1. PROTAC
    Apoptosis
  2. Ligand for E3 Ligase
    Apoptosis
  3. Cereblon modulator 1

Cereblon modulator 1 

Cat. No.: HY-130800 Purity: 99.51%
Handling Instructions

Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3).

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

Cereblon modulator 1 Chemical Structure

Cereblon modulator 1 Chemical Structure

CAS No. : 1860875-51-9

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Description

Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3)[1][2].

IC50 & Target[1]

Cereblon

 

In Vitro

A different CRBN-binding compound, Cereblon modulator 1 (compound F), that demonstrates anti-proliferative activity in non-AML hematological cancer cell lines (such as multiple myeloma) does not inhibit cell growth in any of the 11 AML cell lines tested, including the ten cell lines that are sensitive to the growth inhibitory activity of Compound D. However, when excess Cereblon modulator 1 is added to KG-1 AML cell cultures in the presence of Compound D, the anti-proliferative activity of Compound D is reduced, presumably due to competition for binding of Compound D to CRBN. The relative impact of Cereblon modulator 1 on the anti-proliferative effect of Compound D progressively increased with increasing concentrations of Cereblon modulator 1. In the presence of 100 µΜ Cereblon modulator 1, the potency of Compound D in inhibiting cell growth reduced by approximately 60-fold, and the potency of Compound D in inducing apoptosis reduced by approximately 40-fold[1].

Molecular Weight

461.85

Formula

C₂₂H₁₈ClF₂N₃O₄

CAS No.

1860875-51-9

SMILES

O=C(NCC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2)=O)C=C1)C(F)(F)C4=CC=C(Cl)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (541.30 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1652 mL 10.8260 mL 21.6521 mL
5 mM 0.4330 mL 2.1652 mL 4.3304 mL
10 mM 0.2165 mL 1.0826 mL 2.1652 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Cereblon modulator 1Cereblon modulator1Cereblon modulator-1Ligand for E3 LigaseApoptosisE3 ligase-recruiting MoietyCRBNIRF4c-mycanti-cancerdegradationproteasome-mediatedIKZF1IKZF3T-lymphocytesInhibitorinhibitorinhibit

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Cereblon modulator 1
Cat. No.:
HY-130800
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