| DC67333 |
MYC degrader 1 TFA
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MYC degrader 1 TFA (compound A80.2HCl) is an orally available molecular glue degrader targeting MYC, exhibiting significant anti-tumor activity. It restores pRB1 protein function and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. |
| DC67332 |
GBD-9
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GBD-9 is a dual-mechanism degrader that effectively targets BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It functions both as a PROTAC molecule to degrade BTK and as a molecular glue to induce GSPT1 degradation. GBD-9 demonstrates potent inhibition of cancer cell growth. |
| DC67331 |
MMH2
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MMH2 is a novel BRD4 molecular glue degrader that operates by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2). |
| DC67330 |
MYC degrader 1
|
MYC degrader 1 (compound A80.2HCl) is an orally available molecular glue degrader targeting MYC, with significant anti-tumor activity. It restores pRB1 protein function and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. |
| DC67329 |
TMX1
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TMX1 is a covalent molecular glue degrader targeting BRD4. It selectively recruits DCAF16 to the BRD4BD2 domain, resulting in the degradation of BRD4. |
| DC67328 |
ALV1
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ALV1 is a molecular glue degrader targeting Ikaros (IKZF1) and Helios (IKZF2), with DC50 values of 2.5 nM and 10.3 nM, respectively. It binds to CRBN with an IC50 of 0.55 µM and induces CRBN-Helios dimerization. ALV1 is a valuable tool for studying the properties and functions of regulatory T cells (Treg cells). |
| DC67327 |
Lenalidomide hemihydrate
|
Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of thalidomide, functions as a molecular glue and is an orally active immunomodulator. It acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN), facilitating the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase complex. Lenalidomide hemihydrate specifically inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and promotes the release of IL-2 from T cells.
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| DC67326 |
LYG-409
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LYG-409 is an orally active degrader of GSPT1, demonstrating significant efficacy against acute myeloid leukemia and prostate cancer in vivo, with tumor growth inhibition (TGI) rates of 94.34% and 104.49%, respectively. In vitro, LYG-409 effectively inhibits KG-1 cells by degrading GSPT1, exhibiting an IC50 of 9.50 nM and a DC50 of 7.87 nM. |
| DC67325 |
(S)-ACE-OH
|
(S)-ACE-OH is a molecular glue exhibiting anticancer properties by facilitating the degradation of nucleoporins and disrupting nucleocytoplasmic transport. It achieves this by inducing an interaction between the E3 ubiquitin ligase TRIM21 and the nucleoporin NUP98. |
| DC67324 |
VAV1 degrader-3
|
VAV1 degrader-3 (Example 185) is an orally active molecular glue degrader targeting VAV1, with a DC50 of 7 nM. It effectively reduces immune cell activation, proliferation, and cytokine production, making it a promising candidate for studying inflammatory and autoimmune disorders. Additionally, VAV1 degrader-3 demonstrates efficacy in inhibiting disease progression in experimental models such as autoimmune encephalomyelitis (EAE) and collagen-induced arthritis (CIA) in mice. |
