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Cat. No.: HY-119884

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DC-120

Name: DC-120
Brand: MedChemExpress
SKU: HY-119884
Availability: PreOrder

DC-120 is an ATP-competitive AKT inhibitor, with particular activity against AKT1 (an IC₅₀ of 0.153 μM). DC-120 functionally blocks AKT kinase activity and reduces the phosphorylation levels of FOXO3a and GSK-3β. DC-120 induces cancer cell apoptosis (apoptosis) and inhibits cancer cell proliferation. DC-120 activates the mTORC1 pathway via the Ca²⁺/calmodulin (calmodulin)/hVps34 signaling pathway. DC-120 abrogates AKT-mediated inhibition of CRAF, thereby activating the MEK/ERK MAPK pathway. DC-120 exerts anti-tumor activity in a nude mouse hepatocellular carcinoma xenograft model. DC-120 can be used for hepatocellular carcinoma-related research.

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CAS No.: 1261080-40-3
화학식: C₁₈H₁₈Cl₂N₆OS
분자량:437.35

보관:

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

DC-120 Chemical Structure

CAS No.: 1261080-40-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

Akt1

0.153 μM (IC₅₀)

All Akt Isoforms :

All FOXO Isoforms :

FOXO1
FOXO3

All GSK-3 Isoforms :

All Calmodulin Isoforms :

All Raf Isoforms :

All MEK Isoforms :

All ERK Isoforms :

All mTOR Isoforms :

In Vitro

Anti-cancerApoptosis

Anti-cancer

DC-120 (0.1-1 μM) potently and selectively inhibits AKT1 kinase activity in a cell-free system, with an IC₅₀ of 0.153 μM, while exerting no significant inhibitory effect on PKA, PKC, ADCK3, CSNK1D or DYRK1B kinases^[1].
DC-120 (1.25-40 μM; 72 h) inhibits the proliferation of HepG2, SMMC7721, Bel7402 and Huh7 hepatocellular carcinoma cells in a dose-dependent manner, with IC₅₀ values ranging from 7.73 to 13.32 μM. It exhibits selectivity over normal LO2 hepatocytes (IC₅₀ 62.99 μM), exerts growth inhibitory effects in an AKT-dependent manner, and shows stronger activity in PTEN-deficient cells^[1].
DC-120 (5-20 μM; 0-24 h) activates the mTORC1 pathway in HepG2 and Bel7402 hepatocellular carcinoma cells via an AKT inhibition-dependent increase in intracellular Ca²⁺ levels; this elevation of Ca²⁺ enhances the phosphorylation of P70S6K and 4E-BP1 through the Ca²⁺/CaM/hVps34 axis^[1].
DC-120 (5-20 μM; 6-24 h) activates the MEK/ERK MAPK pathway in HepG2 and Bel7402 hepatocellular carcinoma cells by reducing the inhibitory phosphorylation of C-Raf at the Ser259 site^[1].

Anti-cancer

Apoptosis

DC₅₀-120 (5-20 μM; 6-48 h) inhibits AKT pathway signaling by reducing the phosphorylation levels of FOXO3a and GSK-3β (while increasing the phosphorylation levels of AKT Ser⁴⁷³/Thr³⁰⁸), and induces dose-dependent apoptosis in HepG2 and Bel7402 hepatocellular carcinoma cells^[1].
Pretreatment with RAD001 (HY-10218) (1 μM; 1 h) or U0126 (HY-12031A) (20 μM; 1 h) synergistically enhances the apoptosis-inducing effect of DC-120 (10 μM; 48 h) on HepG2 and Bel7402 hepatocellular carcinoma cells, increasing the apoptosis rate by approximately 2-fold compared with DC-120 monotherapy^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HepG2, SMMC7721, Bel7402, Huh7, LO2
Concentration:

1.25, 2.5, 5, 10, 20, 40 μM
Incubation Time:

72 h
Result:

Inhibited cell viability in a dose-dependent manner across all tested liver cancer cell lines.
Exhibited IC₅₀ values of 10.43 μM for HepG2, 12.51 μM for SMMC7721, 7.73 μM for Bel7402, 13.32 μM for Huh7, and 62.99 μM for normal LO2 liver cells.

Western Blot Analysis^[1]

Cell Line:

HepG2, Bel7402
Concentration:

5, 10, 20 μM
Incubation Time:

6 h
Result:

Reduced phosphorylation of AKT downstream substrates FOXO3a and GSK-3β, while increasing phosphorylation of AKT at Ser473 and Thr308 in a dose-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

HepG2, Bel7402
Concentration:

5, 10, 20 μM
Incubation Time:

48 h
Result:

Induced apoptosis in a dose-dependent manner: at 20 μM, the proportion of apoptotic cells (sub-G1 phase) reached 59.4% in HepG2 and 53.6% in Bel7402.
Induced early apoptosis (Annexin V-positive, PI-negative) reaching 14% in HepG2 and 28.7% in Bel7402 at 10 μM.
Induced Annexin V/PI-double positive cells reaching 75.8% in HepG2 and 67.3% in Bel7402 at 20 μM.
Induced dose-dependent cleavage of caspase-3 and PARP.

Western Blot Analysis^[1]

Cell Line:

HepG2, Bel7402
Concentration:

5-20 μM (dose-dependent analysis); 10 μM (time-dependent analysis)
Incubation Time:

6, 12, 24 h (time-dependent analysis)
Result:

DC-120 activated the MEK/ERK pathway in a dose- and time-dependent manner, as shown by increased phosphorylation of ERK1/2 and MEK.
DC-120 reduced phosphorylation of C-Raf at Ser259 in a dose- and time-dependent manner.
DC-120-induced ERK1/2 phosphorylation was blocked by pretreatment with U0126.

In Vivo

Anti-cancerApoptosis

Anti-cancer

Apoptosis

DC-120 (10-20 mg/kg, i.p.; daily administration; for 21 consecutive days) dose-dependently inhibits the growth of hepatocellular carcinoma xenografts, while regulating the AKT, mTORC1 and MAPK signaling pathways and inducing tumor cell apoptosis in vivo^[1].

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

Animal Model:

BALB/C nude (female)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; daily; 21 days
Result:

Achieved tumor growth inhibitory rates of 37.5% at 10 mg/kg and 56.7% at 20 mg/kg.
Increased phosphorylation of AKT at Ser473 and Thr308, while dramatically suppressing phosphorylation of AKT downstream substrates GSK3β, FOXO3a, and PRAS40.
Increased phosphorylation of P70S6K and 4E-BP1 (mTORC1 pathway markers) and activated ERK1/2 (MAPK pathway marker).
Stimulated a substantial increase in TUNEL-positive apoptotic tumor cells at 20 mg/kg.
Caused no toxicity based on body weight measurements.

Related Protocols :

Chemical Information

CAS No. 1261080-40-3
분자량 437.35
화학식 C₁₈H₁₈Cl₂N₆OS
SMILES

O=C(N[C@H](CN)CC1=C(Cl)C=C(C=C1)Cl)C2=CN=C(S2)C3=NC(NC)=NC=C3
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Yang F, et al. Feedback loops blockade potentiates apoptosis induction and antitumor activity of a novel AKT inhibitor DC120 in human liver cancer. Cell death & disease. 2014 Mar 13;5(3):e1114. [Content Brief]

Calculators

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Mass Mass

Concentration Concentration

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Molecular Weight Molecular Weight

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

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100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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DC-120

All Akt Isoforms

All FOXO Isoforms

All GSK-3 Isoforms

All Calmodulin Isoforms

All Raf Isoforms

All MEK Isoforms

All ERK Isoforms

All mTOR Isoforms