SAG dihydrochloride
Based on 40 publication(s) in Google Scholar
SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
For research use only. We do not sell to patients.
- Purity: 98.23%
- CAS No.: 2702366-44-5
- Formula: C28H30Cl3N3OS
- Molecular Weight:562.98
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Stem Cell Signaling Compound Library
HY-L017
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Reprogramming Compound Library
HY-L039
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Heterocyclic Compound Library
HY-L138
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) SAG dihydrochloride
More- Cell Res. 2022 Mar;32(3):288-301. [Abstract]
- Cell Stem Cell. 2025 Jul 3;32(7):1071-1086.e8. [Abstract]
- Nat Commun. 2026 May 15. [Abstract]
- Nat Commun. 2024 Feb 2;15(1):987. [Abstract]
- Adv Sci (Weinh). 2025 Jan 9:e2411675. [Abstract]
- Sci Adv. 2025 Jan 10;11(2):eads5434. [Abstract]
- Sci Adv. 2023 Jun 16;9(24):eadf6927. [Abstract]
- Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]
- Cell Rep. 2020 Apr.
- Ecotoxicol Environ Saf. 2025 Aug 6:303:118813. [Abstract]
- Biochem Pharmacol. 2021 Aug:190:114593. [Abstract]
- J Pathol. 2025 Nov 6. [Abstract]
- Glia. 2026 Jun;74(6):e70151. [Abstract]
- Glia. 2021 Jul;69(7):1782-1798. [Abstract]
- Molecules. 2017 Dec 31;23(1). pii: E85. [Abstract]
- Cell Rep Methods. 2024 May 8:100777. [Abstract]
- Cancer Sci. 2021 Oct;112(10):4176-4186. [Abstract]
- J Cell Mol Med. 2022 Jun;26(11):3213-3222. [Abstract]
- Drug Dev Res. 2019 Nov;80(7):992-999. [Abstract]
- iScience. 2024 Feb 5;27(3):109111. [Abstract]
- iScience. 2022 Dec 26;26(1):105898. [Abstract]
- Toxins. 2021 Aug 22;13(8):585. [Abstract]
- Sci Rep. 2025 Oct 14;15(1):35928. [Abstract]
- J Biomed Mater Res A. 2025 Oct;113(10):e38001. [Abstract]
- Biomedicines. 2022 Apr 18;10(4):928. [Abstract]
- Development. 2018 Sep 20;145(18). pii: dev164830. [Abstract]
- J Pharm Biomed Anal. 2017 Aug 5:142:201-209. [Abstract]
- J Tradit Complement Med. 2025 Jun 14.
- Mol Brain. 2021 Jul 19;14(1):116. [Abstract]
- Exp Eye Res. 2025 May 21:110440. [Abstract]
- Tissue Cell. 2024 Nov 28:92:102643. [Abstract]
- bioRxiv. 2026 Apr 15:2026.04.09.717542. [Abstract]
- bioRxiv. 2026 Feb 16:2026.02.13.705790. [Abstract]
- Res Sq. 2026 Feb 2.
- bioRxiv. 2025 July 21.
- bioRxiv. 2025 March 25.
- Patent. US20240247230A1.
- UNIVERSIDAD DE CONCEPCIÓN. 2023 Apr.
- Research Square Preprint. 2021 Sep.
- University of Bonn. 2021 May 21.
Customer Validation & Images
-
RT-PCR
-
WB
-
IF
-
IF
-
RT-PCR
Biological Activity
EC50: 3 nM (Smo)[1]
SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM and then inhibits expression at higher concentrations[1].
SAG (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (Kd) of 59 nM for the SAG/Smo complex[1].
SAG (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin[2].
SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells[3].
SAG (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells[3].
SAG (250 nM; 24 h) increases MDAMB231 cells migration[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SAG (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Pregnant C57BL/6J mice[5]
-
Dosage:15, 17, 20 mg/kg
-
Administration:A single i.p.
-
Result:Effective in ca. 80% of the embryos and increased Gli1 and Gli2 mRNA expression in the limb bud, with Gli1 mRNA being the most upregulated at the dose of 20 mg/kg.
Chemical Information
-
CAS No. 2702366-44-5
-
Appearance Solid
-
Molecular Weight 562.98
-
Formula C28H30Cl3N3OS
-
Color Light yellow to light brown
-
SMILES
O=C(C1=C(Cl)C2=CC=CC=C2S1)N([C@H]3CC[C@H](NC)CC3)CC4=CC=CC(C5=CC=NC=C5)=C4.[H]Cl.[H]Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (40)
-
Journal Impact Factor
-
Most Recent
-
Cell Res
Cholesterylation of Smoothened is a calcium-accelerated autoreaction involving an intramolecular ester intermediate. [Abstract]2022 Mar;32(3):288-301. PMID: 35121857
SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Mar;32(3):288-301. [Abstract]
SAG (5-200 nM)-induced Gli1 expression is independent of extracellular Ca2+ concentration. Sub-confluent NIH3T3 cells were serum-starved in 0.5% FCS overnight and switched to normal DMEM or Ca2+-free DMEM containing indicated concentration of SAG. Cells were harvested for RNA extraction after 6 hours.
