Search Result
Results for "
molecular degrader
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-129917
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PROTACs
Epigenetic Reader Domain
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Cancer
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KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
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- HY-129610
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PROTACs
FKBP
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Cancer
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KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF .
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- HY-144981
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CDK
Molecular Glues
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Cancer
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HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .
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- HY-130122
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Molecular Glues
PROTACs
Apoptosis
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Cancer
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MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
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- HY-164891
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Molecular Glues
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Others
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EM12-FS is a cereblon (CRBN) ligand that binds CRBN at His353 and a molecular glue degrader of NTAQ1. EM12-FS has a human plasma half-life of 196 min .
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-
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- HY-156730
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Molecular Glues
STAT
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Cancer
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KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
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- HY-156730B
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Molecular Glues
STAT
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Cancer
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KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
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-
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- HY-156730A
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Molecular Glues
STAT
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Cancer
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KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .
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-
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- HY-160525
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Molecular Glues
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Cancer
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CDO1 degrader-1 (compound 8) is a molecular glue degrader that targets cysteine dioxygenase (CDO1) .
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- HY-163640
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-
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- HY-169343
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Molecular Glues
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Cancer
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FIZ1 degrader 1 (compound 1) is an IMiD-based molecular glue degrader targeting FIZ1 .
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- HY-156747
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Molecular Glues
DNA/RNA Synthesis
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Cancer
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GSPT1 degrader-2 (Compound 210) is a potent and orally active GSPT1 molecular glue degrader (DC50: < 30 nM). GSPT1 degrader-2 is an antitumor agent .
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- HY-163813
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- HY-160533
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Molecular Glues
IKZF Family
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Cancer
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IKZF1-degrader-2 (Compound 3) is an IKZF1 molecular glues degrader. IKZF1-degrader-2 has anticancer activity and low toxicity .
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- HY-163810
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- HY-163811
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- HY-168624
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Molecular Glues
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Inflammation/Immunology
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VAV1 degrader-2 (Example 176) is a molecular glue degrader based on targeting VAV 1 with a DC50 of 4.41 nM. VAV1 degrader-2 can be used in the study of inflammatory and autoimmune diseases .
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- HY-160531
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Molecular Glues
IKZF Family
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Cancer
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IKZF1-degrader-1 (Compound 9-B) is a IKZF1 molecular glue degrader with the DC50 value of 0.134 nM. IKZF1-degrader-1 can be used to degrader tumors .
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- HY-163641
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Molecular Glues
Androgen Receptor
E1/E2/E3 Enzyme
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Cancer
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AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells .
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-
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- HY-163638
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-
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- HY-162331
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Molecular Glues
STING
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Inflammation/Immunology
Cancer
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STING Degrader-1 (compound 2), a molecular glue, is a potent STING degrader that covalently binds to STING and E3 ligase. STING Degrader-1 exhibits a "hook effect", that degrades 75% STING protein at 10 μM, and degrades ca. 30% STING protein at 30 μM .
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- HY-153385
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- HY-169077
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Molecular Glues
IKZF Family
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Cancer
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IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC50=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3 .
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- HY-163812
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Molecular Glues
Estrogen Receptor/ERR
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Cancer
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ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
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- HY-148523
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Molecular Glues
CDK
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Cancer
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HQ005 is a potent CCNK degrader with an DC50 value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation .
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- HY-163639
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Molecular Glues
Epigenetic Reader Domain
E1/E2/E3 Enzyme
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Cancer
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BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
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- HY-141676
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EGFR
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Others
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HyT36 is a low molecular weight hydrophobic tag that promotes the degradation of fusion protein and pseudokinase Her3 .
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- HY-163064
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Molecular Glues
LRRK2
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Cancer
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CC-3240 (compound 13) is a molecular glue degrader of CaMKK2 based on CC-8977, with the IC50 of 9 nM .
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- HY-155552
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Molecular Glues
Apoptosis
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Cancer
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GSPT1 degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system, serves as one of Molecular Glues. GSPT1 degrader-1 also induces cell G0/G1 phase arrest and apoptosis .
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- HY-153803
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PROTACs
Molecular Glues
Btk
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Cancer
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GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth .
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- HY-144976
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Molecular Glues
CDK
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Cancer
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dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
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- HY-144977
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Molecular Glues
CDK
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Cancer
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dCeMM4 (Compound 5) is a molecular glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
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- HY-P2839
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Heparinase I
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Endogenous Metabolite
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Metabolic Disease
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Heparinase (Heparinase I) degrades heparin to oligosaccharide or unsaturated disaccharide. Heparinase can be used in the preparation of low molecular weight heparin (LMWH) .
