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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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