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| | (R)-SKBG-1 Basic information |
| Product Name: | (R)-SKBG-1 | | Synonyms: | (R)-SKBG-1;2-Piperazinecarboxamide, 4-(2-chloroacetyl)-N-[(4-methoxyphenyl)methyl]-1-[(4-methoxyphenyl)sulfonyl]-, (2R)-;(3R)-1-(2-chloroacetyl)-4-(4-methoxycyclohexylsulfonyl)-3-(3-methoxyphenyl) piperidine-2-one | | CAS: | 2955634-67-8 | | MF: | C22H26ClN3O6S | | MW: | 495.98 | | EINECS: | | | Product Categories: | | | Mol File: | 2955634-67-8.mol |  |
| | (R)-SKBG-1 Chemical Properties |
| density | 1.350±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | | storage temp. | -10 to -25°C | | solubility | DMSO: 2mg/mL, clear | | form | Solid | | pka | 13.71±0.20(predicted) | | color | Light yellow to yellow |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | (R)-SKBG-1 Usage And Synthesis |
| Uses | (R)-SKBG-1 is a covalent inhibitor targeting the RNA binding protein NONO. (R)-SKBG-1 can reduce the expression of androgen receptor (AR) and its splice variants, inhibiting cancer cell proliferation. (R)-SKBG-1 inhibits androgen receptor expression with IC50 of 3.1 μM and 5.5 μM for AR-FL mRNA and AR-V7 mRNA, respectively. (R)-SKBG-1 interferes with the gene regulatory network of cancer cells and inhibits cancer cell growth by stabilizing the interaction between NONO and mRNA. (R)-SKBG-1 can be used in the study of cancers related to NONO dysfunction, such as prostate cancer[1][2][3]. | | Biological Activity | Cell permeable high affinity ligand of RNA-binding protein NONO; stabilize NONO–RNA interactions and rapidly reduces the expression of transcripts encoding AR and AR variants.
(R)-SKBG-1 is a cell permeable high affinity ligand of RNA-binding protein NONO th at binds to Cys 145 of NONO and stabilize NONO–RNA interactions. (R)-SKBG-1 rapidly and stereoselectively reduces the expression of transcripts encoding the androgen receptor (AR) and its splice variants in prostate cancer cells. | | References | [1] Kathman SG, et al. Remodeling oncogenic transcriptomes by small molecules targeting NONO. Nat Chem Biol. 2023 Jul;19(7):825-836. DOI:10.1038/s41589-023-01270-0
[2] Takeiwa T, et al. Role of RNA binding proteins of the Drosophila behavior and human splicing (DBHS) family in health and cancer. RNA Biol. 2024 Jan;21(1):1-17. DOI:10.1080/15476286.2024.2332855
[3] Schmeing S, et al. Challenges in Therapeutically Targeting the RNA-Recognition Motif. Wiley Interdiscip Rev RNA. 2024 Nov-Dec;15(6):e1877. DOI:10.1002/wrna.1877 |
| | (R)-SKBG-1 Preparation Products And Raw materials |
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