1233533-04-4

1233533-04-4 structure

Name: kb-NB142-70
Chemical Name: 3,4-Dihydro-9-hydroxy-[1]benzothieno[2,3-f]-1,4-thiazepin-5(2H)-one
CAS Number: 1233533-04-4
Molecular Formula: C₁₁H₉NO₂S₂
Molecular Weight: 251.325
Catalog: Signaling Pathways Apoptosis PKD
Create Date: 2017-10-16 15:12:16
Modify Date: 2025-08-21 20:10:49
kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.

Name	3,4-Dihydro-9-hydroxy-[1]benzothieno[2,3-f]-1,4-thiazepin-5(2H)-one
Synonyms	[1]Benzothieno[2,3-f]-1,4-thiazepin-5(2H)-one, 3,4-dihydro-9-hydroxy- 9-Hydroxy-3,4-dihydro[1]benzothieno[2,3-f][1,4]thiazepin-5(2H)-one 9-hydroxy-3,4-dihydro-2H-[1]benzothiolo[2,3-f][1,4]thiazepin-5-one kb NB 142-70

Description	kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.
Related Catalog	Signaling Pathways >> Apoptosis >> PKD Research Areas >> Cancer
Target	PKD1:28.3 nM (IC50) PKD3:53.2 nM (IC50) PKD2:58.7 nM (IC50)
In Vitro	kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also inhibits Ser916 phosphorylation of PKD1 (IC50, 2.2 ± 0.6 μM) in LNCaP cells. Moreover, kb NB 142-70 is cytotoxic against PC3 cells with an EC50 of 8.025 μM[1]. kb NB 142-70 (0-5 μM) concentration-dependently prevents ANG II-induced phosphorylation of HDAC4 at Ser246 and Ser632, HDAC5 at Ser259 and Ser498, and HDAC7 at Ser155 in IEC-18 cells. In addition, kb NB 142-70 (3.5 μM) also suppresses HDAC4, HDAC5, and HDAC7 phosphorylation in IEC-18 cells stimulated with ANG II for 0-240 min or with vasopressin, lysophosphatidic acid (LPA), or phorbol 12,13-dibutyrate (PDBu)[2].
Cell Assay	Briefly, PC3 cells are treated with kb NB 142-70 at 10 μM concentration for 48 h, and then fixed in 70% ice-cold ethanol overnight and labeled with propidium iodide. The labeled cells are analyzed using a FACScan Benchtop Cytometer[1].
References	[1]. Lavalle CR, et al. Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility. BMC Chem Biol. 2010 May 5;10:5. [2]. James Sinnett-Smith, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15; 306(10): C961-C971.

Density	1.5±0.1 g/cm3
Boiling Point	601.9±55.0 °C at 760 mmHg
Molecular Formula	C₁₁H₉NO₂S₂
Molecular Weight	251.325
Flash Point	317.8±31.5 °C
Exact Mass	251.007462
PSA	106.36000
LogP	2.39
Appearance	white solid
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.746
Storage condition	-20℃

RIDADR	NONH for all modes of transport

1259977-97-3

~94%

1233533-04-4

Literature: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION; WIPF, Peter; WANG, Qiming, Jan Patent: WO2012/78859 A2, 2012 ; Location in patent: Page/Page column 50-51 ;

1259977-93-9

1233533-04-4

Literature: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION; WIPF, Peter; WANG, Qiming, Jan Patent: WO2012/78859 A2, 2012 ;

122024-71-9

1233533-04-4

Literature: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION; WIPF, Peter; WANG, Qiming, Jan Patent: WO2012/78859 A2, 2012 ;

122024-75-3

1233533-04-4

Literature: Bravo-Altamirano, Karla; George, Kara M.; Frantz, Marie-Celine; Lavalle, Courtney R.; Tandon, Manuj; Leimgruber, Stephanie; Sharlow, Elizabeth R.; Lazo, John S.; Wang, Q. Jane; Wipf, Peter ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 2 p. 154 - 159

14755-02-3

1233533-04-4

Precursor 4
1259977-93-9 122024-71-9 122024-75-3 14755-02-3
DownStream 0

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