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Art. -Nr.: HY-187439

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Truly-4

Truly-4 is a bifunctional Rpn13 PROTAC and CRBN ByeTAC degrader. Degradation of Rpn13 relies on CRBN-mediated E3 ubiquitin ligase activity, while degradation of CRBN itself proceeds via a ByeTAC mechanism of action. Truly-4 induces selective cytotoxicity in hematological cancer cells and solid cancer cells, but not in healthy cells, despite comparable levels of Rpn13 depletion in both cell types. Truly-4 can be used in studies related to B-cell lymphoma and triple-negative breast cancer.
(Pink: Rpn13 ligand (HY-159808); Blue: Cereblon ligand (HY-139539); Black: linker (HY-W008352)).

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Formel: C₄₃H₄₄BrClN₈O₁₀S
Molecular Weight:980.28

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Truly-4 Chemical Structure

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
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Classifications
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Biologische Aktivität

Beschreibung

Truly-4 is a bifunctional Rpn13 PROTAC and CRBN ByeTAC degrader. Degradation of Rpn13 relies on CRBN-mediated E3 ubiquitin ligase activity, while degradation of CRBN itself proceeds via a ByeTAC mechanism of action. Truly-4 induces selective cytotoxicity in hematological cancer cells and solid cancer cells, but not in healthy cells, despite comparable levels of Rpn13 depletion in both cell types. Truly-4 can be used in studies related to B-cell lymphoma and triple-negative breast cancer^[1]. (Pink: Rpn13 ligand (HY-159808); Blue: Cereblon ligand (HY-139539); Black: linker (HY-W008352)).

IC₅₀ & Target^[1]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

Truly-4 (0.5-10 μM; 18 h) induces concentration-dependent degradation of CRBN (via E-ligase-independent ByeTAC mechanism) and Rpn13 (via ubiquitin-dependent PROTAC mechanism) in Ramos B-cell lymphoma cells, with 10 μM treatment reducing CRBN to 48% and Rpn13 to 35% of baseline levels after 18 h^[1].
Truly-4 (0.5-10 μM; 18 h) induces concentration-dependent degradation of CRBN and Rpn13 in MDA-MB-468 triple-negative breast cancer cells, with 10 μM treatment reducing CRBN to 56% and Rpn13 to 39% of baseline levels after 18 h^[1].
Truly-4 (0.001-100 μM; 48 h) induces selective cytotoxicity in Ramos B-cell lymphoma and MDA-MB-468 triple-negative breast cancer cells after 48 h incubation, with no significant toxicity observed in HEK-293T or MRC-5 nonmalignant cells^[1].
Truly-4 (0.5-10 μM; 18 h) induces concentration-dependent degradation of Rpn13 but does not degrade CRBN in HEK-293T nonmalignant cells, with CRBN levels remaining stable or slightly elevated^[1].

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

Western Blot Analysis^[1]

Cell Line:

Ramos B-cell lymphoma suspension cells
Concentration:

0.5, 1 and 10 μM (18 h incubation); 10 μM (18 h incubation with co-reagents); 25 μM (2 h co-immunoprecipitation; 18 h incubation with pre-treatment reagents); 10 μM (4, 8, 48 h time-course)
Incubation Time:

18 h (0.5-10 μM; 10 μM with co-reagents; 25 μM with pre-treatment reagents); 2 h (25 μM co-immunoprecipitation); 4, 8, 48 h (10 μM time-course)
Result:

Reduced CRBN levels to 88% and Rpn13 levels to 76% of baseline at 0.5 μM.
Reduced CRBN to 52% and Rpn13 to 60% of baseline at 1 μM.
Reduced CRBN to 48% and Rpn13 to 35% of baseline at 10 μM.
Fully abrogated degradation of both CRBN and Rpn13 when co-treated with 20 nM proteasome inhibitor MG-132.
Rescued Rpn13 degradation but did not affect CRBN degradation when co-treated with 10 nM ubiquitin-activating enzyme inhibitor TAK-243 or 10 nM NEDD8-activating enzyme inhibitor MLN4924.
Increased ubiquitinated Rpn13 levels by 51% relative to control at 25 μM.
Blocked CRBN degradation but modestly enhanced Rpn13 degradation when pre-treated with 25 μM Rpn2 peptide.
Attenuated degradation of both proteins when pre-treated with 25 μM TCL1 or immunomodulatory imide drug thalidomide.
Induced rapid and sustained degradation of both proteins over 48 h in time-course experiments.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468 triple-negative breast cancer adherent cells
Concentration:

0.5, 1 and 10 μM
Incubation Time:

18 h
Result:

Reduced CRBN levels to 72% and Rpn13 levels to 61% of baseline at 0.5 μM.
Reduced CRBN to 65% and Rpn13 to 64% of baseline at 1 μM.
Reduced CRBN to 56% and Rpn13 to 39% of baseline at 10 μM.

Western Blot Analysis^[1]

Cell Line:

HEK-293T nonmalignant adherent cells
Concentration:

0.5, 1 and 10 μM
Incubation Time:

18 h
Result:

Reduced Rpn13 levels to 71% of baseline (CRBN levels remained at 100%) at 0.5 μM.
Reduced Rpn13 to 51% of baseline (CRBN levels increased to 117%) at 1 μM.
Reduced Rpn13 to 49% of baseline (CRBN levels increased to 112%) at 10 μM.

Cell Viability Assay^[1]

Cell Line:

Ramos B-cell lymphoma, MDA-MB-468 triple-negative breast cancer, HEK-293T nonmalignant, MRC-5 nonmalignant fibroblast cells
Concentration:

0.001, 0.1, 1, 10 and 100 μM
Incubation Time:

48 h
Result:

Induced potent cytotoxicity in Ramos and MDA-MB-468 cancer cells, with viability dropping to near 0% at 100 μM.
Caused no measurable loss of viability in HEK-293T and MRC-5 nonmalignant cells even at the highest concentration tested.

Chemical Information

Molecular Weight 980.28
Formel C₄₃H₄₄BrClN₈O₁₀S
SMILES

O=C(NCCOCCOCCOCCOCCNC(C1=CC2=C(C(N(C2=O)C3CCC(NC3=O)=O)=O)C=C1)=O)CC4SC5=NN=C(N5N=C4C6=CC=C(C=C6)Cl)CC7=CC=C(C=C7)Br
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Loy CA, et al. Two Mechanisms One Molecule: Developing a 'Truly' Bifunctional Degrader Targeting Rpn13 and CRBN. Journal of the American Chemical Society. 2026 Jul 29;148(29):30850-30860.

Calculators

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)}

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.

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MOQ

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100 mg

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Biologische Aktivität
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- IC₅₀ & Target
- In Vitro
Chemical Information
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Truly-4

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Truly-4 Related Classifications

HY-187439 Related Classifications

Bioz