Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC IRAK4 Degrader
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. -
PROTAC IRAK4 Degrader
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. -
PROTAC IRAK4 Degrader
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. -
IRAK3 PROTAC Degrader
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. -
PROTAC IRAK4 Degrader
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. -
PROTAC IRAK4 Degrader
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. -
IRAK3 Degrader PROTAC
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. -
PROTAC IRAK4 Degrader
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. -
PROTAC IRAK4 Degrader
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. -
PROTAC IRAK4 Degrader
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. -
PROTAC IRAK4 Degrader
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. -
PROTAC IRAK4 Degrader
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. -
PROTAC K-Ras Degrader
PROTAC K-Ras Degrader-2 is a selective PROTAC degrader designed to target pan-KRAS mutants, exhibiting an IC50 of ≤200 nM against KRAS G12V and RAF1. This compound effectively degrades KRAS G12D in SW620 cells with a DC50 of ≤200 nM and inhibits cell growth in 3D cultures at an IC50 of ≤20 nM. PROTAC K-Ras Degrader-2 is a valuable tool for investigating therapeutic strategies in colorectal cancer research. -
KRAS G12C Degrader
KRAS G12C degrader-1 is a potent degrader targeting the KRAS G12C mutation, exhibiting a DC50 of less than 100 nM. This compound functions as a chaperone-mediated protein degrader (CHAMP), leveraging HSP90 to promote the degradation of KRAS G12C. It is invaluable for cancer research, particularly in studies aimed at delineating the impact of KRAS mutations on tumorigenesis and therapeutic resistance. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-5 is a potent PROTAC compound that targets SOS1 for ubiquitin-proteasome mediated degradation. It exhibits strong biological activity, demonstrated by a DC50 value of 13 nM and an IC50 of 5 nM in inhibiting the proliferation of NCI-H358 cells. This reagent is valuable for research applications investigating the role of SOS1 in cancer biology and provides insights into targeted protein degradation strategies. -
KRAS Degrader
KRAS degrader-1 is a selective KRAS degrader that induces targeted proteolysis of KRAS proteins via the autophagy-lysosomal degradation pathway. This compound demonstrates robust biological activity in modulating KRAS signaling, making it a valuable tool for research into KRAS-driven cancers. Its application in understanding the dynamics of protein degradation could provide insights into therapeutic strategies for targeting KRAS-dependent malignancies. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-7 is a targeted degradation compound designed to selectively degrade SOS1, a critical regulator in tumorigenesis. This PROTAC exhibits anti-tumor activity by promoting the ubiquitination and subsequent proteasomal degradation of SOS1. It is useful for researchers investigating the effects of SOS1 inhibition in cancer models and exploring potential therapeutic strategies for malignancies involving aberrant SOS1 signaling pathways. -
Target Protein Ligand for PROTAC K-Ras Degrader-3
KRAS ligand 5 is a target protein ligand utilized in the development of PROTAC K-Ras Degrader-3. This compound specifically facilitates the degradation of KRAS mutated proteins, making it a vital tool for research focused on targeted protein degradation. It is particularly relevant in studies addressing KRAS-related oncogenesis and potential therapeutic applications in cancer treatment. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-6 is a targeted degradative compound designed to selectively degrade the SOS1 protein through a PROTAC mechanism. By utilizing a ligand for SOS1, an E3 ubiquitin ligase ligand, and an effective linker, this reagent enhances the efficacy of KRASG12C inhibitors. Its application is primarily in the study of KRAS-driven cancers and the exploration of protein homeostasis through targeted protein degradation pathways. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-9 is a PROTAC (Proteolysis Targeting Chimeras) compound designed for targeted degradation of the SOS1 protein. It employs a specific ligand to bind SOS1, linking it to an E3 ligase for ubiquitination and subsequent proteasomal degradation. This compound is useful in research applications focused on elucidating SOS1's role in cellular signaling pathways and its implications in disease contexts such as cancer. -
PROTAC SOS1 Degrader
(4S)-PROTAC SOS1 degrader-1 is a selective degrader targeting SOS1 through the PROTAC mechanism. This compound effectively reduces the expression of phosphorylated ERK (pERK) and levels of RAS-GTP in a dose-dependent manner, making it a valuable tool for studying RAS signaling. Its ability to significantly inhibit tumor growth in vivo underscores its potential applications in cancer research and therapy. -