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- HY-146184
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Molecular Glues
Bcl-2 Family
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Cancer
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CCT373567 is a potent molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity .
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- HY-160501
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Molecular Glues
CDK
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Cancer
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DS17 is a molecular glue that acts as a potent degrader of cyclin K, with an EC50 of 13 nM. DS17 plays an important role in cancer research .
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- HY-160528
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Molecular Glues
Epigenetic Reader Domain
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Cancer
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IBG3 is a dual-JQ1-containing BET molecular glue degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively .
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- HY-10984
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CC-4047
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Cancer
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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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- HY-139972
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- HY-162318
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Molecular Glues
c-Myc
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Cancer
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MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
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- HY-168625
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Molecular Glues
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Inflammation/Immunology
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VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). VAV1 degrader-3 reduces immune cell activation, immune cell proliferation and the production of various cytokines. VAV1 degrader-3 can be used for research of inflammatory or autoimmune disorder. VAV1 degrader-3 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc. .
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- HY-159098
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Molecular Glues
Histone Acetyltransferase
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Others
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dWIZ-1 is a potent WIZ molecular glue degrader. dWIZ-1 recruitments WIZ(ZF7) to cereblon (CRBN) induces WIZ degradation. dWIZ-1 has the potential for the research of sickle cell disease (SCD) .
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- HY-162318A
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Molecular Glues
c-Myc
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Cancer
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MYC degrader 1 TFA (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 TFA restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
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- HY-144971
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Molecular Glues
CDK
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Cancer
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dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
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- HY-132199
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Molecular Glues
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Cancer
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SJ6986 is a potent, selective and orally active GSPT1/2 Molecular Glue degrader, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1 .
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- HY-160444
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Molecular Glues
Casein Kinase
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Cancer
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SJ3149 is a selective and potent molecular glue degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research .
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- HY-144841
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CFT7455
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Molecular Glues
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Cancer
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Cemsidomide (CFT7455) is a ubiquitin ligase pathway Ikaros/Aiolos degrader with molecular glue activity . Cemsidomide has a GI50 of 0.05 nM for NCIH929.1 cells.
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- HY-156828
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- HY-156827
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-
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- HY-146185
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Molecular Glues
Bcl-2 Family
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Cancer
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CCT373566 is a potent and orally active molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo .
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- HY-144998
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Molecular Glues
IKZF Family
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Inflammation/Immunology
Cancer
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NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
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- HY-161235
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Molecular Glues
Ras
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Cancer
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BTX-7312 is a cereblon-based SOS1 bifunctional degrader and a molecular glue. BTX-7312 reduces downstream signaling markers pERK and pS6 and shows antiproliferative activity in various KRAS-mutated cells .
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- HY-169325
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Molecular Glues
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Cancer
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(S)-ACE-OH is a molecular glue with anticancer activity. (S)-ACE-OH promotes nucleoporin degradation and disruption of nucleocytoplasmic trafficking by inducing the interaction between E3 ubiquitin ligase TRIM21 and nucleoporin NUP98 .
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- HY-10984R
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Cancer
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Pomalidomide (Standard) is the analytical standard of Pomalidomide. This product is intended for research and analytical applications. 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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- HY-161883
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- HY-137206
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Molecular Glues
Ligands for E3 Ligase
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Cancer
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ALV2 is a potent and selective Helios molecular glue degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment .
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- HY-W181530
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Molecular Glues
CDK
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Cancer
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NCT02 is a cyclin K molecular glue. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC) .
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- HY-161236
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Molecular Glues
Ras
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Cancer
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KRAS ligand 4 (compound 2) is a bifunctional molecular glue degrader based on SOS1. KRAS ligand 4 reduces downstream signaling markers pERK and pS6 and displays anti-additional activity in cells with multiple KRAS mutations .
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- HY-122311
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SMTP-7
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Reactive Oxygen Species
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Neurological Disease
Inflammation/Immunology
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Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS .
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- HY-130800
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- HY-144841A
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(Rac)-CFT7455
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Molecular Glues
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Cancer
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(Rac)-Cemsidomide ((Rac)-CFT7455) is the racemate of Cemsidomide (HY-144841) with antitumor activity . Cemsidomide is a ubiquitin ligase pathway Ikaros/Aiolos degrader with molecular glue activity. Cemsidomide has a GI50 of 0.05 nM for NCIH929.1 cells.
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- HY-161779
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Molecular Glues
Epigenetic Reader Domain
Apoptosis
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Cancer
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PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models .
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- HY-10984S3
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- HY-159647
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Molecular Glues
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Cancer
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PLX-4545 is an orally available, cereblon-based molecular glue degrader of IKZF2 (zinc finger transcription factor Helios), which can reprogram immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses .
