9-cis-UAB30
9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly decreases the proliferation, viability, and motility of both patient-derived xenografts (PDXs). 9-cis-UAB30 induced cell-cycle arrest as demonstrated by the significant increase in the percentage of cells in G1 and a decrease in the percentage of cells in S phase by downregulating SKP2 and/or 20S proteasome activity, which leads to increased p27kip1 protein stability. 9-cis-UAB30 downregulates the abundance of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the abundance of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). 9-cis-UAB30 has no adverse effects on the central nervous system and cardiovascular system at the tested dose. 9-cis-UAB30 can be used for the study of neuroblastoma, cutaneous T-cell lymphomas, and breast cancer.
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- CAS No.: 205252-57-9
- 화학식: C20H22O2
- 분자량:294.39
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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
Biological Activity
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Skp2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
820 nM
Compound: 9cUAB30
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Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay
Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay
|
[PMID: 24801499] |
9-cis-UAB30 (0-50 μM, 96 h) induces neurite outgrowth in COA6 cells as low as 10 μM[1].
9-cis-UAB30 (0-100 μM, 96 h) significantly reduces the proliferation and survival rate of COA3 and COA6 cells[1].
9-cis-UAB30 (25-50 μM, 3-7 days) significantly reduces the migration and invasion abilities of COA3 and COA6 cells[1].
9-cis-UAB30 (0-50 μM, 24 h) significantly increases the proportion of G1 phase and decreases the proportion of S phase in COA3 and COA6 cells, indicating that cell cycle arrest occurred at the G1/S transition point[1].
9-cis-UAB30 (0-100 μM, 24-96 h) significantly reduces and effectively targets CD133-positive or CD133-enriched cells in both COA3 and COA6 cells[1].
9-cis-UAB30 (0-50 μM, 7 days) significantly reduces the number of tumor spheroids formed in COA3 and COA6 cells[1].
9-cis-UAB30 (0-25 μM, 72 h) significantly downregulates the mRNA abundance of stem cell markers (Oct4, Nanog, Sox2, nestin) in COA3 and COA6 PDX cells, and upregulates the mRNA abundance of differentiation markers (β3-tubulin, NSE, HOXC9, GAP43)[1].
9-cis-UAB30 (5-50 μM, 42-48 h) significantly inhibits the viability of MyLa and HuT78 cells after 24 and 48 hours of treatment[2].
9-cis-UAB30 exhibits strong inhibitory activity against CTCL cell lines, including MyLa cells (IC50 = 34.7 μM), HuT78 cells (IC50 = 34.7 μM), and HH cells (IC50 = 34.7 μM)[2].
9-cis-UAB30 (10-25 μM, 6-24 h) increases the p27kip1 protein level in MyLa cells, HuT78 cells, and HH cells, while decreasing the SKP2 protein level[2].
9-cis-UAB30 (10-25 μM, 6-24 h) does not change the homeostatic level of p27kip1 mRNA in MyLa cells, HuT78 cells and HH cells, but significantly reduces the level of SKP2 mRNA; CKS1B mRNA is unaffected[2].
9-cis-UAB30 (25 μM, 12-24 h) inhibits 20S proteasome activity, but the effect varied among cell lines: significant inhibition was observed in HuT78 cells at 18-24 h, inhibition was observed in HH cells at 24 h, and no significant effect was observed in MyLa cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:COA3 and COA6 PDX cells
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Concentration:0 μM, 10 μM, 25 μM, 50 μM, 100 μM
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Incubation Time:96 h
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Result:Significantly reduced the proliferation rate of COA3 and COA6 cells.
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Cell Line:COA3 and COA6 PDX cells
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Concentration:0 μM, 10 μM, 25 μM
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Incubation Time:72 h
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Result:Downregulated the mRNA abundance of stem cell markers (Oct 4, Nanog, Sox 2, nestin).
Upregulated the mRNA abundance of differentiation markers (β3-tubulin, NSE, HOXC9, GAP43).
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Cell Line:MyLa cells, HuT78 cells
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Concentration:0 μM, 10 μM, 25 μM
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Incubation Time:72 h
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Result:In MyLa cells, 50 μM reduced cell number within 24 hours; at 48 hours, both 25 μM and 50 μM inhibited cell viability.
In HuT78 cells, 5 μM inhibited cell viability within 24 hours.
| Species | Dose | Route | Note | AUC0-24 | AUC0-∞ | Cmax | Tmax | T1/2 | T1/2 (Elimination) |
|---|---|---|---|---|---|---|---|---|---|
| Dog[3][4] | 10 mg/kg | p.o. | / | 4365.9 ng·h/mL | 5250 ng·h/mL | 1625.63 ng/mL | 2 h | 3.75 h | / |
| Dog[3][4] | 100 mg/kg | p.o. | / | 12802 ng·h/mL | 13421.3 ng·h/mL | 1625.63 ng/mL | 3.5 h | 2.68 h | / |
| Dog[3][4] | 30 mg/kg | p.o. | / | 4191.1 ng·h/mL | 7744.3 ng·h/mL | 566.3 ng/mL | 3.3 h | 4.01 h | / |
| Mice[3][4] | 100 mg/kg | p.o. | Male | / | 34 μg·h/mL | 4.9 μg/mL | 2 h | / | 5.4 h |
| Mice[3][4] | 100 mg/kg | p.o. | Female | / | 40 μg·h/mL | 7.2 μg/mL | 3 h | / | 6.2 h |
| Mice[3][4] | 300 mg/kg | p.o. | Male | / | 49 μg·h/mL | 9.3 μg/mL | 1.5 h | / | 4.5 h |
| Mice[3][4] | 300 mg/kg | p.o. | Female | / | 52 μg·h/mL | 10.6 μg/mL | 2 h | / | 3 h |
9-cis-UAB30 (0-100 mg/kg, p.o., once daily for 28 days) does not produce any toxicity in beagles and has no adverse effects on the central nervous system and cardiovascular system[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 205252-57-9
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분자량 294.39
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화학식 C20H22O2
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SMILES
O=C(O)/C=C(C)/C=C/C=C(C)\C=C1CCCC2=C/1C=CC=C2
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Synonyms
(9Z)-UAB-30
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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]. Marayati R, et al. 9-cis-9-cis-UAB30, a novel rexinoid agonist, decreases tumorigenicity and cancer cell stemness of human neuroblastoma patient-derived xenografts. Transl Oncol. 2021 Jan;14(1):100893. [Content Brief]
[2]. Chou CF, et al. The retinoid X receptor agonist, 9-cis UAB30, inhibits cutaneous T-cell lymphoma proliferation through the SKP2-p27kip1 axis. J Dermatol Sci. 2018 Jun;90(3):343-356. [Content Brief]
[3]. Lindeblad M, et al. Assessment of oral toxicity and safety of 9-cis-UAB30, a potential chemopreventive agent, in rat and dog studies. Drug Chem Toxicol. 2011 Jul;34(3):300-10. [Content Brief]
[4]. Kapetanovic IM, et al. Murine oncogenicity and pharmacokinetics studies of 9-cis-UAB30, an RXR agonist, for breast cancer chemoprevention. Int J Toxicol. 2010 Mar-Apr;29(2):157-64. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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