Catalog No.
Product Name
Application
Product Information
Citations
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MEKs Degrade PROTAC
Folate-MS432 selectively targets MEKs through a PROTAC mechanism, facilitating their degradation in a folate receptor-dependent manner. This compound demonstrates significant efficacy in cancer cells, providing a powerful tool for investigating the role of MEK degradation in tumor biology. Folate-MS432 is valuable for research applications focusing on therapeutic strategies that manipulate signaling pathways in cancer treatment. -
PROTAC ERα Degrader
NEP168 is a potent ERα PROTAC degrader that utilizes the GID4 E3 ligase for targeted protein degradation. This compound effectively reduces ERα levels, offering valuable insights into estrogen receptor-related signaling pathways. NEP168 serves as a crucial tool for investigating breast cancer biology and may aid in the development of novel therapeutic strategies. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-7 is a selective protein degrader that targets SMARCA2 and SMARCA4 proteins. Demonstrating effective degradation in A549 cells, it achieves DC50 values of less than 100 nM and results in more than 90% degradation after 24 hours of treatment. This compound serves as a valuable tool for investigating the roles of SMARCA2 and SMARCA4 in cancer biology and other research applications involving epigenetic regulation. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-22 is a targeted protein degradation reagent designed to selectively degrade SMARCA2 and SMARCA4 proteins. This compound effectively reduces SMARCA2 and SMARCA4 levels in A549 cells, achieving DC50 values of less than 100 nM and exceeding 90% maximum degradation rate after 24 hours of treatment. It is a valuable tool for research into the role of these proteins in various biological processes and disease states. -
mini-PROTAC ERRα Degrader
Arg-TERRα is a mini-PROTAC designed to target estrogen-related receptor alpha (ERRα). This compound facilitates the degradation of ERRα via the N-end rule pathway, effectively suppressing the proliferation and migration of MCF7 breast cancer cells. Arg-TERRα serves as a valuable tool for investigating the role of ERRα in breast cancer research and therapeutic development. -
PROTACs
PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9 through the PROTAC mechanism, facilitating targeted protein degradation. This compound exhibits potent biological activity by selectively degrading BRD9, which plays a critical role in various cancer pathways. It is intended for use in cancer research to elucidate the functional significance of BRD9 and to explore novel therapeutic strategies in oncology. -
ITK Degrader
ITK Degrader 2 is a PROTAC-based compound that specifically targets and degrades the interleukin-2-inducible T-cell kinase (ITK) with a DC50 value of less than 10 nM. In pharmacokinetic studies in mice, this orally active degrader demonstrates a maximum concentration (Cmax) of 0.87 μM and achieves peak plasma levels (Tmax) at 2 hours post-administration. At a dosage of 90 mg/kg, ITK Degrader 2 effectively reduces ITK levels by 20% within 6 hours, making it a valuable tool for exploring ITK-related signaling pathways and their implications in immune responses. -
BRD9 PROTAC Degrader
PROTAC BRD9 Degrader-8 is a selective BRD9 PROTAC degrader that operates through targeted protein degradation, exhibiting a DC50 of 16 pM. This compound effectively induces cell cycle arrest in the G1 phase and promotes apoptosis, making it a valuable tool for studies focused on acute myeloid leukemia and diffuse large B-cell lymphoma. Its mechanism provides a unique approach to modulating BRD9 levels in therapeutic research. -
PROTAC degrader
PROTAC SMARCA2/4-degrader-11 is a targeted protein degradation tool that specifically promotes the degradation of the SMARCA family of proteins. With a DC50 value of less than 100 nM, this compound effectively induces the destruction of SMARCA2 and SMARCA4. Its unique design features an inhibitor component, a linker, and an E3 ligase ligand, facilitating the targeted removal of these proteins, making it a valuable reagent for research into cancer biology and epigenetic regulation. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-15 is a targeted PROTAC that selectively degrades the SMARCA2 protein. Demonstrating a DC50 value of less than 100 nM, this compound achieves over 90% maximum degradation (Dmax%) within 24 hours in A549 cells. Its ability to modulate SMARCA2 levels makes it a valuable tool for research exploring the role of this protein in cancer biology and epigenetic regulation. -
Proteolysis Targeting Chimera
BT-PROTAC is a proteolysis targeting chimera (PROTAC) that enables the targeted degradation of specific proteins through a bioorthogonal activation mechanism. By accurately controlling PROTAC activity, it facilitates the selective modulation of protein levels within cells. This compound is valuable for research applications focused on the study of protein function, cellular signaling pathways, and the development of targeted therapeutic strategies. -
AR PROTAC Degrader
