PROTAC Degrader

Cat. No.

A63765

CAS No.

2913185-35-8

PROTAC SOS1 degrader-1

PROTAC SOS1 degrader-1 is a targeted degrader that effectively induces the degradation of SOS1, with an observed DC50 value of 98.4 nM. This compound exhibits significant antiproliferative activity against cancer cells harboring various KRAS mutations. Additionally, PROTAC SOS1 degrader-1 demonstrates notable antitumor effects while maintaining low toxicity, making it a valuable tool for research in cancer therapeutics.

Cat. No.

A63769

CAS No.

3062106-15-1

SIAIS562055

SIAIS562055 is a cereblon-based PROTAC targeting the SOS1 protein, exhibiting a dissociation constant (Kd) of 95.9 nM. This compound effectively induces degradation of SOS1, leading to downstream inhibition of ERK signaling pathways. Notably, SIAIS562055 blocks the interaction of KRASG12C and KRASG12D with SOS1, with IC50 values of 95.7 nM and 134.5 nM, respectively. Its potent anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A64132

CAS No.

3005272-36-3

BMS-986458

BMS-986458 is a selective cereblon-based BCL6 degrader that exerts antitumor effects through the targeted degradation of the BCL6 protein. By binding to cereblon and interacting with the BTB domain of BCL6, it modulates key pathways such as cell cycle regulation, antiproliferative signals, and interferon responses, while also enhancing CD20 expression and distribution. BMS-986458 influences follicular helper T cell physiology and reduces circulating tumor DNA levels. Its combination with CD20xCD3 bispecific antibodies has been shown to improve T cell infiltration and expansion in tumors. This compound is applicable in research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma.

Cat. No.

A64133

CAS No.

3005272-58-9

PROTAC BCL6 Degrader-3

PROTAC BCL6 Degrader-3 is a selective degrader targeting the BCL6 protein through the proteolysis-targeting chimera (PROTAC) approach. This compound mediates the ubiquitination and subsequent degradation of BCL6, facilitating the modulation of pathways associated with cancer and autoimmune diseases. It serves as a valuable tool for researchers exploring therapeutic strategies aimed at BCL6 inhibition and the underlying mechanisms of related diseases.

Cat. No.

A64140

CAS No.

3084696-50-1

BCL6-760

BCL6-760 is an orally active BCL-6 PROTAC degrader that selectively targets and degrades BCL-6 with an EC50 of 0.8 nM, without affecting other CRBN substrates. This compound exhibits notable efficacy in orthotopic xenograft mouse models of OCI-LY-1 tumors. BCL6-760 serves as a valuable tool for investigating diffuse large B-cell lymphoma (DLBCL) and for exploring mechanisms related to BCL-6 signaling pathways in cancer research.

Cat. No.

A64141

CAS No.

2257479-54-0

BCL6 PROTAC 1

BCL6 PROTAC 1 is a selective proteolysis targeting chimera (PROTAC) that targets B-cell lymphoma 6 (BCL6) for degradation. It exhibits potent inhibitory activity on BCL6 cell reporter assays, with an IC50 value of 8.8 µM. This reagent effectively induces degradation of BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines, making it a valuable tool for tumor-related research applications.

Cat. No.

A64582

CAS No.

3118499-89-8

PROTAC cGAS degrader-1

PROTAC cGAS degrader-1 is a selective degrader targeting cGAS through a proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces proteasome-mediated degradation of cGAS, leading to the inhibition of the cGAS signaling pathway and a reduction in double-stranded DNA-induced cGAS activation in both human and mouse cell models. This compound is particularly relevant for research applications in inflammatory diseases such as ulcerative colitis.

Cat. No.

A64875

CAS No.

2504235-67-8

Cemsidomide

Synonyms: CFT7455

Cemsidomide is a PROTAC degrader targeting IKZF1 and IKZF3, utilizing the ubiquitin ligase pathway. It exhibits potent biological activity with a GI50 of 0.05 nM against NCIH929.1 cells. This compound is primarily employed in the exploration of multiple myeloma (MM) research, facilitating the study of targeted protein degradation in cancer therapeutics.

Cat. No.

A64912

CAS No.

