ligands for e3 ligase

PT-179 is a novel IMiD derivative, a molecular gel.

2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}acetic acid (trifluoroacetic acid) is mainly used in compounds Synthesis.

(R)-Thalidomide is a COX 1/2 inhibitor that induces apoptosis in MCF-7, IM-9, HS-Sultan, KB and other cancer cells.

Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride, incorporating an E3 ligase ligand and a linker, can be used as an immunomodulator for the treatment of cancer.

SJ6145 is an effective ligand for KLHDC2SBD, exhibiting a dissociation constant (Kd) of 16.9 μM as determined by Surface Plasmon Resonance (SPR) testing. It has shown an inhibitory concentration 50% (IC50) value of 42 μM in assays testing the inhibition of the binding between KLHDC2SBD and a diglycol degradation peptide.

CST 530 is a monovalent IAP antagonist. It induces cIAP1 and cIAP2 autodegradation in MM.1S cells (cIAP1 degradation at 0.1 μM and cIAP2 degradation at 1 μM after 16 hours). CST 530 reduces cell viability in multiple cancer cell lines including SUDHL6, MOLM13, and HEL (IC50 values ​​of 170 nM, 420 nM, and 450 nM, respectively).

4-Me-Thalidomide is an E3 ligase activator that includes a methyl group. The E3 ligase is a protein that tags other proteins with ubiquitin, leading to their breakdown through proteolysis.

Thalidomide 4-chloro is a chlorinated E3 ligase activator, which can be further derivatized through chlorine substitution.

PROTACMAGLdegrader-1 is an orally active PROTAC agent that simultaneously targets both monoacylglycerol lipase (MAGL) and the E3 ubiquitin ligase MDM2. It functions by degrading MAGL and inhibiting the interaction between MDM2 and p53. Additionally, PROTACMAGLdegrader-1 has partial blood-brain barrier (BBB) penetration and can induce apoptosis in glioblastoma stem cells (GSC).

SJF 0661 is the negative control for SJF 0628. Binds BRAF without inducing degradation.

cisVH 298 is a negative control for VH 298. Exhibits no detectable binding of VHL.

Thalidomide-piperazine hydrochloride is a chemical compound with potential applications in the research of leprosy and multiple myeloma. It serves as a valuable tool in developmental biology, facilitating significant discoveries in the biochemical pathways of limb development [1].

CCW16 is a covalent E3 ubiquitin ligase RNF4 ligand exhibiting cysteine reactivity, capable of inducing ferroptosis in AML cells by activating ROS signalling. CCW16 may be utilised in synthesising PROTAC degraders such as CCW 28-3.

ALV1 is a molecular glue degrader that targets and degrades Ikaros (IKZF1) and Helios (IKZF2), with DC50 values of 2.5 nM and 10.3 nM, respectively. ALV1 binds to CRBN with an IC50 of 0.55 μM and induces the dimerization of CRBN and Helios. It can be used to investigate the properties and functions of regulatory T cells .

2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione is a useful organic compound for research related to life sciences. The catalog number is T64589 and the CAS number is 2154356-63-3.

2-(2,6-Dioxopiperidin-3-yl)-4-iodoisoindoline-1,3-dione is a useful organic compound for research related to life sciences. The catalog number is T64605 and the CAS number is 959150-64-2.

3-(6-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione is a useful organic compound for research related to life sciences. The catalog number is T64632 and the CAS number is 2304513-76-4.

MEL24, an Mdm2 E3 ligase inhibitor, diminishes cell viability and enhances sensitivity to DNA-damaging agents in a p53-dependent manner, suggesting its potential for in vitro antitumor research [1].

VL285 Phenol is an analogue of VL285 featuring a Phenol group. As a small molecule VHL ligand, VL285 serves as a degrader in HaloPROTAC3 synthesis, effectively degrading HaloTag7 fusion proteins (IC 50 = 0.34 μM) [1].

TRIM7-IN-1 (compound89) is an effective inhibitor of TRIM7 with a KD value of 2.6 µM.

Thalidomide-CH2NH2 hydrochloride is an analog of Thalidomide, characterized by a primary amine group. This primary amine is a versatile functional group that can participate in numerous reactions.

tDHU, acid is a dihydropyrimidine cereblon ligand consisting of an E3 ligase ligand and a benzoic acid linker. It serves as an E3 ubiquitin ligase ligand-linker conjugate in the development of PROTACs.

Thalidomide-5-NH-PEG1-NH2 hydrochloride is a Thalidomide-based cereblon ligand designed for CRBN protein recruitment. It facilitates the formation of PROTAC molecules by linking to target protein ligands, such as THAL-SNS-032, via a connector.

Thalidomide-5-NH-PEG3-NH2 hydrochloride is a cereblon ligand based on Thalidomide that targets CRBN proteins. It utilizes a linker to attach to a target protein ligand, facilitating the formation of a PROTAC molecule, such as THAL-SNS-032.