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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
97 Results for "
GSPT
" in MedChemExpress (MCE) Product Catalog:
Products (97)
97 Results for "GSPT" in MCE Product Catalog:
Cat. No.: HY-155552
CAS No.: 3037491-05-4
Research Areas:
GSPT1 degrader-1 is a highly selective degrader targeting GSPT1. GSPT1 degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G0/G1 phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research .
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-170952
CAS No.: 3053857-55-6
Research Areas:
LYG-409 is a highly potent, selective, and orally active GSPT1 molecular glue degrader. LYG-409 induces GSPT1 degradation in KG-1 cells with a DC50 of 7.87 nM. LYG-409 binds to Cereblon with an IC50 of 191 nM, promotes the formation of the CRBN-GSPT1 ternary complex, and induces proteasome-dependent degradation of GSPT1. LYG-409 exhibits broad antiproliferative and GSPT1-degrading activities in a variety of hematologic and solid tumor cells. LYG-409 can be used for studies related to GSPT1-targeted protein degradation, acute myeloid leukemia, and prostate cancer .
Research Areas:
Sontigidomide is a protein molecular glue degrader that can effectively degrade IKZF1/3 and GSPT1 proteins. Sontigidomide can be used to study inflammatory and immune system diseases .
GSPT1/IKZF1/3 Molecular Glue Degrader
Cat. No.: HY-151123
CAS No.: 1637637-70-7
Synonyms: AKCEA-APO(a)-LRx; ISIS 681257; TQJ230
Target:
Research Areas:
Pelacarsen (ISIS 681257) is a GalNAc3-conjugated 2′-MOE-modified antisense oligonucleotide. Pelacarsen reduces apo (a) .
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-W599279
CAS No.: 2761170-84-5
Research Areas:
ABS-752 is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 shows no cytotoxicity in primary human hepatocytes. ABS-752 can be used in the research of hepatocellular carcinoma .
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 .
Cat. No.: HY-175334
CAS No.: 2920443-08-7
Research Areas:
DHC-286 is a molecular glue degrader targeting GSPT1. DHC-286 recruits GSPT1 to the CRL4CRBN ubiquitin ligase complex, promoting GSPT1 ubiquitination and proteasomal degradation, inducing cytotoxicity. DHC-286 is promising for research of cancers such as acute myeloid leukemia .
Cat. No.: HY-147406
CAS No.: 2589926-20-3
Synonyms: ION-904
Target:
Research Areas:
Tonlamarsen (ION-904) is a GalNAc-conjugated antisense oligonucleotide and Angiotensinogen synthesis inhibitor. Tonlamarsen specifically reduces the production of Angiotensinogen in the liver and plasma, and exhibits extremely low activity in the kidneys. Tonlamarsen can be used in research related to hypertension and heart failure .
Cat. No.: HY-170405
CAS No.: 2940242-88-4
Research Areas:
YB-3-17 is a blood-brain barrier permeable mTOR inhibitor (IC50 = 0.22 nM) and GSPT1 PROTAC degrader. YB-3-17 inhibits mTORC1/2, CK1δ/ε, mutant ALK and HER2 kinases, induces CRBN-dependent selective GSPT1 degradation, ablates mTOR downstream phosphorylation, downregulates c-Myc/Cyclin D1 to impair tumor translation, triggers p53-mediated apoptosis, suppresses tumor proliferation and xenograft tumor growth, and can be used for the study of glioma, neuroblastoma, breast cancer, lymphoma, colorectal cancer and lung cancer .
Cat. No.: HY-176128
Research Areas:
BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
Cat. No.: HY-175810
Research Areas:
GSPT1 degrader-8 is a potent and orally active G1 to S phase transition 1 (GSPT1) molecular glue degrader. GSPT1 degrader-8 induces GSPT1 degradation and inhibits tumor growth. GSPT1 degrader-8 can be used for the research of cancer, such as breast cancer .
Cat. No.: HY-174238
CAS No.: 3082942-43-3
Research Areas:
GSPT1 degrader-7 (Example 43) is a molecular glue degrader targeting GSPT1. GSPT1 degrader-7 has an EC50 of 0.2 nM in DF15 multiple myeloma cells. GSPT1 degrader-7 can be used in the study of cancer .
Cat. No.: HY-156747
CAS No.: 2803879-60-7
Research Areas:
GSPT1 degrader-2 is an orally active GSPT1 molecular glue degrader that promotes the degradation of intracellular GSPT1 protein, with DC50 values of 3 nM and 22 nM in NCI-H1155 and ABC-1 cells with high N-Myc expression, respectively. GSPT1 degrader-2 can be used in the research of N-Myc-driven cancers, such as lung cancer .
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-175283
CAS No.: 2438239-83-7
Research Areas:
ABT-002 is a molecular glue degrader targeting GSPT1 and NEK7. ABT-002 is the active metabolite of ABS-752 (HY-W599279). ABT-002 is promising for research of hepatocellular carcinoma (HCC) .
Cat. No.: HY-175040
Research Areas:
PROTAC FLT-3 degrader 5 is an orally active FLT3 PROTAC degrader with a DC50 of 1.2 nM. PROTAC FLT-3 degrader 5 also acts as a molecular glue to degrade GSPT1 and IKZF1/3, with DC50 values of 8.54 nM, 0.02 nM and 0.79 nM, respectively. PROTAC FLT-3 degrader 5 mediates the degradation of FLT3, GSPT1 and IKZF1/3 through interaction with the cereblon E3 ubiquitin ligase complex. PROTAC FLT-3 degrader 5 can be used in the research of acute myeloid leukemia .
Cat. No.: HY-177758
PROTAC HDAC6 degrader 8 is a potent and selective HDAC6 PROTAC degrader with a DC50 of 1.94 nM. PROTAC HDAC6 degrader 8 induces HDAC6 degradation in cancer cells with a hook effect, and exerts no impact on other HDAC subtypes, IKZF1, IKZF3 or GSPT1. PROTAC HDAC6 degrader 8 can be used in studies related to multiple myeloma .
Cat. No.: HY-170982
CAS No.: 2756323-28-9
MS910 is a CRBN-recruiting MEK1/2 PROTAC degrader, with a DC50 of 94 nM against MEK1 and 38 nM against MEK2 in SK-MEL-28 cells. MS910 induces the degradation of GSPT1, IKZF1/3 and ZFP91, thereby inhibiting the downstream ERK signaling pathway and cancer cell growth. MS910 is applicable to research related to colorectal cancer and melanoma .
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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!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
