| Field | Specification |
|---|---|
| Target | |
| Alternative names | A3051 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C17H11Cl2N3O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
KY19382, also known as A3051, is a potent, orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50 values of 19 nM and 10 nM, respectively. It activates Wnt/β-catenin signaling through inhibitory effects on both the CXXC5-DVL interaction and GSK3β activity, and it can be used in research on high-fat-diet (HFD)-induced metabolic disease[1][2]. It is supplied as a brown to reddish brown solid (C17H11Cl2N3O2, MW 360.19) at 98.0% purity.
Physical & Chemical Properties
| CAS Number | 2226664-93-1 |
|---|---|
| Molecular Formula | C17H11Cl2N3O2 |
| Molecular Weight | 360.19 g/mol |
| Purity | 98.0% |
| Appearance | Solid |
| Color | Brown to reddish brown |
| SMILES | O=C1NC2=C(C=C(Cl)C(Cl)=C2)/C1=C3NC4=C(C=CC=C4)C/3=N/OC |
| Target | CXXC5-DVL, GSK3β |
| Signaling Pathway | PI3K/Akt/mTOR; Stem Cell/Wnt |
| Solubility | In Vitro: DMSO: 4.17 mg/mL (11.58 mM; Requires sonication and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
CXXC5-DVL 19 nM (IC50) |
GSK3β 10 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Choi KY, et al. Compositions and methods for suppressing and/or treating metabolic diseases and/or a clinical condition thereof. WO2020079569.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 4.17 mg/mL (11.58 mM) | requires sonication and warming and heat to 80°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
KY19382 (0.01 and 0.1 μM; 48 h) promotes proliferation of ATDC5 cells[1]. KY19382 (0.1 μM; 3 d) up-regulates mRNA levels of chondrogenic differentiation markers in ATDC5 and C28/I2 cells[1]. In ATDC5 cells, KY19382 (0.01 and 0.1 μM; 24 h) inactivates GSK3α/β[1]. In ATDC5 cells, KY19382 (0.1 μM; 4 h) disrupts the CXXC5-DVL interaction[1]. In HEK293 reporter cells, KY19382 (0.001-10 μM; 18 h) enhances TOPFlash activity[1]. In ATDC5 cells, KY19382 (0.1 μM; 48 h) increases nuclear translocation of β-catenin[1].
Cell Proliferation Assay[1]
| Cell Line | ATDC5 cells |
|---|---|
| Concentration | 0, 0.01, 0.1 μM |
| Incubation Time | 48 hours |
| Result | Enhanced the number of BrdU-positive ATDC5 cells. |
Cell Proliferation Assay[1]
| Cell Line | ATDC5 cells |
|---|---|
| Concentration | 0, 0.01, 0.1 μM |
| Incubation Time | 24 hours |
| Result | Increased the level of β-catenin in a dose-dependent manner. |
In Vivo
In mice, KY19382 (i.p. once daily for 2 weeks at 0.1 mg/kg) delays growth plate senescence in older animals and promotes growth plate maturation in rapidly growing young animals[1]. KY19382 (0.1 mg/kg; i.p. once daily for 10 weeks) significantly lengthens tibiae in mice[1]. KY19382 (5 mg/kg; i.p.) shows a relatively favorable bioavailability (F=16.74%), with an exposure level of 6,555.79 ng?h/ml and a half-life of 16.20 h[1]. KY19382 (A3051) (25 mg/kg; p.o. once daily for 16 weeks) reduces adipocyte size and shows anti-inflammatory effects[2]. A3051 (25 mg/kg; p.o. once daily for 5 days) lowers fasting glucose in mice[2]. A3051 (25 mg/kg; p.o. once daily for 3 weeks) reduces hepatosteatosis in mice[2].
| Animal Model | C57BL/6 male mice (7-weeks-old or 3-weeks-old)[1] |
|---|---|
| Dosage | 0.1 mg/kg |
| Administration | I.p. once daily for 2 weeks |
| Result | Increased nuclear β-catenin in the growth plate chondrocytes dramatically. Elevated the height of each growth plate zone and BrdU-positive cells. Did not affect the cartilage resorption of rapidly growing young mice. |
| Animal Model | SD male rats[1] |
|---|---|
| Dosage | 1 mg/kg for i.v. and 5 mg/kg for i.p. (Pharmacokinetic Analysis) |
| Administration | I.v. and i.p. administration |
| Result | I.v.: t1/2=3.33 h; AUC=7832.81 ng∙h/mL; CL=0.12 L/h/kg. I.p.: t1/2=16.20 h; F=16.74%; Cmax=463.37 ng/mL. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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CXXC5 function blockade promotes diabetic wound healing through stimulating fibroblast and vascular endothelial cell activation. Cell Commun Signal 2025 Feb 25;23(1):108. PMID: 40001144
Mechanistic insights into 5-aminolevulinic acid photodynamic therapy for acne vulgaris: targeting lipogenesis via the OLR1-Wnt/β-catenin pathway. Mol Med 2025 Feb 4;31(1):41. PMID: 39905294
The TEAD4-DYNLL1 axis accelerates cell cycle progression and augments malignant properties of lung adenocarcinoma cells. Eur J Med Res 2025 Apr 1;30(1):221. PMID: 40170083
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