A031 is a potent PROTAC degrader targeting the androgen receptor (AR), demonstrating an IC50 value of less than 0.25 μM for effective AR protein degradation. This compound has shown a significant inhibitory effect on tumor growth in zebrafish models of human prostate cancer (VCaP). A031 is a valuable tool for investigating AR-mediated signaling pathways and potential therapeutic strategies in prostate cancer research. -
PROTAC HMGCR Degrader
PROTAC HMGCR Degrader-2 selectively targets HMG-CoA reductase (HMGCR) for degradation through the VHL-dependent ubiquitin-proteasome system, exhibiting an IC50 value of 0.25 μM and a DC50 of 0.12 μM in Insig-silenced HepG2 cells. This compound effectively reduces cellular cholesterol levels, making it valuable for research related to hyperlipidemia. Its mechanism of action enables precise modulation of cholesterol biosynthesis pathways, providing insights into lipid metabolism and potential therapeutic interventions. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-23 is a targeted proteolysis-targeting chimera (PROTAC) designed to degrade SMARCA2 and SMARCA4 proteins. This compound effectively induces degradation of both targets in A549 cells, exhibiting a DC50 of less than 100 nM and achieving a maximum degradation rate exceeding 90% after 24 hours of treatment. It is suitable for use in studies aimed at understanding the functional roles of SWI/SNF chromatin remodeling complexes in cancer and other disease models. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-10 is a targeted protein degrader that specifically engages and promotes the degradation of SMARCA2. This compound demonstrates effective degradation of SMARCA2 proteins in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. It serves as a valuable tool for research applications focused on elucidating the biological roles of SMARCA2 and its implications in cancer biology and therapeutics. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-6 (compound I-427) is a PROTAC agent specifically designed to target and induce the degradation of SMARCA2 proteins. This compound effectively degrades SMARCA2 in A549 cells, achieving a DC50 value of less than 100 nM and demonstrating a maximum degradation rate exceeding 90% within 24 hours of treatment. It serves as a powerful tool for investigating the role of SMARCA2 in various biological processes and potential therapeutic applications in cancer research. -
CRBN Degrader PROTAC
ZXH-4-137 is a potent and selective CRBN degrader that utilizes the PROTAC mechanism to promote targeted protein degradation. This compound effectively recruits the E3 ubiquitin ligase CRBN to facilitate the degradation of specific proteins, making it a valuable tool for studying protein function and regulation. It has applications in cellular assays and therapeutic research aimed at diseases associated with protein homeostasis. -
Cbl-b PROTAC Degrader
PROTAC Cbl-b-IN-1 is a potent Cbl-b PROTAC degrader, exhibiting a DC50 of less than 30 nM. This compound effectively induces the targeted degradation of the Cbl-b protein, making it a valuable tool for cancer research. Its ability to modulate protein levels through degradation pathways allows for in-depth studies of Cbl-b's role in tumor biology and therapeutic interventions. -
PROTAC erf3a Degrader
PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC designed to target and degrade eRF3a (GSPT1) and SRD5A3 proteins. By inducing the ubiquitination and subsequent proteasomal degradation of these proteins, it effectively inhibits cancer cell proliferation in various models, including the 22Rv1 prostate cancer cell line. PROTAC erf3a Degrader-2 is applicable for research related to multiple cancer types, including prostate, ovarian, liver, cervical, and breast cancers, as well as leukemia. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-3 is a potent SMARCA2/4 degrader that utilizes the VH032-NH2 framework for targeted protein degradation. It exhibits a degradation potency (DC50) of less than 100 nM in MV4-11 cells, facilitating the selective depletion of SMARCA2 and SMARCA4 proteins. This compound is valuable for research applications involving chromatin remodeling and cancer biology, providing insights into the functional roles of these proteins in various cellular contexts. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-1 is a PROTAC degrader specifically designed to target SMARCA2 and SMARCA4 proteins. It effectively degrades these proteins in A549 cells, exhibiting a DC50 of less than 100 nM and achieving over 90% degradation after 24 hours of treatment. This compound is suitable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in various biological processes and disease models. -
SRC-1 Degrader/PROTAC
