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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
50 Results for "
CRBN-dependent degrader
" in MedChemExpress (MCE) Product Catalog:
Products (50)
50 Results for "CRBN-dependent degrader" in MCE Product Catalog:
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2 Cited Publications
Research Areas:
JQAD1 is a EP300 PROTAC degrader. JQAD1 selectively targets EP300 and induces its degradation via the CRBN-dependent proteasomal pathway. JQAD1 reduces the levels of H3K27ac and the expression of MYCN. JQAD1 induces apoptosis (apoptosis) and inhibits cancer cell growth. JQAD1 exerts anti-neuroblastoma effects in vivo in a CRBN-dependent manner. JQAD1 can be used for the research of neuroblastoma .
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1 Cited Publications
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PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-175751
CAS No.: 3063346-83-5
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LRK-4189 is an orally active CRBN-dependent PIP4K2C molecular glue degrader. LRK-4189-mediated degradation of PIP4K2C leads to intrinsic cell death and upregulation of the STAT1 pathway and signaling in microsatellite stable colorectal cancer (MSS CRC) cells. LRK-4189 can be used for the research of microsatellite-stable colorectal cancer .
Cat. No.: HY-173523
CAS No.: 3054009-82-1
KI-CDK9d-32 is a selective CDK9 PROTAC degrader (IC50 = 3 nM; DC50 = 0.89 nM). KI-CDK9d-32 induces CDK9 degradation via the ubiquitin-proteasome pathway to abrogates CDK9 enzymatic and scaffolding functions, downregulates MYC expression and MYC-dependent signaling, represses TNF-alpha signaling pathways activity and pre-rRNA levels. KI-CDK9d-32 disrupts nucleolar homeostasis, blocks cell cycle progression and cellular translation by reducing 4EBP1 phosphorylation, and elicits cancer cell cytotoxicity in a CRBN-dependent manner, while high ABCB1 activity attenuates the efficacy. KI-CDK9d-32 can be used for the research of acute lymphoblastic leukemia, rhabdomyosarcoma, pancreatic adenocarcinoma .
Cat. No.: HY-137465
CAS No.: 2412055-93-5
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CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma .
Cat. No.: HY-168654
CAS No.: 3090685-34-7
WEE1 degrader 1 (Compound 10) is a CRBN-dependent molecular glue degrader of WEE1 and casein kinase 1α (CK1α) with sub-2 nM DC50 values for both targets. WEE1 degrader 1 can be used for the research of acute lymphoblastic leukemia, acute monocytic leukemia, acute promyelocytic leukemia, colorectal adenocarcinoma, diffuse large b cell lymphoma .
Cat. No.: HY-172931
CAS No.: 2734910-37-1
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DEG-35 is a CRBN-dependent, dual IKZF2 and CK1α molecule glue degrader, with DC50 values of 1.4 nM and 4.4 nM for CK1α and IKZF2, respectively. DEG-35 activates the p53 apoptosis pathway. DEG-35 can be used in the research for Acute Myeloid Leukemia (AML) .
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ZXH-1-161 is a potent CRBN modulator that selectively induces the degradation of GSPT1 in a CRBN-dependent manner. ZXH-1-161 can inhibit the proliferation of multiple myeloma cells and exhibits antitumor activity .
Cat. No.: HY-132941
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CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer .
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SJPYT-195 is a molecular glue degrader targeting GSPT1, with a DC50 of 310 nM. SJPYT-195 mediates CRBN-dependent and proteasome-dependent degradation of GSPT1 by forming a stable ternary complex with CRBN and GSPT1. As a secondary effect of GSPT1 degradation, SJPYT-195 induces a decrease in PXR protein levels. SJPYT-195 is applicable to research related to acute myeloid leukemia .
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SP27 is a PROTAC PLK4 degrader with an IC50 of 8.4 nM and a DC50 of 19.5 nM against PLK4. SP27 induces PLK4 degradation via the CRBN-dependent ubiquitin-proteasome pathway, inhibits PLK4 downstream signal transduction, and suppresses the growth of TRIM37-amplified breast cancer cells. SP27 is applicable for breast cancer-related research .
Cat. No.: HY-174371
CAS No.: 3032576-92-1
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INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.
Cat. No.: HY-173154B
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NK7-902 diTFA is a selective and orally active CRBN-dependent NEK7 molecular glue degrader with Kd values of 1.5 and 2.6 μM for hNEK7 and mNEK7. NK7-902 diTFA fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 diTFA shows activity in murine systems and induces a profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation. NK7-902 diTFA can be used for the research of inflammation, such as cryopyrin-associated periodic syndromes .
Cat. No.: HY-178486
CAS No.: 2619408-35-2
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SH6 is a CRBN-dependent proteasome degrader that targets ZBTB7A. SH6 can be used in the research of sickle cell disease and β-thalassemia .
Cat. No.: HY-161101
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GSPT1 degrader-19 is a molecular glue degrader targeting GSPT1, IKZF1 and IKZF3, with DC50 values of 0.88 nM, 11.54 nM and 13.84 nM, respectively, in MM.1S multiple myeloma cells. GSPT1 degrader-19 induces cereblon (CRBN)-dependent ubiquitination and proteasomal degradation of IKZF1, IKZF3, GSPT1 and GSPT2, and also reduces ZFP91 protein levels via a CRBN-dependent pathway. GSPT1 degrader-19 exerts antiproliferative effects on cancer cells, induces global proteomic changes including downregulation of novel substrates, and exhibits activity against multiple myeloma and leukemia cell lines. GSPT1 degrader-19 can be used in research related to multiple myeloma and leukemia .
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 .
Cat. No.: HY-W998345
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models .
Cat. No.: HY-161696
CAS No.: 491586-42-6
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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-168135
CAS No.: 3056647-52-7
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PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC50 of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer .
Cat. No.: HY-169343
CAS No.: 1957235-62-9
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FIZ1 degrader 1 is an IMiD-based molecular glue degrader. FIZ1 degrader 1 induces CRBN-dependent FIZ1 ubiquitination and proteasomal degradation; inhibition of the proteasome, ubiquitination or ubiquitination-like processes blocks this degradation. FIZ1 degrader 1 also induces the degradation of IKZF1, IKZF3 and ZFP91. FIZ1 degrader 1 is applicable to molecular glue-related research .
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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
