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製品番号: HY-115569

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DC-34

DC-34 is a selective stabilizer of MYC G-quadruplexes (G4s), with measured K_d 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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1966107-70-9
分子式: C₂₄H₂₅F₃N₂O₃
分子量:446.47

保管条件:

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

DC-34 構造式

CAS 番号: 1966107-70-9

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Cellular Effect

Cell Line	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]

体外実験

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.

Western Blot Analysis^[1]

Cell Line:

L363 multiple myeloma cells, CA46 Burkitt's lymphoma cells, 293T cells transfected with CMV-MYC plasmid
Concentration:

0.1, 1 and 10 μM
Incubation Time:

4, 24, 48 and 72 h
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).

Real Time qPCR^[1]

Cell Line:

L363 multiple myeloma cells
Concentration:

2.5-7.5 μM
Incubation Time:

24 h, 48 h
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).

Cell Cycle Analysis^[1]

Cell Line:

L363 multiple myeloma cells
Concentration:

5 μM
Incubation Time:

48 h
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.

Western Blot Analysis^[1]

Cell Line:

L363 multiple myeloma cells
Concentration:

5 μM (co-treated with 10 μg/mL Cycloheximide (HY-12320))
Incubation Time:

up to 75 min
Result:

Did not alter the stability of MYC protein over 75 min, as MYC degradation rates were identical in treated and untreated cells.

Related Protocols :

化学情報

CAS 番号 1966107-70-9
分子量 446.47
分子式 C₂₄H₂₅F₃N₂O₃
SMILES

O=C(NC1=CC=C(C=C1)C(F)(F)F)C2=C(OC3=CC=C(O)C(=C32)CN4CCCCCC4)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Calabrese DR, et al. Chemical and structural studies provide a mechanistic basis for recognition of the MYC G-quadruplex. Nature communications. 2018 Oct 12;9(1):4229. [Content Brief]

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