Cat. No.: HY-187997

ADAR1-IN-2

ADAR1-IN-2 is an adenosine analog and an orally active ADAR1 inhibitor with antiproliferative activity against multiple ADAR1-dependent cancer cell lines. ADAR1-IN-2 inhibits ADAR1-mediated A‑to‑I editing of partial RNA substrates (APOBEC3D), thereby activating the RIG‑I/MDA5‑MAVS signaling pathway, inducing G0/G1 cell cycle arrest and apoptosis in tumor cells, and suppressing tumor cell migration and invasion. ADAR1-IN-2 inhibits tumor growth in DU-145 and HUCCT1 xenograft models. ADAR1-IN-2 can be used in research related to cancers such as prostate cancer and breast cancer.

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Formule: C₁₀H₁₁ClFN₅O₂
Masse moléculaire:287.68

Stockage:

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

ADAR1-IN-2 Chemical Structure

Stock

Quantité

Amount: USD 0.00

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Use of MCE Products

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	IC50	0.04 μM	Antiproliferative activity against human prostate cancer DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human prostate cancer DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
PC-3	IC50	402.03 nM	Antiproliferative activity against human cancer PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human cancer PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
HCC1806	IC50	576.83 nM	Antiproliferative activity against human cancer HCC-1806 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human cancer HCC-1806 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
HCT-116	IC50	74.83 nM	Antiproliferative activity against human cancer HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human cancer HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
HuCCT-1	IC50	145.10 nM	Antiproliferative activity against human cancer HUCCT1 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human cancer HUCCT1 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
TPC1	IC50	258.93 nM	Antiproliferative activity against human cancer TPC1 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human cancer TPC1 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
AGS	IC50	170.90 nM	Antiproliferative activity against human cancer AGS cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human cancer AGS cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
HGC-27	IC50	75.88 nM	Antiproliferative activity against human cancer HGC27 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against human cancer HGC27 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
HCC1806	IC50	0.58 μM	Antiproliferative activity against ADAR1-dependent human cancer HCC1806 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against ADAR1-dependent human cancer HCC1806 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
MDA-MB-468	IC50	0.61 μM	Antiproliferative activity against ADAR1-dependent human cancer MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against ADAR1-dependent human cancer MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917
MCF7	IC50	270.14 μM	Antiproliferative activity against ADAR1-independent human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay. Antiproliferative activity against ADAR1-independent human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by Cell Counting Kit-8 assay.	42593917

In Vitro

ADAR1-IN-2 (H13) (72 h) potently inhibits the proliferation of human prostate cancer DU-145 cells with an IC₅₀ of 0.04 μM, and exhibits broad-spectrum antiproliferative activity across a variety of human cancer cell lines, with the strongest activity observed in HCT116 (74.83 nM) and HGC27 (75.88 nM) cells; additionally, it shows significantly higher antiproliferative activity in ADAR1-dependent HCC1806 and MDA-MB-468 cells than in ADAR1-independent MCF-7 cells^[1].
ADAR1-IN-2 (50-200 nM; followed by 10 days of culture) inhibits colony formation of human prostate cancer DU-145 cells in a dose-dependent manner^[1].
ADAR1-IN-2 (0.1-100 μM; 4 h) dose-dependently enhances the stability of ADAR1 in lysates of human prostate cancer DU-145 cells^[1].
ADAR1-IN-2 (50-200 nM; 48 h) selectively and dose-dependently reduces ADAR1-mediated A-to-I editing of APOBEC3D in human prostate cancer DU-145 cells^[1].
ADAR1-IN-2 (50-200 nM; 48 h) induces G0/G1 cell cycle arrest in human prostate cancer DU-145 cells, which correlates with decreased expression of CDK2 and phosphorylated RB; it also induces apoptosis in a dose-dependent manner, accompanied by increased expression levels of activated Caspase-3, activated Caspase-7, and activated PARP1^[1].
ADAR1-IN-2 (50-200 nM; 48 h) dose-dependently inhibits migration and invasion of human prostate cancer DU-145 cells, which is associated with downregulated expression of N-cadherin^[1].

