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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
209 Results for "
proteasome system
" in MedChemExpress (MCE) Product Catalog:
Products (209)
209 Results for "proteasome system" in MCE Product Catalog:
Synonyms: ASC-JM17; ALZ-003
Target:
Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy
Research Areas:
Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma .
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PROTAC ER Degrader-4 is a potent ERα PROTAC degrader, with an IC50 of 0.8 nM against human ERα. PROTAC ER Degrader-4 recruits the VHL E3 ligase to ERα, and triggers the ubiquitination modification and degradation of ERα via the UP/26S proteasome system. PROTAC ER Degrader-4 can be used in related research on breast cancer .
Cat. No.: HY-176792
CAS No.: 3097985-19-5
ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRAS G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .
PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer .
PROTAC BCR-ABL Degrader-1 is a PROTAC degrader targeting BCR-ABL, and also selectively inhibits cancer cell proliferation. PROTAC BCR-ABL Degrader-1 induces degradation via the ubiquitin-proteasome system to reduce protein levels. PROTAC BCR-ABL Degrader-1 can be used for research on chronic myeloid leukemia .
Cat. No.: HY-175370
Target:
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PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 induces complete degradation of RIPK1 through the ubiquitin-proteasome system by bridging the target protein RIPK1 and VHL E3 ubiquitin ligase. PROTAC RIPK1 Degrader-1 is applicable to melanoma-related research .
Cat. No.: HY-178861
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dCDK9-202 is a CDK9 PROTAC degrader with a DC50 of 3.5 nM. dCDK9-202 induces CDK9 degradation via the ubiquitin-proteasome system. dCDK9-202 inhibits the growth of cancer cells in vitro and suppresses tumor growth in mouse xenograft models. dCDK9-202 is applicable for cancer-related research .
Cat. No.: HY-172946
CAS No.: 3054116-24-1
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SD-2301 is a selective STAT3 PROTAC degrader with a DC50 of 4 nM. By bridging the target protein STAT3 and VHL-1 E3 ubiquitin ligase, SD-2301 induces efficient degradation of STAT3 via the ubiquitin-proteasome system, thereby exerting potent anti-tumor and immunomodulatory effects. SD-2301 can be used in research related to lymphoma, melanoma, colon cancer and other tumors .
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PROTAC Bcl-xL degrader-2 is a selective Bcl-xL PROTAC degrader with a DC50 of 4.8 nM against Bcl-xL. PROTAC Bcl-xL degrader-2 forms a ternary complex with VHL E3 ligase, thereby redirecting the ubiquitin-proteasome system to mediate the degradation of Bcl-xL. PROTAC Bcl-xL degrader-2 triggers Apoptosis. PROTAC Bcl-xL degrader-2 can be used in the research of solid tumors and hematologic malignancies .
Cat. No.: HY-168566
CAS No.: 2247047-81-8
EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer .
Cat. No.: HY-175764
CAS No.: 3091132-73-6
Research Areas:
FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis .
PROTAC EGFR degrader 2 is an EGFR-targeting PROTAC and antitumor agent. PROTAC EGFR degrader 2 induces degradation of EGFR protein via the ubiquitin-proteasome system, requiring binding to both EGFR and the VHL E3 ubiquitin ligase. PROTAC EGFR degrader 2 exerts antitumor efficacy following EGFR degradation. PROTAC EGFR degrader 2 is released from the NTR-responsive caged-PROTAC 17-1 upon activation by nitroreductase in hypoxic tumor tissues. PROTAC EGFR degrader 2 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-171825
CAS No.: 2570251-63-5
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SIAIS001 is a CRBN-dependent ALK PROTAC degrader with a DC50 of 3.9 nM. SIAIS001 induces ALK protein degradation via the ubiquitin-proteasome system. SIAIS001 induces G1/S phase cell cycle arrest and inhibits proliferation of cancer cells. SIAIS001 can be used for the research of anaplastic large-cell lymphomas .
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MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
Cat. No.: HY-161696
CAS No.: 491586-42-6
Research Areas:
AN5777 is a GSPT1 Molecular glue degrader with a DC50 of less than 10 μM. AN5777 degrades GSPT1 in a CRBN-dependent manner via the ubiquitin-proteasome system. AN5777 induces G1 phase arrest and Apoptosis in cancer cells. AN5777 is applicable to research related to acute myeloid leukemia, multiple myeloma, and chronic myeloid leukemia .
Cat. No.: HY-175381
CAS No.: 3058911-16-0
Research Areas:
DeFer-2 is a Ferritin PROTAC degrader with a Kd value of 17.1 μM. DeFer-2 recruits the VHL E3 ligase to induce targeted degradation of ferritin via the ubiquitin-proteasome system, triggers iron overload stress in cancer cells, and further activates caspase 3-GSDME-mediated pyroptosis through massive ROS production. DeFer-2 can be used for research related to melanoma .
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PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC50 = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies .
MS9449 is a potent PROTAC EGFR degrader, with Kd values of 17 nM and 10 nM for wild-type EGFR and mutant EGFR L858R, respectively, and a DC50 of 7.1 nM for EGFR Del19. MS9449 effectively induces the degradation of mutant EGFR through the ubiquitin-proteasome system (UPS) and the autophagy-lysosome pathway. MS9449 exhibits anticancer activity against non-small cell lung cancer. MS9449 can be applied in related research on non-small cell lung cancer .
Cat. No.: HY-175541
CAS No.: 2926610-43-5
TQ-3959 is an orally active BTK PROTAC degrader with a DC50 of 0.4 nM. TQ-3959 selectively and efficiently degrades BTK by recruiting the CRBN E3 ubiquitin ligase and utilizing the ubiquitin-proteasome system. TQ-3959 can be applied in the research of B-cell malignancies and lymphomas .
Cat. No.: HY-157216
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HDAC1 Degrader-1 is a HDAC1 degrader with an IC50 of 192.3 nM. HDAC1 Degrader-1 induces degradation of HDAC1 in multiple myeloma cells via the proteasome system and enhances apoptosis of multiple myeloma cells. HDAC1 Degrader-1 can be used for research on multiple myeloma .
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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
