Cat. No.: HY-B0877

Halcinonide

(Synonyms: SQ-18566)

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Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke.

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Pureté: 98.29%
CAS No.: 3093-35-4
Formule: C₂₄H₃₂ClFO₅
Masse moléculaire:454.96

Stockage:

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

Halcinonide Chemical Structure

CAS No.: 3093-35-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Cdk6/cyclin D2

Caspase 3

Voir tous les produits spécifiques à Isoform Caspase :

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In Vitro

Halcinonide (1-25 μM; 48 h) acts as a Smoothened agonist to up-regulate MBP, PLP, CNP, MOG, RxRγ, and Gli1 gene expression in Oli-neuM mouse oligodendrocyte cells, with 10 μM treatment for 48h driving significant myelin gene induction that is dependent on both Smoothened and RxRγ activation^[1].
Halcinonide (0-10 μM; 2 h) acts as a Smo agonist in U2OS cells stably expressing Smo-633 and βarr2-GFP, inducing βarr2-GFP aggregation with an EC₅₀ of 1,100 nM and an efficacy of 0.99^[2].
Halcinonide (0-10 μM; 30 h) activates downstream Hedgehog signaling in Shh-LIGHT2 cells, inducing Gli-luciferase activity with an EC₅₀ of 1.8 nM and an efficacy of 0.74, and synergizes with Shh to enhance this activity^[2].
Halcinonide (25 μM; 64 h) up-regulates cyclin D2 expression and inhibits caspase-3 degradation in primary mouse cerebellar granule cell precursors^[2].
Halcinonide (10-100 nM; 24 h) protects PC12 cells from H₂O₂-induced oxidative stress, improving cell viability and reducing intracellular ROS generation^[3].
Halcinonide (10-100 nM; 24 h) modulates the Shh signaling pathway and Bcl-2/Bax-mediated apoptosis in PC12 cells treated with H₂O₂, upregulating SMO and Bcl-2 while downregulating Sufu, Bax, and Caspase-3^[3].

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

Western Blot Analysis^[3]

Cell Line:

PC12 cells (under OGD/R stress)
Concentration:

10 nM, 100 nM (24 h pre-incubation)
Incubation Time:

24 h (pre-incubation); 6 h (OGD); 24 h (reperfusion)
Result:

Reversed OGD/R-induced decreases in SMO and Bcl-2 protein levels.
Reversed OGD/R-induced increases in Sufu, Bax, and Caspase-3 protein levels.

In Vivo

Halcinonide (20 mg/kg; p.o.; daily; 7 days) ameliorates ischemic stroke injury in MCAO rats by reducing cerebral infarction, improving neurological function, suppressing apoptosis, restoring redox homeostasis, and reducing inflammation via activation of the SMO/Shh pathway^[3].

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

Animal Model:

Sprague-Dawley rat with Ischemic stroke (male, 2-3 months old, 180-220 g, SPF grade, middle cerebral artery occlusion/reperfusion model)^[3]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 7 days
Result:

Reduced neurological deficit scores relative to untreated MCAO rats.
Reduced cerebral infarction volume relative to untreated MCAO rats.
Improved abnormal brain histological features observed via H&E staining.
Reduced the number of TUNEL-positive apoptotic cells in brain tissue.
Upregulated SMO and Bcl-2 protein expression in brain tissue.
Downregulated Sufu, Bax, and Caspase-3 protein expression in brain tissue.
Increased serum LDH activity.
Reduced serum lactic acid levels.
Restored serum MPO, MDA, SOD, GSH, and GSSG levels toward normal.
Reduced serum TNF-α and IL-6 levels.

Chemical Information

CAS No. 3093-35-4
Appearance Solid
Masse moléculaire 454.96
Formule C₂₄H₃₂ClFO₅
Color Light yellow to yellow
SMILES

C[C@@]12[C@@]3(C(CCl)=O)[C@@](OC(C)(O3)C)([H])C[C@@]1([H])[C@]4([H])CCC5=CC(CC[C@]5(C)[C@@]4(F)[C@@H](O)C2)=O
Synonyms

SQ-18566
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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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Journal Impact Factor

Nat Commun

Coronavirus envelope protein activates TMED10-mediated unconventional secretion of inflammatory factors. [Abstract]

2024 Oct 8;15(1):8708. PMID: 39379362

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (219.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1980 mL

10.9900 mL

21.9800 mL

5 mM

0.4396 mL

2.1980 mL

4.3960 mL

10 mM

0.2198 mL

1.0990 mL

2.1980 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 KB)
SDS (418 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[1]. Porcu G, et al. Clobetasol and Halcinonide Act as Smoothened Agonists to Promote Myelin Gene Expression and RxRγ Receptor Activation. PLoS One. 2015;10(12):e0144550. Published 2015 Dec 10. [Content Brief]

[2]. Wang J, et al. Identification of select glucocorticoids as Smoothened agonists: potential utility for regenerative medicine. Proc Natl Acad Sci U S A. 2010;107(20):9323-9328. [Content Brief]

[3]. Liu J, et al. Halcinonide activates smoothened to ameliorate ischemic stroke injury. Life Sci. 2025;361:123324. [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	2.1980 mL	10.9900 mL	21.9800 mL	54.9499 mL
	5 mM	0.4396 mL	2.1980 mL	4.3960 mL	10.9900 mL
	10 mM	0.2198 mL	1.0990 mL	2.1980 mL	5.4950 mL
	15 mM	0.1465 mL	0.7327 mL	1.4653 mL	3.6633 mL
	20 mM	0.1099 mL	0.5495 mL	1.0990 mL	2.7475 mL
	25 mM	0.0879 mL	0.4396 mL	0.8792 mL	2.1980 mL
	30 mM	0.0733 mL	0.3663 mL	0.7327 mL	1.8317 mL
	40 mM	0.0549 mL	0.2747 mL	0.5495 mL	1.3737 mL
	50 mM	0.0440 mL	0.2198 mL	0.4396 mL	1.0990 mL
	60 mM	0.0366 mL	0.1832 mL	0.3663 mL	0.9158 mL
	80 mM	0.0275 mL	0.1374 mL	0.2747 mL	0.6869 mL
	100 mM	0.0220 mL	0.1099 mL	0.2198 mL	0.5495 mL

Halcinonide

1 Cited Publications

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Halcinonide

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Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Halcinonide Related Classifications

HY-B0877 Related Classifications