Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
3 Results for "
pRB phosphorylation
" in MedChemExpress (MCE) Product Catalog:
Products (3)
3 Results for "pRB phosphorylation" in MCE Product Catalog:
1
Gatsuciclib (AZD8421) is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9). Gatsuciclib has no significant kinase inhibition outside the CDK family. Gatsuciclib inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. Gatsuciclib can be studied in research for breast cancer and ovarian cancer .
Cat. No.: HY-201330
CAS No.: 2531743-46-9
Synonyms: RGT-419B
GDC-4198 (RGT-419B) is an orally active CDK4/2 inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer .
Cat. No.: HY-186132
CAS No.: 3030276-48-0
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer) .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
