepepeepepepepepararaarararararara atataatattttatattttataatttatatiiiiiioioioiiioioioioioioioooooionnn n nnn nnnnnn method The solubility of this compound in DDDDDDDDDDDDDDDDDMSMSSSMSSSSMSMSMSMSMSMSMSMSMSMSO O O O OO O OOOOO isisisisisisisisisisisiss >> 18.6 mg/mL. General tips for

    obtaining a higher concentration: PlPPlPlPlPlPPlPlPlPlPP eaeaeaeaeaeaeaeaeaaeaaeaeaeaasesesesesesesesseseseseses 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.

    Reacting conditions: 10 μM; 10 hrs

    Applications: In HaCaT cells, Tubastatin A HCl selectively inhibited HDAC6, preventing

    Product Name: Tubastatin A HClRevision Date: 01/10/ 02020

    etProduct Data Shee

    Solvent & Soluuuuuubbbbbbiiiiiillllllllliiiittttttttyyyyyyyyyy

    Biologicaaaallllll AAAAAAActivity

  • 2 | www.apexbt.com

    sodium arsenite-induced association of Nrf2 mRNA with ribosomes and

    elevation of Nrf2 protein.

    In Vivo

    Animal experiment

    Animal models: B6/Rag1-/- mice adoptively transferred with 1 × 106 WT CD4+ CD45RBhi cells

    Dosage form: 25 mg/kg; i.p.; q.d., for 14 days

    Applications: Adoptively transferred B6/Rag1-/- mice which were treated with Tubastatin A

    HCl recovered body weights and normal stool formation. In addition, the

    histologic examination showed reduced mononuclear cell infiltration,

    preservation of goblet cells, as well as intact mucosal surfaces.

    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.

    See more customer validations on www.apexbt.com.

    [1]. Kyle V. Butler, Jay Kalin, Camille Brochier, et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6

    Inhibitor, Tubastatin A [J]. J. Am. Chem. Soc., 2010, 132 (31), pp 10842–10846.

    [2]. Kappeler KV, Zhang J, Dinh TN, et al. Histone deacetylase 6 associates with ribosomes and regulates de novo protein translation

    during arsenite stress [J]. Toxicol Sci. 2012 May;127(1):246-255.

    [3]. de Zoeten EF, Wang L, Butler K, Beier UH, Akimova T, Sai H, Bradner JE, Mazitschek R, Kozikowski AP, Matthias P, Hancock

    WW. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011

    May;31(10):2066-78.

    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.

    Product Citations

    References

    Caution

    2 | www.apeexbt.commmmmmmmmmmmmmm

    sodium arsenite-induced association of Nrf2 mRNA with ribosomes and

    elevation of Nrf2 protein.

    In Vivo

    Animal experiment

    Animal models: B6/Rag1-/- mice adoptively transferred with 1 × 106 WT CD4+ CD45RBhi cells

    Dosage form: 25 mg/kg; i.p.; q.d., for 14 days

    Applicationsnsnsnssnsnsssnsnsnsnsns::::::: Adoptively transferred B6/Rag1-/- mice which werererererererererereeeeeee eee e eee eee trtrtrtrtrtrtrtrtrttt eaeaeaeaeaeaeaeaeaeaeaaateteteteteteteteteteeeted with Tubastatin A

    HCl recovered body weights and normamamamamamamamamaaal llllllll ststststststststststooooooooooooooooooooolll lllll l l l ll ll fofofofofofofffofofof rmation. In addition, the

    histologic examination showed rererererererererereererereduduuuduuuuudddududduddudddd cececececececececececeedddddddddddddd mononuclear cell infiltration,

    preservation of goblet cells, as well asasasasasasasasasasasssaa iiiiiintact mucosal surfaces.

    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.

    See more cusssssssssssstototototototototototototototomememememememememememeeeememmeeemeem rr rrrrrrrr validations on www.apexbt.com.

    [1]. Kyle V. Butler, Jay Kalin, Camille Brochier, et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6

    Inhibitor, Tubastatin A [J]. J. Am. Chem. Soc., 2010, 132 (31), pp 10842–10846.

