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).

BMS-986449 is an IKZF2 (Helios)/IKZF4 (Eos) degrader and CELMoD molecular glue. It redirects the interaction between the E3 ubiquitin ligase Cereblon and Helios/Eos in primary Treg cells, inducing their degradation, and may be utilised for anti-tumour immunotherapy.

BMS-986470 is a CRBN E3 ubiquitin ligase modulator (CELMoD) that can activate fetal hemoglobin (HbF). It is an orally-administered dual-target molecular glue degrader, primarily acting on ZBTB7A and WIZ proteins. This compound can significantly promote the expression of γ-globin and has significant application value in the study of 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.

AMPTX-1 is a molecular glue functioning as a potent, selective, and reversible covalent degrader of BRD9 by recruiting it to the E3 ligase DCAF16.

dGEM3 is a molecular glue degrader targeting GEMIN3 (a component of the survival of motor neuron complex). It is applicable in research on diseases related to abnormal protein regulation, such as cancer and neurodegenerative disorders.

KMG-1068 (Compound 4a), a molecular glue, acts as a GSPT1/2 degrader. By binding to the IMiD binding site on CRBN, KMG-1068 efficiently induces CRBN-dependent degradation of GSPT1/2 and facilitates the formation of a ternary complex with GSPT1/2. KMG-1068 holds potential for use in cancer research.

(S)-dHTC1 is a molecular glue degrader specifically targeting the transcriptional coactivator ENL. It exhibits high affinity binding to E3 ligase only upon formation of the ENL:(S)-dHTC1 complex, with an IC50 of 93 nM. In MV4;11 cells, (S)-dHTC1 degrades ENL with a DC50 of 26 nM. This compound can be utilized for acute myeloid leukemia research.

BWA-6047 is a dual AR/AR-V7 and GSPT1 PROTAC-type degrader (AR: DC50= 3.7 nM; AR-V7: DC50= 3.0 nM; GSPT1: DC50= 1.2 nM). It facilitates the ubiquitination and degradation of AR/AR-V7 and, through molecular glue properties, induces a PPI between GSPT1 and CRBN, leading to GSPT1 degradation. BWA-6047 is applicable in prostate cancer research.

IKZF2-degrader 1 (Compound 31) is a molecular glue-type degrader of IKZF2 with a DC50 of 0.5 nM. It exhibits relatively low degradation activity against CK1α, with a DC50 of 210 nM. This compound is applicable in research focused on IKZF2-dependent cancers.

BTX-7312 is a cereblon-based SOS1 bifunctional degrader and acts as a molecular glue (molecular glue). It reduces downstream signaling markers pERK and pS6 and demonstrates antiproliferative activity in cells with various KRAS mutations.

CDO1 degrader-1 (compound 8) is a molecular glue degrader specifically targeting cysteine dioxygenase (CDO1).

IBG3 is a bifunctional BET molecular glue degrader containing two JQ1 moieties, designed to target and degrade proteins through an intramolecular bivalent mechanism. It acts as a degrader for BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively.

KRAS ligand 4 (Compound 2) is a dual-functional molecular glue degrader based on SOS1. It reduces downstream signaling markers pERK and pS6, and exhibits antiproliferative activity in cells with various KRAS mutations.

BRD4 degrader-2 (Compound JP-2-197) is a covalent and monovalent molecule glue-type BRD4 degrader. It targets RNF126 (E3 ligase) to degrade both long and short isoforms of BRD4 in cells.

CDK4 degrader1 (ML 1–71) is a molecular glue degrader specifically targeting CDK4.

BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue-type degrader targeting BRD4. It specifically directs the degradation of BRD4 long and short isoforms in cells by targeting DCAF16 (E3 ligase).

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.