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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
8 Results for "
RB axis
" in MedChemExpress (MCE) Product Catalog:
Products (8)
8 Results for "RB axis" in MCE Product Catalog:
5
5 Cited Publications
BSJ-03-123 is a selective PROTAC degrader of CDK6. BSJ-03-123 degrades CDK6, thereby inhibiting Rb S780 phosphorylation and inducing G1 phase arrest, while remodeling cell cycle and transcriptional signaling, with no effect on CDK4-dependent cancer cells. BSJ-03-123 reduces CDK6 protein levels in mouse ovarian tissues, increases the proportion of primordial follicles, and induces granulosa cell apoptosis, without impairing the ability of oocytes to resume meiosis and mature to the MII stage. BSJ-03-123 alleviates uveitis by blocking the HDACs-CDK6/ID2 axis. BSJ-03-123 can be used in studies related to acute myeloid leukemia, mantle cell lymphoma and autoimmune uveitis .
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1 Cited Publications
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AD4 is a PROTAC that induces the degradation of PCLAF by recruiting cereblon. AD4 is also an artemisinin derivative. AD4 directly binds to PCLAF with a KD of 6.1 μM, and induces apoptosis and G1-phase cell cycle arrest. By degrading PCLAF, AD4 upregulates p21, reduces Rb phosphorylation, downregulates Bcl-2 and upregulates Bax, thereby activating the p21/Rb axis. AD4 can be used in studies related to acute B-lymphoblastic leukemia and PCLAF-dependent anticancer mechanisms .
Cat. No.: HY-168996
CAS No.: 3032908-44-1
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
Cat. No.: HY-182036
Research Areas:
KWZL-7f15 is a dual CDK6/BRD4 inhibitor with an IC50 of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and BRD4-Myc axis, and also acts as a pan-BET inhibitor. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models. KWZL-7f15 can be used in studies related to triple-negative breast cancer .
Cat. No.: HY-189404
VEGFR-2-IN-92 is a potent VEGFR-2 inhibitor (IC50 = 0.208 μM). VEGFR-2-IN-92 occupies the inactive conformation of VEGFR-2 to inhibit its kinase activity, thereby disrupting the Cyclin D1-CDK4/6-Rb signaling axis and the p-FAK-related survival pathway, ultimately leading to cell cycle arrest and apoptosis in cancer cells. VEGFR-2-IN-92 can be used for research on colorectal cancer .
Cat. No.: HY-189637
PLK2-IN-1 is a selective PLK2 inhibitor (IC50 0.78 μM). PLK2-IN-1 induces Apoptosis and cell cycle arrest, reduces AKT and mTOR phosphorylation, and decreases Cyclin E expression as well as downregulates the CDK2/Rb/E2F1 axis. PLK2-IN-1 inhibits tumor growth in colorectal cancer xenograft models. PLK2-IN-1 can be used for research on colorectal cancer .
Cat. No.: HY-189230
CAS No.: 3108114-67-3
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NEP48 is a small-molecule antagonist targeting the ZER1 (E3 ubiquitin ligase)-E7 oncogenic axis. NEP48 binds to the MHGD/N-degron binding pocket within the ARM repeat domain of ZER1, competitively blocking E7-ZER1 binding and ZER1-mediated substrate degradation. NEP48 disrupts the ZER1-E7 interaction, leading to Rb stabilization and silencing of E2F-driven transcriptional programs. NEP48 inhibits the proliferation of HPV-positive cancer cells and can be used for research on HPV-positive cervical cancer .
Cat. No.: HY-111556R
CAS No.: 2361493-16-3
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BSJ-03-123 (Standard) is the analytical standard of BSJ-03-123 (HY-111556). This product is intended for research and analytical applications. BSJ-03-123 is a selective PROTAC degrader of CDK6. BSJ-03-123 degrades CDK6, thereby inhibiting Rb S780 phosphorylation and inducing G1 phase arrest, while remodeling cell cycle and transcriptional signaling, with no effect on CDK4-dependent cancer cells. BSJ-03-123 reduces CDK6 protein levels in mouse ovarian tissues, increases the proportion of primordial follicles, and induces granulosa cell apoptosis, without impairing the ability of oocytes to resume meiosis and mature to the MII stage. BSJ-03-123 alleviates uveitis by blocking the HDACs-CDK6/ID2 axis. BSJ-03-123 can be used in studies related to acute myeloid leukemia, mantle cell lymphoma and autoimmune uveitis .
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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
