Catalog No.
Product Name
Application
Product Information
Citations
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sEH PROTAC Degrader
PROTAC sEH-degrader-3 is a selective sEH PROTAC degrader that specifically targets soluble epoxide hydrolase (sEH) in the cytosol, sparing its activity in peroxisomes. This compound induces degradation of sEH via a CRBN-mediated lysosomal pathway, exhibiting an IC50 of 0.8 nM against human sEH. PROTAC sEH-degrader-3 is valuable for research focusing on endoplasmic reticulum stress, inflammation, and metabolic diseases, offering insights into therapeutic strategies targeting these pathways. -
PROTAC IKZF1/IKZF3 Degrader
(Rac)-Cemsidomide is a PROTAC degrader targeting IKZF1 and IKZF3, exhibiting potent antitumor activity through its molecular glue mechanism. This compound demonstrates a GI50 of 0.05 nM in NCIH929.1 cells, making it a valuable tool for research applications focused on the degradation of Ikaros and Aiolos proteins. Its unique properties facilitate investigations into mechanisms of action related to targeted protein degradation in cancer therapies. -
BRD4 PROTAC
Lenalidomide-CO-C7-NH2 is a CRBN-dependent intermediate designed as a BRD4-targeting PROTAC degrader. This compound facilitates the selective degradation of the oncoprotein BRD4, leading to decreased cancer cell proliferation, cell cycle arrest, and enhanced apoptosis. It demonstrates noteworthy anti-tumor efficacy in xenograft models, making Lenalidomide-CO-C7-NH2 a valuable tool for investigating mechanisms in acute myeloid leukemia research. -
PROTAC α-Synuclein Degrader
PROTAC α-synuclein degrader 5 is a potent small-molecule degrader targeting α-synuclein aggregates through the PROTAC mechanism. This compound demonstrates a DC50 value of 7.51 μM and achieves a maximal degradation rate (Dmax) of 89%. Incorporating the probe molecule sery308 and E3 ligase ligands, this degrader is suitable for research on neurological diseases, facilitating studies on the pathophysiology of synucleinopathies. -
α-synuclein Degrader
PROTAC α-synuclein degrader 3 is a selective degrader targeting α-synuclein via the ubiquitin-proteasome system. This compound facilitates the ubiquitination and subsequent degradation of α-synuclein, making it a valuable tool for researching Parkinson's disease mechanisms. Its unique design incorporates specific ligands and linkers to optimize efficacy in targeted protein degradation, aiding investigations into therapeutic strategies for neurodegenerative disorders. -
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. -
NR4A1 PROTAC Degrader
NR-V04 is a selective degrader targeting NR4A1 via a PROTAC mechanism. It facilitates the formation of a ternary complex with NR4A1 and the VHL E3 ligase, promoting proteasome-dependent degradation of NR4A1. Through its action, NR-V04 has been shown to enhance the infiltration of tumor-associated B cells and effector memory CD8+ T cells while decreasing monocytic myeloid-derived suppressor cells within tumor microenvironments. This compound is valuable for research related to melanoma and colon cancer. -
CRBN Degrader
ZXH-4-130 TFA is a potent and selective degrader of Cereblon (CRBN), functioning as a CRBN-VHL heterobifunctional protein degrader (PROTAC). This compound exhibits significant biological activity, inducing approximately 80% CRBN degradation at a concentration of 10 nM in MM1.S cells. ZXH-4-130 TFA is a valuable tool for investigating CRBN-mediated pathways and protein degradation mechanisms in various research applications. -
LDH-targeted PROTAC
MS6105 is a selective LDH-targeted PROTAC that induces the degradation of LDHA and LDHB through the ubiquitin-proteasome system. This compound exhibits notable anticancer activity, making it a valuable tool for cancer research. Additionally, MS6105 features an alkyne group, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, enabling diverse applications in chemical biology and drug discovery. -
PD-L1-PROTAC Degrader
PROTAC PD-L1 degrader-1 is a CRBN-based protein degrader targeting PD-L1, facilitating the selective degradation of the PD-L1 protein. This compound demonstrates potent PD-L1 degradation in 4T1 cells, with a DC50 value of 0.609 μM. It serves as a valuable tool for investigating therapeutic approaches in breast cancer research. -
PROTAC ERα Degrader
ERD-3111 is an orally active PROTAC degrader targeting estrogen receptor alpha (ERα) with a reported DC50 of 0.5 nM. This compound effectively inhibits tumor growth in both wild-type MCF-7 xenograft models and in models harboring clinically relevant ESR1 mutations. ERD-3111 is a valuable tool for research focused on estrogen receptor-positive breast cancer, facilitating investigations into targeted degradation pathways and therapeutic strategies. -
