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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
199 Results for "
proteasome complex
" in MedChemExpress (MCE) Product Catalog:
Products (199)
199 Results for "proteasome complex" in MCE Product Catalog:
Cat. No.: HY-183755
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YSA64 is an orally active RBM39-targeting molecular glue. YSA64 promotes degradation via formation of a DCAF15/DDB1 ternary complex, dependent on Cullin-RING E3 ligase and proteasome activity. YSA64 can be used for the research of acute myeloid leukemia and Ewing sarcoma .
Cat. No.: HY-187801
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SH-CER-6 is a double-warhead C 2-COUPL derived from Ceritinib (HY-187801) that targets the EML4-ALK fusion protein complex and induces its degradation. SH-CER-6 simultaneously binds to structures near the ALK inhibitor-binding region and forms a covalent conjugate with a protein cysteine, thereby promoting ubiquitination and proteasome-dependent degradation of the EML4-ALK complex, which in turn inhibits the ALK signaling pathway. SH-CER-6 is useful for research related to ALK-positive non-small cell lung cancer .
Cat. No.: HY-181405
CAS No.: 2387704-74-5
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SR-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM; Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer .
Cat. No.: HY-187502
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Jak1 RIMTAC-1 is a JAK1 RIMTAC degrader (a PROTAC-like agent) with a DC50 of 322.8 nM. Jak1 RIMTAC-1 forms a ternary complex with JAK1 and RIPK1, thereby recruiting the VHL E3 ligase complex to ubiquitinate JAK1 via the ubiquitin-proteasome system and mediate its subsequent proteasomal degradation. Jak1 RIMTAC-1 does not alter JAK1 mRNA levels (pink: Jak1 ligand-1 (HY-187503); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-B0704)) .
Cat. No.: HY-183073
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TZ1104 is a PROTAC-based CDK7 degrader, with a DC50 of 0.88 nM. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia .
Cat. No.: HY-138642B
CAS No.: 2614417-52-4
Synonyms: rel-ARV-471; rel-PF-07850327
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(Rac)-Vepdegestrant is the relative configuration of Vepdegestrant (HY-138642). Vepdegestrant is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
Cat. No.: HY-184362
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P-SETDB1-4 is a SETDB1 PROTAC degrader with a Kd of 86 nM. P-SETDB1-4 recruits CRBN to SETDB1, induces proteasome-dependent degradation of SETDB1, and forms a ternary complex with CRBN to achieve targeted degradation. P-SETDB1-4 reduces DNA synthesis. P-SETDB1-4 exhibits anticancer activity against breast cancer. P-SETDB1-4 can be used in breast cancer-related research .
Cat. No.: HY-184913
JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications .
Cat. No.: HY-184457
CAS No.: 2441860-09-7
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NH2-C-Ph-hexyne-C4-NH2 is a PROTAC linker. NH2-C-Ph-hexyne-C4-NH2 can connect the BRD4 ligand JQ1 (HY-13030) with the SYVN1 ligand Clofibric acid (HY-B1415), thereby achieving the degradation of BRD4 via the PROTAC mechanism. NH2-C-Ph-hexyne-C4-NH2 can be used for the synthesis of PROTAC BRD4 Degrader-47 (HY-184455) .
Cat. No.: HY-182350
CAS No.: 3081876-96-9
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FXR DUBTAC modulator-1 is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC modulator-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC modulator-1 can be used in the research of cholestatic liver injury .
Cat. No.: HY-181392
CAS No.: 3034875-56-1
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PROTAC EZH2 Degrader-35 (compound U3i (44)) is a PROTAC protein degrader targeting EZH2 with a human EZH2 Ka of 16.19 nM. PROTAC EZH2 Degrader-35 exhibits antiproliferative activity in triple-negative breast cancer cells and minimal cytotoxicity in normal human epithelial, hepatic, renal cells.PROTAC EZH2 Degrader-35 can be used for the research of triple-negative breast cancer .
Cat. No.: HY-184455
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PROTAC BRD4 Degrader-47 is a heterobifunctional PROTAC that selectively degrades BRD4 in a SYVN1-dependent manner, with a DC50 of 0.93 μM. PROTAC BRD4 Degrader-47 can be used in cancer-related research such as breast cancer .
Cat. No.: HY-138642R
CAS No.: 2229711-68-4
Synonyms: ARV-471 (Standard); PF-07850327 (Standard)
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Vepdegestrant (Standard) is the analytical standard of Vepdegestrant (HY-138642). This product is intended for research and analytical applications. Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
Cat. No.: HY-162106
CAS No.: 3035509-76-0
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PROTAC GPX4 degrader-2 is a cIAP-recruiting GPX4 PROTAC degrader with a DC50 of 1.68 μM. PROTAC GPX4 degrader-2 forms a ternary complex with GPX4 and cIAP, and induces GPX4 degradation via the ubiquitin-proteasome system pathway. PROTAC GPX4 degrader-2 induces Mitochondrial depolarization and Ferroptosis. PROTAC GPX4 degrader-2 exhibits antiproliferative effects in cancer cells. PROTAC GPX4 degrader-2 can be used for the research of fibrosarcoma .
Cat. No.: HY-162749
CAS No.: 3097803-96-5
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G9D-4 is a G9a PROTAC degrader. G9D-4 induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 can be used for research on pancreatic cancer .
Cat. No.: HY-164891
CAS No.: 2839138-44-0
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EM12‑FS is a selective covalent molecular glue degrader of NTAQ1 that binds to CRBN with an IC50 of 256 nM. EM12‑FS covalently modifies the His353 residue of CRBN via chemical modification, reshapes the surface conformation of CRBN protein, selectively recruits NTAQ1 to form a ternary complex, and mediates the degradation of NTAQ1 protein in a CRL4 CRBN E3 ubiquitin-proteasome pathway-dependent manner. EM12‑FS can be used in cancer-related research .
Cat. No.: HY-168131
CAS No.: 3098718-46-5
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PROTAC EZH2 Degrader-3 is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 induces the global degradation of the PRC2 complex (including EZH2, SUZ12, EED, RbAp48) via the ubiquitin-proteasome pathway and downregulates H3K27me3 levels. PROTAC EZH2 Degrader-3 inhibits cancer cell proliferation and induces their apoptosis. PROTAC EZH2 Degrader-3 can be used in research related to lymphoblastoma and diffuse large B-cell lymphoma .
Cat. No.: HY-172615
CAS No.: 3033019-04-1
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AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies .
Cat. No.: HY-175435
CAS No.: 3094183-98-6
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CST905 is a potent BRAF-V600E PROTAC degrader with a DC50 of 18 nM. CST905 recruits the VHL E3 ligase to form a ternary complex, mediating the degradation of BRAF-V600E via the ubiquitin-proteasome pathway. The ligand of CST905 disrupts the RAF dimerization interface, thereby preventing the aberrant activation of the harmful MAPK/ERK pathway in RAS-mutated cells while degrading the target protein. CST905 can be used in studies related to malignant melanoma and neuroblastoma .
Cat. No.: HY-183007
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LJM133 is a SMARCA2/PBRM1/SMARCA4 PROTAC degrader with DC50 values of 3.5 nM, 7 nM, and 6.4 nM. LJM133 induces ternary complex formation with VHL E3 ligase to drive proteasome-mediated degradation of target proteins. LJM133 suppresses cell proliferation and exhibits significant antitumor efficacy in a SMARCA4 mutant cancer xenograft model. LJM133 can be used for the research of cancer, such as SMARCA4 mutant non-small cell lung cancer .
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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
