Art. -Nr.: HY-119264

PRLX-93936

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PRLX-93936 is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 inhibits HIF-1 under hypoxic conditions (IC₅₀ = 0.09 μM in cell-based reporter gene assay). PRLX-93936 suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 is applicable to research related to pancreatic cancer and multiple myeloma.

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Reinheit: 98.31%
CAS. Nr.: 903499-49-0
Formel: C₂₁H₂₄N₄O₂
Molecular Weight:364.44

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

PRLX-93936 Chemical Structure

CAS. Nr.: 903499-49-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Ras Isoform-spezifische Produkte anzeigen :

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
ME-180	IC₅₀	0.09 μM Compound: 16	Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay	[PMID: 21831635]

In Vitro

PRLX-93936 (72 h) selectively inhibits the viability of human cancer cell lines, with the strongest activity observed in pancreatic and head and neck cancer cell lines, and reduces the survival rate of human cancer cell lines with high TRIM21 expression^[1].
PRLX-93936 (500 nM; 30 min-10 h) induces TRIM21-dependent degradation of nuclear pore complex proteins and MCL1 in PANC-1 human pancreatic cancer cells^[1].
PRLX-93936 (500 nM; 30 min) induces TRIM21-dependent ubiquitination of nuclear pore complex proteins in human pancreatic cancer cell line PANC-1 pretreated with MG132 (HY-13259)^[1].
PRLX-93936 (cells are pretreated with 1 μM MG132 for 30 min, followed by treatment with 500 nM PRLX-93936 for 30 min or 2 h, and co-treated with 100 nM biotin for 30 min) induces the translocation of TRIM21 to the nuclear pore complex in human pancreatic cancer cell line PANC-1. Treatment with 500 nM PRLX-93936 for 30 min or 2 h results in close proximity between TRIM21 and nucleoporins such as NUP98^[1].
PRLX-93936 (2 h) acts as a molecular glue that induces a direct, dose-dependent interaction between TRIM21 and NUP98 in HEK293T cells^[1].
PRLX-93936 (for 5 days) potently reduces the viability of cholangiopancreatic organoids with high TRIM21 expression, and induces TRIM21-dependent degradation of nuclear pore complex proteins.
PRLX-93936 (1-10 μM) reduces HIF-1α protein accumulation under hypoxic conditions^[3].

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

In Vivo

PRLX-93936 (50-100 mg/kg, i.p.; 1-2 times daily; 21 days) induces tumor volume reduction in PANC-1 and HS766T pancreatic cancer xenograft mice models, and triggers degradation of nuclear pore complex components in PANC-1 pancreatic cancer xenografts^[1].

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

Animal Model:

NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (female, 6 weeks old, subcutaneous xenograft with 5×10⁶ PANC-1 cells/HS766T cells/PANC-1 cells)^[1]
Dosage:

50, 100 mg/kg
Administration:

i.p.; daily; 21 days/i.p.; two daily doses
Result:

Reduced average tumor volume.
Depleted several nucleoporins (NUP98, NUP96, NUP35) in tumor tissue, confirming on-target degradation of nuclear pore complex components in vivo.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 903499-49-0
Appearance Solid
Molecular Weight 364.44
Formel C₂₁H₂₄N₄O₂
Color White to off-white
SMILES

O=C1N(C(CN2CCNCC2)=NC3=C1C=CC=C3)C4=CC=CC=C4OCC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (274.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7439 mL

13.7197 mL

27.4394 mL

5 mM

0.5488 mL

2.7439 mL

5.4879 mL

10 mM

0.2744 mL

1.3720 mL

2.7439 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (6.86 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (6.86 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yuan L, et al. Defining the Antitumor Mechanism of Action of a Clinical-stage Compound as a Selective Degrader of the Nuclear Pore Complex. Cancer Discov. 2025;15(12):2505-2529. [Content Brief]

[2]. Peter M Voorhees, MD, et al. An Open-Label, Dose Escalation, Multi-Center Phase 1 Study of PRLX 93936, an Agent Synthetically Active Against the Activated Ras Pathway, in the Treatment of Relapsed or Relapsed and Refractory Multiple Myeloma. Volume 124, Issue 21, 6 December 2014, Page 2140.

[3]. Huang W, et al. Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5239-43. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7439 mL	13.7197 mL	27.4394 mL	68.5984 mL
	5 mM	0.5488 mL	2.7439 mL	5.4879 mL	13.7197 mL
	10 mM	0.2744 mL	1.3720 mL	2.7439 mL	6.8598 mL
	15 mM	0.1829 mL	0.9146 mL	1.8293 mL	4.5732 mL
	20 mM	0.1372 mL	0.6860 mL	1.3720 mL	3.4299 mL
	25 mM	0.1098 mL	0.5488 mL	1.0976 mL	2.7439 mL
	30 mM	0.0915 mL	0.4573 mL	0.9146 mL	2.2866 mL
	40 mM	0.0686 mL	0.3430 mL	0.6860 mL	1.7150 mL
	50 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3720 mL
	60 mM	0.0457 mL	0.2287 mL	0.4573 mL	1.1433 mL
	80 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8575 mL
	100 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6860 mL

Keywords

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PRLX-93936

Apoptosis Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Molecular Glue Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Ras Isoform-spezifische Produkte anzeigen

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PRLX-93936 Related Classifications

HY-119264 Related Classifications