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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 "
GSPT2
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "GSPT2" in MCE Product Catalog:
20
20 Cited Publications
Research Areas:
CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer [2] .
1
1 Cited Publications
Research Areas:
SJ6986 is an orally active GSPT1/2 molecular glue degrader, with a DC50 of 9.7 nM at 4 h and 2.1 nM at 24 h for GSPT1 degradation in MV4-11 cells. SJ6986 recruits GSPT1/2 to the CRBN E3 ligase complex, inducing ubiquitination and proteasomal degradation of GSPT1/2. SJ6986 triggers activation of the integrated stress response pathway and apoptosis downstream of GSPT1 degradation. SJ6986 serves as a chemical probe for investigating the functions of GSPT1/GSPT2 in vitro and in vivo. SJ6986 can be used for research on acute leukemia and medulloblastoma .
Cat. No.: HY-148837
CAS No.: 2883535-99-5
Target:
PROTACs c-Myc CD276/B7-H3 IAP Casein Kinase Eukaryotic Release Factor (eRF) Oxidative Phosphorylation Apoptosis
Research Areas:
GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC50 of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers [2] .
Cat. No.: HY-177744
CAS No.: 3093413-09-0
Research Areas:
GSPT2 degrader-1 (compound 619) is a selective molecular glue GSPT2 degrader targeting GSPT2. GSPT2 degrader-1 contains Thalidomide (HY-14658) and the linker of MDEG-541 (HY-150259). GSPT2 degrader-1 induces the degradation, but not GSPT1 or myelocytomatosis oncogene (MYC). GSPT2 degrader-1 can be used for research of gastrointestinal cancer .
Cat. No.: HY-150259
Purity: 98.05%
Research Areas:
MDEG-541 is a PROTAC degrader targeting MYC, GSPT1/2 and PLK1. MDEG-541 induces degradation via proteasome- and ubiquitin-dependent pathways. MDEG-541 exhibits anti-tumor activity in gastrointestinal cancer cells and patient-derived organoids. MDEG-541 can be used for the research of gastrointestinal cancer .
Cat. No.: HY-161101
Research Areas:
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-172770
CAS No.: 3113750-79-8
Research Areas:
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 .
Research Areas:
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 .
Cat. No.: HY-177777
Research Areas:
FL2-14 is a CRBN-dependent selective molecular glue degrader of GSPT2. FL2-14 specifically degrades GSPT2 by recruiting the CRBN E3 ligase to recognize the G-loop sequence on the target protein GSPT2. FL2-14 can be used in related research on colorectal cancer .
Cat. No.: HY-RS05869
Target:
Research Areas:
GSPT2 Human Pre-designed siRNA Set A contains three designed siRNAs for GSPT2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-101488R
CAS No.: 1010100-07-8
CC-885 (Standard) is the analytical standard of CC-885 (HY-101488). This product is intended for research and analytical applications. CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer [2] .
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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
