GLPBio

ABC99

Catalog No.: GC42669Purity:>95.00%
ABC99 is an N-hydroxyhydantoin (NHH)-carbamate-based, irreversible and selective inhibitor of Wnt-deacylating enzyme NOTUM.

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ABC99
Cas No.: 2331255-53-7
10mM (in 1mL DMSO)In Stock
$264.00
1
1mgIn Stock
$96.00
1
5mgIn Stock
$262.00
1
10mgIn Stock
$385.00
1

Citations

5 publicationsPublications from researchers using this product
IF 15

Description

ABC99 is an N-hydroxyhydantoin (NHH)-carbamate-based, irreversible and selective inhibitor of Wnt-deacylating enzyme NOTUM[1]. NOTUM is a secreted serine hydrolase that negatively modulates Wnt/β-catenin signaling by removing the essential palmitoleate moiety from Wnt proteins[2]. ABC99 is usually used in models of osteoporosis, colorectal cancer and neurodegenerative diseases where Wnt signaling is insufficient[3][4].

In vitro, ABC99 (2µg/mL; 7–14 days) suppressed odontoblastic differentiation of human stem cells from apical papilla (hSCAPs), reduced ALP activity, blocked mineralized nodule formation, and decreased DSPP, DMP1 and ALP mRNA levels[5]. ABC99 (50nM and 500nM; 14 days) significantly reversed the inhibition of osteogenic differentiation of hPDLSCs by recombinant human NOTUM, restored ALP activity and calcium nodule formation, and increased the protein/mRNA levels of Osterix, OCN and Runx2[6].

In vivo, ABC99 (10mg/kg/day; p.o.; 4 weeks) almost completely prevented liver metastasis and lymph-node metastasis, reduced primary tumor weight, and significantly inhibited Ki67⁺ cell proliferation in orthotopic colorectal cancer mice[7].

References:
[1] Suciu RM, Cognetta AB 3rd, Potter ZE, Cravatt BF. Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling. ACS Med Chem Lett. 2018;9(6):563-568.
[2] Bayle ED, Svensson F, Atkinson BN, et al. Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling. J Med Chem. 2021;64(8):4289-4311.
[3] Zhao Y, Jolly S, Benvegnu S, Jones EY, Fish PV. Small-molecule inhibitors of carboxylesterase Notum. Future Med Chem. 2021;13(11):1001-1015.
[4] Larrick JW, Mendelsohn AR. Roads to the Fountain of Youth? Rejuvenating Intestinal Stem Cells. Rejuvenation Res. 2019;22(4):342-347.
[5] Zhao Q, Ren H, Wang N, Yuan X, Zhao Y, Wen Q. NOTUM plays a bidirectionally modulatory role in the odontoblastic differentiation of human stem cells from the apical papilla through the WNT/β-catenin signaling pathway. Arch Oral Biol. 2024;160:105896.
[6] Yang P, Li C, Kou Y, et al. Notum suppresses the osteogenic differentiation of periodontal ligament stem cells through the Wnt/Beta catenin signaling pathway. Arch Oral Biol. 2021;130:105211.
[7] Tian Y, Wang X, Cramer Z, et al. APC and P53 mutations synergise to create a therapeutic vulnerability to NOTUM inhibition in advanced colorectal cancer. Gut. 2023;72(12):2294-2306.

Protocol

Cell experiment [1]:

Cell lines

Human stem cells from the apical papilla (hSCAPs)

Preparation Method

Human stem cells from the apical papilla (hSCAPs) were recovered and cultured in a cell culture incubator under the conditions of 37°C with 5% CO2 (v/v). The culture medium was refreshed every 3 days. The normal proliferation medium (PM) contained α-MEM, 10% fetal bovine serum, and 1% penicillin. When cells reached 80% confluency, odontoblastic medium (OM) contained α-MEM, 10% fetal bovine serum, 50mg/L L-Ascorbic acid, 5mmol/L sodium β-phosphoglycerate, and 10nmol/L dexamethasone, was used to induce odontoblastic differentiation. To down-regulate the extracellular NOTUM level, ABC99, a small molecule inhibitor of NOTUM, was added to the OM medium at 2ug/ml. Cells were collected on odontoblastic induction day 3, 7, and 14. Alkaline phosphatase (ALP) staining, Alizarin red (ARS) staining and qRT-PCR were performed according to the manufacturer’s Instructions.

Reaction Conditions

2µg/mL; 7–14 days

Applications

ABC99 suppressed odontoblastic differentiation of human stem cells from apical papilla (hSCAPs), reduced ALP activity, blocked mineralized nodule formation, and decreased DSPP, DMP1 and ALP mRNA levels.

Animal experiment [2]:

Animal models

C57BL/6J mice

Preparation Method

8-week-old, specific-pathogen-free C57BL/6J mice were kept in an air-conditioned room at a temperature of 23±1℃, a relative humidity of 50–70%, and a 12h light/dark cycle. APKS tumor organoids were orthostatic implanted into the colonic mucosa of C57BL/6J mice under endoscopic guidance to establish an in situ colorectal cancer model. Mice were treated with ABC99(10mg/kg/day; p.o.) or vehicle (corn oil) control after 4 weeks of engraftment and tumour growth. Mice are treated for indicated number of weeks (week 0-4 weeks post-implantation) (n=7 mice). Tumour weight, number of macrometastases in the liver and number of lymph node metastases in mice were qualified. Bioluminescent imaging (BLI) and Kaplan–Meier survival analysis were performed to monitor tumor burden and compare survival. 

Dosage form

10mg/kg/day; p.o.; 4 weeks

Applications

ABC99 almost completely prevented liver metastasis and lymph-node metastasis, reduced primary tumor weight in orthotopic colorectal cancer mice.

References:
[1] Zhao Q, Ren H, Wang N, Yuan X, Zhao Y, Wen Q. NOTUM plays a bidirectionally modulatory role in the odontoblastic differentiation of human stem cells from the apical papilla through the WNT/?-catenin signaling pathway. Arch Oral Biol. 2024;160:105896.
[2] Tian Y, Wang X, Cramer Z, et al. APC and P53 mutations synergise to create a therapeutic vulnerability to NOTUM inhibition in advanced colorectal cancer. Gut. 2023;72(12):2294-2306.

Product Documents

Purity:>95.00%Appearance:A solid

Chemical Properties

CAS No.
2331255-53-7
Chemical Name
7-(4-chlorobenzyl)-1,3-dioxohexahydroimidazo[1,5-a]pyrazin-2(3H)-yl-2,3-dihydro-4H-benzo[b][1,4]oxazine-4-carboxylate
SMILES
ClC1=CC=C(CN2CC(C(N(OC(N3C(C=CC=C4)=C4OCC3)=O)C5=O)=O)N5CC2)C=C1
Molecular Formula
C22H21ClN4O5
Molecular Weight
456.9
Solubility
1mg/mL in Chloroform, 1mg/mL in acetonitrile, 1mg/mL in methyl acetate
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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