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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M21519 | U7D-1 | U7D-1 is a first-in-class, potent and selective ubiquitin-specific protease 7 USP7 PROTAC depressant in RS4; The DC50 in 11 cells was 33 nM. U7D-1 has anti-cancer activity. |
| M21512 | SR-1114 | SR-1114 is a first-in-class PROTAC ENL depressant. SR-1114 in MV4; ENL degradation was observed in 11, MOLM-13 and OCI/AML-2 cells with DC50 values of 150 nM, 311 nM and 1.65 μM, respectively. |
| M21435 | MS170 | MS170 is a potent selective PROTAC AKT depressant. MS170 consumes total AKT (T-AKT) and has a DC50 value of 32 nM. MS170 binds to AKT1, AKT2 and AKT3 with Kd of 1.3 nM, 77 nM and 6.5 nM, respectively. |
| M21434 | INY-03-041 | INY-03-041 is an effective and highly selective Protac-based pan-Akt degradation consisting of GDC-0068, an ATP-competitive AKT inhibitor conjugated to lenalidomide (Cereblon ligand). INY-03-041 inhibited AKT1, AKT2 and AKT3 with IC50 values of 2.0 nM, 6.8 nM and 3.5 nM, respectively. |
| M21359 | DSPE-PEG-Biotin (MW 2000) | DSPE-PEG-Biotin (MW 2000) is a PROTAC linker, which belongs to the PEG class. It can be used to synthesize PROTAC molecules. |
| M21318 | Biotin-PEG4-amino-t-Bu-DADPS-C6-azide | Biotin-PEG4-amino-t-Bu-DADPS-C6-azide is a PROTAC linker, which belongs to the PEG class. It can be used for the synthesis of PROTAC molecules.*The compound is unstable in solutions, freshly prepared is recommended |
| M21231 | PROTAC CDK9 Degrader-1 | PROTAC CDK9 Degrader-1 is a PROTAC linked by Cereblon ligand and CDK ligand and is a selective CDK9 degrader. |
| M21192 | ARD-2585 | ARD-2585 is a potent, orally active PROTAC reducer of the androgen receptor. |
| M21160 | ARD-61 | ARD-61 is a potent and specific PROTAC androgen receptor (AR) depressant. ARD-61 effectively and efficiently induces AR and progesterone receptor (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and also effectively inhibits tumor growth in a mouse MDA-MB-453 xenograft model. |
| M21153 | MG-277 | MG-277 is a molecular gel degrader that efficiently induces degradation of the translation termination factor GSPT1 based on Cereblon E3 ligands with a DC50 of 1.3 nM. MG-277 inhibits tumor cell growth in a non-p53 manner with an IC50 of 3.5 nM and 3.4 nM for RS4;11 cells and p53 mutant RS4;11/IRMI-2 cells, respectively. MG-277 exhibited potent anticancer activity. |
| M21137 | Folate-MS432 | The FOLR1-targeted folate receptor-dependent PROTAC conjugate, folate-MS432, is a MEK1/2 degrader that targets FOLR1, a receptor highly expressed in many cancer cell types, but less expressed in most cases. |
| M21032 | GMB-475 | GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. |
| 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). |
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