LP-922056
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 574058

CAS#: 1365060-22-5

Description: 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

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LP-922056
CAS# 1365060-22-5

Theoretical Analysis

MedKoo Cat#: 574058
Name: LP-922056
CAS#: 1365060-22-5
Chemical Formula: C11H9ClN2O2S2
Exact Mass: 299.98
Molecular Weight: 300.775
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 2 weeks
50mg USD 950 2 weeks
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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:
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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 77.5 257.80

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.

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. 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: 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 vivo protocol: TBD

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