2. PROTAC MAPK/ERK Pathway GPCR/G Protein Apoptosis Metabolic Enzyme/Protease
  3. Molecular Glues Ras Apoptosis HIF/HIF Prolyl-Hydroxylase
  4. PRLX-93936

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.

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

PRLX-93936

PRLX-93936 Chemical Structure

CAS No. : 903499-49-0

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Description

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[1][2][3].

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.

PRLX-93936 Related Antibodies
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
Molecular Weight

364.44

Formula

C21H24N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7439 mL 13.7197 mL 27.4394 mL
5 mM 0.5488 mL 2.7439 mL 5.4879 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 (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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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V2

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 (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.

    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 (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.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

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

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
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 (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.

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
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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:

PRLX-93936903499-49-0PRLX93936PRLX 93936Molecular GluesRasApoptosisHIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHmolecular Gluespancreatic cancermultiple myelomaPANC-1 human pancreatic cancer cellsHEK293T cellsNOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ miceInhibitorinhibitorinhibit

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