Art. -Nr.: HY-112134

CSN5i-3

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC₅₀ value of 5.8 nM.

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Reinheit: 99.95%
CAS. Nr.: 2375740-98-8
Formel: C₂₈H₂₉F₂N₅O₂
Molecular Weight:505.56

Speicherung:

-20°C, protect from light, stored under nitrogen

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

CSN5i-3 Chemical Structure

CAS. Nr.: 2375740-98-8

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC₅₀ value of 5.8 nM^[1].

IC₅₀ & Target

IC50: 5.8 nM (CSN5)^[1]

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen :

In Vitro

CSN5i-3 traps CRLs in the neddylated state, which leads to inactivation of a subset of CRLs by inducing degradation of their substrate recognition module^[1].

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

In Vivo

CSN5i-3 shows a good pharmacokinetic profile. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction^[1].

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

Chemical Information

CAS. Nr. 2375740-98-8
Appearance Solid
Molecular Weight 505.56
Formel C₂₈H₂₉F₂N₅O₂
Color White to light yellow
SMILES

O=C(C1=CC(C(F)F)=NN1C(C)C)NC2=CC(C3=CC=CC=C3)=C([C@@H]4N5C(CCC[C@@H]4O)=CN=C5)C=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light, stored under nitrogen

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

Publications (24)

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Journal Impact Factor

Nature

CSN5i-3 is an orthosteric molecular glue inhibitor of COP9 signalosome. [Abstract]

2026 Apr;652(8112):1375-1383. PMID: 41673158
Nature

C-terminal amides mark proteins for degradation via SCF-FBXO31. [Abstract]

2025 Feb;638(8050):519-527. PMID: 39880951
Cell

Systemwide disassembly and assembly of SCF ubiquitin ligase complexes. [Abstract]

2023 Apr 27;186(9):1895-1911.e21. PMID: 37028429
Nat Commun

Unveiling the hidden interactome of CRBN molecular glues. [Abstract]

2025 Jul 24;16(1):6831. PMID: 40707481
Sci Immunol

Pharmacological targeting of NLRP3 deubiquitination for treatment of NLRP3-associated inflammatory diseases. [Abstract]

2021 Apr 30;6(58):eabe2933. PMID: 33931568
Mol Cell

An interactome-based framework for DDB1- and CUL4-associated factor prioritization in targeted protein degradation. [Abstract]

2026 Apr 2;86(7):1397-1416.e11. PMID: 41932313
Mol Cell

E3 ligase autoinhibition by C-degron mimicry maintains C-degron substrate fidelity. [Abstract]

2023 Mar 2;83(5):770-786.e9. PMID: 36805027
Nat Chem Biol

Activity-based profiling of cullin-RING E3 networks by conformation-specific probes. [Abstract]

2023 Dec;19(12):1513-1523. PMID: 37653169
J Clin Invest

Jab1 promotes immune evasion and progression in acute myeloid leukemia models under oxidative stress. [Abstract]

2025 Aug 5:e183761. PMID: 40763038
Int J Biol Sci

A novel CSN5/CRT O-GlcNAc/ER stress regulatory axis in platinum resistance of epithelial ovarian cancer. [Abstract]

2024 Jan 27;20(4):1279-1296. PMID: 38385070
Nat Struct Mol Biol

CAND1 inhibits Cullin-2-RING ubiquitin ligases for enhanced substrate specificity. [Abstract]

2024 Feb;31(2):323-335. PMID: 38177676
Cell Rep

Hormone-mediated disassembly and inactivation of a plant E3 ubiquitin ligase complex. [Abstract]

2024 Oct 3;43(10):114802. PMID: 39365702
Gastric Cancer

COPS5 inhibition synergizes with the antitumor effect of trastuzumab by PTEN upregulation in HER2-amplified gastric cancer. [Abstract]

2025 Oct 2. PMID: 41039054
EMBO Rep

HSC70 coordinates COP9 signalosome and SCF ubiquitin ligase activity to enable a prompt stress response. [Abstract]

