DC49931 |
NVP-DKY709
Featured
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NVP-DKY709 is a powerful IKZF2 inhibitor with significant potential for cancer therapy. |
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DC50173 |
dCeMM4
Featured
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dCeMM4 (Compound 5) is a molecular glue degrader that facilitates the ubiquitination and degradation of cyclin K. It achieves this by promoting an interaction between the CDK12-cyclin K complex and the CRL4B ligase complex. |
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DC50183 |
dCeMM2
Featured
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dCeMM2 (Compound 2) is a molecular glue degrader that drives the ubiquitination and degradation of cyclin K. It achieves this by facilitating an interaction between the CDK12-cyclin K complex and the CRL4B ligase complex. |
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DC50184 |
dCeMM3
Featured
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dCeMM3 (Compound 3) is a molecular glue degrader that facilitates the ubiquitination and degradation of cyclin K. It achieves this by promoting an interaction between the CDK12-cyclin K complex and the CRL4B ligase complex. |
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DC50245 |
CFT7455
Featured
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CFT7455 is an orally bioavailable degrader of the zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3). It functions as an anticancer agent by binding with high affinity to the cereblon E3 ligase, exhibiting a Kd of 0.9 nM (WO2022032132A1; Compound 1). |
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DC70109 |
(R)-CR8
Featured
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(R)-CR8 (CR8), a second-generation derivative of Roscovitine, is a highly effective inhibitor of CDK1/2/5/7/9. It exhibits inhibitory activity against 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 demonstrates neuroprotective properties. Additionally, it functions as a molecular glue degrader, specifically targeting and depleting cyclin K. |
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DC70900 |
WBC100
Featured
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WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active molecular glue degrader targeting c-Myc. It facilitates the degradation of c-Myc through the ubiquitin E3 ligase CHIP-mediated 26S proteasome pathway. WBC100 is specifically utilized for research involving c-Myc overexpressing tumors. |
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DC70978 |
Thalidomide-piperazine hydrochloride
Featured
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Thalidomide-piperazine hydrochloride represents a chemically modified derivative of the prototypic immunomodulatory drug, featuring a piperazine moiety that enhances solubility while preserving the compound's unique biological properties. |
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DC71590 |
(Rac)-CFT7455
Featured
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(Rac)-CFT7455 is a potent, racemic small-molecule degrader of the zinc finger transcription factors IKZF1 (Ikaros) and IKZF3 (Aiolos), operating through ubiquitin-proteasome-mediated degradation. It demonstrates exceptional cellular potency, with a GI50 of 0.05 nM in NCI-H929.1 cells. As the racemic form of CFT7455, it retains the same anticancer activity by selectively targeting IKZF1/3 for proteasomal destruction. |
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DC60254 |
HQ461
Featured
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HQ461 is a molecular glue degrader that facilitates the interaction between CDK12 and the DDB1-CUL4-RBX1 E3 ubiquitin ligase, resulting in the polyubiquitination and subsequent degradation of the CDK12-interacting protein Cyclin K (CCNK). This degradation impairs CDK12 function, leading to reduced phosphorylation of its substrates, downregulation of DNA damage response genes, and ultimately, cell death. |
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DC71971 |
SJPYT-195
Featured
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SJPYT-195 is a potent cytotoxic degrader of GSPT1, serving as a valuable compound for PROTAC (proteolysis-targeting chimera) synthesis and targeted protein degradation research. |
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DC72103 |
Golcadomide(CC-99282)
Featured
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Golcadomide (CC-99282) is a highly potent and orally bioavailable CRBN E3 ligase modulator (CELMoD). It interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, facilitating the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide holds significant promise for research in cancer-related areas, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL). |
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DC60460 |
SJ3149
Featured
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SJ3149 is a highly selective and potent molecular glue degrader targeting CK1α protein, exhibiting broad antiproliferative activity. It is a valuable tool for cancer research. |
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DC60777 |
EN450
Featured
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EN450 is a cysteine-reactive covalent molecular glue degrader specifically designed to target NF-κB. |
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DC60500 |
NVS-STG2
Featured
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NVS-STG2 is a molecular glue that targets STING and activates STING-mediated immune signaling. It promotes higher-order oligomerization of human STING by binding to pockets between adjacent STING dimer transmembrane domains, effectively functioning as a molecular glue. NVS-STG2 enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. It demonstrates significant antitumor activity in animal models. |
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DCC3332 |
Mg-277
Featured
