| 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. |
| 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). |
| 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. |
| M25607 | ARV-766 | ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations. ARV-766 has the potential to be first- and best-in class PROTAC AR degrader in mCRPC. |
| M25507 | dCBP-1 | dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression. |
| M22449 | Pomalidomide-PEG2-COOH | Pomalidomide-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology. |
| M22448 | Thalidomide-NH-PEG3-propionic acid | Thalidomide-NH-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology. |
| 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. |
| M21159 | SD-36 | SD-36 is a potent STAT3 PROTAC degradation agent (Kd=~50 nM) with a high selectivity compared to other STAT members. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase. |
| M21158 | Vepdegestrant (ARV-471) | Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer.ARV-471 is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes.ARV-471 causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome.ARV-471 potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM. |
| 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). |
| 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. |
| M14870 | dTRIM24 | dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24. |
| 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 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. |
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