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PROTAC Proteolysis Targeting Chimeric Molecules

Cat.No.  Name Information
M40697 NX-5948 NX-5948 (BTK-IN-24) is an orally active, blood-brain barrier-penetrating, BTK-targeting degradation agent for the study of B-cell malignancies and autoimmune diseases. NX-5948 induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation.
M10423 DT2216 DT2216 is a BCL-XL protein hydrolysis targeting chimera (PROTAC) that ligates and degrades BCL-XL with E3 ubiquitin (E3) ligase. DT2216 is effective against a variety of BCL-XL-dependent leukemias and cancer cells.
M10382 PROTAC SGK3 degrader-1 PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a potent SGK3 degrader, it is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3.
M59143 AK-1690 AK-1690 is a potent and selective STAT6 PROTAC degrader. AK-1690 reduces the levels of STAT6 protein in cells (DC50=1 nM) and depletes STAT6 protein in mouse tissues.
M58355 xStAx-VHLL TFA xStAx-VHLL TFA, a PROTAC, sustains β-catenin degradation and manifested strong inhibition of Wnt signaling. xStAx-VHLL TFA promotes β-catenin ubiquitination.
M58163 (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level.
M50170 ARV-393 ARV-393 is an orally active PROTAC degrader targeting BCL6 for studies related to diffuse large B-cell lymphoma. ARV-393 utilizes the ubiquitin-proteasome system to target the degradation of BCL6.
M41654 SMD-3040 SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM).
M40698 KT-333 KT-333 is a heterobifunctional degradation agent (PROTAC) of the transcriptional regulator STAT3 and can be used in studies related to T-cell malignancies and solid tumors. KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity.
M40692 BGB-16673 BGB-16673 is an orally active chimeric degradation-activating compound targeting BTK that degrades wild-type BTK and a variety of mutant BTKs, and can be used in studies related to B-cell malignancies as well as non-Hodgkin's lymphoma.
M31304 AU-15330 AU-15330 is a protein hydrolysis-targeted chimeric (PROTAC) degradation of SWI/SNF ATPase subunits SMARCA2 and SMARCA4, and also induces effective tumor growth inhibition in a prostate cancer xenograft model.
M31275 JQAD1  JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
M29649 PROTAC PD-1/PD-L1 degrader-1  PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
M29635 PROTAC IRAK4 degrader-7  PROTAC IRAK4 degrader-7 (Compound I-417) is a potentially first-in-class, orally active PROTAC IRAK4 degrader with antitumor activity for studies related to hidradenitis suppurativa (HS) and atopic dermatitis (AD).
M29586 KB02-JQ1  KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
M29577 PROTAC Bcl2 degrader-1  PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.
M29440 TL12-186  TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM).
M29378 MS177  MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
M29324 dBRD9  dBRD9 is a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.
M29228 BRD4 degrader AT1  BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in cells.




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