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MG-277, a molecular glue degrader, efficiently induces the degradation of the translation termination factor GSPT1, based on the Cereblon E3 ligand, with a DC50 of 1.3 nM. It potently inhibits tumor cell growth in a p53-independent manner, demonstrating IC50 values of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells. MG-277 exhibits significant anticancer activity. |
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DCC5425 |
Voclosporin
Featured
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Voclosporin (ISAtx-247) is an inhibitor of calcineurin (PP2B), also known as CN, exhibiting its activity through targeted suppression of this enzyme. |
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DCC5670 |
Zxh-1-161
Featured
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ZXH-1-161 is a potent cereblon (CRBN) modulator, demonstrating an IC50 value of 39 nM in MM1.S wild-type cells. It exhibits selective degradation activity toward GSPT1 and is a valuable tool for researching multiple myeloma. |
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DC65810 |
KT-333
Featured
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KT-333 is a first-in-class molecular glue that induces selective degradation of STAT3 via the ubiquitin-proteasome system by simultaneously engaging STAT3 and the VHL E3 ligase. This novel mechanism enables potent STAT3 depletion with minimal off-target effects, demonstrating strong anti-tumor activity in hematologic malignancies. |
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DC60549 |
IBG3
Featured
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IBG3 is a PROTAC-like degrader that exhibits superior degradation efficiency for BRD4 and BRD2 compared to IBG1, with DC50 values of 6.7 pM and 8.6 pM, respectively. |
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DC60559 |
PT-179
Featured
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PT-179 is a novel orthogonal immunomodulatory drug (IMiD) derivative that selectively binds to CRBN without inducing degradation of off-target proteins. It demonstrates potent activity in degrading proteins fused to SD40, regardless of whether the fusion occurs at the N or C terminus. |
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DC73095 |
CCT373566
Featured
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CCT373566 is a highly potent, in vivo active BCL6 degrader, demonstrating an IC50 of 2.2 nM in TR-FRET assays and a DC50 of 0.7 nM in cellular BCL6 degradation assays. |
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DC73176 |
NCT02
Featured
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NCT02 is a small molecule that triggers the ubiquitination of cyclin K (CCNK), leading to its proteasomal degradation along with its complex partner CDK12. |
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DC74482 |
CC-3240
Featured
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CC-3240 is an optimized molecular glue degrader derived from CC-8977, demonstrating high-affinity binding to CaMKK2 (IC50 = 9 nM) and potent degradation efficacy (DC50 = 100 nM in THP1 cells, Dmax = 92%). This novel compound effectively hijacks the ubiquitin-proteasome system to induce targeted CaMKK2 depletion, offering a superior pharmacological approach over traditional kinase inhibition. |
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DC74572 |
DEG-77
Featured
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DEG-77 is a cereblon-dependent degrader targeting IKZF2 and casein kinase 1α (CK1α). It effectively blocks cell growth and delays leukemia progression in both murine and human acute myeloid leukemia (AML) mouse models. |
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DC60567 |
dCeMM1
Featured
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dCeMM1 is a molecular glue degrader targeting RBM39. It functions by redirecting the activity of the CRL4DCAF15 ligase, leading to a reduction in RBM39 levels in WT KBM7 cells. |
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DC60572 |
NST-628
Featured
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NST-628 is a brain-penetrant molecular glue targeting the MAPK pathway, effectively inhibiting RAF phosphorylation and MEK activation. By binding to RAF, it disrupts the formation of BRAF-CRAF and BRAF-ARAF heterodimers, thereby blocking the RAS-MAPK signaling cascade. NST-628 exhibits potent anti-tumor activity in RAS- and RAF-driven cancers, demonstrating significant efficacy in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumor models. |
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DC60617 |
dWIZ-1
Featured
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dWIZ-1 is a first-in-class molecular glue degrader that specifically targets the WIZ transcription factor for proteasomal degradation, leading to potent induction of fetal hemoglobin (HbF) in erythroblasts. This novel compound functions by enhancing the interaction between CRBN and WIZ, demonstrating an EC50 of 547 nM for CRBN-WIZ complex formation. |
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DC60624 |
OPB-171775
Featured
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OPB-171775 represents a breakthrough in GIST treatment as a first-in-class, non-tyrosine kinase inhibitor (non-TKI) compound that demonstrates potent antitumor activity independent of KIT mutation status. Unlike conventional TKIs that target oncogenic kinases, OPB-171775 operates through an innovative mechanism by orchestrating a protein-protein interaction between phosphodiesterase 3A (PDE3A) and Schlafen 12 (SLFN12). |
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DC60634 |
LL-K12-18
Featured
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LL-K12-18 is a highly potent dual-site molecular glue that induces the formation of the CDK12-DDB1 complex, exhibiting an EC50 of 0.37 nM. It demonstrates 80-fold greater potency than SR-4835 in MDA-MB-231 cells and a remarkable 307-fold increase in potency (EC50 = 0.03 nM) in MDA-MB-468 cells, while its degradation efficiency (DC50 = 0.38 nM) is 50-fold enhanced. |
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