2. PROTAC Immunology/Inflammation Apoptosis
  3. PROTACs IFNAR c-Myc
  4. dIRF4-2

dIRF4-2 is a selective IRF4 PROTAC degrader with a DC50 value of 2.2 μM. dIRF4-2 forms a ternary complex between IRF4 and CRBN, inducing ubiquitination and proteasomal degradation of IRF4. dIRF4-2 downregulates MYC. dIRF4-2 exhibits anticancer activity against myeloma. dIRF4-2 acts as a chemical probe for investigating IRF4 function, mimicking the IRF4 gene knockout phenotype. dIRF4-2 can be used in the research of multiple myeloma.
(Pink: IFNAR ligand (HY-185698); Blue: Cereblon ligand (HY-14658); Black: linker).

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

dIRF4-2

dIRF4-2 Chemical Structure

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dIRF4-2 Related Antibodies

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Description

dIRF4-2 is a selective IRF4 PROTAC degrader with a DC50 value of 2.2 μM. dIRF4-2 forms a ternary complex between IRF4 and CRBN, inducing ubiquitination and proteasomal degradation of IRF4. dIRF4-2 downregulates MYC. dIRF4-2 exhibits anticancer activity against myeloma. dIRF4-2 acts as a chemical probe for investigating IRF4 function, mimicking the IRF4 gene knockout phenotype. dIRF4-2 can be used in the research of multiple myeloma[1]. (Pink: IFNAR ligand (HY-185698); Blue: Cereblon ligand (HY-14658); Black: linker).

In Vitro

dIRF4-2 (1-20 μM; 24 h) induces dose-dependent proteasomal degradation of IRF4 in MM1.S and OPM2 multiple myeloma cell lines, with DC50 values of 2.2 μM and 2.3 μM respectively after 24 h of treatment[1].
dIRF4-2 (2.5 μM; 2-10 h) induces rapid and sustained degradation of IRF4 (initiated within 2 h), and treatment with 2.5 μM for up to 10 h does not affect the off-target novel substrate IKZF3 in MM1.S and OPM2 multiple myeloma cell lines[1].
dIRF4-2 (2.5 μM; 2 h) induces the degradation of IRF4 in MM1.S multiple myeloma cells, and this degradation process is proteasome-dependent; co-treatment with 1 μM bortezomib or 1 μM MG132 followed by a 2-hour incubation restores IRF4 levels[1].
dIRF4-2 (2.5 μM; 4 h) induces highly selective degradation of IRF4 in MM1.S multiple myeloma cells, and exerts no significant effects on other IRF family members or novel CRBN substrates after 4 h of treatment at 2.5 μM[1].
dIRF4-2 (100 μM three-fold dilution series; 96 h, with second dose at 48 h) induces potent, IRF4-dependent cytotoxicity in all tested multiple myeloma cell lines after 96 h of treatment (IC50 0.68-8 μM), while exerting no effect on IRF4-independent HEK293T cells (IC50 > 50 μM)[1].

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

dIRF4-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: MM1.S, OPM2
Concentration: 1, 2.5, 5, 10, 20 μM
Incubation Time: 24 h
Result: Induced dose-dependent degradation of IRF4 in both MM1.S and OPM2 cell lines.
Reached half-maximal degradation concentration (DC50) of 2.2 μM for MM1.S and 2.3 μM for OPM2.

Western Blot Analysis[1]

Cell Line: MM1.S, OPM2
Concentration: 2.5 μM
Incubation Time: 2, 4, 6, 8, 10 h
Result: Induced rapid depletion of IRF4 within 2 hours, with sustained degradation through 10 hours.
Showed no degradation of the off-target neosubstrate IKZF3 at any timepoint.

Cell Viability Assay[1]

Cell Line: 12 human multiple myeloma cell lines, HEK293T
Concentration: 100 μM three-fold dilution series
Incubation Time: 96 h (with second dose at 48 h)
Result: Exhibited IRF4-dependent cytotoxicity across all multiple myeloma cell lines tested, with IC50 values ranging from 0.68 μM (Karpas-707) to 8 μM (MOLP-2).
Showed no cytotoxicity in non-IRF4-dependent HEK293T cell line, with an IC50 > 50 μM.
Molecular Weight

786.87

Formula

C43H46N8O7
SMILES

COC1=CC=C(C2(CC2)C(N[C@H](C(NC)=O)C3=CC=CC(C4=CN(CCCN5CCN(C6=CC=C(C(N(C7C(NC(CC7)=O)=O)C8=O)=O)C8=C6)CC5)N=C4)=C3)=O)C=C1
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Room temperature in continental US; may vary elsewhere.
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dIRF4-2 Related Classifications

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Help & FAQs
  • 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:

dIRF4-2PROTACsIFNARc-MycInterferon-α/β receptorInterferon-alpha/beta receptor MycOPM2HEK293TIKZF3MYCRPMI-8226myeloma cellsMM1.SIRF4multiple myelomaCRBNInhibitorinhibitorinhibit

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