2. Stem Cell/Wnt
  3. Hedgehog
  4. JK184

JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.

For research use only. We do not sell to patients.

JK184 Chemical Structure

JK184 Chemical Structure

CAS No. : 315703-52-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 95 In-stock
50 mg USD 330 In-stock
100 mg USD 530 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

JK184 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.

IC50 & Target

IC50: 30 nM (Hedgehog)[1]
In Vitro

JK184 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)[1]. 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)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JK184 Related Antibodies
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. However, JK184 has a poor pharmacokinetic profile and bioavailability[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

350.44

Formula

C19H18N4OS
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

CC1=C(C2=CSC(NC3=CC=C(OCC)C=C3)=N2)N4C=CC=CC4=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (142.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8536 mL 14.2678 mL 28.5356 mL
5 mM 0.5707 mL 2.8536 mL 5.7071 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Five-week-old female athymic (nu/nu) mice are used. BxPC-3 and Panc-1 tumors are established by s.c. injection of 1×107 cells. Mice bearing tumors around 100 mm3 are selected and randomized into treatment groups (5 mice per group). Mice are injected intravenously every day for 30 days with 100 μL of NS (control), blank micelles, free JK184 (5 mg/kg body weight), or JK184 micelles (5 mg/kg body weight), respectively. Tumor length and width are determined every 3 days and tumor volume (TV) is calculated using the following formula: TV=0.5×length×width2. At the end of experiment, mice are sacrificed. Solid tumors are removed and processed for immunohistochemical analysis and terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8536 mL 14.2678 mL 28.5356 mL 71.3389 mL
5 mM 0.5707 mL 2.8536 mL 5.7071 mL 14.2678 mL
10 mM 0.2854 mL 1.4268 mL 2.8536 mL 7.1339 mL
15 mM 0.1902 mL 0.9512 mL 1.9024 mL 4.7559 mL
20 mM 0.1427 mL 0.7134 mL 1.4268 mL 3.5669 mL
25 mM 0.1141 mL 0.5707 mL 1.1414 mL 2.8536 mL
30 mM 0.0951 mL 0.4756 mL 0.9512 mL 2.3780 mL
40 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7835 mL
50 mM 0.0571 mL 0.2854 mL 0.5707 mL 1.4268 mL
60 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1890 mL
80 mM 0.0357 mL 0.1783 mL 0.3567 mL 0.8917 mL
100 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7134 mL
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JK184 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JK184315703-52-7JK 184JK-184HedgehogInhibitorinhibitorinhibit

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