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- HY-145319
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- HY-122704A
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Aminoquinuride dihydrochloride
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FGFR
HSV
VEGFR
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Infection
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Surfen dihydrochloride is a potent HS (heparan sulfate) antagonist. Surfen binds to glycosaminoglycans. Surfen neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen affects sulfation of heparin and inhibits degradation by heparin lyases. Surfen inhibits FGF2 binding and signaling. Surfen inhibits cell attachment, and virus infection .
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- HY-131863
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide 4'-alkylC8-acid is an E3 ubiquitin ligase ligand-Linker conjugate containing Pomalidomide (HY-10984). Pomalidomide is a third-generation immunomodulator that acts like a molecular glue. Pomalidomide interacts with the E3 ligase cereblon to induce degradation of the essential Ikaros transcription factor .
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- HY-122704
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Aminoquinuride
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FGFR
HSV
VEGFR
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Infection
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Surfen is a potent HS (heparan sulfate) antagonist. Surfen binds to glycosaminoglycans. Surfen neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen affects sulfation of heparin and inhibits degradation by heparin lyases. Surfen inhibits FGF2 binding and signaling. Surfen inhibits cell attachment, and virus infection .
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- HY-145776
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- HY-169133
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PROTACs
Glutathione Peroxidase
Ferroptosis
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Cancer
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GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenous GPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)) .
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- HY-W012935
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Piperidine-4-carboxaldehyde
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PROTAC Linkers
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Cancer
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Piperidine-4-carbaldehyde (Piperidine-4-carboxaldehyde) is a PROTAC Linker. Piperidine-4-carbaldehyde can be used to optimize combined with the target protein affinity, thus improve the PROTAC the molecular degradation efficiency. Piperidine-4-carbaldehyde can be used in the CDK2 PROTACs (HY-161708) .
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- HY-159099
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Molecular Glues
Histone Acetyltransferase
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Others
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HbF inducer 3 (Compound dWIZ-2) is an orally active molecular glue, which degrades the WIZ transcription factor (DC50=13 nM in primary human erythroid precursor cell) and induces the expression of fetal hemoglobin (HbF) (EC50=100 nM). HbF inducer 3 exhibits good pharmacokinetic characteristics in cynomolgus monkeys .
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- HY-169347
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LC-05-004
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Molecular Glues
Casein Kinase
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Cancer
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dCK1α-2 is an orally active CK1α molecular glue degrader that targets p53 pathway-related targets. dCK1α-2 exhibits anti-tumor efficacy in mouse models and can increase the expression of p53-related genes. .
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- HY-148776
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Biochemical Assay Reagents
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Others
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PLGA-PEG-MAL (20kDA-5.0kDA, LA:GA ratio 50:50) is a kind of poly(lactide-co-glycolide)-block-poly(ethylene glycol) (PLGA-PEG-Mal) nanoparticles. PLGA-PEG-MAL (20kDA-5.0kDA, LA:GA ratio 50:50) has a molecular weight of 20kDA to 5.0kDA and contains a 50:50 ratio of lactic acid (LA) to glycolic acid (GA) molecules. The molecular ratio of LA to GA determines the rate of matrix degradation and protein re-release .
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- HY-150641
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CDK
Apoptosis
DNA/RNA Synthesis
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Cancer
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CDK-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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- HY-161767
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Molecular Glues
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Cancer
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JWJ-01-306 is a molecular glue that targets the C2H2 zinc finger transcription factor ZBTB11. JWJ-01-306 degrades ZBTB11, reduces the oxidative phosphorylation (OXPHOS) and tricarboxylic acid (TCA) cycle, and inhibits the proliferation of KAS-resistant PDAC cells. JWJ-01-306 exhibits good pharmacokinetic characteristics in mouse model .
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- HY-160695
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Ligands for E3 Ligase
Molecular Glues
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Cancer
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PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms .
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- HY-49444
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NF-κB
Molecular Glues
E1/E2/E3 Enzyme
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Cancer
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EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .
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- HY-141881
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PROTACs
Apoptosis
SF3B1
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Cancer
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PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells .
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- HY-115461
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Insulin Receptor
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Metabolic Disease
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MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake .
