9-cis-UAB30  (Synonyms: (9Z)-UAB-30)

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^[1][2][3].

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.

9-cis-UAB30 (0-100 mg/kg, p.o., once daily for 28 days) primarily targets the liver in rats. The no-observed-adverse-effect level (NOAEL) with repeated 28-day administration is 3 mg/kg/day, while doses of 15-100 mg/kg show some hepatotoxicity^[3].
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.

294.39

C₂₀H₂₂O₂

205252-57-9

O=C(O)/C=C(C)/C=C/C=C(C)\C=C1CCCC2=C/1C=CC=C2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.

  [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.

  [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.

  [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.