LP-922056 | CAS# 1365060-22-5 | Notum Pectinacetylesterase Inhibitor

MedKoo Cat#: 574058 | Name: LP-922056

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Description:

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

LP-922056 is a Notum pectinacetylesterase inhibitor which activates wnt signalling. LP-922056 increases cortical bone thickness in a mouse model of bone growth.

Chemical Structure

LP-922056

CAS#1365060-22-5

Theoretical Analysis

MedKoo Cat#: 574058

Name: LP-922056

CAS#: 1365060-22-5

Chemical Formula: C11H9ClN2O2S2

Exact Mass: 299.9794

Molecular Weight: 300.78

Elemental Analysis: C, 43.93; H, 3.02; Cl, 11.79; N, 9.31; O, 10.64; S, 21.32

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 weeks
50mg	USD 950.00	2 weeks

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Related CAS #

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Synonym

LP-922056, LP922056, LP 922056

IUPAC/Chemical Name

2-[(6-Chloro-7-cyclopropylthieno[3,2-d]pyrimidin-4-yl)thio]acetic acid

InChi Key

LJYRIWUQISYYHA-UHFFFAOYSA-N

InChi Code

InChI=1S/C11H9ClN2O2S2/c12-10-7(5-1-2-5)8-9(18-10)11(14-4-13-8)17-3-6(15)16/h4-5H,1-3H2,(H,15,16)

SMILES Code

OC(CSC1=C2SC(Cl)=C(C2=NC=N1)C3CC3)=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:

LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively.

In vitro activity:

Reliable screening technologies are available to identify inhibitors of Notum, and structural studies are accelerating the discovery of new inhibitors. A selection of these hits have been optimized to give fit-for-purpose small molecule inhibitors of Notum. Three noteworthy examples are LP-922056 (26), ABC99 (27), and ARUK3001185 (28), which are complementary chemical tools for exploring the role of Notum in Wnt signaling. Reference: J Med Chem. 2021 Apr 22;64(8):4289-4311. https://pubmed.ncbi.nlm.nih.gov/33783220/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	77.5	257.80

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 300.78 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. Bayle ED, Svensson F, Atkinson BN, Steadman D, Willis NJ, Woodward HL, Whiting P, Vincent JP, Fish PV. Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling. J Med Chem. 2021 Apr 22;64(8):4289-4311. doi: 10.1021/acs.jmedchem.0c01974. Epub 2021 Mar 30. PMID: 33783220; PMCID: PMC8172013.

In vitro protocol:

In vivo protocol:

TBD