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- HY-160777
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Galeterone 3β-imidazole
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Molecular Glues
Androgen Receptor
MNK
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Cancer
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VNPP433-3β is a 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 inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
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- HY-A0003
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Lenalidomide
Maximum Cited Publications
39 Publications Verification
CC-5013
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Inflammation/Immunology
Cancer
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Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-A0003B
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CC-5013 hemihydrate
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Cancer
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Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-A0003A
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CC-5013 hydrochloride
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Ligands for E3 Ligase
Molecular Glues
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Inflammation/Immunology
Cancer
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Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-163944
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Molecular Glues
CDK
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Cancer
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LL-K12-18 is a two-site molecular glue that enhances the protein-protein interaction of the CDK12-DDB1 complex, stabilizing the CDK12-DDB1 complex and promoting the degradation of cyclin K (EC50=0.37 nM). LL-K12-18 exhibits strong gene transcription inhibition and anti-proliferation effects in tumor cells. LL-K12-18 can be used in cancer research .
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- HY-N10502
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MDM-2/p53
HSP
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Cancer
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Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo .
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- HY-A0003R
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Ligands for E3 Ligase
Molecular Glues
Apoptosis
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Inflammation/Immunology
Cancer
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Lenalidomide (Standard) is the analytical standard of Lenalidomide. This product is intended for research and analytical applications. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-149127
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ASC-JM17; ALZ-003
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Keap1-Nrf2
Androgen Receptor
HSP
Mitophagy
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Metabolic Disease
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Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
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- HY-A0003S2
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CC-5013-13C5,15N
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Ligands for E3 Ligase
Apoptosis
Molecular Glues
Isotope-Labeled Compounds
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Inflammation/Immunology
Cancer
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Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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- HY-18340
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CR8, (R)-Isomer
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Molecular Glues
CDK
Apoptosis
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Neurological Disease
Cancer
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(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .
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- HY-18340A
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CR8, (R)-Isomer trihydrochloride
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Molecular Glues
CDK
Apoptosis
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Neurological Disease
Cancer
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(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .
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- HY-145448
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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MC-VC-PABC-amide-PEG1-CH2-CC-885 (compound III) is a neoDegrader, a conjugate of the GSPT1 degrader/molecular glue CC-885 (HY-101488) and a linker. MC-VC-PABC-amide-PEG1-CH2-CC-885 can be conjugated to the antibody DAR3.7 that specifically targets CD56 to synthesize Antibody-Drug Conjugates (ADCs). MC-VC-PABC-amide-PEG1-CH2-CC-885 can also be conjugated to Belantamab (HY-P9980), Daratumumab (HY-P9915), huMy9-6 IgG1, Indatuximab (HY-P990607), Isatuximab (HY-P9976), lintuzumab IgG1, Pertuzumab (HY-P9912), OR000213, Rituximab (HY-P9913), Sacituzumab (HY-P99045), Trastuzumab (HY-P9907)and U3-1784 (HY-P990672) to form conjugates .
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HY-L137
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54 compounds
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Targeted protein degradation(TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention.
Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy.
MCE supplies a unique collection of 54 molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.
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HY-L183
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287 compounds
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Pesticide is a single substance or mixture that can be used to prevent, mitigate, iminate pests or as a plant conditioner, defoliant or desiccant. In recent years, scientists have proposed the concept of "Molecules to Ecosystems", bringing the concept of molecular biology to understand the impact of pesticides, degradation and relationship with the environment or organisms. MCE integrates effective compounds approved as pesticides by agencies such as the Environmental Protection Agency (EPA) and some insecticidal compounds with potential for agricultural applications.
MCE can provide a library of 287 pesticide compounds that are tool compounds for relevant research.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-106263B
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Peptides
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Cancer
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Tyroserleutide hydrochloride, isolated from the degradation products of porcine spleen , is a small molecular tripeptide which inhibits tumor growth both in vitro and in vivo .
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- HY-106263
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Peptides
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Cancer
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Tyroserleutide (YSL), isolated from the degradation products of porcine spleen , is a small molecular tripeptide which inhibits tumor growth both in vitro and in vivo .
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- HY-106263A
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Peptides
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Cancer
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Tyroserleutide TFA, isolated from the degradation products of porcine spleen , is a small molecular tripeptide which inhibits tumor growth both in vitro and in vivo .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-10984S3
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Pomalidomide- 15N, 13C5 is 15N and 13C labeled Pomalidomide (HY-10984). 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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- HY-A0003S2
-
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Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
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Cat. No. |
Product Name |
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Classification |
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- HY-148776
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Polymers
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PLGA-PEG-MAL (20kDA-5.0kDA, LA:GA ratio 50:50) is a kind of poly(lactide-co-glycolide)-block-poly(ethylene glycol) (PLGA-PEG-Mal) nanoparticles. PLGA-PEG-MAL (20kDA-5.0kDA, LA:GA ratio 50:50) has a molecular weight of 20kDA to 5.0kDA and contains a 50:50 ratio of lactic acid (LA) to glycolic acid (GA) molecules. The molecular ratio of LA to GA determines the rate of matrix degradation and protein re-release .
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