HhAntag

Cat. No.: HY-15412 Purity: 99.40%: FAQs
Data Sheet SDS COA Handling Instructions

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HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.

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

HhAntag Chemical Structure

CAS No. : 496794-70-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 130	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 130	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 34	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 460	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 782	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1251	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Biological Activity
Purity & Documentation
References
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Description

HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway^[1].

In Vitro

HhAntag (2-30 µM; 72 hours) demonstrates to be 10-times more potent than the natural product SMO antagonist, cyclopamine, at inhibiting Hh pathway activity and it inhibits Hh signalling pathway sensitivitive cells with IC₅₀ values ranging from 2 µM to >30 µM^[1].
HhAntag inhibits AsPC-1, BXPC-3, CFPAC, HPAC, HPAF-II, KP4, Panc 03.27, PA-TU-8902, PSN-1, SU.86.86 cells with IC₅₀ values of 30 µM, 5.4 µM, 5.8 µM, 2.7 µM, 6.2 µM,10.3 µM, 2.5 µM, 2.9 µM, 5.8 µM and 2.7 µM, respectively^[1].
HhAntag (100 nM) is needed to completely inhibit Hh signalling in a Hh-responsive human mesenchymal cell line (HEPM) expressing a GLI luciferase reporter construct (HEPM-rep), the IC₅₀ of 5 nM 400-times lower than that required to inhibit cell growth by 50% in the most sensitive cancer cell line (1.9 μM)^[1].

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

In Vivo

HhAntag (oral administraion; 75 mg/kg or 100 mg/kg; twice daily; 25 days) results in significant growth delay in HT55 and HT-29 colorectal cell line xenografts models, with average tumour growth inhibitions of 29% and 48%, respectively. Whereas HhAntag had no effect on the growth of DLD-1 xenografts^[1].

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

Animal Model:	Primary human xenografts in female CD1 nu/nu mice of 6–8 weeks (DLD-1, HT55 and HT-29 cells)^[1]
Dosage:	75 mg/kg or 100 mg/kg
Administration:	Oral administraion; twice daily; 25 days
Result:	Resulted in growth delay of HT55 and HT-29 xenografts, but had no effects on DLD-1 xenografts.

Molecular Weight

450.92

Formula

C₂₄H₂₃ClN₄O₃

CAS No.

496794-70-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=C(Cl)C(C2=NC3=CC=C(N(C)C)C=C3N2)=C1)C4=CC(OC)=CC(OC)=C4

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 : ≥ 100 mg/mL (221.77 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	2.2177 mL	11.0884 mL	22.1769 mL
5 mM	0.4435 mL	2.2177 mL	4.4354 mL
10 mM	0.2218 mL	1.1088 mL	2.2177 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 3 mg/mL (6.65 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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% Corn Oil
Solubility: ≥ 3 mg/mL (6.65 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.40%

Select Batch:

Data Sheet (273 KB) SDS (392 KB)

COA (249 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[1]. Neeraj Mahindroo, et al. Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway. Bioorg Med Chem. 2010 Jul 1;18(13):4801-11. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2177 mL	11.0884 mL	22.1769 mL	55.4422 mL
	5 mM	0.4435 mL	2.2177 mL	4.4354 mL	11.0884 mL
	10 mM	0.2218 mL	1.1088 mL	2.2177 mL	5.5442 mL
	15 mM	0.1478 mL	0.7392 mL	1.4785 mL	3.6961 mL
	20 mM	0.1109 mL	0.5544 mL	1.1088 mL	2.7721 mL
	25 mM	0.0887 mL	0.4435 mL	0.8871 mL	2.2177 mL
	30 mM	0.0739 mL	0.3696 mL	0.7392 mL	1.8481 mL
	40 mM	0.0554 mL	0.2772 mL	0.5544 mL	1.3861 mL
	50 mM	0.0444 mL	0.2218 mL	0.4435 mL	1.1088 mL
	60 mM	0.0370 mL	0.1848 mL	0.3696 mL	0.9240 mL
	80 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6930 mL
	100 mM	0.0222 mL	0.1109 mL	0.2218 mL	0.5544 mL

HhAntag 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:

HhAntag496794-70-8SmoSmoothenedInhibitorinhibitorinhibit

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