PROTAC ER Degrader
PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROTAC that targets the estrogen receptor (ER). It demonstrates high potency, binding to ER with an IC50 of 0.8 nM, and effectively induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM. This compound is valuable for research applications focused on hormone receptor signaling and targeted protein degradation. -
VHL-type PROTAC degrader
PROTAC VHL-type degrader-1 is a VHL-type PROTAC degrader that facilitates the targeted degradation of the ATM protein. This compound enhances the efficacy of the ATR inhibitor AZD6738 through a synergistic mechanism, making it a valuable tool for investigating the interplay between ATM and ATR signaling pathways. It is applicable in research focusing on cancer therapeutics and cellular response to DNA damage. -
PROTACs
AZ'6421 is a Protcolysis Targeting Chimera (PROTAC) designed to selectively degrade estrogen receptor alpha. It exhibits potent anti-tumor activity, effectively inhibiting uncontrolled cellular proliferation associated with malignancies. AZ'6421 is primarily utilized in cancer research, particularly for investigating breast cancer and its therapeutic strategies. -
PCLAF Inhibitor
AD4 is a proteolytic targeting chimera (PROTAC) designed to inhibit PCLAF. This compound effectively degrades PCLAF in RS4;11 cells with an IC50 of 0.6 nM, leading to the activation of the p21/Rb pathway and demonstrating anti-tumor effects. In vivo studies have shown that AD4 prolongs survival in RS4;11-transplanted NOD/SCID mice, highlighting its potential for cancer research applications. -
SMARCA2 PROTAC degrader
YD54 is a PROTAC designed to induce degradation of the SMARCA2 protein, exhibiting a DC50 of 3.5 nM. This compound utilizes a targeted approach to promote the ubiquitination and proteasomal degradation of SMARCA2, making it a valuable tool for studying SMARCA2-dependent biological processes. YD54 is suitable for applications in cancer research and cellular signaling investigations, where modulation of SWI/SNF complex activity is critical. -
PARK7 Degrader
JYQ-194 is a proteolysis-targeting chimera (PROTAC) designed to degrade human PARK7, a protein implicated in Parkinson's disease. This reagent serves as a valuable tool for investigating the underlying mechanisms of neurodegeneration and cancer biology. Its ability to selectively target and degrade PARK7 highlights its potential utility in therapeutic applications and biological research related to Parkinson's disease and other neurodegenerative conditions. -
PROTAC Axl Degrader
PROTAC Axl Degrader 2 is a selective proteolysis-targeting chimera (PROTAC) that degrades Axl with an IC50 of 1.61 μM. This compound exhibits significant anti-proliferation and anti-migration activities in vitro. Additionally, PROTAC Axl Degrader 2 induces mehuosis, making it a valuable tool for studying Axl’s role in cancer progression and therapeutic resistance. Potential research applications include investigations into targeted degradation as a therapeutic strategy in oncology. -
STAT3 PROTAC Degrader
PROTAC STAT3 degrader-3 (S3D1) targets the STAT3 protein through a PROTAC-mediated degradation mechanism. This compound exhibits potent anticancer activity by facilitating the ubiquitination and subsequent proteasomal degradation of STAT3, a key oncogenic transcription factor. It is primarily applied in research focused on cancer biology, particularly in studies investigating the therapeutic potential of targeting the STAT3 signaling pathway. -
Threonine Tyrosine Kinase PROTAC Degrader
PROTAC TTK degrader-1 is a selective threonine tyrosine kinase (TTK) PROTAC degrader designed to induce target degradation. It demonstrates potent biological activity, with DC50 values of 1.7 nM and 5.8 nM in COLO-205 and HCT-116 cell lines, respectively. This compound exhibits significant anticancer efficacy in xenograft mouse models utilizing COLO-205 human colorectal cancer cells, making it a valuable tool for research in cancer therapeutics and targeted protein degradation. -
DDR1 PROTAC Degrader
PROTAC DDR1 degrader-1 is a PROTAC-based degrader designed to selectively target the discoidin domain receptor 1 (DDR1) for proteasomal degradation. This compound utilizes a specific DDR1 inhibitor linked to an E3 ligase ligand, facilitating targeted protein degradation. It exhibits potential applications in elucidating DDR1's role in various cellular processes and disease states, providing valuable insights for therapeutic research. -
