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ALV2

Katalog-Nr.GC63535 Copy One-Click Copy Product Info

ALV2 ist ein potenter und selektiver Helios-Abbauer. ALV2 bindet CRBN mit einem IC50 von 0,57 μM. Helios ist der Zinkfinger-Transkriptionsfaktor, der einen stabilen Treg-Zell-PhÄnotyp in der Mikroumgebung des entzÜndlichen Tumors aufrechterhalten kann.

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ALV2 Chemische Struktur

Cas No.: 2438124-95-7

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1 mg
130,00 $
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5 mg
405,00 $
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10 mg
720,00 $
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25 mg
1.485,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of ALV2

ALV2 is an effective and selective degrader of Helios (IKZF2). ALV2 binds to CRBN with an IC50 of 0.57μM[1-2]. Helios is a zinc-finger transcription factor that maintains a stable regulatory T cell (Treg) phenotype within the inflammatory tumor microenvironment. ALV2 is used in research investigating the regulation of T cell function and the tumor immune microenvironment[3-4].

In vitro, ALV2 (1μM) was used to pre-treat human naive CD4+ T cells for 5 days, followed by activation with anti-CD3/CD28 antibodies for 2 days. This treatment significantly upregulated the production of CD25 and effector cytokines (such as IL-21 and IFNγ), and enhanced the ability of these cells to infiltrate inflammatory tissues in a human-synovial tissue-mouse chimeric model[5]. In RAW 264.7 murine macrophages infected with Salmonella for 1 hour, ALV2 (10μM; 24-hour treatment) significantly reduced the secretion of tumor necrosis factor-alpha (TNF-α)[6].

In vivo, in a mouse model with the humanized CrbnI391Vgenotype, administration of ALV2 via intraperitoneal injection (100mg/kg; twice daily; for 7 days) significantly reduced the protein levels of Helios (IKZF2) in splenic CD4+ FoxP3+ regulatory T cells (Tregs), without affecting Ikaros (IKZF1) levels[7].

References:
[1] Zhang Y, Li L, Xu J, et al. A Novel Paradigm for Targeting Challenging Targets: Advancing Technologies and Future Directions of Molecular Glue Degraders. Molecules (Basel, Switzerland). 2026 Jan;31(3):459.
[2] Słabicki M, Park J, Nowak RP, et al. Expanding the druggable zinc-finger proteome defines properties of drug-induced degradation. Molecular Cell. 2025 Aug;85(16):3184-3201.e14.
[3] Xue F, Zhang M, Li S, et al. SE(3)-equivariant ternary complex prediction towards target protein degradation. Nature Communications. 2025 Jul;16(1):5514.
[4] Chen Z, Dhruv H, Zhang X, et al. Development of PVTX-405 as a potent and highly selective molecular glue degrader of IKZF2 for cancer immunotherapy. Nature Communications. 2025 May;16(1):4095.
[5] Zhang H, Jadhav RR, Cao W, et al. Aging-associated HELIOS deficiency in naive CD4+ T cells alters chromatin remodeling and promotes effector cell responses. Nat Immunol. 2023 Jan;24(1):96-109.
[6] Santelices J, Schultz A, Walker A, et al. Targeting deubiquitinating enzymes and ubiquitin pathway modulators to enhance host defense against bacterial infections. mBio. 2025 Oct 8;16(10):e0031225.
[7] Wang ES, Verano AL, Nowak RP, et al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.

Protocol of ALV2

Cell experiment [1]:

Cell lines

RAW 264.7 macrophages (a murine macrophage cell line)

Preparation Method

RAW 264.7 macrophages were cultured in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin. For high-throughput screening, cells were seeded into 96-well plates and infected with green fluorescent protein (GFP)-labeled SalmonellaTyphimurium UK-1. Following infection, cells were treated with ALV2 (10μM).

Reaction Conditions

10μM; 2 or 24 hours.

Applications

ALV2 significantly reduced the secretion of TNF-α.

Animal experiment [2]:

Animal models

Humanized CrbnI391Vmice (a mouse model with a CRBN mutation that renders it permissive to IMiD-induced degradation).

Preparation Method

Mice were treated with ALV2 (100mg/kg; twice daily for 7 days) via intraperitoneal injection.

Dosage form

100mg/kg; i.p.; twice daily for 7 days.

Applications

ALV2 administration induced selective and significant degradation of the Helios (IKZF2) protein in splenic CD4+ FoxP3+ regulatory T cells (Tregs).

References:
[1] Santelices J, Schultz A, Walker A, et al. Targeting deubiquitinating enzymes and ubiquitin pathway modulators to enhance host defense against bacterial infections. mBio. 2025 Oct 8;16(10):e0031225.
[2] Wang ES, Verano AL, Nowak RP, et al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.

Chemical Properties of ALV2

Cas No. 2438124-95-7 SDF
Formula C26H26ClN5O5 M.Wt 523.97
Löslichkeit DMSO : 160 mg/mL (305.36 mM; Need ultrasonic)|Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ALV2

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.9085 mL 9.5425 mL 19.0851 mL
5 mM 381.7 μL 1.9085 mL 3.817 mL
10 mM 190.9 μL 954.3 μL 1.9085 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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