glue degrader

dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) is a glue degrader. dCeMM3 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, result in inducing ubiquitination and degradation of cyclin K.

dCeMM1, a RBM39 glue degrader, re-directs the activity of the CRL4DCAF15 ligase and decreases RBM39 expression levels in WT KBM7 cells.

dWIZ-1 ((rac)-dWIZ-1) is a potent WIZ molecular gel degrader that recruits WIZ (ZF7) to the cereblon thereby inducing degradation and thus induction of haemoglobin fetalis (HbF) in erythroblasts, which can be used to study sickle cell disease (SCD).

(R)-CR8 trihydrochloride (CR8, (R)-Isomer trihydrochloride) is a CDK1 2 5 7 9 inhibitor that acts as a molecular glue degrader with neuroprotective activity and induces apoptosis.

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader, also known as a molecular glue, that facilitates the degradation of nuclear FKBP12 by covalently modifying DCAF16, an E3 ligase. SLF acts as a linker, binding to the ubiquitin E3 ligase ligand KB02, thus forming KB02-SLF[1] and enhancing the longevity of protein degradation in biological systems.

SJ46411-Br is an orally effective CK1α molecular glue (Molecular Glue) degrader. It binds with CRL2^KLHDC2 to facilitate the formation of a cooperative homoselective ternary complex. Furthermore, SJ46411-Br is coupled with the BET ligand JQ1 through a PROTAC linker, enabling the synthesis of corresponding PROTACs.

QXG-6442 is a molecular glue degrader targeting CK1α, demonstrating a degradation potency with a DC50 of 5.7 nM and a Dmax of 90%. In the MOLM-14 cell line, QXG-6442 induces antiproliferative effects.

dCeMM4 (Compound 5) is a glue degrader that promotes cyclin K ubiquitination and degradation by facilitating the interaction between CDK12-cyclin K and a CRL4B ligase complex [1].

dCeMM2 is a glue degrader. dCeMM2 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, leading to the ubiquitination and degradation of cyclin K.

WBC100 (14-D-Valine-TPL) is a potent, selective, orally active c-Myc glue degrader targeting the ubiquitin E3 ligase CHIP-mediated 26S proteasome pathway, primarily used in research for c-Myc overexpressing tumors [1].

GBD-9, a dual-mechanism degrader, effectively promotes the degradation of BTK and GSPT1 through recruitment of E3 ligase cereblon (CRBN). As a PROTAC molecule, GBD-9 induces BTK degradation, while also acting as a molecular glue for GSPT1 degradation, demonstrating potent inhibition of cancer cell growth [1].

PROTACGSPT1 degrader-2 (compound A) acts as a molecular glue for GSPT1, achieving degradation efficiencies exceeding 95%. Meanwhile, GSPT1 degrader-8 exhibits inhibitory effects on HL-60 cells, demonstrating an IC50 of 10 nM.

BRD9 Degrader-3 (compound B20) is a molecular glue for BRD9 with a DC50 of less than 1.25 nM.

JP-2-249, a molecular glue, serves as an effective degrader of SMARCA2. At concentrations ranging from 1-10 μM, JP-2-249 reduces the protein levels of SMARCA2 in MV-4-11 cells.

HQ461 is a molecular glue that promotes CDK12-DDB1 interaction, triggering cyclin K degradation, decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death.