CRBN-type PROTAC
WH-10417-099 is a CRBN-type PROTAC designed to induce the degradation of over 125 unique kinases through the ubiquitin biotinylation (E-STUB) mechanism. Its structure comprises a PI3Kγ ligand, a Thalidomide 4-fluoride E3 ubiquitin ligase ligand, and an Amino-PEG5-C2-acid linker. This compound is valuable for research into targeted protein degradation and multi-kinase signaling pathways, with potential applications in cancer and other diseases characterized by dysregulated kinase activity. -
PROTAC erf3a Degrader
PROTAC erf3a Degrader-1 is a potent oral degrader designed to target the erf3a protein. This compound exhibits significant anti-proliferative activity against various cancer cell lines, including 22Rv1, making it a valuable tool in cancer research. PROTAC erf3a Degrader-1 is particularly relevant for studies focused on prostate, ovarian, liver, cervical, and breast cancers, as well as leukemia, facilitating the investigation of targeted protein degradation in these malignancies. -
USP7 PROTAC Degrader
CST967 is a USP7 PROTAC degrader that facilitates targeted degradation of the USP7 protein through the ubiquitin-proteasome pathway. By modulating PROTAC concentration, researchers can significantly enhance the degradation rate of USP7, a key regulator in various cellular processes. This compound is valuable in cancer research for investigating the functional consequences of USP7 inhibition and exploring novel therapeutic strategies. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-8 is a selective degrader targeting the SMARCA2 protein, exhibiting a DC50 of 28 nM in A375 cells. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, thereby effectively reducing its cellular levels. It is particularly useful for studies investigating the role of SMARCA2 in various cancer types and for elucidating its mechanisms of action in cellular processes. -
CRBN Degrader
ZXH-4-130 is a selective degrader of cereblon (CRBN) utilizing the CRBN-VHL mechanism. This compound effectively facilitates the degradation of target proteins through the ubiquitin-proteasome pathway, making it a valuable tool in studying protein homeostasis and degradation processes. Its applications extend to research in targeted protein degradation and the exploration of CRBN's role in various biological contexts. -
BRD4 PROTAC
MS83 is a novel PROTAC that employs a KEAP1 ligand to target and degrade BRD4, along with its homologs BRD3 and BRD2. By harnessing the ubiquitin-proteasome system, MS83 facilitates targeted protein degradation, providing a powerful tool for dissecting the functional roles of BRD4 in cellular processes. This compound is particularly relevant for research on cancer and epigenetic regulation, offering insights into therapeutic strategies that leverage targeted protein degradation. -
BRD9 Degrader PROTAC
PROTAC BRD9 Degrader-5 is a proteolysis-targeting chimera (PROTAC) that facilitates the targeted degradation of the bromodomain-containing protein BRD9. This compound employs the cellular ubiquitin-proteasome pathway to promote the selective elimination of BRD9, leading to the modulation of biological pathways associated with cancer and other diseases. It serves as a valuable tool for researchers investigating the role of BRD9 in various cellular processes and therapeutic interventions. -
PROTAC Pirin Degrader
CCT367766 is a third-generation heterobifunctional PROTAC designed to target and degrade the pirin protein through the CRBN-DDB1 complex. This compound effectively reduces pirin expression at low concentrations, demonstrating an IC50 of 490 nM. It exhibits high binding affinities for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. CCT367766 serves as a valuable chemical tool for probing the biological functions of pirin and advancing research in proteolysis-targeting chimeras. -
Photocaged-PROTAC
phoBET1 is a photocaged-PROTAC targeting BRD4 for selective degradation. This compound harnesses light-activated control to induce the degradation of BRD4 protein, resulting in significant suppression of tumor growth. Its unique photocaging mechanism allows for spatial and temporal regulation of protein activity, making it a valuable tool for studying the role of BRD4 in cancer biology and therapeutic applications. -
Threonine Tyrosine Kinase PROTAC Degrader
