NSC117079 | CAS# 500363-63-3 | pan-PHLPP inhibitor

MedKoo Cat#: 574816 | Name: NSC117079

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Description:

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

NSC117079 is a pan-PHLPP inhibitor selective for PHLPP1 and PHLPP2.

Chemical Structure

NSC117079

CAS#500363-63-3

Theoretical Analysis

MedKoo Cat#: 574816

Name: NSC117079

CAS#: 500363-63-3

Chemical Formula: C20H15N3O7S2

Exact Mass: 473.0351

Molecular Weight: 473.47

Elemental Analysis: C, 50.74; H, 3.19; N, 8.88; O, 23.65; S, 13.54

Price and Availability

Size	Price	Availability
5mg	USD 295.00	2 Weeks
10mg	USD 485.00	2 Weeks
25mg	USD 865.00	2 Weeks
50mg	USD 1,305.00	2 Weeks
100mg	USD 2,015.00	2 Weeks

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Related CAS #

No Data

Synonym

NSC-117079; NSC 117079; NSC117079

IUPAC/Chemical Name

1-Amino-9,10-dioxo-4-(3-sulfamoylanilino)anthracene-2-sulfonic acid

InChi Key

LHSBZAWDPSTOEY-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H15N3O7S2/c21-18-15(32(28,29)30)9-14(23-10-4-3-5-11(8-10)31(22,26)27)16-17(18)20(25)13-7-2-1-6-12(13)19(16)24/h1-9,23H,21H2,(H2,22,26,27)(H,28,29,30)

SMILES Code

O=S(C(C(N)=C1C2=O)=CC(NC3=CC=CC(S(=O)(N)=O)=C3)=C1C(C4=C2C=CC=C4)=O)(O)=O

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

Shelf Life

>3 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

Product Data

Instruction

View handling instruction

Biological target:

NSC117079 is a novel PHLPP inhibitor.

In vitro activity:

The Phlpp inhibitors NSC 117079 and NSC 45586 were highly stable in vitro and stimulated GAG, Sox9, proteoglycan 4 and collagen 2 production in maturing but not more differentiated chondrocytes in vitro. Both molecules reduced Phlpp1/2 levels and suppressed matrix degradation to functionally extend their inhibitory effect on these phosphatases. Reference: Osteoarthr Cartil Open. 2021 Jun 8;3(3):100190. https://pubmed.ncbi.nlm.nih.gov/36474816/

In vivo activity:

A single intra-articular injection of the Phlpp inhibitor NSC117079 attenuated mechanical allodynia and slowed articular cartilage degradation in joints with a destabilized meniscus. Mice treated with the Phlpp inhibitor 7 weeks after injury maintained normal activity levels, while those in the control group traveled shorter distances and were less active 3 months after the joint injury. NSC117079 also increased production of cartilage extracellular matrix components (glycosaminoglycans and aggrecan) in over 90% of human articular cartilage explants from OA patients and increased phosphorylation of Phlpp1 substrates (AKT2, ERK1/2, and PKC) in human articular chondrocytes. Reference: J Orthop Res. 2018 May;36(5):1487-1497. https://pubmed.ncbi.nlm.nih.gov/29068480/

	Solvent	mg/mL	mM
Solubility
	DMSO	50.0	105.60

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 473.47 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.

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. Taylor EL, Weaver SR, Zars EL, Turner CA, Buhrow SA, Reid JM, Bradley EW, Westendorf JJ. Chondrocytic and pharmacokinetic properties of Phlpp inhibitors. Osteoarthr Cartil Open. 2021 Jun 8;3(3):100190. doi: 10.1016/j.ocarto.2021.100190. PMID: 36474816; PMCID: PMC9718091. 2. Jackson TC, Verrier JD, Drabek T, Janesko-Feldman K, Gillespie DG, Uray T, Dezfulian C, Clark RS, Bayir H, Jackson EK, Kochanek PM. Pharmacological inhibition of pleckstrin homology domain leucine-rich repeat protein phosphatase is neuroprotective: differential effects on astrocytes. J Pharmacol Exp Ther. 2013 Nov;347(2):516-28. doi: 10.1124/jpet.113.206888. Epub 2013 Sep 10. PMID: 24023368; PMCID: PMC3807060. 3. Hwang SM, Feigenson M, Begun DL, Shull LC, Culley KL, Otero M, Goldring MB, Ta LE, Kakar S, Bradley EW, Westendorf JJ. Phlpp inhibitors block pain and cartilage degradation associated with osteoarthritis. J Orthop Res. 2018 May;36(5):1487-1497. doi: 10.1002/jor.23781. Epub 2017 Nov 28. PMID: 29068480; PMCID: PMC5985222.

In vitro protocol:

In vivo protocol:

1. Hwang SM, Feigenson M, Begun DL, Shull LC, Culley KL, Otero M, Goldring MB, Ta LE, Kakar S, Bradley EW, Westendorf JJ. Phlpp inhibitors block pain and cartilage degradation associated with osteoarthritis. J Orthop Res. 2018 May;36(5):1487-1497. doi: 10.1002/jor.23781. Epub 2017 Nov 28. PMID: 29068480; PMCID: PMC5985222. 2. Jackson TC, Verrier JD, Drabek T, Janesko-Feldman K, Gillespie DG, Uray T, Dezfulian C, Clark RS, Bayir H, Jackson EK, Kochanek PM. Pharmacological inhibition of pleckstrin homology domain leucine-rich repeat protein phosphatase is neuroprotective: differential effects on astrocytes. J Pharmacol Exp Ther. 2013 Nov;347(2):516-28. doi: 10.1124/jpet.113.206888. Epub 2013 Sep 10. PMID: 24023368; PMCID: PMC3807060.

1. Hwang SM, Feigenson M, Begun DL, Shull LC, Culley KL, Otero M, Goldring MB, Ta LE, Kakar S, Bradley EW, Westendorf JJ. Phlpp inhibitors block pain and cartilage degradation associated with osteoarthritis. J Orthop Res. 2018 May;36(5):1487-1497. doi: 10.1002/jor.23781. Epub 2017 Nov 28. PMID: 29068480; PMCID: PMC5985222. 2. Hwang SM, Feigenson M, Begun DL, Shull LC, Culley KL, Otero M, Goldring MB, Ta LE, Kakar S, Bradley EW, Westendorf JJ. Phlpp inhibitors block pain and cartilage degradation associated with osteoarthritis. J Orthop Res. 2018 May;36(5):1487-1497. doi: 10.1002/jor.23781. Epub 2017 Nov 28. PMID: 29068480; PMCID: PMC5985222.