Cat. No.: HY-15412

HhAntag

Name: HhAntag
Brand: MedChemExpress
SKU: HY-15412
Price: 120.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.40%
CAS No.: 496794-70-8
화학식: C₂₄H₂₃ClN₄O₃
분자량:450.92

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

HhAntag Chemical Structure

CAS No.: 496794-70-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

Cellular Effect

Cell Line	Type	Value	Description	References
C3H 10T1/2	IC₅₀	100 nM Compound: 2, HhAntag	Inhibition of Hh signal-induced alkaline phosphatase activity in mouse C3H10T1/2 cells after 4 days Inhibition of Hh signal-induced alkaline phosphatase activity in mouse C3H10T1/2 cells after 4 days	[PMID: 20605720]
Shh Light II	EC₅₀	40 nM Compound: 96	Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay	[PMID: 19309080]

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.

Chemical Information

CAS No. 496794-70-8
Appearance Solid
분자량 450.92
화학식 C₂₄H₂₃ClN₄O₃
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
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Cell Signal

Hedgehog pathway inhibitor HhAntag suppresses virus infection via the GLI-S1PR axis. [Abstract]

2025 Aug:132:111807. PMID: 40239727

용액&용해도

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.2177 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

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HhAntag

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