Eukaryotic Release Factor (eRF) Degrader

Lenalidomide 4'CH2NH2, 6'F is a molecular glue degrader targeting GSPT1 protein. Lenalidomide 4'CH2NH2, 6'F modulates ubiquitin E3 ligase activity and shifts substrate specificity, resulting in altered substrate degradation. Lenalidomide 4'CH2NH2, 6'F inhibits cancer cell proliferation. Lenalidomide 4'CH2NH2, 6'F can be used in research related to acute myeloid leukemia.

GSPT1 degrader-11 is a CRBN-dependent molecular glue degrader targeting GSPT1, with a DC₅₀ of 67.7 nM. GSPT1 degrader-11 induces CRBN-dependent degradation of GSPT1 via the ubiquitin-proteasome pathway. GSPT1 degrader-11 exhibits CRBN-dependent growth inhibitory activity in cancer cells. GSPT1 degrader-11 can be used for the research of triple-negative breast cancer.

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.

GSPT1 degrader-6 is a GSPT1 molecular glue degrader that recruits cereblon (CRBN), with a DC₅₀ of 13 nM. GSPT1 degrader-6 induces GSPT1 protein degradation via the ubiquitin-proteasome pathway. GSPT1 degrader-6 can be used in breast cancer-related research.

GSPT1 degrader-9 (Compound F) is a cereblon-based molecular glue degrader for G1 to S phase transition protein 1 (GSPT1) that degrades GSPT1 with a rate of 95% (1 μM) GSPT1 and 86% (0.1 μM). GSPT1 degrader-9 inhibits the cell viability of HL-60 with an IC₅₀ of 9.2 nM.

GSPT1 degrader-12 is a selective molecular glue GSPT1 degrader. GSPT1 degrader-12 exhibits antiproliferative activity against cancer cells in a CRBN- and GSPT1-dependent manner. GSPT1 degrader-12 can be used for leukemia research.

WB156 is a dual MDM2 and GSPT1 PROTAC degrader with a DC₅₀ of 23 nM against MDM2. WB156 induces the degradation of MDM2 and GSPT1 via the ubiquitin-proteasome system. WB156 upregulates the levels of p53 and p21, and triggers Apoptosis through the cleavage of PARP and Caspase-3. WB156 can be used in leukemia-related research.

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.

GSPT1 degrader-10 (compound A) is a cereblon-based molecular glue degrader of GSPT1 with more than 95% degradation. GSPT1 degrader-8 inhibits cell viability in HL-60 cells with an IC₅₀ of 10 nM.

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.

PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-2 inhibits protein expression of SRD5A3 and GSPT1(eRF3a). PROTAC erf3a Degrader-2 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-2 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer.

GSPT1 degrader-18 is a GSPT1 degrader that inhibits the proliferation of cancer cells. GSPT1 degrader-18 has weak ability to induce the formation of the GSPT1-CRBN/DDB1 ternary complex and belongs to a weak molecular glue. GSPT1 degrader-18 can be used in cancer-related research.

GSPT1 degrader-14 is a selective molecular glue GSPT1 degrader. GSPT1 degrader-14 exhibits antiproliferative activity against cancer cells in a CRBN- and GSPT1-dependent manner. GSPT1 degrader-14 can be used for leukemia research.

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.

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 K_d 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.

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.