| 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. |
| 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. |
| 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. |
| M29154 | FKBP12 PROTAC dTAG-13 | FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12F36V and CRBN, thereby selectively degrading FKBP12F36V. |
| 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. |
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