MCE products for research use only. We do not sell to patients.

HX531

MCE China：HX531

Brand：MedChemExpress (MCE)

Cat. No.HY-108521

CAS：188844-34-0

Purity：99.87%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：HX531 is an effective RXR antagonist with oral activity, with an IC50 of 18 nM, with activity against black melanoma. HC531 can eliminate the anti-apoptotic effects of all-trans-retinoic acid (t-RA) and exerts anti-obesity and anti-diabetic effects through leptin-dependent pathways and the p53-p21Cip1 pathway, resulting in G0/G1 cell cycle arrest.

In Vitro：HX531 (2.5 μM, 30 min) eliminates the anti-apoptotic effect of t-RA[1]. HX531 (0-10 μM, 24 h) has no significant effect on transcriptional activation induced by PPARα/RXR agonists and molecular expression induced by PPARγ agonists[2]. HX531 (2.5 μM, 0-10 days) upregulates the p53-p21Cip1 pathway, inducing G0/G1 cell cycle arrest and inhibiting the differentiation of human visceral preadipocytes HPV[3]. HX531 (2.5 μM, 0-10 days) reverses high glucose-induced G0/G1 cell cycle arrest to normal glucose levels in normal human mesangial cells (NHMCs)[3]. HX531 delays resistance to melanoma and prevents M2 macrophage polarization in the tumor microenvironment[4].

In Vivo：HX531 (0.1% and 0.3% food additive, oral, for two weeks) prevents weight gain in mice on a high-fat diet and stops high blood sugar and high insulin levels induced by the high-fat diet, while increasing leptin levels[2]. HX531 (0.1% and 0.3% food additive, oral, for two weeks) blocks the enlargement of fat cells and alleviates insulin resistance[2]. HX531 (0.1% and 0.3% food additive, oral, for two weeks) directly antagonizes PPARγ/RXR, reducing molecules involved in fatty acid influx and fat formation in skeletal muscle, while increasing molecules involved in energy expenditure[2]. HX531 (0.1% and 0.3% food additive, oral, for 3-4 weeks) leads to a rebound in high blood sugar and insulin resistance associated with fat atrophy[2]. HX531 (10mg/kg, oral, daily, for 30 weeks) reduces body weight in rats, inhibits fat cell enlargement, and induces G0/G1 cell cycle arrest in fat cells[3].

Hot selling product：Phenylephrine (hydrochloride)  | Sildenafil  | Bepirovirsen  | Cholic acid  | Irinotecan (hydrochloride)  | Chetomin  | Asciminib  | Myristoleic acid  | Fosmanogepix  | Itraconazole

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References：

[1]. Konta T, et al. Selective roles of retinoic acid receptor and retinoid x receptor in the suppression of apoptosis by all-trans-retinoic acid. J Biol Chem. 2001 Apr 20;276(16):12697-701.  [Content Brief]

[2]. Yamauchi T, et al. Inhibition of RXR and PPARgamma ameliorates diet-induced obesity and type 2 diabetes. J Clin Invest. 2001 Oct;108(7):1001-13.  [Content Brief]

[3]. Atsuko Nakatsuka, et al. RXR antagonism induces G0 /G1 cell cycle arrest and ameliorates obesity by up-regulating the p53-p21(Cip1) pathway in adipocytes. J Pathol. 2012 Apr;226(5):784-95.  [Content Brief]

[4]. Wenrui Zhao, et al. RXR signaling targeted cancer therapy. January 2023The Innovation Life 1(1):100014