Cat. No.: HY-180654

JWZ-8-103

Name: JWZ-8-103
Brand: MedChemExpress
SKU: HY-180654
Price: 590.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Customer Review

Based on 1 Customer Validation

JWZ-8-103 is an orally active analog of PRLX-93936 (HY-119264) and a molecular glue targeting TRIM21. JWZ-8-103 increases the thermal stability of TRIM21. JWZ-8-103 promotes rapid and efficient interaction between TRIM21 and NUP98 (the apparent EC₅₀ for ternary complex formation with the PRYSPRY domain of TRIM21 and the APD domain of NUP98 is approximately 20 μM), induces extensive ubiquitination and proteasomal degradation of numerous adjacent nucleoporins (NUPs, and thereby triggers cellular apoptosis. JWZ-8-103 can be used for the research of pancreatic cancer.

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

Purity: 98.04%
CAS No.: 3110272-60-8
Formula: C₂₁H₂₂ClFN₄O₂
Molecular Weight:416.88

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

JWZ-8-103 Chemical Structure

CAS No.: 3110272-60-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

apparent EC₅₀ = ∼20 μM (ternary complex formation between TRIM21 PRYSPRY and NUP98 APD in the presence of JWZ-8-103)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
PANC-1	IC50	9.5 nmol/L	Reduction of cell viability against wild-type PANC-1 human pancreatic cancer cells assessed via CellTiter-Glo luminescent assay after 72 h incubation. Reduction of cell viability against wild-type PANC-1 human pancreatic cancer cells assessed via CellTiter-Glo luminescent assay after 72 h incubation.	40891634
PANC-1	IC50	>10 μmol/L	Reduction of cell viability against TRIM21 knockout PANC-1 human pancreatic cancer cells assessed via CellTiter-Glo luminescent assay after 72 h incubation. Reduction of cell viability against TRIM21 knockout PANC-1 human pancreatic cancer cells assessed via CellTiter-Glo luminescent assay after 72 h incubation.	40891634
NCI-H661	IC50	<10 nmol/L	Reduction of cell viability against TRIM21-overexpressing H661 human lung cancer cells assessed via CellTiter-Glo luminescent assay after 72 h incubation. Reduction of cell viability against TRIM21-overexpressing H661 human lung cancer cells assessed via CellTiter-Glo luminescent assay after 72 h incubation.	40891634

In Vitro

JWZ-8-103 (10-100 μM; 1 h) enhances the thermal stability of TRIM21 protein in PANC-1 cell lysates^[1].
JWZ-8-103 (10 μM; 1 h) functions to promote the interaction between TRIM21 and NUP98 in lysates of PANC-1 cells with TRIM21 knockout and Flag-TRIM21 re-expression^[1].
JWZ-8-103 (100 nM; 6 h) broadly induces TRIM21-dependent nucleoporin degradation in wild-type PANC-1 cells^[1].
JWZ-8-103 (up to 10 μM; monitored continuously for up to 2 h) rapidly induces the proximity interaction between TRIM21 and NUP98 in HEK293T cells, and confirms that there is no direct interaction between TRIM21 and MCL1^[1].
JWZ-8-103 (20 μM; for approximately 1 h) promotes the direct binding between TRIM21 PRYSPRY and GST-NUP98 APD in purified proteins in vitro^[1].
JWZ-8-103 (15-20 nM; 21-22 days) exhibits significant cytotoxicity in PANC-1 cells, and this effect depends on specific amino acid binding sites on TRIM21^[1].
JWZ-8-103 (0.5 μM; 6 h) blocks mRNA nuclear export and causes the retention of MCL1 and c-MYC transcripts in the nucleus in PANC-1 cells^[1].
JWZ-8-10 (2-24 h) exhibits significant differential toxicity in PANC-1 and non-malignant RPE1-hTERT cells: transient treatment induces irreversible cell death in PANC-1 cells, while RPE1-hTERT cells survive and recover^[1].
JWZ-8-103 (72 h) exhibits potent anti-proliferative activity in wild-type PANC-1 cells (IC₅₀ = 9.5 nM) and TRIM21-overexpressing H661 cells (IC₅₀ < 10 nM), but loses this activity in TRIM21-knockout cells^[1].
JWZ-8-103 (for 5 days) exhibits potent activity in inhibiting cell viability and degrading NUP98, GLE1 and MCL1 proteins in TRIM21-highly expressed pancreaticobiliary organoids (HCMI PDOs, including PDM-30, PDM-31, PDM-39, PDM-166), but shows no efficacy in low-expression models^[1].
JWZ-8-103 (0.1-5 μM; 6 h) exhibits activity that induces substantial degradation of nuclear pore complex proteins and short-lived anti-apoptotic proteins in PANC-1, KP3, Hs766T, and MIA PaCa-2 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

PANC-1, KP3, Hs766T, MIA PaCa-2 cells
Concentration:

6 h, 24 h
Incubation Time:

0.1, 0.5, 1, 5 μM
Result:

Induced a marked decrease in downstream nuclear pore target proteins and short-lived transcript-derived proteins, accompanied by observed cleavage/activation of Caspase-3, Caspase-7, and PARP at 24 hours.