KRAS PROTAC Degrader
PROTAC K-Ras Degrader-6 is a cereblon-based KRAS PROTAC degrader that effectively targets and promotes the degradation of KRAS proteins. With a DC50 of ≤100 nM, it exhibits significant anticancer activity, making it a valuable tool for research in cancer biology. This compound is particularly relevant for studies focusing on KRAS-driven malignancies and the development of targeted therapies that leverage the ubiquitin-proteasome system. -
PROTAC Degrader
LC-2 epimer is a differential isomer of LC-2, functioning as a PROTAC degrader. This compound selectively targets mutant KRAS through its unique linkage of a von Hippel-Lindau (VHL) E3 ligase ligand and the KRAS inhibitor MRTX849. LC-2 epimer is intended for research applications focused on targeted protein degradation and the study of KRAS-related pathways in cancer. -
PROTAC SOS1 Degrader
PROTAC SOS1 Degrader-10 is a novel PROTAC compound designed to target and degrade the son of sevenless 1 (SOS1) protein via a cereblon (CRBN) and proteasome-dependent pathway. It effectively reduces SOS1 levels in KRAS mutant cancer cell lines, including SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. In addition to inducing degradation, PROTAC SOS1 Degrader-10 also inhibits cell proliferation in these models, displaying IC50 values of 36.7, 52.2, and 107 nM. Furthermore, it inhibits ERK phosphorylation, highlighting its potential role in cancer research and therapeutic applications targeting the RAS signaling pathway. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-3 is a targeted protein degradation compound that selectively promotes the degradation of SOS1 via the ubiquitin-proteasome pathway. This degrader exhibits potent activity in downregulating SOS1, a key player in RAS signaling pathways. It is useful for researchers studying the roles of SOS1 in cancer biology and therapeutic interventions that disrupt aberrant signaling associated with this target. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-8 is a PROTAC-based molecule designed to target and degrade the SOS1 protein. By utilizing a specific SOS1 ligand, a linker, and an E3 ligase ligand, this compound promotes the ubiquitination and subsequent proteasomal degradation of SOS1. Its primary biological activity involves the modulation of downstream signaling pathways associated with oncogenic processes. This reagent is suitable for research applications focused on elucidating the role of SOS1 in cancer biology and exploring novel therapeutic strategies. -
PROTAC SOS1 degrader
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. -
PROTAC SOS1 Degrader
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. -
BCL6 Degrader
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. -
PROTAC BCL6 Degrader
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. -
BCL-6 PROTAC Degrader
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. -
BCL6 PROTAC
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. -
IDO1 PROTAC Degrader
NU227326 is a potent IDO1 PROTAC degrader designed to penetrate the blood-brain barrier, exhibiting a DC50 of 4.5 nM in HiBiT degradation assays. It effectively degrades IDO1 in human glioblastoma cell lines U87 and GBM43, with DC50 values of 7.1 nM and 11.8 nM, respectively, as demonstrated in Western blot assays. This compound is valuable for research into various malignancies, including glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer. -
PROTAC IDO1 Degrader
NU223612 is a selective PROTAC designed to target and degrade indoleamine 2,3-dioxygenase 1 (IDO1) through CRBN-mediated proteasomal degradation, exhibiting a Kd of 640 nM. With a binding affinity for CRBN of 290 nM, NU223612 effectively reduces IDO1 protein levels, making it a valuable tool in the study of immune modulation and tumor microenvironments. Additionally, NU223612 demonstrates the ability to cross the blood-brain barrier, enhancing its potential utility in neurobiological research. -
PROTAC TG2 degrader
PROTAC TG2 degrader-1 is a von Hippel-Lindau (VHL)-based PROTAC designed to specifically target tissue transglutaminase (TG2) with a dissociation constant (KD) of 68.9 μM. This compound effectively induces the degradation of TG2 in ovarian cancer cells through a proteasome-dependent mechanism. It serves as a valuable tool for research investigating the role of TG2 in cancer biology and potential therapeutic applications. -
PROTAC HPK1 Degrader
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. -
PROTAC HPK1 Degrader
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. -
PROTAC HPK1 Degrader
