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Art. -Nr.: HY-149962

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PROTAC CDK9 degrader-5

PROTAC CDK9 degrader-5 is a PROTAC degrader that specifically targets CDK9. PROTAC CDK9 degrader-5 degrades CDK9, with DC₅₀ values of 0.10 μM and 0.14 μM for the CDK9₄₂ and CDK9₅₅ isoforms, respectively. PROTAC CDK9 degrader-5 induces ubiquitination of CDK9 followed by proteasomal degradation. PROTAC CDK9 degrader-5 reduces the expression levels of the short-lived pro-survival proteins MCL-1 and c-Myc. PROTAC CDK9 degrader-5 can be used for research related to acute myeloid leukemia.
(Pink: CDK9/Cyclin T ligand (HY-50940); Blue: Cereblon ligand (HY-103597); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2935587-89-4
Formel: C₄₂H₄₈Cl₂N₈O₉
Molecular Weight:879.78

Speicherung:

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

Data Sheet (272 KB)

PROTAC CDK9 degrader-5 Chemical Structure

CAS. Nr.: 2935587-89-4

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Preis

Verfügbarkeit

Menge

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC CDK9 degrader-5 is a PROTAC degrader that specifically targets CDK9. PROTAC CDK9 degrader-5 degrades CDK9, with DC₅₀ values of 0.10 μM and 0.14 μM for the CDK9₄₂ and CDK9₅₅ isoforms, respectively. PROTAC CDK9 degrader-5 induces ubiquitination of CDK9 followed by proteasomal degradation. PROTAC CDK9 degrader-5 reduces the expression levels of the short-lived pro-survival proteins MCL-1 and c-Myc. PROTAC CDK9 degrader-5 can be used for research related to acute myeloid leukemia^[1]. (Pink: CDK9/Cyclin T ligand (HY-50940); Blue: Cereblon ligand (HY-103597); Black: linker).

IC₅₀ & Target

^[1]

CDK9₄₂

0.10 μM (DC₅₀)

CDK9₅₅

0.14 μM (DC₅₀)

Mcl-1

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	0.04 μM Compound: 15e	Anticancer activity against human MOLM-13 cells assessed as cell growth inhibition measured after 48 hrs by MTS assay Anticancer activity against human MOLM-13 cells assessed as cell growth inhibition measured after 48 hrs by MTS assay	[PMID: 37071962]
MV4-11	EC₅₀	0.4 μM Compound: 15e	Anticancer activity against human MV4-11 cells assessed as cell growth inhibition for 6 hrs followed by compound washout measured after 24 hrs by Annexin V/Propidium iodide staining based flow cytometric analysis Anticancer activity against human MV4-11 cells assessed as cell growth inhibition for 6 hrs followed by compound washout measured after 24 hrs by Annexin V/Propidium iodide staining based flow cytometric analysis	[PMID: 37071962]

In Vitro

Anti-cancerApoptosisCell Cycle Regulation

Anti-cancer

PROTAC CDK9 degrader-5 (48 h) exhibits antiproliferative activity in Molm-13 acute myeloid leukemia (AML) cells with an IC₅₀ of 0.21 μM^[1].

Anti-cancer

Apoptosis

PROTAC CDK9 degrader-5 (0.01-10 μM; 6 h + 24 h post-exposure assessment) exhibits cytotoxic activity in MV4-11 acute myeloid leukemia (AML) cells with an EC₅₀ of 0.4 μM and has a unique effect on the downstream pro-survival proteins MCL-1 and c-Myc^[1].

Anti-cancer

Cell Cycle Regulation

PROTAC CDK9 degrader-5 (Compd 15e) (1 μM; 1-6 h, 6 h + post-washout up to 48 h) potently degrades CDK9 and reduces MCL-1 levels in MV4-11 acute myeloid leukemia (AML) cells through a cereblon- and proteasome-dependent mechanism, and produces sustained inhibition of CDK9 for up to 24 h after washout^[1].
PROTAC CDK9 degrader-5 (0.01-5 μM; 6 h) selectively degrades CDK9 in Molm-13 acute myeloid leukemia (AML) cells, with limited off-target degradation effects on other kinases^[1].

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

Western Blot Analysis^[1]

Cell Line:

Human MV4-11 acute myeloid leukemia (AML) cells
Concentration:

1 μM
Incubation Time:

1, 2, 4, 6 h
Result:

Induced significant degradation of CDK9 and reduction in MCL-1 levels at 1 μM after 6 hours, with no effect on BCL-2.
Started CDK9 degradation at 2 hours and reached a plateau at 4 hours.
Kept CDK9 suppressed for 24 hours post-washout, with partial recurrence at 48 hours.

Western Blot Analysis^[1]

Cell Line:

human Molm-13 AML cells, multiple B/T cell lymphoma cell lines
Concentration:

0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM
Incubation Time:

6 h
Result:

Showed little effect on CDK5, CDK7, CDK13, GSK3α, GSK3β, or TAOK1 in Molm-13 cells, with some CDK2 degradation observed at higher concentrations.
Reduced only CDK9 by greater than 2-fold in Molm-13 cells per proteomics analysis.
Caused more substantial CDK2 degradation in B/T cell lymphoma cell lines with higher CDK2 expression.
Had no effect on Ikaros or Aiolos levels.

Cell Viability Assay^[1]

Cell Line:

human MV4-11 and Molm-13 AML cells
Concentration:

0.01-10 μM
Incubation Time:

6 h incubation, followed by viability assessment at 24 h post-treatment
Result:

Achieved an EC₅₀ of 0.4 μM in MV4-11 cells.
Showed greater potency than AT7519 (EC₅₀ 1.1 μM) in MV4-11 cells .
Had a greater impact on MCL-1 levels in Molm-13 cells.

Related Protocols :

RNA extraction experimental

Chemical Information

CAS. Nr. 2935587-89-4
Molecular Weight 879.78
Formel C₄₂H₄₈Cl₂N₈O₉
SMILES

O=C(NCCCCCCCCCCC(N1CCC(CC1)NC(C2=NNC=C2NC(C3=C(C=CC=C3Cl)Cl)=O)=O)=O)COC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tokarski RJ, et al. Bifunctional degraders of cyclin dependent kinase 9 (CDK9): Probing the relationship between linker length, properties, and selective protein degradation. European journal of medicinal chemistry. 2023 Jun 05;254:115342. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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Art. -Nr.:
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PROTAC CDK9 degrader-5

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen