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Cat. No.: HY-119709

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AQ-101

AQ-101 is a MDM2 degrader. Upon binding to MDM2, it blocks the MDM2-MDM4 interaction, inducing autoubiquitination and proteasome-mediated degradation of MDM2. AQ-101 activates p53, upregulates downstream targets including p21 and PUMA, and induces apoptosis and cell cycle arrest in tumor cells. AQ-101 inhibits the progression of acute lymphoblastic leukemia in xenograft animal models. AQ-101 can be used for research related to acute lymphoblastic leukemia.

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

CAS No.: 1353384-61-8
Formula: C₁₆H₁₀ClNO₅
Molecular Weight:331.71

Storage:

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

AQ-101 Chemical Structure

CAS No.: 1353384-61-8

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC50	2.21 μM	Cytotoxicity against human cervical cancer HeLa (p53-repressed) cells assessed by MTT assay after 24 h incubation. Cytotoxicity against human cervical cancer HeLa (p53-repressed) cells assessed by MTT assay after 24 h incubation.	31324563
T98G	IC50	>12.5 μM	Cytotoxicity against human glioblastoma multiforme T98G (mutant p53) cells assessed by MTT assay after 24 h incubation. Cytotoxicity against human glioblastoma multiforme T98G (mutant p53) cells assessed by MTT assay after 24 h incubation.	31324563
K562	IC50	0.93 μM	Cytotoxicity against human leukemia K562 (p53-null) cells assessed by MTT assay after 24 h incubation. Cytotoxicity against human leukemia K562 (p53-null) cells assessed by MTT assay after 24 h incubation.	31324563
MOLT-4	IC50	0.69 μM	Cytotoxicity against human leukemia Molt-4 (wild-type p53) cells assessed by MTT assay after 24 h incubation. Cytotoxicity against human leukemia Molt-4 (wild-type p53) cells assessed by MTT assay after 24 h incubation.	31324563

In Vitro

AQ-101 binds non-covalently to the MDM2 RING domain with a K_d of 0.31 μM, and does not bind to the MDM4 RING domain; it also binds to MDM2 with a K_d of 0.37 μM, and does not bind to MDM4^[1].
AQ-101 (0.25-2 μM; 0-24 h) induces dose-dependent downregulation of MDM2 protein, which starts at 2 h post-treatment, while upregulating p53 expression in EU-1 ALL cells. It reduces the stability of MDM2 protein and increases the stability of p53 protein in EU-1 ALL cells, and the degradation of MDM2 depends on the proteasome pathway^[1].
AQ-101 (0.25-2 μM; 20-24 h) potently induces cytotoxicity in ALL cell lines (Sup-B13, EU-1, EU-3) expressing wild-type p53/MDM2, but shows reduced activity in the ALL cell line expressing mutant p53/MDM2 (EU-6) and the p53-deficient/MDM2-deficient ALL cell line (EU-8); it also exhibits only extremely low cytotoxicity against normal human NBMM cells^[1].
AQ-101 (0.5-1 μM; 10 days) potently inhibits the colony-forming growth of EU-1 ALL cells, shows weak activity against EU-6 and EU-8 ALL cells, and exerts only extremely weak inhibitory effects on the colony-forming growth of normal human NBMM cells^[1].
AQ-101 (24 h) induces cytotoxicity in HeLa, K562, Molt-4 and EU-1 cancer cell lines, with IC₅₀ values ranging from 0.69 µM to 2.21 µM^[2].
AQ-101 (0.5-1 μM; 24 h) potently induces apoptosis in acute lymphoblastic leukemia (ALL) cell lines (Sup-B13, EU-1, EU-3) expressing wild-type p53/MDM2, while its activity is reduced in ALL cell lines expressing mutant p53/MDM2 (EU-6) as well as those with p53 deletion/MDM2 deletion (EU-8)^[1].
AQ-101 (0.5-1 μM; 8 h) induces p53-dependent G₁ cell cycle arrest in wild-type p53 EU-1 acute lymphoblastic leukemia (ALL) cells, and G₂-M cell cycle arrest in mutant p53 EU-6 ALL cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

EU-1 ALL cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Induced remarkable downregulation of MDM2 but not other tested protein levels.

Western Blot Analysis^[1]

Cell Line:

EU-1 ALL cells
Concentration:

0, 0.25, 0.5, 1, 2 μM (dose-response)
1 μM (time-course)
Incubation Time:

8 h
0, 2, 4, 8, 24 h
Result:

Showed the dose-response
(left) and time-course (right) of MDM2 and p53 expression in EU-1 cells treated by
AQ-101.

Real Time qPCR^[1]

Cell Line:

EU-1 ALL cells
Concentration:

1 μM
Incubation Time:

0, 2, 4, 8 h
Result:

Demonstrated no inhibition of MDM2 mRNA expression by AQ‑101; instead, significantly elevated the MDM2 mRNA level upon AQ‑101 exposure.

