PROTAC CDK9 Degrader-1

 CAS No.: 2118356-96-8  Cat No.: BP-400051 4.5  

PROTAC CDK9 Degrader-1 is a pioneering chemical compound designed for targeted protein degradation, specifically targeting Cyclin-Dependent Kinase 9 (CDK9). This molecule operates by binding to the ATP-binding site of CDK9, effectively linking it to an E3 ubiquitin ligase through a bifunctional linker. The molecular architecture of PROTAC CDK9 Degrader-1 includes a ligand for CDK9, a linker, and a ligand for an E3 ligase, facilitating the ubiquitination and subsequent proteasomal degradation of CDK9. By selectively degrading CDK9, this compound interrupts transcriptional regulation and cell cycle progression, offering a precise mechanism for studying CDK9-dependent pathways. Its primary role in PROTAC design is to serve as a bridge between the target protein and the ubiquitin-proteasome system, promoting targeted degradation. PROTAC CDK9 Degrader-1 is invaluable in research focused on elucidating the role of CDK9 in cancer biology and other diseases, enabling the exploration of novel therapeutic strategies through the modulation of protein levels rather than activity alone. This compound is essential for advancing the understanding of targeted protein degradation mechanisms and their applications in drug discovery.

PROTAC CDK9 Degrader-1

Structure of 2118356-96-8

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Category
PROTAC
Molecular Formula
C33H35N5O7
Molecular Weight
613.66

* For research and manufacturing use only. Not for human or clinical use.

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Solubility
DMSO : ≥ 104 mg/mL
Storage
Powder<br/>-20°C<br/>3 years<br/><br/><br/> <br/>4°C<br/>2 years<br/><br/><br/>In solvent<br/>-80°C<br/>6 months<br/><br/><br/> <br/>-20°C<br/> 1 month
Shipping
Room temperature in continental US; may vary elsewhere
Synonyms
CDK9PROTAC; CDK9 PROTAC; CDK9-PROTAC; N-(5-cyclobutyl-1H-pyrazol-3-yl)-2-[4-[5-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxypentoxy]phenyl]acetamide
InChI Key
WCEHIDWONYOKOJ-UHFFFAOYSA-N
InChI
InChI=1S/C33H35N5O7/c39-28-15-14-25(31(41)35-28)38-32(42)23-8-5-9-26(30(23)33(38)43)45-17-3-1-2-16-44-22-12-10-20(11-13-22)18-29(40)34-27-19-24(36-37-27)21-6-4-7-21/h5,8-13,19,21,25H,1-4,6-7,14-18H2,(H,35,39,41)(H2,34,36,37,40)
SMILES
C1CC(C1)C2=CC(=NN2)NC(=O)CC3=CC=C(C=C3)OCCCCCOC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O
Mechanism

Target: Targets CDK9 cyclin-dependent kinase for experimental targeted protein degradation studies.

Binding Site: Binds the CDK9 ATP-binding pocket and cereblon thalidomide-binding domain to support productive ternary complex formation.

Mechanism of Action: PROTAC CDK9 Degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward CDK9 cyclin-dependent kinase. The bifunctional molecule links a target-recognition element to cereblon, promoting proximity between the protein of interest and ubiquitination machinery. Productive ternary-complex formation can drive polyubiquitination and proteasome-dependent target depletion, allowing researchers to compare pharmacological inhibition with protein removal. It is suitable for evaluating degradation potency, kinetics, pathway selectivity, and downstream signaling consequences in engineered or disease-relevant cellular models.

Applications

• PROTAC-Mediated CDK9 Degradation: This product is designed for the selective degradation of Cyclin-Dependent Kinase 9 (CDK9), a crucial regulator of transcription elongation. By facilitating the ubiquitination and subsequent proteasomal degradation of CDK9, researchers can study the effects of its depletion on gene expression and cell cycle progression.

• Targeted Protein Degradation in Cancer Research: PROTAC CDK9 Degrader-1 is instrumental in investigating the role of CDK9 in cancer cell survival. By targeting CDK9 for degradation, researchers can explore therapeutic strategies to disrupt aberrant transcriptional programs in cancer cells, providing insights into novel anti-cancer approaches.

• Functional Genomics via PROTACs: Utilize this degrader to dissect the functional role of CDK9 in various cellular processes. By achieving targeted protein degradation, researchers can perform loss-of-function studies to understand CDK9's involvement in transcriptional regulation, potentially revealing new biological pathways and targets.

• Drug Discovery and Development: PROTAC CDK9 Degrader-1 serves as a valuable tool in the early stages of drug discovery. By degrading CDK9, researchers can evaluate its potential as a therapeutic target and screen for synergistic effects with other compounds, accelerating the development of innovative treatments.

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L

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g

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