Molecular Glues
Protein degradation agents based on the ubiquitin-proteasome pathway include a part of molecular glues. Molecular glues are a class of small molecule compounds that can induce or stabilize the interaction between proteins. If one of the protein is ubiquitin ligase, molecular glue can cause another protein to undergo ubiquitin modification and degradation through the proteasome pathway, which is similar to PROTAC. However, these molecules are classified as ligand for E3 ligase as functional molecules in subsequent classification. Older drugs, thalidomide, lenalidomide, and pomalidomide, together with CC-90009 and CC-92480 reported later all belong to this category.
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Molecular Glues Related Products (382)
Related Products (382)
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Related Compound Screening Libraries (1)
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EST1140
0 ImagesCat. No.: HY-187458CAS No.: 3105892-11-0EST1140 is a covalent molecular glue degrader targeting RNF126 for AR/AR-V7, with DC50 values of 33 μM and 30 μM, respectively, in 22Rv1 cells. EST1140 covalently binds to the E3 ligase RNF126 to achieve targeted protein degradation. EST1140 can be used in the research of androgen-independent prostate cancer.
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NEK7 degrader-2
0 ImagesCat. No.: HY-177559CAS No.: 3037413-54-7NEK7 degrader-2 is a NEK7 molecular glue degrader that promotes the formation of the NEK7-compound-CRBN/DDB1 ternary complex. NEK7 degrader-2 reduces the release of IL-1β after NLRP3 inflammasome activation induced by LPS (HY-D1056). NEK7 degrader-2 can be applied in studies related to NEK7-dependent NLRP3 inflammasome activation and inflammatory responses.
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JADA3
0 ImagesCat. No.: HY-W450772CAS No.: 2573901-15-0JADA3 is a molecular glue degrader targeting IKZF1 and IKZF3. JADA3 induces proteasome-mediated degradation of the target transcription factors by binding to the E3 ubiquitin ligase Cereblon. JADA3 can be used in research related to acute myeloid leukemia.
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GSPT1 degrader-6
0 ImagesCat. No.: HY-162535CAS No.: 3034764-41-2GSPT1 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.
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GSPT1 degrader-9
0 ImagesCat. No.: HY-159609CAS No.: 3034310-17-0GSPT1 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.
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LC-MG-10
0 ImagesCat. No.: HY-184322LC-MG-10 is a selective molecular glue degrader targeting FGFR2, with a DC50 of 230.2 nM in KATO III cells. LC-MG-10 induces proteasomal degradation of FGFR2 via a covalent molecular glue mechanism. LC-MG-10 inhibits cancer cell proliferation. LC-MG-10 suppresses FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways. LC-MG-10 can be used in studies related to gastric cancer.
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IKZF2-degrader 1
0 ImagesCat. No.: HY-172882CAS No.: 2983840-43-1IKZF2-degrader 1 is a potent and selective molecular glue degrader that selectively degrades IKZF2, with DC50 values of 0.6 nM and 2.0 nM in HEK293T cells and Jurkat cells, respectively. IKZF2-degrader 1 exerts no degrading effect on CK1α, IKZF1 and GSPT1, and shows weak activity against IKZF3. IKZF2-degrader 1 can be used in studies related to IKZF2-dependent cancers.
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SR-5037
0 ImagesSR-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM; Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer.
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(R)-MRT-6160
0 ImagesCat. No.: HY-164773CAS No.: 3050683-63-8(R)-MRT-6160 is a molecular glue degrader targeting VAV1, with a DC50 of 40.93 nM. (R)-MRT-6160 induces VAV1 ubiquitination and proteasomal degradation by forming a CRBN-(R)-MRT-6160-VAV1 ternary complex, thereby inhibiting signaling downstream of the T/B cell receptor. (R)-MRT-6160 can be used in leukemia-related research.
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WIZ degrader 2
0 ImagesCat. No.: HY-163818CAS No.: 2839552-69-9WIZ degrader 2 (Compound 142) is a molecular glue degrader for widely interspaced zinc (WIZ) finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research related to hereditary blood disorders, such as sickle cell disease (SCD) and thalassemia.
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TR-213
0 ImagesCat. No.: HY-177743CAS No.: 2980502-40-5
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PinA1
0 ImagesCat. No.: HY-189201PinA1 is a selective Molecular glue degrader of CK1α with an EC50 of 2.09 µM. PinA1 induces the formation of a stable CRBN-PinA1-CK1α ternary complex to promote the polyubiquitination and subsequent proteasomal degradation of CK1α. PinA1 activates the p53 signaling pathway. PinA1 induces G1 cell cycle arrest. PinA1 induces p53-dependent Apoptosis. PinA1 can be used in studies related to acute myeloid leukemia.
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Z6466608628
0 ImagesCat. No.: HY-175599CAS No.: 2869183-63-9Z6466608628 is a selective PPIL4 molecular glue degrader with human PPIL4 EC50 values of 0.34 µM. Z6466608628 functionally recruits PPIL4 to CRBN, induces CRL4CRBN-mediated ubiquitylation and degradation of PPIL4. Z6466608628 can be used for the research of intracranial aneurysms.
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Lenalidomide 5'-acetamide
0 ImagesCat. No.: HY-W945703CAS No.: 2651996-37-9Lenalidomide 5'-acetamide is a molecular glue.
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ABS-752
0 ImagesCat. No.: HY-W599279CAS No.: 2761170-84-5ABS-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.
