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PROTAC Proteolysis Targeting Chimeric Molecules

Inhibitors

Cat.No.  Name Information
M14876 THAL-SNS-032 THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
M14875 PROTAC FAK degrader 1 PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM.
M14874 PROTAC BET degrader-2 PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
M14873 PROTAC BET Degrader-1 PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
M14872 MD-224 MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept.
M14871 Gefitinib-based PROTAC 3 Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
M14870 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.
M14869 CP-10 CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM).
M14862 (S,R,S)-AHPC-PEG4-NH2 hydrochloride (S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
M14861 Thalidomide-O-amido-C8-NH2 TFA Thalidomide-O-amido-C8-NH2 TFA (Cereblon Ligand -Linker Conjugates 2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
M13401 SD-36 SD-36 is an effective antiseptic for STAT3 PROTAC (Kd=~50 nM). Sd-36 effectively degraded the mutated STAT3 protein in cells and inhibited the transcriptional activity of STAT3 (IC50=10 nM).
M13398 BSJ-03-204 BSJ-03-204 is a Cereblon ligand linked to THE CDK ligand PROTAC, which is an effective, selective cdK4/6 dual inhibitor based on Palbociclib (HY-50767). The IC50 of CDK4/D1 and CDK6/D1 were 26.9 nM and 10.4 nM, respectively.
M13389 ACBI1 ACBI1 is an effective and synergistic PROTAC inhibitor of SMARCA2, SMARCA4 and PBRM1, with DC50 of 6 nM, 11 nM and 32 nM in MV-4-11 cells, respectively. ACBI1 can induce antiproliferative effect and apoptosis.
M10423 DT2216 DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC).
M10386 MT-802 MT-802 is a potent BTK degrader based on PROTAC technology, it induces Bruton's tyrosine kinase (BTK) knockdown.
M10385 PROTAC KRASG12C Degrader-LC-2 PROTAC KRASG12C Degrader-LC-2 is a potent first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM.
M10384 Homo-PROTAC pVHL30 degrader 1 Homo-PROTAC pVHL30 degrader 1 is a pVHL30 degrader based on PROTAC and a potent VHL inhibitor.
M10383 Homo-PROTAC cereblon degrader 1 (OUN20985) Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
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.
M10381 TD-165 TD-165 is a PROTAC-based cereblon (CRBN) degrader.



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