BS148
BS148 is a selective sigma-2 receptor (S2R) agonist with a Ki 20 nM. BS148 shows >80-fold selective for S2R than S1R. BS148 activates the endoplasmic reticulum stress response through the upregulation of protein kinase R-like ER kinase (PERK), activating transcription factor 4 (ATF4) genes, and C/EBP homologous protein (CHOP). BS148 induces apoptosis in melanoma cell. BS148 downregulates genes related to the cholesterol pathway and activates the MAPK signaling pathway. BS148 can be used for the study of melanoma.
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- CAS No.: 2162116-09-6
- 화학식: C21H31NS2
- 분자량:361.61
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Sigma Receptor Isoforms
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Biological Activity
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Sigma 2 Receptor 20 nM (Ki) |
Sigma 1 Receptor 540 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-MEL-28 | IC50 |
22 μM
Compound: 10
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Anti-proliferative against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Anti-proliferative against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 36202063] |
| SK-MEL-28 | IC50 |
52 μM
Compound: 10
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Anti-proliferative against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Anti-proliferative against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 36202063] |
Chemical Information
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CAS No. 2162116-09-6
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분자량 361.61
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화학식 C21H31NS2
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SMILES
N1(CC2SC3(CCCCC3)SC2)CCC(CC4=CC=CC=C4)CC1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Claudia Sorbi, et al. BS148 Reduces the Aggressiveness of Metastatic Melanoma via Sigma-2 Receptor Targeting. Int J Mol Sci. 2023 Jun 2;24(11):9684. [Content Brief]
[2]. Franchini S, et al. Structure-Activity Relationships within a Series of σ1 and σ2 Receptor Ligands: Identification of a σ2 Receptor Agonist (BS148) with Selective Toxicity against Metastatic Melanoma. ChemMedChem. 2017 Nov 22;12(22):1893-1905. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BS148 Related Classifications
HY-121033 Related Classifications
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