-
Cell Stem Cell
Establishing dorsal-ventral patterning in human neural tube organoids with synthetic organizers. [Abstract]2025 Jul 3;32(7):1071-1086.e8. PMID: 40373768 -
Nat Commun
Identification of a component of the tubulin poly-glutamylase complex required for phosphoinositide homeostasis and cilium assembly and maintenance. [Abstract]2026 May 15. PMID: 42140944 -
Nat Commun
Phosphorylation of human glioma-associated oncogene 1 on Ser937 regulates Sonic Hedgehog signaling in medulloblastoma. [Abstract]2024 Feb 2;15(1):987. PMID: 38307877 -
Adv Sci (Weinh)
Primary Cilia Formation Mediated by Hsa_Circ_0005185/OTUB1/RAB8A Complex Inhibits Prostate Cancer Progression by Suppressing Hedgehog Signaling Pathway. [Abstract]2025 Jan 9:e2411675. PMID: 39785769 -
Sci Adv
Noncanonical UPR factor CREB3L2 drives immune evasion of triple-negative breast cancer through Hedgehog pathway modulation in T cells. [Abstract]2025 Jan 10;11(2):eads5434. PMID: 39792663 -
Sci Adv
Yap controls notochord formation and neural tube patterning by integrating mechanotransduction with FoxA2 and Shh expression. [Abstract]2023 Jun 16;9(24):eadf6927. PMID: 37315133
SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 16;9(24):eadf6927. [Abstract]
Representative immunofluorescent images of TdTomato (tdTom) and brachyury (T) at E10.5 in trunk cross sections of indicated genotypes with or without small molecule agonist (SAG, 20 mg/kg; i.p.) treatment. Scale bar, 100 μm.
-
Cell Commun Signal
TGFβ1-induced hedgehog signaling suppresses the immune response of brain microvascular endothelial cells elicited by meningitic Escherichia coli. [Abstract]2024 Feb 15;22(1):123. PMID: 38360663
SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]
qPCR detecting expression alterations of IL-6, MIP-2, and E-selectin in RS218 infected hBMECs with or without SAG pre-treatment (at 10 μM).
SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]
Western blot detecting expression of E-selectin, KRAS and ERK1/2 phosphorylation in RS218 infected hBMECs with or without SAG pre-treatment (at 10 μM).
SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]
IF assays showing the E-selectin and KRAS expression in brains of mice challenged by RS218 with or without SAG (10 mg/kg, i.v.; single dose) pre-treatment. The E-selection and KRAS were stained in red. CD31 was specifically applied for labeling the micro-vessels in green. The cell nucleus was stained in blue with DAPI. Scale bar = 50 μm
-
-
Ecotoxicol Environ Saf
Zearalenone at environmental levels promoted ER- positive breast cancer cell lines through the hedgehog pathway. [Abstract]2025 Aug 6:303:118813. PMID: 40773915 -
Biochem Pharmacol
Identification of pseudolaric acid B as a novel Hedgehog pathway inhibitor in medulloblastoma. [Abstract]2021 Aug:190:114593. PMID: 33964282 -
J Pathol
Transcriptomic profiling reveals the role of Hedgehog signaling as a biomarker and in the pathogenesis of Ménétrier's disease. [Abstract]2025 Nov 6. PMID: 41199529 -
Glia
RXR Gamma Enables Oligodendrocyte Differentiation by Suppressing Sonic Hedgehog Signaling. [Abstract]2026 Jun;74(6):e70151. PMID: 41934103 -
Glia
2021 Jul;69(7):1782-1798. PMID: 33694203 -
Molecules
2017 Dec 31;23(1). pii: E85. PMID: 29301237 -
Cell Rep Methods
2024 May 8:100777. PMID: 38744289 -
Cancer Sci
Transcription factor POU4F2 promotes colorectal cancer cell migration and invasion through hedgehog-mediated epithelial-mesenchymal transition. [Abstract]2021 Oct;112(10):4176-4186. PMID: 34327778 -
J Cell Mol Med
Whole-exome sequencing identified novel variants in CPLANE1 that causes oral-facial-digital syndrome Ⅵ by inducing primary cilia abnormality. [Abstract]2022 Jun;26(11):3213-3222. PMID: 35582950 -
Drug Dev Res
Curcumin mitigates the epithelial-to-mesenchymal transition in biliary epithelial cells through upregulating CD109 expression. [Abstract]2019 Nov;80(7):992-999. PMID: 31403228 -
iScience
