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JK184

Catalog No. T3588 CAS 315703-52-7

JK184 is a potent Hedgehog (Hh) pathway inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

JK184, CAS 315703-52-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 78.00
25 mg	In stock	$ 179.00
50 mg	In stock	$ 309.00
100 mg	In stock	$ 512.00
500 mg	In stock	$ 1,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 99.89%

Purity: 99.09%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	JK184 is a potent Hedgehog (Hh) pathway inhibitor.
Targets&IC50	Hedgehog:30 nM
In vitro	JK184 is specifically designed to counteract Hedgehog (Hh) signaling through the inhibition of glioma-associated oncogene (Gli)-dependent transcriptional activity in a dose-dependent fashion. It effectively reduces the growth of human umbilical vein endothelial cells (HUVECs) with a half maximal inhibitory concentration (IC50) of 6.3 μg/mL following a three-day incubation period. Moreover, MTT assays reveal that JK184 significantly restricts tumor growth in Panc-1 and BxPC-3 cell lines, demonstrating IC50 values of 23.7 ng/mL and 34.3 ng/mL, respectively. Notably, cell lines characterized by lower levels of the tight junction protein claudin show increased sensitivity to JK184, with the compound inducing a dose-dependent reduction in both GLI1 mRNA and protein expressions. Additionally, administering JK184 at the IC50 concentration significantly increases Annexin-V staining in HMLE-shEcad cells while maintaining negativity for propidium iodide (PI) staining, indicating a pronounced pro-apoptotic effect without compromising cell membrane integrity (P<0.0001, t-test)[1][2].
In vivo	JK184 (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. Histological analysis showed that JK184 improved anti-tumor activity by inducing more apoptosis, decreasing microvessel density, and reducing expression of CD31, Ki67, and VEGF in tumor tissues. However, JK184 has a poor pharmacokinetic profile and bioavailability[1].
Cell Research	JK184 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. The Shh-LIGHT2 cells are seeded in 96-well plates and grown to confluency. The Shh-LIGHT2 cells are treated with various concentrations of JK184 micelles or free JK184 or micelles in DMEM containing 0.5% CS, 0.1 mg/mL streptomycin, 100 U/mL penicillin, 5% Shh-N conditioned medium obtained from Shh-N-producing HEK293 cells. The treated cells are cultured further for 60 h, and firefly and Renilla luciferase activities are measured using a dual luciferase kit. Proliferation assay or apoptosis evaluation of HUVECs is measured using MTT method or FCM analysis, respectively. HUVECs are treated with a series concentration of free JK184, JK184 micelles, or blank MPEG-PCL micelles for 48 h, respectively. The mean percentage of cell inhibition or apoptosis is calculated[1].

Molecular Weight	350.44
Formula	C19H18N4OS
CAS No.	315703-52-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.5 mg/mL (10 mM), Sonication is recommended.

References and Literature

1. Zhang N, et al. Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth through inhibiting Hedgehog signaling pathway. Nanoscale. 2015 Feb 14;7(6):2609-24. 2. Colavito, S., Zou, M., Yan, Q., Nguyen, D., & Stern, D. (2014). Significance of glioma-associated oncogene homolog 1 (GLI1)expression in claudin-low breast cancer and crosstalk with the nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB) pathway. Breast Cancer Research, 16(5). doi: 10.1186/s13058-014-0444-4

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Inhibitor Library GPCR Compound Library Target-Focused Phenotypic Screening Library Anti-Aging Compound Library Reprogramming Compound Library Anti-Prostate Cancer Compound Library Osteogenesis Compound Library Anti-Cancer Compound Library Wnt/Hedgehog/Notch Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

JK184 315703-52-7 GPCR/G Protein Stem Cells Hedgehog/Smoothened inhibit Inhibitor JK-184 Hedgehog JK 184 inhibitor

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