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 (380)
Related Products (380)
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Related Compound Screening Libraries (1)
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MI-2-80
0 ImagesCat. No.: HY-175600CAS No.: 1010099-35-0MI-2-80 is a molecular glue degrader. MI-2-80 induces proteins (such as IKZF1/3 and CSNK1A1) to bind to CRBN, promoting their ubiquitination and degradation.
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GSPT1 degrader-10
0 ImagesCat. No.: HY-159610CAS No.: 3024909-61-0GSPT1 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.
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Pomalidomide-d5
0 ImagesCat. No.: HY-10984SCAS No.: 1377838-49-7Synonyms: CC-4047-d5Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
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LC-MG-5
0 ImagesCat. No.: HY-184321LC-MG-5 is a selective molecular glue degrader targeting FGFR2, with a DC50 of 231.7 nM in KATO III cells. LC-MG-5 induces proteasomal degradation of FGFR2 in a DCAF16-dependent manner via a covalent molecular glue mechanism. LC-MG-5 inhibits cancer cell proliferation. LC-MG-5 suppresses PI3K/AKT and MAPK/ERK signaling pathways mediated by FGFR2. LC-MG-5 can be used in the research of gastric cancer.
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Cyclosporin A-OVA
0 ImagesCat. No.: HY-NP194ACyclosporin A-OVA is a conjugate of Cyclosporin A (HY-B0579) and OVA. Cyclosporin A is an immunosuppressant which binds to the cyclophilin .
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KAT2A degrader-2
0 ImagesCat. No.: HY-187169KAT2A degrader-2 is a selective molecular glue degrader targeting KAT2A, with a DC50 of 22 nM in Kelly cells. KAT2A degrader-2 acts as a molecular glue to recruit KAT2A to CRBN, forming a ternary complex that drives the polyubiquitination and proteasome-dependent degradation of KAT2A. KAT2A degrader-2 reduces the acetylation level of histone H3 lysine 9 via the ubiquitin-like and proteasome-dependent pathway. KAT2A degrader-2 can be used for the research of acute myeloid leukemia.
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CDK-IN-9
0 ImagesCat. No.: HY-150641CAS No.: 3031561-92-6CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.
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MNN-02-155
0 ImagesCat. No.: HY-173641CAS No.: 3067681-22-2MNN-02-155 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. MNN-02-155 induces potent activation of the BCL6-target reporter gene and cell death. MNN-02-155 can be used for the study of diffuse large B cell lymphomas (DLBCLs).
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MG-Lin1
0 ImagesCat. No.: HY-177731MG-Lin1 is a Lin28/Lin28A molecular glue degrader with a DC50 of approximately 0.7 μM. It induces Lin28 degradation via the ubiquitin-proteasome pathway by forming a ternary complex, thereby upregulating the levels of let-7 miRNA and reducing the expression of its downstream oncogenic targets KRAS and PDK1, and inhibiting cancer cell migration. MG-Lin1 can be used in studies of ovarian cancer and choriocarcinoma.
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VNPP433-3β hydrochloride
0 ImagesCat. No.: HY-160777BCAS No.: 3026905-91-6Synonyms: Galeterone 3β-imidazole hydrochlorideVNPP433-3β (Galeterone 3β-imidazole) hydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β hydrochloride induces cell apoptosis. VNPP433-3β hydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
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WB214
0 ImagesCat. No.: HY-182623CAS No.: 2640723-72-2WB214 is an MDM2 and GSPT1 molecular glue degrader with human MDM2 Ki >10 μM. WB214 induces a neo-interaction between MDM2 and the cereblon E3 ligase complex, triggering MDM2 ubiquitination, proteasomal degradation, and bystander p53 degradation, and does not bind MDM2’s p53 binding region. WB214 induces GSPT1 degradation, and exhibits anti-proliferative activity in leukemia cells. WB214 can be used for the research of leukemia.
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GSPT2 degrader-1
0 ImagesCat. No.: HY-177744CAS No.: 3093413-09-0GSPT2 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.
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Cyclin K degrader 2
0 ImagesCat. No.: HY-177780Cyclin K degrader 2 is a molecular glue degrader of Cyclin K. By bridging CDK12 and DDB1, the receptor of the CRL4 E3 ligase, Cyclin K degrader 2 specifically induces the targeted degradation of Cyclin K within the CDK12-Cyclin K complex. Cyclin K degrader 2 can be used in studies related to acute myeloid leukemia.
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SJ46411-Br
0 ImagesCat. No.: HY-168646SJ46411-Br is one of CRL2KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs.
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EN171
0 ImagesEN171 is a covalent 14-3-3σ molecular glue ligand that sequesters neonuclear substrates, including BRD4 and BLC6, into the cytoplasm by recruiting 14-3-3σ. EN171 covalently targets C38 and C96 on 14-3-3 to enhance the interaction between 14-3-3 and ERα, YAP, and TAZ (with EC50 values of 9 μM for human ERα, 45 μM for YAP, and 107 μM for TAZ). EN171 inhibits the transcriptional activity of estrogen receptors and the Hippo pathway in breast cancer cells. EN171 can be used in studies related to breast cancer.
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GSPT1 degrader-18
0 ImagesCat. No.: HY-188006CAS No.: 3052938-18-5GSPT1 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.
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WIZ degrader 3
0 ImagesCat. No.: HY-163819CAS No.: 2839637-72-6WIZ degrader 3 (Compound 29) is a molecular glue degrader for widely interspaced zinc finger motifs (WIZ), with an AC50 of 6.4 nM. WIZ degrader 3 induces the expression of fetal hemoglobin (HbF), with an EC50 of 45 nM. WIZ degrader 3 can be used for the research of blood disorders, such as sickle cell disease and β- thalassemia.
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Lck degrader-1
0 ImagesCat. No.: HY-175280CAS No.: 3095033-62-5Lck degrader-1 is a molecular glue degrader that recruits cereblon to target LCK and CK1α. Lck degrader-1 promotes the formation of the LCK/CRBN-DDB1 ternary complex with an EC50 of 77.1 nM, and induces the degradation of LCK and CK1α. LCK degradation induced by Lck degrader-1 depends on the G415-containing helical G-loop degron, and maintains LCK-degrading activity in cells with the LCK T316I gatekeeper mutation. Lck degrader-1 can be used for research related to T-cell acute lymphoblastic leukemia (T-ALL) and LCK inhibitor resistance.
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JP-2-196
0 ImagesCat. No.: HY-W854844CAS No.: 2913587-30-9JP-2-196 is a molecular glue that covalently targets the RING family E3 ligase RNF126. JP-2-196 also binds to RNF40, MID2, RNF219, RNF14, and LRSAM1. JP-2-196 induces the formation of ternary complexes between RNF126 and target proteins (e.g., BRD4, AR-V7), thereby promoting their ubiquitination and proteasomal degradation. JP-2-196 has potential for cancer research (such as prostate cancer and leukemia).
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CYB-5067
0 ImagesCat. No.: HY-184598CYB-5067 is a FGFR molecular glue degrader with a DC50 of 27 nM against FGFR2. CYB-5067 inhibits FGFR1, FGFR3, FGFR4 and downstream FGFR signaling pathways, induces antiproliferative activity in vitro, and exhibits sustained target protein inhibition in vivo without obvious hook effect. CYB-5067 shows significant tumor growth inhibitory activity in the ETV6-FGFR2 fusion Ba/F3 xenograft model. CYB-5067 can be used for the research of FGFR-driven cancers.
