2. Stem Cell/Wnt Apoptosis Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Smo Caspase RAR/RXR CDK
  4. Halcinonide

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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Halcinonide

Halcinonide Estructura química

No. CAS : 3093-35-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Halcinonide:

Halcinonide Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Halcinonide

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Descripciòn

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[1][2][3].

IC50 & Target

Cdk6/cyclin D2

 

Caspase 3

 

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.

Halcinonide Related Antibodies

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.
Peso molecular

454.96

Fòrmula

C24H32ClFO5
No. CAS
Appearance

Solid

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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1980 mL 10.9900 mL 21.9800 mL
5 mM 0.4396 mL 2.1980 mL 4.3960 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.

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

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In Vivo Dissolution Calculator
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Pureza y Documentación
Referencias

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 2.1980 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
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Halcinonide 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:

Halcinonide3093-35-4SQ-18566SQ18566SQ 18566SmoCaspaseRAR/RXRCDKSmoothenedRetinoic acid receptorsRetinoid X receptorsCyclin dependent kinaseOli-neuM mouse oligodendrocyte cellsRxRγPC12 cellsprimary mouse cerebellar granule cell precursorsShh-LIGHT2 cellsHEK293 cellsHedgehog signalingU2OS cellsGli transcription factorsInhibitorinhibitorinhibit

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Nombre del producto:
Halcinonide
Cat. No.:
HY-B0877
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