PROTAC TTK degrader-2 is a potent degrader that targets threonine tyrosine kinase (TTK), demonstrating DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. This compound effectively induces target protein degradation and exhibits anticancer activity in a xenograft mouse model of human colorectal cancer derived from COLO-205 cells. It serves as a valuable tool for investigating TTK's role in cancer biology and may aid in the development of novel therapeutic strategies. -
SIAIS630121 Negative Control
SIAIS630121-NC is a negative control compound designed for use alongside the NAMPT (nicotinamide phosphoribosyltransferase) PROTAC degrader SIAIS630121. This compound demonstrates no degradation activity on NAMPT, serving as a baseline reference for experimental validation. SIAIS630121-NC is essential for researchers studying the effects of NAMPT degradation and the role of PROTAC technology in targeted protein modulation. -
SMARCA2 Degrader degrader
SMARCA2 degrader-20 is a potent PROTAC that targets the SMARCA2 protein for degradation, exhibiting a DC50 of less than 100 nM in A549 cells. This degrader is valuable for studying the functional consequences of SMARCA2 depletion in cancer biology and epigenetic regulation. Its high efficacy facilitates research into targeted protein degradation strategies and their therapeutic potential in oncology. -
PROTAC ER Degrader
(Rac)-Vepdegestrant targets the estrogen receptor (ER) as a PROTAC (proteolysis-targeting chimera) degrader, effectively inducing the proteasomal degradation of estrogen receptors in breast cancer cells. This hetero-bifunctional compound enhances the interaction between ER-alpha and an E3 ligase complex, resulting in significant ubiquitylation. (Rac)-Vepdegestrant exhibits potent biological activity, showcasing a half-maximal degradation concentration (DC50) of approximately 2 nM in ER-positive breast cancer cell lines, making it a valuable tool for studying ER-related signaling pathways and potential therapeutic applications in breast cancer research. -
PROTAC
ERK-CLIPTAC is a PROTAC molecule designed to selectively induce the degradation of extracellular signal-regulated kinase (ERK). By harnessing the cellular ubiquitin-proteasome system, it offers a novel approach to modulate ERK activity. This compound is valuable for research applications focused on ERK-related signaling pathways and their implications in various diseases, including cancer and neurodegenerative disorders. -
PHOTACs
Photo-lenalidomide-acid is a photochemical agent designed for use in PHOTACs (photo-controllable PROTACs). This compound consists of an E3 ligase ligand linked to a photoswitch and a ligand specific to a protein of interest, allowing precise optical control of protein degradation. Its innovative mechanism facilitates targeted protein modulation in cellular studies and therapeutic applications, making it a valuable tool for researchers investigating protein dynamics. -
PROTAC VHL Degrader
CMP98 is a PROTAC designed as a negative control for CM11, targeting the von Hippel-Lindau (VHL) protein. Unlike its active counterparts, CMP98 does not induce degradation of VHL, making it a valuable tool for validating the specificity and efficacy of VHL-dependent degradation studies. This compound can be utilized in research applications involving protein degradation pathways and the exploration of PROTAC mechanisms. -
ERα Y537S Degrader
PROTAC ERα Y537S degrader-1 is designed to selectively target and degrade the estrogen receptor-alpha (ERα) variant Y537S by recruiting an E3 ubiquitin ligase. This molecular tool facilitates the modulation of estrogen signaling pathways, providing a research application in the study of hormone-driven cancers. By utilizing a combination of a linker and a protein-binding domain, it enhances the degradation efficiency of the mutant receptor, enabling insights into the role of ERα Y537S in tumor biology and potential therapeutic strategies. -
PROTACs
PROTAC BRD9 Degrader-2 is a bifunctional degrader that targets the BRD9 protein utilizing the PROTAC mechanism. This compound facilitates the targeted ubiquitination and subsequent degradation of BRD9, thus significantly influencing cancer-related pathways. It is instrumental in cancer research, particularly in studies aimed at understanding the role of BRD9 in tumorigenesis and developing potential therapeutic strategies. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-17 (compound I-290) is a potent PROTAC degrader designed to selectively target and degrade the SMARCA2 protein. It demonstrates effective degradation in A549 cells with a DC50 value of less than 100 nM and achieves a maximum degradation rate exceeding 90% after 24 hours of treatment. This reagent is valuable for research in cancer biology and the investigation of SMARCA2-related pathways. