MedKoo Cat#: 522382 | Name: kb NB 142-70
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

kb NB 142-70 is a selective protein kinase D (PKD) inhibitor with IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively. kb NB 142-70 prevents wound-induced migration of intestinal epithelial cells. PKD1, the most studied member of the PKD family, is implicated in the regulation of a remarkable array of fundamental biological processes, including signal transduction, cell proliferation and differentiation, membrane trafficking, hormone secretion, immune regulation, cardiac hypertrophy, angiogenesis, and cancer.

Chemical Structure

kb NB 142-70
kb NB 142-70
CAS#1233533-04-4

Theoretical Analysis

MedKoo Cat#: 522382

Name: kb NB 142-70

CAS#: 1233533-04-4

Chemical Formula: C11H9NO2S2

Exact Mass: 251.0075

Molecular Weight: 251.32

Elemental Analysis: C, 52.57; H, 3.61; N, 5.57; O, 12.73; S, 25.51

Price and Availability

Size Price Availability Quantity
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
No Data
Synonym
kb NB 142-70; kb NB142-70; kb NB-142-70.
IUPAC/Chemical Name
9-hydroxy-3,4-dihydrobenzo[4,5]thieno[2,3-f][1,4]thiazepin-5(2H)-one
InChi Key
DHUAGGSHTKPOHU-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H9NO2S2/c13-6-1-2-8-7(5-6)9-10(16-8)11(14)12-3-4-15-9/h1-2,5,13H,3-4H2,(H,12,14)
SMILES Code
O=C1NCCSC2=C1SC3=CC=C(O)C=C32
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
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.
In vitro activity:
Treatment with the PKD family inhibitors kb NB 142-70 and CRT0066101 or small interfering RNA-mediated knockdown of PKD1 prevented ANG II-induced phosphorylation of HDAC4, HDAC5, and HDAC7. Reference: Am J Physiol Cell Physiol. 2014 May 15;306(10):C961-71. https://pubmed.ncbi.nlm.nih.gov/24647541/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 30.0 119.37
DMSO 33.9 135.02
DMSO:PBS (pH 7.2) (1:1) 0.5 1.99
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 251.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Sinnett-Smith J, Ni Y, Wang J, Ming M, Young SH, Rozengurt E. 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):C961-71. doi: 10.1152/ajpcell.00048.2014. Epub 2014 Mar 19. PMID: 24647541; PMCID: PMC4024715. 2. Ni Y, Sinnett-Smith J, Young SH, Rozengurt E. PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS One. 2013 Sep 9;8(9):e73149. doi: 10.1371/journal.pone.0073149. Erratum in: PLoS One. 2014;9(1). doi:10.1371/annotation/70d3c7b0-9718-4bb1-abed-d0defc3b7fc4. PMID: 24039875; PMCID: PMC3767810.
In vitro protocol:
1. Sinnett-Smith J, Ni Y, Wang J, Ming M, Young SH, Rozengurt E. 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):C961-71. doi: 10.1152/ajpcell.00048.2014. Epub 2014 Mar 19. PMID: 24647541; PMCID: PMC4024715. 2. Ni Y, Sinnett-Smith J, Young SH, Rozengurt E. PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS One. 2013 Sep 9;8(9):e73149. doi: 10.1371/journal.pone.0073149. Erratum in: PLoS One. 2014;9(1). doi:10.1371/annotation/70d3c7b0-9718-4bb1-abed-d0defc3b7fc4. PMID: 24039875; PMCID: PMC3767810.
In vivo protocol:
TBD
1: Ni Y, Wang L, Zhang J, Pang Z, Liu Q, Du J. PKD1 is downregulated in non-small cell lung cancer and mediates the feedback inhibition of mTORC1-S6K1 axis in response to phorbol ester. Int J Biochem Cell Biol. 2015 Mar;60:34-42. doi: 10.1016/j.biocel.2014.12.018. Epub 2015 Jan 9. PubMed PMID: 25578563. 2: Sinnett-Smith J, Ni Y, Wang J, Ming M, Young SH, Rozengurt E. 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):C961-71. doi: 10.1152/ajpcell.00048.2014. Epub 2014 Mar 19. PubMed PMID: 24647541; PubMed Central PMCID: PMC4024715. 3: Ni Y, Sinnett-Smith J, Young SH, Rozengurt E. PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS One. 2013 Sep 9;8(9):e73149. doi: 10.1371/journal.pone.0073149. eCollection 2013. Erratum in: PLoS One. 2014;9(1). doi:10.1371/annotation/70d3c7b0-9718-4bb1-abed-d0defc3b7fc4. PubMed PMID: 24039875; PubMed Central PMCID: PMC3767810. 4: Young SH, Rozengurt N, Sinnett-Smith J, Rozengurt E. Rapid protein kinase D1 signaling promotes migration of intestinal epithelial cells. Am J Physiol Gastrointest Liver Physiol. 2012 Aug 1;303(3):G356-66. doi: 10.1152/ajpgi.00025.2012. Epub 2012 May 17. PubMed PMID: 22595992; PubMed Central PMCID: PMC3423107.