Cell Viability Assay^[1]

Cell Line:

ALL cell lines (Sup-B13, EU-1, EU-3), mutant p53/MDM2-expressing (EU-6), p53-null/MDM2-null (EU-8) ALL cell lines, Normal human bone marrow mononuclear cells
Concentration:

0.25, 0.5, 1, 2 μM
Incubation Time:

20 h
24 h (NBMM cells)
Result:

Induced apoptosis in wild-type p53/MDM2-expressing ALL cell lines (Sup-B13, EU-1, EU-3).
Reduced activity in mutant p53/MDM2-expressing (EU-6) and p53-null/MDM2-null (EU-8) ALL cell lines.
Exhibited minimal cytotoxicity against normal human NBMM cells.

Apoptosis Analysis^[1]

Cell Line:

ALL cell lines (Sup-B13, EU-1, EU-3)
Concentration:

0.5, 1 μM
Incubation Time:

24 h
Result:

Induced apoptosis in wild-type p53/MDM2-expressing ALL cell lines (Sup-B13, EU-1, EU-3).
Reduced activity in mutant p53/MDM2-expressing (EU-6) and p53-null/MDM2-null (EU-8) ALL cell lines.

Cell Proliferation Assay^[1]

Cell Line:

ALL cell lines (EU-1, EU-6, EU-8)
Concentration:

0.5, 1 μM
Incubation Time:

10 days
Result:

Inhibited clonogenic growth of EU-1 ALL cells, has reduced activity against EU-6 and EU-8 ALL cells.

Cell Cycle Analysis^[1]

Cell Line:

EU-1, EU-1
(+sip53) cells
Concentration:

0.5, 1 μM
Incubation Time:

8 h
Result:

Induced p53-dependent G1 cell-cycle arrest in wild-type p53 EU-1 ALL cells and G2-M cell-cycle arrest in mutant p53 EU-6 ALL cells.

In Vivo

AQ-101 (10-20 mg/kg; i.p.; administered once every 24 hours for 3 days, with repeated dosing after a 4-day interval) increases the survival rate of nude mice inoculated with human acute lymphoblastic leukemia (ALL) xenografts and luciferase-labeled ALL xenografts within 150 days post-inoculation, and eliminates detectable leukemia cells^[1].

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

Animal Model:

Nude mice (5-week-old female; human EU-1 ALL cell line engrafted via tail vein injection of 10⁷ cells/mouse)^[1]
Dosage:

10 mg/kg; 15 mg/kg; 20 mg/kg
Administration:

i.p.; 24-hour intervals for 3 days, repeated after a 4-day rest
Result:

Enabled 62.5% survival rate (5/8 mice) at 10 mg/kg up to 150 days post-inoculation.
Enabled 75% survival rate (6/8 mice) at 15 mg/kg up to 150 days post-inoculation.
Achieved 100% survival rate (8/8 mice) at 20 mg/kg up to 150 days post-inoculation.
Prevented detection of human ALL blasts in peripheral blood and human β-globin gene via PCR at 20 mg/kg.
Allowed weight gain throughout observation period across all doses.

Animal Model:

SCID mice (5-week-old female; luciferase-transfected human EU-1 ALL cell line engrafted via tail vein injection of 10⁷ cells/mouse)^[1]
Dosage:

10 mg/kg; 15 mg/kg; 20 mg/kg
Administration:

i.p.; 24-hour intervals for 3 days, repeated after a 4-day rest
Result:

Enabled 60% survival rate (3/5 mice) at 10 mg/kg up to 150 days post-inoculation.
Enabled 80% survival rate (4/5 mice) at 15 mg/kg up to 150 days post-inoculation.
Achieved 100% survival rate (5/5 mice) at 20 mg/kg up to 150 days post-inoculation.
Eliminated detectable leukemia via bioluminescence imaging at 20 mg/kg.
Allowed weight gain throughout observation period across all doses.

Chemical Information

CAS No. 1353384-61-8
Molecular Weight 331.71
Formula C₁₆H₁₀ClNO₅
SMILES

O=C1C=2C=CC=C(O)C2C(=O)C3=C(O)C=C(C=C13)NC(=O)CCl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Gu L, et al. Inhibition of MDM2 by a Rhein-Derived Compound AQ-101 Suppresses Cancer Development in SCID Mice. Molecular cancer therapeutics. 2018 Feb;17(2):497-507.

[2]. Draganov AB, et al. Upregulation of p53 through induction of MDM2 degradation: Anthraquinone analogs. Bioorganic & medicinal chemistry. 2019 Sep 01;27(17):3860-3865. [Content Brief]

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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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