Home GPCR & G Protein Hedgehog/Smoothened inhibitor JK184 For research use only.

JK184

JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.

JK184 Chemical Structure

JK184 Chemical Structure

CAS No. 315703-52-7

Purity & Quality Control

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

JK184 Related Products

Signaling Pathway

Hedgehog/Smoothened Signaling Pathways

Hedgehog/Smoothened Signaling Pathway

Biological Activity

Description JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.
Targets
Gli [1]
In vitro
In vitro

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

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

Chemical Information & Solubility

Molecular Weight 350.44 Formula

C19H18N4OS
CAS No. 315703-52-7 SDF --
Smiles CCOC1=CC=C(C=C1)NC2=NC(=CS2)C3=C(N=C4N3C=CC=C4)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 70 mg/mL ( (199.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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 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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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