    [2]. Kappeler KV, Zhang J, Dinh TN, et al. Histone deacetylase 6 associates with ribosomes and regulates deeeeeee nnnnnnnnnnovoooooooo o protein translation

    during arsenite stress [J]. Toxicol SccScccccccS i.i.ii.i.i.i.. 22222222222201000000000 2 May;127(1):246-255.

    [3]. de Zoeten EF, Wang L, Butttttttttttlelelelelelelelellell r r rr rr rrr K,K,K,K,K,K,K,K,K,K,KKK BBBBBBBBBBBBeieieieieieieieieieeie er UH, Akimova T, Sai H, Bradner JE, Mazitschek R, KKKKKKozozozozozozozozozoooozikikikikikikikikkikowowowowowowowowowoowowooowwwooo ssssssssssssssssssskikikikikikikikikkikikk AAAAAAAAAAAAP, Matthias P, Hancock

    WW. Histone deacetylasassssssasasaseeeeeeeeeee 6 6666666666 anannnnanaananaananannnnnannannnnndddddddddddddddddd hhhehhhhhhh at shock protein 90 control the functions of Foxp3(+) )))))))) TTTTTTTTTTT---rerererererererereeeguguguguguguguguguguug lalalalalalalalaalaalalaallatototototototototototot ry cells. Mol Cell Biol. 2011

    May;31(10):2066-7878787878878787878787888.......

    FOR RESEARCH PURPOSES ONLY.NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTTIC USE.Specific storage and handling informmmmmmmatatatatatatatatttaaata ioioioioioioioioioooon for each product is indicatted on the product datasheet. Mooostss AAAAAAAAAAAAAAAAAAAAAAAAPEPEPEPEPEPEPEPEPEEPEPEP xBxBxBxBxBxBxBBxBxBBxBBEEEEEEEEEE IOIOIOIOOIOIOIOIOOIOIOIOOIO ble products are stab

    under the recommended conditttttttttttioioioioioioioioioioioioonsnsnsnsnsnsnsnsnsnsnn ...... PrPrPrPrPrPrPrPrPrPrPrPrPrrrododododododododododdodooooo ucts are sometimes shipped at a temperature that dif e recommended storageed at a temperature that diffefefefefefefefeefeffersrsrrsrsrsrsrsrsrsrs fffffffffrororororooroorororoom m m m mmmmm mmmmmmm mmmm mm mmmm thththththththththhththththhe recommended storag

    temperature. Shortterm sssssssssstoototototototototototorararararararararraragegegegegegeeeeegegeegegeeegegeeeeeeeee ooooooooooooooooooof fffff f fffffff mammmm ny products are stable in the sshort-term at temperatatatatatatatturururururururuuuuuruuurresssssesseseessesseseeeeesese ttttttttttthahahahahahahahahahahahah t t t ttttttttttt didididdididddiddid ffer from that required for

    long-term storageee..... WeeeeeeeeWWWWWWWWWeWW eeeeeeeeeensnsnsnsnsnsnsnssnsnsnsurururururururururururuuru eee eeeeeeee that the product is shipped under conditions that will maintttttttttttttaiaiaiaiaiaiaiaiaiiaiaiaaaaaa nn n n nnnnnnnnnnnnn thththththththththhttthththhthe quality of the reagents. Upon receipt e

    of the product, foooooolllllllllllllllllllllllllll owowowowowowowowowowowowwowwowwow tttttttttttttttthhehehehehehehehehehhehehhhhhhh storage recommendations on the product ddata sheet.

    Product Citations

    References

    Caution

  • 3 | www.apexbt.com

    APExBIO Technologywww.apexbt.com

    7505 Fannin street, Suite 410, Houston, TX 77054. Tel: +1-832-696-8203 | Fax: +1-832-641-3177 | Email: [email protected]

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    APExBIO Technologywww.apexbt.com

    7575757575775757575757505 Fannin street, Suite 410, Houston, TX 77054.Tel: ++++++++++++111111111111-------83838383838383838383838888 2222222222222--------69696969696969696969696969996696 66666666-8203 | Fax: +1-832-641-3177 | Email: [email protected]