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-16 (compound I-278) is a PROTAC designed to selectively degrade the SMARCA2 protein. It demonstrates significant biological activity by efficiently reducing SMARCA2 levels in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is invaluable for research applications involving the modulation of SMARCA2 in cancer biology and therapeutic development. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-25 is a potent heterobifunctional molecule that targets SMARCA2 for degradation via the proteasome pathway. With a DC50 value of less than 0.01 μM, this compound efficiently engages the target protein using a specific ligand, a link to facilitate the interaction, and an E3 ligase ligand to promote ubiquitination. Its high efficiency makes it a valuable tool in investigating the role of SMARCA2 in various biological processes and diseases. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-32 is a PROTAC degrader that targets SMARCA2 and SMARCA4 proteins. It demonstrates effective degradation of these proteins in A549 cells, achieving DC50 values below 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is suitable for research applications focusing on the regulation of chromatin remodeling and its implications in various cancers. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-16 (compound I-337) is a potent PROTAC degrader designed to selectively target and degrade SMARCA2 and SMARCA4 proteins. It demonstrates significant biological activity in A549 cells, achieving DC50 values of less than 100 nM and over 90% maximum degradation rate (Dmax%) after 24 hours of treatment. This compound is valuable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in tumor biology and for exploring targeted protein degradation strategies. -
ERα Degrader
PROTAC ERα Degrader-8 is a highly potent degrader of estrogen receptor alpha (ERα), demonstrating a DC50 value of 6 nM in MCF7 breast cancer cells. This compound harnesses the proteolysis-targeting chimera (PROTAC) technology to selectively induce the degradation of ERα, facilitating studies on estrogen signaling pathways and potential therapeutic interventions in hormone-driven cancers. Its application in research provides insight into targeting ERα-related pathways for cancer treatment strategies. -
Ribonuclease-Targeting Chimeras
F1-RIBOTAC is a ribonuclease-targeting chimera (RIBOTAC) that functions by enhancing the activity of RNase L to selectively degrade QSOX1-a mRNA. This targeted approach results in a significant reduction in QSOX1-a expression, making F1-RIBOTAC a valuable tool for cancer research. Its design integrates RNA ligands and RNase L ligands, providing a novel modality for studying RNA degradation pathways in malignant cells. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-12 is a molecule specifically designed to induce degradation of the SMARCA2 protein. This PROTAC exhibits potent biological activity, effectively degrading SMARCA2 proteins in A549 cells with a DC50 value of less than 100 nM and achieving over 90% maximum degradation after 24 hours of treatment. This reagent is suitable for research applications focusing on targeted protein degradation and the functional analysis of SMARCA2 in cancer biology. -
ERα Degrader
PROTAC ERα Degrader-10 (Compound 160a) is a potent degrader targeting estrogen receptor alpha (ERα) with a DC50 of 0.37-1.1 nM in cell lines such as MCF7, T47D, and CAMA-1. This compound effectively induces degradation of ERα, demonstrating significant antitumor activity in mouse models. It is a valuable tool for investigating ERα-related signaling pathways and exploring therapeutic strategies for ERα-positive breast cancers. -
AR PROTAC Degrader
TD-802 is an androgen receptor (AR) PROTAC degrader that demonstrates substantial microsomal stability. It exhibits notable antitumor efficacy in vivo, making it a valuable tool for investigating metastatic castration-resistant prostate cancer. This compound is essential for research aimed at understanding AR modulation and its impacts on cancer progression. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-35 is an efficient degrader targeting the SMARCA2 and SMARCA4 proteins, demonstrating a DC50 of less than 2.5 nM. This compound promotes the ubiquitination and subsequent degradation of the target proteins via the recruitment of E3 ligases. Its potent biological activity makes it valuable for research applications focused on epigenetics and cancer biology, particularly in studies targeting the modulation of chromatin remodeling complexes.