2374122-43-5

PROTAC IRAK4 degrader-3

PROTAC IRAK4 Degrader-3 is a PROTAC-based ligand designed to target and induce the degradation of interleukin-1 receptor-associated kinase 4 (IRAK4) via the von Hippel-Lindau (VHL) E3 ubiquitin ligase. This compound effectively modulates the inflammatory response by selectively degrading IRAK4, making it a valuable tool for exploring therapeutic strategies in inflammatory diseases and immune signaling pathways. Its application in research can provide insights into IRAK4's role in various pathologies, including cancer and autoimmune disorders.

Cat. No.

A64913

CAS No.

2911615-06-8

PROTAC IRAK4 degrader-8

PROTAC IRAK4 Degrader-8 is a targeted protein degradation compound designed to selectively degrade IRAK4, demonstrating an IC50 of 15.5 nM. This reagent effectively induces IRAK4 degradation in THP-1 cells with a DC50 of 1.8 nM. Additionally, PROTAC IRAK4 Degrader-8 inhibits L-6 production in human whole blood and LPS-induced human peripheral blood mononuclear cells, exhibiting IC50 values of 246 nM and 2.2 nM, respectively. This compound is a valuable tool for studying the role of IRAK4 in immune responses and offers potential applications in inflammatory and autoimmune research.

Cat. No.

A64923

CAS No.

2360530-61-4

PROTAC IRAK4 degrader-5

PROTAC IRAK4 Degrader-5 is a Cereblon-based targeted protein degrader specifically designed to induce the degradation of IRAK4. By modulating the ubiquitin-proteasome system, it enhances protein turnover, leading to a decrease in IRAK4 levels. This compound is valuable for research applications focused on inflammation and immune response regulation, enabling the investigation of IRAK4's role in various disease models.

Cat. No.

A64926

CAS No.

2919995-09-6

PROTAC IRAK4 degrader-12

PROTAC IRAK4 degrader-12 is a PROTAC compound designed to selectively target and induce the degradation of IRAK4 via the Cereblon E3 ligase pathway. It demonstrates a significant degradation efficacy, achieving a maximum degradation rate of 108.46% in K562 cells with an IC50 of 4.87 nM. This reagent is particularly useful for research applications focused on inflammatory signaling pathways and therapeutic development targeting IRAK4-related diseases.

Cat. No.

A64932

CAS No.

3072861-91-4

PROTAC IRAK3 degrader-2

PROTAC IRAK3 degrader-2 is a potent IRAK3 PROTAC degrader with a DC50 of less than or equal to 50 nM. This compound promotes the ubiquitination and subsequent degradation of the IRAK3 protein, making it a valuable tool for studying immune-related diseases. Its unique design incorporates ligands for E3 ligase and a linker configuration, facilitating targeted degradation and aiding research into therapeutic strategies for modulating immune responses.

Cat. No.

A64934

CAS No.

2374122-27-5

PROTAC IRAK4 degrader-2

PROTAC IRAK4 Degrader-2 is a PROTAC-based compound designed to target and degrade IRAK4, displaying potent degradation efficacy with a DC50 value of 151 nM in peripheral blood mononuclear cells (PBMCs). It effectively reduces IRAK4 protein levels, achieving a DC50 of 36 nM in these cells. Additionally, PROTAC IRAK4 Degrader-2 inhibits the production of multiple cytokines, making it a valuable tool for research in inflammation and immune response modulation.

Cat. No.

A64935

CAS No.

2573298-14-1

KTX-612

KTX-612 is an orally bioavailable IRAK4 PROTAC degrader with a DC50 value of 7 nM. This compound is designed to selectively target and promote the degradation of IRAK4, a key protein involved in inflammatory and oncogenic signaling pathways. KTX-612 has potential applications in oncology research, facilitating studies focused on the modulation of IRAK4 and its implications in cancer progression and treatment.

Cat. No.

A64938

CAS No.

2712600-00-3

PROTAC IRAK3 degrader-1

PROTAC IRAK3 degrader-1 is a potent and selective degrader targeting IRAK3, with an IC50 of 5 nM. This compound effectively facilitates the ubiquitination and subsequent degradation of IRAK3, thereby modulating inflammatory responses. Its primary research applications include studies on innate immunity and the development of targeted therapies for inflammatory diseases.

Cat. No.

A64939

CAS No.