PROTAC HPK1 Degrader-2 targets HPK1 for degradation via a proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 23 nM in human peripheral blood mononuclear cells (PBMC), this compound is instrumental in elucidating HPK1's functions in cancer biology. The selectivity and potency of PROTAC HPK1 Degrader-2 make it a valuable tool for cancer research applications, enabling the study of targeted protein degradation and its implications in therapeutic strategies. -
PROTAC HPK1 Degrader
HPK1-IN-47 is a selective HPK1 ligand designed for the synthesis of PROTACs, specifically serving as a precursor for PROTAC HPK1 Degrader-2. It exhibits potential in targeting HPK1, which plays a significant role in various HPK1-mediated diseases, particularly cancer. This compound is valuable for research applications focused on elucidating the therapeutic potential of HPK1 degradation in cancer treatment. -
PROTAC HPK1 Degrader
PROTAC HPK1 Degrader-6 is a potent PROTAC compound designed to selectively target and degrade the HPK1 protein, exhibiting an IC50 of less than 50 nM. This compound facilitates the investigation of HPK1's role in leukemia and other related disorders. By employing the dual binding mechanism to HPK1 and the E3 ligase CRBN, it serves as a valuable tool for researchers exploring targeted protein degradation as a therapeutic strategy. -
PROTAC HPK1 Degrader
DD205-291 is an orally active PROTAC HPK1 degrader that exhibits a DC50 value of 5.3 nM. Its primary mechanism involves the targeted degradation of HPK1, leading to the inhibition of SLP-76 phosphorylation. This modulation subsequently results in the enhanced expression of key cytokines such as IL-2 and IFN-γ, making DD205-291 a valuable reagent for studies in immune signaling and related therapeutic applications. -
MEK1/2 PROTAC Degrader
MS910 is a potent and selective PROTAC degrader targeting MEK1 and MEK2 kinases. It demonstrates effective degradation of MEK1 and MEK2 in various cancer cell lines, with reported DC50 values of 118 nM for MEK1 and 55 nM for MEK2 in HT-29 cells, and 94 nM for MEK1 and 38 nM for MEK2 in SK-MEL-28 cells. MS910 is primarily utilized in cancer research to explore the therapeutic potential of targeted protein degradation. -
Mixed Lineage Kinase PROTAC Degrader
PROTAC MLKL Degrader-1 selectively targets and degrades MLKL, achieving a maximum efficacy (Dmax) greater than 90%. This compound incorporates modified CRBN ligands and linker components, functioning effectively in cellular models. PROTAC MLKL Degrader-1 effectively inhibits cell death in a TNF-α, Smac, and zVAD (TSZ) model of necroptosis, making it a valuable tool for investigating necroptosis pathways and their implications in various diseases. -
PROTAC CYP1B1 Degrader
PROTAC CYP1B1 Degrader-1 is a targeted degrader designed to selectively eliminate cytochrome P450 1B1 (CYP1B1), utilizing a α-naphthoflavone chimera derivative. This compound exhibits IC50 values of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2, demonstrating its specificity in degrading CYP1B1. It serves as a valuable tool for investigating the role of CYP1B1 in prostate cancer and may aid in overcoming CYP1B1-mediated drug resistance in therapeutic applications. -
MALT1 PROTAC Degrader
PROTAC MALT1 Degrader-1 is a selective degrader targeting MALT1 through the use of the PROTAC (proteolysis targeting chimera) technology. This compound facilitates the ubiquitination and subsequent proteasomal degradation of MALT1, making it a valuable tool for studies focused on lymphoma and related malignancies. Its mechanism of action enables the investigation of MALT1's role in cellular processes and therapeutic strategies for lymphoma treatment. -
STING PROTAC Degrader
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). -
PROTAC STING Degrader
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. -
cGAS PROTAC Degrader
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. -
PROTAC
PTOTAC HSD17B13 degrader 1 is a PROTAC designed to selectively target and promote the degradation of 17β-Hydroxysteroid dehydrogenase 13 (HSD17B13). This compound consists of a specific ligand for HSD17B13, a linker based on tert-Butyl 5-bromoisoindoline-2-carboxylate, and a ligand for an E3 ubiquitin ligase, enabling effective ubiquitination and subsequent proteasomal degradation of the target protein. PTOTAC HSD17B13 degrader 1 is a valuable tool for studying HSD17B13 functions and has potential applications in therapeutic development and protein regulation research. -
PROTAC BTK Degrader
P131 is a PROTAC molecule that targets Bruton's tyrosine kinase (BTK) for degradation through the Cereblon ligase complex. This compound is effective in degrading both wild-type and C481S mutant BTK with nanomolar potencies. P131 is utilized in research applications focused on the modulation of BTK activity, providing insights into its role in various B-cell malignancies and related signaling pathways.
