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Cat. No.: HY-189826

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AMC-3-221

AMC-3-221 is a cereblon-dependent CDK9 PROTAC degrader with a DC₅₀ of 8 nM (MOLM14 AML cells). AMC-3-221 targets CDK9 with an IC₅₀ of 1.7 nM and a K_d of 4.6 nM. AMC-3-221 decreases MCL-1 and c-MYC protein levels as well as MCL-1, c-MYC, and N-MYC RNA levels. AMC-3-221 induces apoptosis and inhibits proliferation in multiple cancer cell lines. AMC-3-221 exhibits proteasome-dependent CDK9 degradation. AMC-3-221 can be used for research on acute myeloid leukemia (AML).
(Pink: CDK9 ligand (HY-189827); Blue: Cereblon ligand (HY-W093272); Black: linker).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 3106928-52-0
Formule: C₃₅H₃₄Cl₂FN₉O₇
Masse moléculaire:782.60

Stockage:

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

AMC-3-221 Chemical Structure

CAS No.: 3106928-52-0

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

AMC-3-221 is a cereblon-dependent CDK9 PROTAC degrader with a DC₅₀ of 8 nM (MOLM14 AML cells). AMC-3-221 targets CDK9 with an IC₅₀ of 1.7 nM and a K_d of 4.6 nM. AMC-3-221 decreases MCL-1 and c-MYC protein levels as well as MCL-1, c-MYC, and N-MYC RNA levels. AMC-3-221 induces apoptosis and inhibits proliferation in multiple cancer cell lines. AMC-3-221 exhibits proteasome-dependent CDK9 degradation. AMC-3-221 can be used for research on acute myeloid leukemia (AML)^[1]. (Pink: CDK9 ligand (HY-189827); Blue: Cereblon ligand (HY-W093272); Black: linker).

IC₅₀ & Target

^[1]

CDK9/cyclinT1

1.7 nM (IC₅₀)

CDK9

4.6 nM (Kd)

Voir tous les produits spécifiques à Isoform PROTACs :

Voir tous les produits spécifiques à Isoform CDK :

Voir tous les produits spécifiques à Isoform Bcl-2 Family :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-14	IC50	45.8 nM	Antileukemic activity against human MOLM14 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay. Antileukemic activity against human MOLM14 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay.	42828372
MV4-11	IC50	62.1 nM	Antileukemic activity against human MV411 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay. Antileukemic activity against human MV411 AML cells assessed as viability reduction after 48 hrs incubation by alamarBlue assay.	42828372
MOLM-14	DC₅₀	8 nM	Degradation of CDK9 protein in human MOLM14 AML cells incubated 4 hrs by Western blot. Degradation of CDK9 protein in human MOLM14 AML cells incubated 4 hrs by Western blot.	42828372

In Vitro

Cell Cycle RegulationAnti-cancerProtein/Amino Acid MetabolismApoptosis

Cell Cycle Regulation

AMC-3-221 (17 h) inhibits cell-free CDK9/Cyclin T1 kinase activity with an IC₅₀ of 1.7 nM^[1].
AMC-3-221 (1 h) binds to CDK9 with a K_d of 4.6 nM and to CDK2 with a K_d of 120 nM, while showing lower affinity for CDK1, CDK4, CDK5, and CDK6^[1].

Anti-cancer

AMC-3-221 (48 h) inhibits MOLM14 and MV411 AML cell viability with IC₅₀ values of 45.8 nM and 62.1 nM, respectively^[1].

Cell Cycle Regulation

Protein/Amino Acid Metabolism

AMC-3-221 (200 nM; 4 h) selectively reduces CDK9 protein by >95% in MOLM14 AML cells without significantly reducing CDK1, CDK2, CDK4, CDK5, or CDK6^[1].
AMC-3-221 (200 nM; 4 h) reduces MCL-1 and MYC protein levels by >75-90% in MOLM14 AML cells without reducing BCL-2 or BCL-xL^[1].
AMC-3-221 (1-100 nM; 4 h) degrades CDK9 in MOLM14 AML cells with a DC₅₀ of 8 nM^[1].
AMC-3-221 (200 nM; 4 h)-mediated CDK9 degradation in MOLM14 AML cells is proteasome-dependent^[1].

Anti-cancer

Apoptosis

AMC-3-221 (200 nM; 18 h) induces apoptosis/death in MOLM14 AML cells, reducing viable cells by approximately 70%^[1].

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

Western Blot Analysis^[1]

Cell Line:

MOLM14 human AML cells
Concentration:

200 nM
Incubation Time:

4 h
Result:

CDK9 protein was reduced by >95%;
CDK1, CDK2, CDK4, CDK5, and CDK6 were not significantly reduced.\nMCL-1 and MYC protein levels were reduced by >75-90%;
BCL-2 and BCL-xL levels were not reduced.

Western Blot Analysis^[1]

Cell Line:

MOLM14 human AML cells
Concentration:

1, 2, 5, 10, 20, 50, 100 nM
Incubation Time:

4 h
Result:

DC₅₀ for CDK9 protein level was 8 nM.

Western Blot Analysis^[1]

Cell Line:

MOLM14 human AML cells
Concentration:

5 μM (MG-132 (HY-13259)); 200 nM (AMC-3-221)
Incubation Time:

4 h (MG-132); 4 h (AMC-3-221)
Result:

Without MG-132 pretreatment, CDK9 protein was reduced by >80%;
with MG-132 pretreatment, CDK9 protein was not reduced.

Apoptosis Analysis^[1]

Cell Line:

MOLM14 human AML cells
Concentration:

200 nM
Incubation Time:

18 h; 3 h (early Annexin V+ cells)
Result:

Viable cells were reduced by ~70%, with corresponding increases in early and late apoptotic cells.

Related Protocols :

Chemical Information

CAS No. 3106928-52-0
Masse moléculaire 782.60
Formule C₃₅H₃₄Cl₂FN₉O₇
SMILES

FC1=CC2=C(C(N(C3C(NC(CC3)=O)=O)C2=O)=O)C=C1N(CC4)CCN4C(CN5CCC(NC(C6=NNC=C6NC(C7=C(Cl)C=CC=C7Cl)=O)=O)CC5)=O
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]. Chan AM, et al. Proteolysis Targeting Chimera (PROTAC) Linkerology Enhances the CDK-Degradation Selectivity Profile of a Multi-CDK Inhibitor: Discovery of Potent, Anti-Leukemic CDK9 Degraders. ACS Pharmacol Transl Sci. 2026 Aug 28;9(9):2560-2584.

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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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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AMC-3-221

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