DC-34
DC-34 is a selective stabilizer of MYC G-quadruplexes (G4s), with measured Kd values of 9.4 μM (FIA), 1.4 μM (SPR), and 16.5 μM (NMR) across different assays. DC-34 downregulates MYC levels in cancer cells in a G4-dependent manner, reduces cell viability, and induces G0-G1 cell cycle arrest and p16-marked senescence in MYC-driven multiple myeloma cells. DC-34 can serve as a probe for G4-dependent gene regulation studies and is applicable to research on multiple myeloma.
For research use only. We do not sell to patients.
- CAS No.: 1966107-70-9
- Formula: C24H25F3N2O3
- Molecular Weight:446.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AMO1 | IC50 |
5.92 μM
Compound: 28
|
Cytotoxicity against human AMO1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human AMO1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
| CA46 | IC50 |
9.2 μM
Compound: 28
|
Cytotoxicity against human CA46 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human CA46 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
| Fibroblast | IC50 |
19.55 μM
Compound: 28
|
Cytotoxicity against human Fibroblast cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human Fibroblast cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
| HEK-293T | IC50 |
34 μM
Compound: 28
|
Cytotoxicity against human HEK293T cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human HEK293T cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
| KMM-1 | IC50 |
4.13 μM
Compound: 28
|
Cytotoxicity against human KMM-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human KMM-1 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
| KMS-12-PE | IC50 |
5.3 μM
Compound: 28
|
Cytotoxicity against human KMS-12-PE cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human KMS-12-PE cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
| L-363 | IC50 |
3.4 μM
Compound: 28
|
Cytotoxicity against human L-363 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human L-363 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
| NCI-H929 | IC50 |
4.89 μM
Compound: 28
|
Cytotoxicity against human NCI-H929 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human NCI-H929 cells assessed as inhibition of cell viability incubated for 72 hrs by MTS assay
|
[PMID: 33355454] |
DC-34 (up to 100 μM; 24-72 h) inhibits L363 multiple myeloma cell viability with IC50 values of 3.4 μM (24 h), 3.4 μM (48 h), and 3.1 μM (72 h)[1].
DC-34 (0.1-10 μM; 4-72 h) potently and selectively reduces MYC protein levels in L363 multiple myeloma cells (IC50 = 1.9 μM at 24 h) by a MYC G-quadruplex-dependent mechanism, with no effect in cells lacking the MYC G-quadruplex promoter sequence[1].
DC34 (2.5-7.5 μM; 24-48 h) potently downregulates MYC transcription in L363 multiple myeloma cells in vitro in a time- and dose-dependent manner, with minimal effects on other tested G4-driven oncogenes[1].
DC34 (5 μM; up to 75 min) does not affect MYC protein stability in L363 multiple myeloma cells, indicating its inhibitory effect on MYC occurs at the transcriptional level[1].
DC50-34 (5 μM; 48 h) induces G0/G1 cell cycle arrest (63.54% of cells) and senescence marker p16 expression in L363 multiple myeloma cells after 48 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L363 multiple myeloma cells, CA46 Burkitt's lymphoma cells, 293T cells transfected with CMV-MYC plasmid
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Concentration:0.1, 1 and 10 μM
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Incubation Time:4, 24, 48 and 72 h
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Result:At 10 μM, reduced MYC protein levels in L363 cells to 0.4% of untreated levels.
Had an IC50 of 1.9 μM for MYC protein inhibition in L363 cells at 24 h.
Sustained reduced MYC protein levels in L363 cells over 72 h when treated with 5 μM.
Up to 5 μM had no effect on MYC protein levels in CA46 cells (lacking the MYC G-quadruplex promoter) and 293T cells transfected with CMV-MYC (lacking the MYC G-quadruplex).
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Cell Line:L363 multiple myeloma cells
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Concentration:2.5-7.5 μM
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Incubation Time:24 h, 48 h
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Result:Reduced MYC mRNA levels in a time- and dose-dependent manner, with dramatic decreases observed at 5 μM (24 h and 48 h) and 7.5 μM (48 h).
Had significantly weaker effects on the mRNA levels of other G4-driven genes (BCL2, HIF1α, KRAS, VEGFA).
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Cell Line:L363 multiple myeloma cells
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Concentration:5 μM
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Incubation Time:48 h
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Result:Caused 63.54% of L363 cells to accumulate in the G0/G1 phase, compared to 49.37% of untreated cells.
Induced p16 expression, a marker of senescence, especially at high concentrations.
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Cell Line:L363 multiple myeloma cells
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Concentration:5 μM (co-treated with 10 μg/mL Cycloheximide (HY-12320))
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Incubation Time:up to 75 min
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Result:Did not alter the stability of MYC protein over 75 min, as MYC degradation rates were identical in treated and untreated cells.
Chemical Information
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CAS No. 1966107-70-9
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Molecular Weight 446.47
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Formula C24H25F3N2O3
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SMILES
O=C(NC1=CC=C(C=C1)C(F)(F)F)C2=C(OC3=CC=C(O)C(=C32)CN4CCCCCC4)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)