2360528-45-4

PROTAC IRAK4 degrader-4

PROTAC IRAK4 degrader-4 is a Cereblon-based bifunctional molecule designed to degrade interleukin-1 receptor-associated kinase 4 (IRAK4). This compound facilitates targeted protein degradation, leading to effective modulation of IRAK4 levels in cells. Research applications include investigating inflammatory signaling pathways and therapeutic approaches for autoimmune diseases.

Cat. No.

A64940

CAS No.

2432993-46-7

KTX-497

KTX-497 is a potent IRAK4 degrader utilizing the PROTAC technology, exhibiting a DC50 value of 3 nM. This compound effectively targets and degrades IRAK4, making it a valuable tool for oncology research. Its mechanism allows for the selective modulation of signaling pathways implicated in cancer progression, facilitating the exploration of novel therapeutic strategies.

Cat. No.

A64941

CAS No.

2573302-50-6

KTX-955

KTX-955 is a potent IRAK4 degrader that facilitates the targeted degradation of IRAK4 protein. With DC50 values of 5 nM for IRAK4 and 130 nM for Ikaros, this compound demonstrates significant efficacy in modulating signaling pathways involved in tumorigenesis. KTX-955 comprises a CRBN ligand derived from Pomalidomide and a specific ligand targeting IRAK4, making it a valuable tool for research into cancer biology and therapeutic interventions.

Cat. No.

A64947

CAS No.

3033829-95-4

PROTAC IRAK4 degrader-10

PROTAC IRAK4 Degrader-10 is a potent IRAK4 degrader that utilizes a Cereblon ligand to initiate targeted protein degradation. It demonstrates remarkable biological activity, achieving a maximum degradation of 95.94% with a DC50 value of 7.68 nM in HEK293 cells. This compound is essential for research applications focused on inflammatory signaling pathways and therapeutic strategies targeting IRAK4.

Cat. No.

A64948

CAS No.

2360530-72-7

PROTAC IRAK4 degrader-6

PROTAC IRAK4 Degrader-6 is a Cereblon-based PROTAC designed to selectively degrade interleukin-1 receptor-associated kinase 4 (IRAK4). This compound targets IRAK4 for ubiquitination and subsequent proteasomal degradation, effectively modulating inflammatory signaling pathways. It is utilized in research applications focused on understanding the role of IRAK4 in immune responses and developing novel therapeutic strategies for inflammatory diseases.

Cat. No.

A65574

CAS No.

3109967-69-0

PROTAC STING degrader-3

PROTAC STING degrader-3 is a potent STING PROTAC degrader that operates through the ubiquitin-proteasome pathway, exhibiting a DC50 of 0.62 μM. This compound facilitates STING degradation, resulting in the inhibition of STING/TBK1/NF-κB signaling, thereby exerting notable anti-inflammatory effects. Additionally, PROTAC STING degrader-3 demonstrates renal protective properties and serves as a valuable tool for investigating acute kidney injury (AKI).

Cat. No.

A65611

CAS No.

3023095-61-3

PROTAC STING Degrader-2

PROTAC STING Degrader-2 is a targeted protein degrader that specifically induces the degradation of the Stimulator of Interferon Genes (STING) through a covalent interaction with STING and an E3 ubiquitin ligase. With a DC50 value of 0.53 μM, this compound facilitates the study of STING's biological functions, particularly in the context of autoinflammatory and autoimmune diseases. This reagent is instrumental for researchers exploring the therapeutic potential and role of STING in immune regulation.

Cat. No.

A65742

CAS No.

3034182-97-0

PROTAC HPK1 Degrader-1

PROTAC HPK1 Degrader-1 is a selective HPK1 degrader that exhibits a DC50 value of 1.8 nM, demonstrating its potency in degrading HPK1. This compound effectively inhibits the phosphorylation of the SLP76 protein, with an IC50 of 496.1 nM. PROTAC HPK1 Degrader-1 serves as a valuable tool for investigating HPK1's role in T cell receptor (TCR) signaling pathways.

Cat. No.

A65747

CAS No.

2636072-62-1

SS47

SS47 is a PROTAC-based HPK1 degrader that facilitates proteasome-mediated degradation of the HPK1 protein. By targeting HPK1 for destruction, SS47 significantly enhances antitumor efficacy, making it a valuable tool for cancer research. Its applications include investigating the role of HPK1 in tumorigenesis and evaluating the efficacy of targeted protein degradation strategies in oncology.