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JK184
CAS No. 315703-52-7
JK184( JK-184 | JK 184 )
Catalog No. M14026 CAS No. 315703-52-7
JK184 is an ntagonist of the hedgehog (Hh) signaling pathway and Gli inhibitor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 43 | In Stock |
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| 10MG | 70 | In Stock |
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| 25MG | 161 | In Stock |
|
| 50MG | 278 | In Stock |
|
| 100MG | 461 | In Stock |
|
| 500MG | 972 | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameJK184
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NoteResearch use only, not for human use.
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Brief DescriptionJK184 is an ntagonist of the hedgehog (Hh) signaling pathway and Gli inhibitor.
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DescriptionJK184 is an ntagonist of the hedgehog (Hh) signaling pathway and Gli inhibitor; inhibits GLI1 mRNA expression and decreases the number of colonies formed in TN-IBC (SUM149) and TNBC (MDA-MB-231 and SUM159) cell lines; significantly down-regulates GLI1 targets that regulate cell cycle (cyclin D and E) and apoptosis (Bcl2); JK184 is a potent inhibitor of microtubule assembly and that microtubule-depolymerizing agents can either negatively or positively regulate the Gli family of transcription factors, dependending on the mechanism by which the pathway is activated.
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In VitroJK184 is designed to antagonize Hh signaling by inhibiting glioma (Gli)-dependent transcriptional activity in a dose dependent manner. JK184 significantly inhibitts proliferation of HUVECs with IC50 of 6.3 μg/mL after three days incubation. To evaluate anti-tumor effect of JK184, MTT assay is conducted in Panc-1 and BxPC-3 cells after administration with indicated concentrations of compounds, half maximal inhibitory concentration (IC50) of JK184 (23.7 ng/mL in anc-1 and 34.3 ng/mL in BxPC-3). Claudin-low cell lines are more sensitive to JK184 treatment than are MCF10a, MTSV1-7, or HMLE-shGFP and HMLE-pBP cells, and JK184 induced a dose-dependent decrease in glioma-associated oncogene homolog 1 (GLI1) transcript and protein levels in these cells. Treatment with the IC50 dose of JK184 enhances the proportion of HMLE-shEcad cells that stained with Annexin-V, but are negative for propidium iodide (PI) (P<0.0001, t test).
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In VivoJK184 (5 mg/kg, injected intravenously) exhibits good anti-proliferative activity in subcutaneous Panc-1 and BxPC-3 tumor models, and is a good candidate as antitumor drug targeted Hh signaling. However, JK184 has a poor pharmacokinetic profile and bioavailability.
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SynonymsJK-184 | JK 184
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PathwayWnt/Notch/Hedgehog
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TargetGli
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RecptorHedgehog
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number315703-52-7
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Formula Weight350.44
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Molecular FormulaC19H18N4OS
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESCC1=C(C2=CSC(NC3=CC=C(OCC)C=C3)=N2)N4C=CC=CC4=N1
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Chemical Name2-Thiazolamine, N-(4-ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Cupido T, et al. Angew Chem Int Ed Engl. 2009;48(13):2321-4.
2. Colavito SA, et al. Breast Cancer Res. 2014 Sep 25;16(5):444.
3. Oladapo HO, et al. Cancer Lett. 2017 Dec 28;411:136-149.
4. Lee J, et al. Chembiochem. 2007 Nov 5;8(16):1916-9.
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