SML0573
Ro 41-5253
≥98% (HPLC)
别名:
4-(2-(7-(Heptyloxy)-3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)-1-propenyl)-Benzoic acid, S,S-dioxide, 4-[(1E)-2-[7-(Heptyloxy)-3,4-dihydro-4,4-dimethyl-1,1-dioxido-2H-1-benzothiopyran-6-yl]-1-propen-1-yl]-benzoic acid, 4-[2-(7-Heptoxy-4,4-dimethyl-1,1-dioxo-2,3-dihydrothiochromen-6-yl)prop-1-enyl]benzoic acid, GR110, LG-629, RO 415253, Ro41-5253
SMILES string
[S]1(=O)(=O)CCC(c2c1cc(c(c2)\C(=C\c3ccc(cc3)C(=O)O)\C)OCCCCCCC)(C)C
InChI
1S/C28H36O5S/c1-5-6-7-8-9-15-33-25-19-26-24(28(3,4)14-16-34(26,31)32)18-23(25)20(2)17-21-10-12-22(13-11-21)27(29)30/h10-13,17-19H,5-9,14-16H2,1-4H3,(H,29,30)/b20-17+
InChI key
JEIWQRITHXYGIF-LVZFUZTISA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
−20°C
Quality Level
Application
Ro 41-5253 has been used as a retinoic acid receptor-α (RAR-α) antagonist to study its effect on hepatitis B virus (HBV) infection.
Biochem/physiol Actions
Ro 41-5253 ( GR110) is a potent (IC50 = 16 nM) and selective retinoic acid receptor-α (RARα) antagonist, with some recently discovered activity as a PPARγ agonist at 50-fold higher concentrations (EC50 = 810 nM).
Ro 41-5253 ( GR110) is a potent (IC50 = 16 nM) and selective retinoic acid receptor-α (RARα) antagonist, with some recently discovered activity as a PPARγ agonist at 50-fold higher concentrations (EC50 = 810 nM). Ro 41-5253 inhibited differentiation and prevented the loss of human HSCs that otherwise occurs in short-term culture.
Ro 41-5253 is a member of an interesting class of retinoids with anti-proliferative properties. It can repress the activity of retinoic acid receptor-α (RAR-α) in rat embryonic gonad culture. Ro 41-5253 can decrease the expression stimulated by the retinoic acid gene 8 (STRA8) gene. It can prevent multiplication and stimulate apoptosis in breast cancer cell lines.
Features and Benefits
This compound is featured on the Nuclear Receptors (Non-Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
S Toma et al.
International journal of cancer, 78(1), 86-94 (1998-09-02)
Ro 41-5253 is a RARalpha-selective antagonist that binds RARalpha but does not induce transcriptional activation and does not influence RAR/RXR heterodimerization and DNA binding. This retinoid inhibits proliferation and induces apoptosis in MCF-7 and ZR-75.1 estrogen-receptor-positive breast-carcinoma cells in a
Yuehong Tao et al.
FEMS immunology and medical microbiology, 47(3), 444-450 (2006-07-29)
We investigated the effects of all-trans-retinoic acid on dendritic cells derived from human cord blood monocytes to clarify how vitamin A affects immune function in children. Monocytes were separated from 18 cord blood samples, and dendritic cells were differentiated by
Ingo Stuckmann et al.
Developmental biology, 255(2), 334-349 (2003-03-22)
We have established a heart slice primary culture, which allows us to mechanically separate distinct cardiac cell populations and assay their relative mitogenic and trophic effects on cardiac myocyte proliferation and survival. Using this system, we have found that a
J Hamzah et al.
Acta tropica, 87(3), 345-353 (2003-07-24)
Retinol (vitamin A alcohol) may have a beneficial role in the host response to malaria in humans and previously published data have suggested that it has a direct inhibitory effect on the growth of Plasmodium falciparum in vitro. To further
P E Lovat et al.
European journal of cancer (Oxford, England : 1990), 33(12), 2075-2080 (1998-03-28)
We investigated the potential for 9-cis-retinoic acid in the differentiation therapy of neuroblastoma using an N-type neuroblastoma cell line, SH SY 5Y, as an experimental model. In these cells, 9-cis-retinoic acid is more effective than other isomers at inducing the
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