2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Apoptosis
  3. RAR/RXR Apoptosis
  4. HX531

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.

For research use only. We do not sell to patients.

HX531 Chemical Structure

HX531 Chemical Structure

CAS No. : 188844-34-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 90 In-stock
Solution
10 mM * 1 mL in DMSO USD 90 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 85 In-stock
10 mg USD 150 In-stock
25 mg USD 330 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

HX531 Related Antibodies

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RXRα RXRβ RXRγ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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[1][2][3].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HX531 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Mesangial cells
Concentration: 2.5 μM
Incubation Time: 30 min
Result: Increased the activity of AP-1, eliminating the anti-apoptotic effect of t-RA.

Western Blot Analysis[2]

Cell Line: FAO
Concentration: 0, 1, 10 μM
Incubation Time: 24 h
Result: Had no significant effect on transcriptional activation induced by PPARα/RXR agonists and molecular expression induced by PPARγ agonists.

Western Blot Analysis[3]

Cell Line: HVP; NHMCs
Concentration: 2.5 μM
Incubation Time: 0, 2, 4, 6, 8, 10 days
Result: Reduced the number and size of lipid droplets, upregulated cell cycle regulators p53, p21Cip1, cyclin D1, Fbxw7, and Skp2, and enhanced the expression of pAMPKα in HVP.
ShRNA lentivirus knockdown of p53 reversed the HX531-induced upregulation of p21Cip1 in HVP.
Suppressed the expression of p21Cip1, p27Kip1, p53, and cyclin D1, while the phosphorylation levels of p44/42 MAPK and p38 MAPK returned to baseline levels under normal glucose conditions in NHMCs.

Cell Cycle Analysis[3]

Cell Line: NHMCs
Concentration: 2.5 μM
Incubation Time: 0, 2, 4, 6, 8, 10 days
Result: Reversed high sugar-induced G0/G1 cell cycle arrest back to normal glucose levels.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: KKAy mouse induced by HF or HC[2]
Dosage: 0.1% and 0.3% food additive, 2 weeks
Administration: Oral
Result: Reduced the body weight of mice, fasting blood glucose, fasting plasma insulin, and insulin tolerance. Increased Rectal temperature, rosed oxygen consumption , and serum leptin levels went up.
Lowered the expression of fatty acid translocase/CD36, increased the expression of β3-adrenergic receptors (β3-AR), and decreased free fatty acids (FFA), TNF-α, and resistin.
Reduced the expression of lipogenic enzymes SREBP1 and SCD1, increased the expression of molecules involved in fatty acid burning like ACO, and molecules that dissipate energy like UCP2, lowered long-chain FA-CoA and triglyceride levels in muscle.
Animal Model: PPARγ deficient mice [2]
Dosage: 0.1% and 0.3% food additive, 3 and 4 weeks
Administration: Oral
Result: Prevented the reoccurrence of high blood sugar and insulin resistance associated with fatty atrophy.
Animal Model: LETO and OLETF rats[3]
Dosage: 10 mg/kg, daily, 30 weeks
Administration: Oral
Result: Suppressed weight gain and reduced the excretion of urinary albumin.Led to G0/G1 cell cycle arrest, inhibited adipocyte hypertrophy, and suppressed the proliferation activity of fat cells.
Molecular Weight

483.56

Formula

C29H29N3O4
CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

O=C(O)C1=CC=C(C2=NC3=CC([N+]([O-])=O)=CC=C3N(C)C4=CC5=C(C(C)(C)CCC5(C)C)C=C42)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (68.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0680 mL 10.3400 mL 20.6800 mL
5 mM 0.4136 mL 2.0680 mL 4.1360 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.17 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.87%

COA (261 KB) HNMR (270 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0680 mL 10.3400 mL 20.6800 mL 51.6999 mL
5 mM 0.4136 mL 2.0680 mL 4.1360 mL 10.3400 mL
10 mM 0.2068 mL 1.0340 mL 2.0680 mL 5.1700 mL
15 mM 0.1379 mL 0.6893 mL 1.3787 mL 3.4467 mL
20 mM 0.1034 mL 0.5170 mL 1.0340 mL 2.5850 mL
25 mM 0.0827 mL 0.4136 mL 0.8272 mL 2.0680 mL
30 mM 0.0689 mL 0.3447 mL 0.6893 mL 1.7233 mL
40 mM 0.0517 mL 0.2585 mL 0.5170 mL 1.2925 mL
50 mM 0.0414 mL 0.2068 mL 0.4136 mL 1.0340 mL
60 mM 0.0345 mL 0.1723 mL 0.3447 mL 0.8617 mL
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HX531 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HX531188844-34-0HX 531HX-531RAR/RXRApoptosisRetinoic acid receptorsRetinoid X receptorsCell cycle arrestFat cellsDiabetesObesityInhibitorinhibitorinhibit

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