2025 Mar;26(5):1344-1366. PMID: 39915298
Structure

CAND1 and CAND2 drive CUL4 substrate receptor exchange with largely comparable biochemical efficiency, unlike their relative effects on CUL1. [Abstract]

2026 Mar 20:S0969-2126(26)00056-0. PMID: 41864201
iScience

A LisH-domain protein interaction map reveals a Lis1-ARIH2-dynein regulatory axis. [Abstract]

2025 Oct 30;28(11):113912. PMID: 41312386
iScience

Cullin-RING E3 ubiquitin ligase 4 regulates neurite morphogenesis during neurodevelopment. [Abstract]

2024 Jan 17;27(2):108933. PMID: 38318354
ACS Chem Biol

Identification and Characterization of Novel Small-Molecule Enhancers of the CUL3LZTR1 E3 Ligase KRAS Complex. [Abstract]

2024 Sep 20;19(9):1942-1952. PMID: 39194017
Biochem Biophys Res Commun

CRL4 mediates autoubiquitination of DDB1 upon deneddylation inhibition. [Abstract]

2025 Oct 30:786:152772. PMID: 41066978
Biochem Biophys Res Commun

Differential dynamics of cullin deneddylation via COP9 signalosome subunit 5 interaction. [Abstract]

2022 Dec 31:637:341-347. PMID: 36423380
bioRxiv

Targeting the COP9 signalosome overcomes platinum resistance in ovarian cancer through two distinct genome stability mechanisms. [Abstract]

2025 Aug 6:2025.08.04.668450. PMID: 40799594
bioRxiv

2025 April 08.
Research Square Preprint

2023 May 3.
bioRxiv

August 09, 2021.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (197.80 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

1.9780 mL

9.8900 mL

19.7800 mL

5 mM

0.3956 mL

1.9780 mL

3.9560 mL

10 mM

0.1978 mL

0.9890 mL

1.9780 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, stored under nitrogen). 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 (4.95 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.95 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

Protokoll

Cell Assay

Cell viability is measured using the CellTiter-Glo Assay. Cells (THP-1, HCT116, NCI-H2030 and TE-1) are treated with CSN5i-3 (1 nM, 10 nM, 100 nM, 1 μM, 10 μM) for 72 hours^[1].

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

Animal Administration^[1]

Mice^[1]

SU-DHL-1 xenografts were grown in SCID-bg mice and dosed by oral administration with either vehicle control or CSN5i-3 at the indicated doses (50 mg/kg BID, 100mg/kg QD) and schedules (3, 7, 10, 14 day). Tumour response is reported as percentage change in tumour volume at the last day of treatment relative to start of treatment.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)

Verweise

[1]. Schlierf A, et al. Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat Commun. 2016 Oct 24;7:13166. [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	1.9780 mL	9.8900 mL	19.7800 mL	49.4501 mL
	5 mM	0.3956 mL	1.9780 mL	3.9560 mL	9.8900 mL
	10 mM	0.1978 mL	0.9890 mL	1.9780 mL	4.9450 mL
	15 mM	0.1319 mL	0.6593 mL	1.3187 mL	3.2967 mL
	20 mM	0.0989 mL	0.4945 mL	0.9890 mL	2.4725 mL
	25 mM	0.0791 mL	0.3956 mL	0.7912 mL	1.9780 mL
	30 mM	0.0659 mL	0.3297 mL	0.6593 mL	1.6483 mL
	40 mM	0.0495 mL	0.2473 mL	0.4945 mL	1.2363 mL
	50 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9890 mL
	60 mM	0.0330 mL	0.1648 mL	0.3297 mL	0.8242 mL
	80 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6181 mL
	100 mM	0.0198 mL	0.0989 mL	0.1978 mL	0.4945 mL

Keywords

CSN5i-3

24 Cited Publications

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CSN5i-3

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CSN5i-3

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CSN5i-3

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CSN5i-3

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CSN5i-3 Related Classifications

HY-112134 Related Classifications