Immunofluorescence^[1]

Cell Line:

PANC-1 cells
Concentration:

6 h
Incubation Time:

0.5 μM
Result:

Resulted in severe abnormal nuclear retention of mRNAs encoding key pro-survival factors (MCL1 and c-MYC), demonstrating a clear blockade of nucleocytoplasmic transport.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_last	CL	F
Mice^[1]	1 mg/kg	i.v.	2.00 h	0.08 h	2.61 μM	2.13 μM·h	17.87 mL/min/kg	/
Mice^[1]	3 mg/kg	i.p.	2.02 h	0.25 h	2.78 μM	6.17 μM·h	18.27 mL/min/kg	/
Mice^[1]	6 mg/kg	p.o.	2.32 h	1.67 h	2.12 μM	8.89 μM	24.45 mL/min/kg	74.0 %

In Vivo

JWZ-8-103 (15-50 mg/kg; i.p.; once daily; for 21 consecutive days) significantly inhibits tumor growth and effectively induces targeted degradation of the nuclear pore complex in the PANC-1 pancreatic cancer xenograft model^[1].
JWZ-8-103 (15 mg/kg; i.p.; once daily; for 21 consecutive days) induces near-complete tumor regression in HS766T pancreatic cancer xenograft models with good tolerability^[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 of PANC-1 human pancreatic cancer cells)^[1]
Dosage:

15 mg/kg; 50 mg/kg
Administration:

i.p.; once daily; 21 days
Result:

Reduced mean tumor volume to 71 mm³ (87.0% reduction vs. vehicle) at 15 mg/kg.
Reduced mean tumor volume to 77 mm³ (85.8% reduction vs. vehicle) at 50 mg/kg.
Achieved tumor regression relative to baseline at both doses.
Depleted nuclear pore complex proteins (NUPs) in tumor tissue collected 2 hours after the second daily dose.
Was well tolerated with no signs of toxicity.

Animal Model:

NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (female, 6 weeks old, subcutaneous xenograft of HS766T human pancreatic cancer cells)^[1]
Dosage:

15 mg/kg
Administration:

i.p.; once daily; 21 days
Result:

Reduced mean tumor volume to 0.5 mm³ (>99% reduction vs. vehicle), representing near-complete tumor regression.
Was well tolerated with no evidence of body weight loss.

Chemical Information

CAS No. 3110272-60-8
Appearance Solid
Molecular Weight 416.88
Formula C₂₁H₂₂ClFN₄O₂
Color White to off-white
SMILES

CCOC1=CC(Cl)=CC=C1N2C(C3=CC(F)=CC=C3N=C2CN4CCNCC4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (239.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.3988 mL

11.9939 mL

23.9877 mL

5 mM

0.4798 mL

2.3988 mL

4.7975 mL

10 mM

0.2399 mL

1.1994 mL

2.3988 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (6.00 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 (6.00 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 (6.00 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

References

[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 discovery. 2025 Dec 02;15(12):2505-2529. [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	2.3988 mL	11.9939 mL	23.9877 mL	59.9693 mL
	5 mM	0.4798 mL	2.3988 mL	4.7975 mL	11.9939 mL
	10 mM	0.2399 mL	1.1994 mL	2.3988 mL	5.9969 mL
	15 mM	0.1599 mL	0.7996 mL	1.5992 mL	3.9980 mL
	20 mM	0.1199 mL	0.5997 mL	1.1994 mL	2.9985 mL
	25 mM	0.0960 mL	0.4798 mL	0.9595 mL	2.3988 mL
	30 mM	0.0800 mL	0.3998 mL	0.7996 mL	1.9990 mL
	40 mM	0.0600 mL	0.2998 mL	0.5997 mL	1.4992 mL
	50 mM	0.0480 mL	0.2399 mL	0.4798 mL	1.1994 mL
	60 mM	0.0400 mL	0.1999 mL	0.3998 mL	0.9995 mL
	80 mM	0.0300 mL	0.1499 mL	0.2998 mL	0.7496 mL
	100 mM	0.0240 mL	0.1199 mL	0.2399 mL	0.5997 mL

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JWZ-8-103

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

JWZ-8-103 Related Classifications

HY-180654 Related Classifications

Bioz