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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
13 Results for "
IMiDs
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "IMiDs" in MCE Product Catalog:
1
1 Cited Publications
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CRBN-6-5-5-VHL is a potent and selective VHL E3 ligand-based Cereblon (CRBN) PROTAC degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL forms a heterotrimeric complex with CRBN and VHL E3 ligase, thereby promoting CRBN ubiquitination and proteasomal degradation without inducing VHL degradation. CRBN-6-5-5-VHL protects myeloma from the toxic effects of IMiDs. CRBN-6-5-5-VHL can be used in the research of multiple myeloma .
Cat. No.: HY-159098
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dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease .
KTX-951 is an orally active PROTAC degrader of IRAK4 and IMiD (Ikaros/Aiolos) substrates (Kd = 3.5 nM). KTX-951 induces IRAK4 degradation, and the degradation efficiency is independent of IRAK4 binding affinity. The DC50 values of KTX-951 for IRAK4, Ikaros and Aiolos are 13 nM, 14 nM and 13 nM, respectively. The IC50 of KTX-951 against OCl-Ly10 CTG is 35 nM. KTX-951 exhibits antitumor activity .
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Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs . Thalidomide-propargyl 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-169343
CAS No.: 1957235-62-9
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FIZ1 degrader 1 (compound 1) is an IMiD-based molecular glue degrader targeting FIZ1 .
Cat. No.: HY-172770
CAS No.: 3113750-79-8
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KMG-1068 is a molecular glue degrader that induces proteasomal degradation of GSPT1 and GSPT2 with DC50 values of 126.7 nM and 42.2 nM, respectively. KMG-1068 binds to the C-terminal IMiD-binding site of CRBN, forms ternary complexes with GSPT1 and GSPT2, and mediates proteasomal degradation of target proteins via the CRL4 ubiquitination pathway. KMG-1068 is applicable to research related to acute myeloid leukemia .
Cat. No.: HY-172368
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PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research . (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
Cat. No.: HY-153959
CAS No.: 2473270-96-9
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Thalidomide-O-amido-C11-COOH (compound IMiD acid 1) is an E3 ligase ligand and linker CRBN (Cereblon) conjugate. Thalidomide-O-amido-C11-COOH can be used to synthesize PROTAC that target the degradation of DOT1L .
Cat. No.: HY-131970
CAS No.: 2738306-38-0
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LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM) .
Cat. No.: HY-128408
CAS No.: 2893795-12-3
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PROTAC BTK Degrader-4 (compound 15) is a potent PROTAC Bruton's tyrosine kinases (BTK) degrader (DC50 < 100 nM) with little immunomodulatory imide drug (IMiD) activity (DC50 = 0.345 μM, Dmax = 27.4%). PROTAC BTK Degrader-4 can be used for cancers, autoimmune diseases, and inflammatory diseases that are mediated by BTK .
Cat. No.: HY-W947273
CAS No.: 2766178-72-5
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CRBN ligand-898 is a CRBN ligand with a Kd of 216 nM. CRBN ligand-898 binds to CRBN, and when incorporated into proteolysis targeting chimeras (PROTACs), mediates degradation of intended target proteins. CRBN ligand-898 does not induce degradation of IMiD-associated neosubstrates Ikaros (IKZF1) and Aiolos (IKZF3). CRBN ligand-898 can be used to synthesize PROTACs .
Cat. No.: HY-181023
PROTAC HDAC8 Degrader-3 (Compound BP1) is an efficient and selective HDAC8 PROTAC degrader with a DC50 of 20 nM. PROTAC HDAC8 Degrader-3 exhibits IC50 for HDAC8 and CRBN of 0.46 and 7.5 μM, respectively. PROTAC HDAC8 Degrader-3 exhibits potent anti-proliferative activity against MM.1S and HL-60 cells. PROTAC HDAC8 Degrader-3 can be used for research on multiple myeloma and acute myeloid leukemia .
Cat. No.: HY-D3392
Thalidomide-cyanine 5 is a fluorescent probe prepared by conjugating the CRBN binder Thalidomide (HY-14658) with the near-infrared fluorescent dye Cy5. Thalidomide-cyanine 5 binds to DDB1-CRBN protein complex with a Kd of 121.6 nM. Thalidomide-cyanine 5 binds to CRBN to form a binary complex, and is mainly used for the visual tracking research of degradants such as PROTAC (Ex/Em = 650/665 nm) .
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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
