Home GPCR & G Protein Hedgehog/Smoothened inhibitor JK184

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JK184 Hedgehog/Smoothened inhibitor

Cat.No.S6565

JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.
JK184 Hedgehog/Smoothened inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 350.44

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S656501 DMSO]70 mg/mL]false]Ethanol]14 mg/mL]false]Water]Insoluble]false Purity: 99.56%
99.56

Chemical Information, Storage & Stability

Molecular Weight 350.44 Formula

C19H18N4OS

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 315703-52-7 -- Storage of Stock Solutions

Synonyms N/A Smiles CCOC1=CC=C(C=C1)NC2=NC(=CS2)C3=C(N=C4N3C=CC=C4)C

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
Gli [1]
In vitro

JK184 antagonizes Hh signaling by inhibiting Gli-dependent transcriptional activity in a dose dependent manner. This compound has a stronger inhibiting effects in mammalian cells with the IC50 of 30 nM compared with cyclopamine (IC50 = 250 nM)[1].
In vivo

JK184 has a poor pharmacokinetic profile and bioavailability, because the half-life and Cmax of this compound is lower compared with cyclopamine. Its micelles are a promising drug candidate for treating pancreatic tumors with high inhibitory effect on Hh activity[1].
References

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