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CRBN-DDB1 Protein, Human (sf9, His, Avi)

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CRBN-DDB1, CUL4, and Rbx1 form an E3 ubiquitin ligase complex. CRBN-DDB1 is necessary for lenalidomide (HY-A0003) and pomalidomide (HY-10984) to exert T cell immunomodulatory functions and upregulate IL-2 and TNF-α. CRBN-DDB1 mediates the anti-proliferative and cell cycle arrest effects of both classes of drugs in myeloma cells and regulates p21WAF1 expression. CRBN-DDB1 can serve as a molecular glue platform to recruit novel small molecule degraders and target kinases such as WEE1 and CK1α. CRBN-DDB1 protein, Human (sf9, His, Avi) is a recombinant CRBN-DDB1 protein expressed from Sf9 insect cells with N-His, N-Avi tags.

For research use only. We do not sell to patients.
  • Species: Human
  • Source: Sf9 insect cells
  • Storage:
    Stored at -80°C for 1 year from date of receipt. It is stable at -20°C for 3 months after opening. It is recommended to freeze aliquots at -80°C for extended storage. Avoid repeated freeze-thaw cycles.
  • CRBN-DDB1 Protein, Human (sf9, His, Avi) Product Image
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609-228-6898
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Find Your Local Distributor Your local distributor: Hycultec GmbHHycultec
  • Biological Activity
  • Technical Parameters
  • Product Properties
  • Documentation
  • References
  • Help & FAQs
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Use of MCE Products

Biological Activity

Description

CRBN-DDB1, CUL4, and Rbx1 form an E3 ubiquitin ligase complex. CRBN-DDB1 is necessary for lenalidomide (HY-A0003) and pomalidomide (HY-10984) to exert T cell immunomodulatory functions and upregulate IL-2 and TNF-α. CRBN-DDB1 mediates the anti-proliferative and cell cycle arrest effects of both classes of drugs in myeloma cells and regulates p21WAF1 expression. CRBN-DDB1 can serve as a molecular glue platform to recruit novel small molecule degraders and target kinases such as WEE1 and CK1α. CRBN-DDB1 protein, Human (sf9, His, Avi) is a recombinant CRBN-DDB1 protein expressed from Sf9 insect cells with N-His, N-Avi tags[1][2][3].

Background

CRBN-DDB1 constitutes a functional CUL4-Rbx1 E3 ubiquitin ligase complex and represents the direct protein target of thalidomide, lenalidomide and pomalidomide. CRBN-DDB1 binds lenalidomide and pomalidomide with significantly higher affinity than thalidomide and exhibits no binding to phthalimide. CRBN-DDB1 acts as a drug-dependent substrate adaptor that promotes the ubiquitination and proteasomal degradation of IKZF1 and IKZF3 upon lenalidomide treatment. CRBN-DDB1 is essential for the immunomodulatory effects of lenalidomide and pomalidomide in T cells, including the upregulation of IL-2 and TNF-α. CRBN-DDB1 mediates the antiproliferative and cell cycle inhibitory activities of lenalidomide and pomalidomide in multiple myeloma cells through induction of p21WAF1. CRBN-DDB1 expression level directly determines myeloma cell sensitivity and resistance to immunomodulatory imide drugs. CRBN-DDB1 serves as a universal molecular glue platform capable of recruiting novel small-molecule degraders targeting kinases such as WEE1 and CK1α[1][2][3].

In Vitro

CRBN-DDB1 Protein, Human (2 μg) combines with lenalidomide, pomalidomide and thalidomide in fluorescence thermal melt assay. The IC50 values of Lenalidomide (HY-A0003), Pomalidomide (HY-10984) and Thalidomide (HY-14658) are approximately 3 μM, 3 μM and 30 μM respectively[3].

Verified Bioactivity

Fluorescence polarization (FP) assay determined the dissociation constant (Kd) of CRBN/DDB1 with thalidomide to be approximately 82 nM.

Technical Parameters

  • Species Human
  • Source Sf9 insect cells
  • Tag N-His;N-Avi
  • Accession

    Q96SW2-1 (M1-L442)&Q16531-1 (M1-H1140)

  • Gene ID
    51185&1642
  • Synonyms

    CRBN; MRT2; Prev. MRT2A; Protein X 0001; Protein Cereblon; Cereblon; Mental Retardation, Non-Syndromic, Autosomal Recessive, 2A; DDB1; XPE-BF; Damage Specific DNA Binding Protein 1; XAP-1; DNA Damage-Binding Protein 1; XAP1; Xeroderma Pigmentosum Group E-

  • Predicted Molecular Mass

    55.3 kDa (CRBN) & 126.9 kDa (DDB1)

  • Molecular Weight

    Approximately 55 kDa (CRBN) & 120 kDa (DDB1), based on SDS-PAGE under reducing conditions.

  • Purity

    ≥ 90%, as determined by reducing SDS-PAGE.

Product Properties

Appearance

Solution

Formulation

Supplied as a 0.22 μm filtered solution of 50 mM HEPES, pH 7.5, 200 mM NaCl, 10% glycerol.

Endotoxin Level

<1 EU/μg, determined by LAL method.

Reconstitution

Please use rapid thawing with running water to thaw the protein.

Storage & Stability

Stored at -80°C for 1 year from date of receipt. It is stable at -20°C for 3 months after opening. It is recommended to freeze aliquots at -80°C for extended storage. Avoid repeated freeze-thaw cycles.

Shipping

Shipping with dry ice.

References

[1]. Lopez-Girona A, et al. Direct Binding with Cereblon Mediates the Antiproliferative and Immunomodulatory Action of Lenalidomide and Pomalidomide. Blood. 2011 Nov 18;118(21):738.

[2]. Krönke J, et al. Lenalidomide Promotes CRBN-Mediated Ubiquitination and Degradation of IKZF1 and IKZF3. Blood. 2013 Nov 15;122(21):LBA-5.

[3]. Razumkov H, et al. Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library. Journal of the American Chemical Society, 2024, 146(46): 31433-31443.

Calculators

Reconstitution Calculator

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Dilution Calculator

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The Specific Activity Calculator Equation
  • Specific Activity (Unit/mg)
  • Biological Activity (ED50)

Specific Activity (Unit/mg) = 106 ÷ Biological Activity (ED50)

Specific Activity (Unit/mg) Specific Activity (Unit/mg)
Unit/mg
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ng/mL
MOQ
Minimum order quantity
100 mg

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Measured by its ability to inhibit anti-CD3-induced proliferation of stimulated CTLL-2 mouse cytotoxic T cells. The ED50 this effect is 0.8023 μg/ml, corresponding to a specific activity is 1246.42 units/mg.

Assay Types
  • CRBN-DDB1 Protein, Human (sf9, His, Avi) Product Image
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  • CRBN-DDB1 Protein, Human (sf9, His, Avi) Product Image