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Pracinostat selectively inhibits HDAC class I, II, IV without class III and HDAC6 in class IIb, but has no effect on other Zn-binding enzymes, receptors, and ion channels. It accumulates in tumor cells and exerts a continuous inhibition to histone deacetylase, resulting in acetylated histones
574:
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Clinical studies suggests that pracinostat has potential best pharmacokinetic properties when compared to other oral HDAC inhibitors. In March 2014, pracinostat has granted
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465:"The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML"
834:
560:
514:"SB939, a Novel Potent and Orally Active Histone Deacetylase Inhibitor with High Tumor Exposure and Efficacy in Mouse Models of Colorectal Cancer"
250:
InChI=1S/C20H30N4O2/c1-4-7-8-19-21-17-15-16(10-12-20(25)22-26)9-11-18(17)24(19)14-13-23(5-2)6-3/h9-12,15,26H,4-8,13-14H2,1-3H3,(H,22,25)/b12-10+
463:
Novotny-Diermayr, V.; Hart, S.; Goh, K. C.; Cheong, A.; Ong, L-C; Hentze, H.; Pasha, M. K.; Jayaraman, R.; Ethirajulu, K.; Wood, J. M. (2012).
260:
InChI=1/C20H30N4O2/c1-4-7-8-19-21-17-15-16(10-12-20(25)22-26)9-11-18(17)24(19)14-13-23(5-2)6-3/h9-12,15,26H,4-8,13-14H2,1-3H3,(H,22,25)/b12-10+
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with potential anti-tumor activity characterized by favorable physicochemical, pharmaceutical, and pharmacokinetic properties.
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Except where otherwise noted, data are given for materials in their
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Veronica
Novotny-Diermayr; et al. (March 9, 2010).
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accumulation, chromatin remodeling, tumor suppressor
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284:CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)/C=C/C(=O)NO
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8:
450:"In vitro enzyme activity of SB939 and SAHA"
383:) is an orally bioavailable, small-molecule
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600:β-Hydroxybutyric acid (β-hydroxybutyrate)
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253:Key: JHDKZFFAIZKUCU-ZRDIBKRKSA-N
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7:
385:histone deacetylase (HDAC) inhibitor
263:Key: JHDKZFFAIZKUCU-ZRDIBKRKBK
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14:
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22:
610:Acetoacetic acid (acetoacetate)
424:(AML) and for the treatment of
361:(at 25 °C , 100 kPa).
835:Histone deacetylase inhibitors
584:Histone deacetylase inhibitors
323:
305:
1:
815:Receptor/signaling modulators
531:10.1158/1535-7163.MCT-09-0689
430:Food and Drug Administration
740:Sodium oxybate (GHB sodium)
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780:Valproic acid (valproate)
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422:acute myelocytic leukemia
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49:-1,3-benzimidazol-5-yl}-
630:Butyric acid (butyrate)
850:Diethylamino compounds
53:-hydroxyprop-2-enamide
745:Sodium phenylbutyrate
595:3,3'-Diindolylmethane
790:Valproate semisodium
469:Blood Cancer Journal
37:Preferred IUPAC name
481:10.1038/bcj.2012.14
412:Clinical medication
402:genes transcription
341: g·mol
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404:, and ultimately,
365:Infobox references
16:
822:
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800:Vorinostat (SAHA)
785:Valproate pivoxil
670:Indole-3-carbinol
650:Diallyl disulfide
373:Chemical compound
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206:CompTox Dashboard
109:Interactive image
45:)-3-{2-Butyl-1--1
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845:Hydroxamic acids
750:Sodium valproate
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524:(3): 642–652.
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452:. 22 Aug 2014.
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811:
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775:Valnoctamide
770:Tucidinostat
755:Sulforaphane
709:
700:Parthenolide
695:Panobinostat
685:Mocetinostat
660:Fimepinostat
640:Citarinostat
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68:Identifiers
60:Other names
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46:
42:
17:Pracinostat
720:Resminostat
715:Quisinostat
710:Pracinostat
690:Niacinamide
680:Martinostat
605:Abexinostat
475:(5): e69–.
418:Orphan Drug
377:Pracinostat
293:Properties
129:CHEBI:95071
85:929016-96-6
62:Pracinostat
829:Categories
795:Valpromide
760:Trapoxin B
725:Romidepsin
665:Givinostat
655:Entinostat
625:Belinostat
436:References
334:Molar mass
194:GPO2JN4UON
140:ChemSpider
96:3D model (
75:CAS Number
812:See also:
730:Scriptaid
635:Capsaicin
406:apoptosis
387:based on
675:Kevetrin
645:Curcumin
620:Apicidin
540:20197387
499:22829971
395:Activity
174:49855250
149:25027185
490:3366067
428:by the
347:Density
339:358.486
161:PubChem
538:
497:
487:
277:SMILES
31:Names
381:SB939
242:InChI
120:ChEBI
98:JSmol
536:PMID
495:PMID
420:for
185:UNII
526:doi
485:PMC
477:doi
211:EPA
164:CID
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379:(
327:2
324:O
321:4
318:N
312:H
306:C
213:)
209:(
100:)
51:N
47:H
43:E
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