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

Real Time qPCR^[1]

Cell Line:

human prostate cancer DU-145 cells
Concentration:

50, 100, 200 nM
Incubation Time:

48 h
Result:

Dose-dependently and significantly reduced A-to-I editing levels of the ADAR1 substrate APOBEC3D, without affecting editing levels of other tested substrates (AZIN1, MDM2, GLI1).

Western Blot Analysis^[1]

Cell Line:

human prostate cancer DU-145 cells
Concentration:

50, 100, 200 nM
Incubation Time:

48 h
Result:

Increased levels of cleaved Caspase-3, cleaved Caspase-7, and cleaved PARP1.

Apoptosis Analysis^[1]

Cell Line:

human prostate cancer DU-145 cells
Concentration:

50, 100, 200 nM
Incubation Time:

48 h
Result:

Dose-dependently triggered apoptosis.

Cell Cycle Analysis^[1]

Cell Line:

human prostate cancer DU-145 cells
Concentration:

50, 100, 200 nM
Incubation Time:

48 h
Result:

Induced G0/G1 phase cell cycle arrest in DU-145 cells, accompanied by reduced levels of CDK2 and phosphorylated RB.

Cell Migration Assay ^[1]

Cell Line:

human prostate cancer DU-145 cells
Concentration:

50, 100, 200 nM
Incubation Time:

48 h
Result:

Dose-dependently inhibited migration of human prostate cancer DU-145 cells.

Cell Invasion Assay^[1]

Cell Line:

human prostate cancer DU-145 cells
Concentration:

50, 100, 200 nM
Incubation Time:

48 h
Result:

Dose-dependently inhibited invasion of human prostate cancer DU-145 cells.

Cell Proliferation Assay^[1]

Cell Line:

human prostate cancer DU-145 cells
Concentration:

50, 100, 200 nM
Incubation Time:

exposed to compounds for 48 h and cultured for 10 days
Result:

Dose-dependently inhibited colony formation of human prostate cancer DU-145 cells.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t	AUC_0-∞	MRT_0-∞	T_1/2	T_max	F	CL	V_ss
Mice^[1]	5 mg/kg	i.v.	3603.33 ng/mL	1163.66 ng·h/mL	1167.84 ng·h/mL	0.21 h	1.00 h	/	/	4.33 L/h/kg	0.91 L/kg
Mice^[1]	10 mg/kg	p.o.	2053.33 ng/mL	744.06 ng·h/mL	749.58 ng·h/mL	0.71 h	1.01 h	0.25 h	31.97 %	/	/

In Vivo

ADAR1-IN-2 (H13) (5-10 mg/kg; p.o.; twice daily) potently inhibits the growth of HUCCT1 cholangiocarcinoma xenografts and DU-145 prostate cancer xenografts, while the 5 mg/kg dose activates the RIG-I/MDA5-MAVS signaling pathway in HUCCT1 cholangiocarcinoma tissues^[1].

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

Animal Model:

BALB/c nu/nu (male, 3-4 weeks old, implanted
with DU-145 cells, compounds were formulated with 2.5% Tween 80 and 97.5% water)^[1]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

p.o.; bid
Result:

Showed no effect on DU-145 xenograft growth at 5 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 86.52% by the end of the experiment at 10 mg/kg.

Animal Model:

BALB/c nu/nu (male, 3-4 weeks old, implanted
with HUCCT1 cells, compounds were formulated with 2.5% Tween 80 and 97.5% water)^[1]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

p.o.; bid
Result:

Dose-dependently delayed HUCCT1 xenograft growth; at 10 mg/kg, mean tumor volume showed minimal increase throughout the experiment.
Significantly activated the RIG-I/MDA5-MAVS signaling pathway in HUCCT1 xenografts at 5 mg/kg.

Related Protocols :

Chemical Information

Masse moléculaire 287.68
Formule C₁₀H₁₁ClFN₅O₂
SMILES

NC1=NC(F)=NC2=C1N=CN2[C@H]3C[C@H](O)[C@@H](CCl)O3
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Wei A, et al. Discovery of Deoxyadenosine Analogues as an Orally Bioavailable ADAR1 Modulator. Journal of medicinal chemistry. 2026 Aug 13;69(15):18147-18161.

Calculators

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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.

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ADAR1-IN-2