Modeling the precise interaction of glioblastoma with human brain region-specific organoids. [Abstract]2024 Feb 5;27(3):109111. PMID: 38390494 -
iScience
Generation of dorsoventral human spinal cord organoids via functionalizing composite scaffold for drug testing. [Abstract]2022 Dec 26;26(1):105898. PMID: 36647382 -
Toxins
2021 Aug 22;13(8):585. PMID: 34437455 -
Sci Rep
2025 Oct 14;15(1):35928. PMID: 41087401 -
J Biomed Mater Res A
GelMA Hydrogel Encapsulating iPSC-Derived Human Spinal Cord Organoids Enhances Neural Regeneration and Restores Motor Function in Rat Spinal Cord Injury. [Abstract]2025 Oct;113(10):e38001. PMID: 41051068 -
Biomedicines
Generation of a Pure Culture of Neuron-like Cells with a Glutamatergic Phenotype from Mouse Astrocytes. [Abstract]2022 Apr 18;10(4):928. PMID: 35453678 -
Development
Enpp1 inhibits ectopic joint calcification and maintains articular chondrocytes by repressing hedgehog signaling. [Abstract]2018 Sep 20;145(18). pii: dev164830. PMID: 30111653
SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Development. 2018 Sep 20;145(18). pii: dev164830. [Abstract]
WT MEF cells are treated with 100 nM SAG, 0.1mM ATP, or 0.1mM NHATP for 10 min (U). p-Creb, total Creb and Tubulin protein levels are detected by Western blotting.
-
J Pharm Biomed Anal
Rapid discovery of cyclopamine analogs from Fritillaria and Veratrum plants using LC-Q-TOF-MS and LC-QqQ-MS. [Abstract]2017 Aug 5:142:201-209. PMID: 28521273 -
-
Mol Brain
Meningitic Escherichia coli α-hemolysin aggravates blood-brain barrier disruption via targeting TGFβ1-triggered hedgehog signaling. [Abstract]2021 Jul 19;14(1):116. PMID: 34281571 -
Exp Eye Res
The effects of pigment epithelium-derived factor and associated peptides on the differentiation of retinal ganglion cells from human-induced pluripotent stem cells. [Abstract]2025 May 21:110440. PMID: 40409357 -
Tissue Cell
The Shh-p38-NFATc1 signaling pathway is essential for osteoclastogenesis during tooth eruption. [Abstract]2024 Nov 28:92:102643. PMID: 39612595 -
bioRxiv
2026 Apr 15:2026.04.09.717542. PMID: 42039637 -
bioRxiv
Neuronal Cell-Cycle Re-entry Defines Divergent Outcomes Through Replication-Dependent DNA Damage in ALS. [Abstract]2026 Feb 16:2026.02.13.705790. PMID: 41756973 -
-
-
-
-
-
-
Solvent & Solubility
H2O : 100 mg/mL (177.63 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (59.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.44 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.44 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (88.81 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[1]. Chen JK, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6. [Content Brief]
[2]. Stanton BZ, et al. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009 Mar;5(3):154-6. [Content Brief]
[3]. Guerrini G, et, al. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec; 233(12): 9799-9811. [Content Brief]
[4]. Lee S, et al. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13. [Content Brief]
[5]. Fish EW, et al. Preaxial polydactyly following early gestational exposure to the smoothened agonist, SAG, in C57BL/6J mice. Birth Defects Res A Clin Mol Teratol. 2016 Nov 1. [Content Brief]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.7763 mL | 8.8813 mL | 17.7626 mL | 44.4066 mL |
| 5 mM | 0.3553 mL | 1.7763 mL | 3.5525 mL | 8.8813 mL | |
| 10 mM | 0.1776 mL | 0.8881 mL | 1.7763 mL | 4.4407 mL | |
| 15 mM | 0.1184 mL | 0.5921 mL | 1.1842 mL | 2.9604 mL | |
| 20 mM | 0.0888 mL | 0.4441 mL | 0.8881 mL | 2.2203 mL | |
| 25 mM | 0.0711 mL | 0.3553 mL | 0.7105 mL | 1.7763 mL | |
| 30 mM | 0.0592 mL | 0.2960 mL | 0.5921 mL | 1.4802 mL | |
| 40 mM | 0.0444 mL | 0.2220 mL | 0.4441 mL | 1.1102 mL | |
| 50 mM | 0.0355 mL | 0.1776 mL | 0.3553 mL | 0.8881 mL | |
| H2O | 60 mM | 0.0296 mL | 0.1480 mL | 0.2960 mL | 0.7401 mL |
| 80 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5551 mL | |
| 100 mM | 0.0178 mL | 0.0888 mL | 0.1776 mL | 0.4441 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Powered by Bioz