2. PROTAC
  3. Ligands for E3 Ligase
  4. CRBN ligand-898

CRBN ligand-898 is a CRBN ligand with a Kd of 216 nM. CRBN ligand-898 binds to CRBN, and when incorporated into proteolysis targeting chimeras (PROTACs), mediates degradation of intended target proteins. CRBN ligand-898 does not induce degradation of IMiD-associated neosubstrates Ikaros (IKZF1) and Aiolos (IKZF3). CRBN ligand-898 can be used to synthesize PROTACs.

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CRBN ligand-898

CRBN ligand-898 Chemical Structure

CAS No. : 2766178-72-5

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CRBN ligand-898 Related Antibodies

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B

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Description

CRBN ligand-898 is a CRBN ligand with a Kd of 216 nM. CRBN ligand-898 binds to CRBN, and when incorporated into proteolysis targeting chimeras (PROTACs), mediates degradation of intended target proteins. CRBN ligand-898 does not induce degradation of IMiD-associated neosubstrates Ikaros (IKZF1) and Aiolos (IKZF3). CRBN ligand-898 can be used to synthesize PROTACs[1].

IC50 & Target[1]

Cereblon

216 nM (Kd)

Cereblon

183 nM (IC50)

In Vitro

CRBN ligand-898 (Compound 2) binds to CRBN with an IC50 of 183 nM and a Kd of 216 nM[1].
CRBN ligand-898 does not inhibit hERG, NaV1.5, Kv4.3 with IC50 >40 μM, or CaV (IC50 >100 μM) ion channels, and does not induce cytotoxicity in THP-1 cells (IC50 >250 μM)[1].
CRBN ligand-898 (1-10 μM; 24 h) does not degrade Ikaros or Aiolos in NB-4 human leukaemia cells[1].
CRBN ligand-898 (0.0001-30 μM; 6 h) dose-dependently inhibits IMiD- and PROTAC-induced Aiolos degradation in HiBiT-IKZF3 MM.1S cells, confirming CRBN engagement and cell permeability[1].
CRBN ligand-898 (1 μM; 24 h) does not reduce levels of any proteins, including IMiD neosubstrates, in NB-4 human leukaemia cells when treated at 1 μM for 24 h[1].

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

CRBN ligand-898 Related Antibodies

Western Blot Analysis[1]

Cell Line: NB-4 human leukaemia cells
Concentration: 1, 10 μM
Incubation Time: 24 h
Result: Did not reduce protein levels of Ikaros or Aiolos at either tested concentration.
In Vivo

CRBN ligand-898 (Compound 2) (10-100 mg/kg; p.o.; single dose) results in dose-dependent plasma exposure and does not induce degradation of the IMiD neosubstrates Ikaros or Aiolos in spleen tissue in CrbnI391V knock mice[1].

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

Animal Model: CrbnI391V knock C57BL/6N (wild-type)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Showed no degradation of Ikaros or Aiolos in spleen tissue.
Exhibited dose-dependent increases in plasma Cmax, reaching 250 µmol/L at 100 mg/kg.
Exhibited dose-dependent increases in plasma AUC, reaching 800 µmol·h/L at 100 mg/kg.
Molecular Weight

229.23

Formula

C12H11N3O2
CAS No.
SMILES

O=C1NC(CCN1C2=CC3=C(C=CN3)C=C2)=O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CRBN ligand-898 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CRBN ligand-8982766178-72-5CRBN ligand898CRBN ligand 898Ligands for E3 LigaseE3 ligase-recruiting MoietyCereblonIkaroshematopoietic stem and progenitor cellAiolosIKZF3proteolysis targeting chimerasIKZF1PROTACsTHP-1 cellsCRBNInhibitorinhibitorinhibit

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