ND1-YL2 is a PROTAC that selectively targets and degrades SRC-1 through the N-degron pathway. This compound has demonstrated significant inhibition of cancer cell invasion and migration both in vitro and in vivo. ND1-YL2 serves as a valuable tool in cancer research, providing insights into the role of SRC-1 in tumor progression and metastasis. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-2 is a molecular degrader specifically designed to target SMARCA2 and SMARCA4 proteins. It effectively induces degradation of these proteins in A549 cell lines with degradation concentrations (DC50s) less than 100 nM, achieving a maximum degradation rate (Dmax%) exceeding 90% after 24 hours of exposure. This compound is valuable for investigating the roles of SMARCA2 and SMARCA4 in various biological processes and may have applications in cancer research and therapeutic development. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-13 is a novel PROTAC targeted at the degradation of SMARCA2 proteins. This compound effectively induces the degradation of SMARCA2 in A549 cells with a DC50 of less than 100 nM, achieving over 90% degradation after 24 hours of treatment. It serves as a valuable tool for studying the functional role of SMARCA2 in cancer biology and other cellular processes. -
AR PROTAC Degrader
PROTAC AR Degrader-5 is a potent androgen receptor (AR) PROTAC degrader, exhibiting an IC50 value of 49 nM. This compound facilitates the targeted degradation of AR, demonstrating significant potential in inhibiting sebaceous plaque formation and promoting hair regeneration. Its mechanism utilizes a bifunctional ligand to recruit an E3 ligase, making it a valuable tool for research in androgen signaling and related therapeutic applications. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-33 (compound I-277) is a targeted protein degradation compound that engages and induces degradation of SMARCA2 and SMARCA4. It demonstrates effective biological activity in A549 cells, with degradation concentrations (DC50s) below 100 nM, achieving over 90% protein degradation (Dmax%) after 24 hours of treatment. This reagent is suitable for research applications involving epigenetic regulation and cancer biology. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-9 (compound I-285) is an innovative PROTAC agent designed to selectively degrade SMARCA2 proteins. It demonstrates potent biological activity with a DC50 value of less than 100 nM, achieving over 90% degradation of SMARCA2 in A549 cell lines after 24 hours of treatment. This compound serves as a valuable tool for research applications aimed at elucidating the role of SMARCA2 in cancer biology and exploring targeted protein degradation strategies. -
YN14 Mixture of Diastereomers
YN14 is a mixture of diastereomers that functions as a proteolysis targeting chimera (PROTAC) specifically targeting KRASG12C. This compound exhibits high potency and selectivity in degrading KRASG12C by forming a stable ternary complex with VHL, characterized by low binding free energy (ΔG). YN14 demonstrates significant antiproliferative activity, effectively inhibiting the growth of KRASG12C-mutant cancer cells, making it a valuable tool for cancer research and drug development. -
PRT3789 Epimer
PRT3789 epimer is an epimer of PRT3789, a selective degrader targeting SMARCA2 through the PROTAC approach. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, thereby providing a valuable tool for studying the role of this protein in cancer and other diseases. It is essential for research applications focused on targeted protein degradation mechanisms and their therapeutic implications. -
PROTAC BCR-ABL Degrader
SNIPER(ABL)-020 is a PROTAC compound designed to selectively degrade the BCR-ABL fusion protein through targeted ubiquitin-proteasome pathway engagement. By conjugating Dasatinib, an ABL inhibitor, with Bestatin, an IAP ligand, SNIPER(ABL)-020 effectively promotes the protein's ubiquitination and subsequent degradation. This reagent is valuable for research focused on chronic myeloid leukemia and BCR-ABL related signaling pathways, offering insights into targeted protein degradation mechanisms in cancer therapeutics. -
PROTAC ER Degrader
SNIPER(ER)-87 is a PROTAC compound designed to efficiently degrade estrogen receptor α (ERα) through targeted ubiquitination. It consists of an IAP ligand (LCL161 derivative) linked to the ERα ligand (4-hydroxytamoxifen) via a PEG linker, resulting in an IC50 of 0.097 μM for ERα degradation. This compound preferentially recruits XIAP, the primary E3 ubiquitin ligase, to facilitate the selective degradation of ERα in cellular contexts. SNIPER(ER)-87 is valuable for research on hormone receptor regulation, breast cancer studies, and the development of targeted protein degradation strategies. -
PROTAC ER Degrader
SNIPER(ER)-110 is a PROTAC compound designed for targeted degradation of the estrogen receptor (ER). Comprising an IAP ligand and an estrogen ligand linked together, SNIPER(ER)-110 effectively induces ER protein degradation, exhibiting DC50 values of less than 3 nM at 4 hours and approximately 7.7 nM at 48 hours. This reagent is valuable for studies investigating ER-related signaling pathways and therapeutic strategies in hormone-dependent cancers. -
BRM2 Degrader
PROTAC SMARCA2 degrader-1 is a targeted degrader designed to selectively degrade BRM2 (SMARCA2) with a DC50 value of less than 0.1 μM. This compound functions as an E3 ubiquitin ligase binding linker, facilitating the targeted degradation of specific proteins. Its application in cancer research makes it a valuable tool for elucidating the role of BRM2 in tumor biology and developing potential therapeutic strategies. -
CYP1B1 Degrader
PROTAC CYP1B1 degrader-2 is a VHL E3 ligase-based degrader targeting CYP1B1, exhibiting a DC50 of 1.0 nM in A549/Taxol cells after 24 hours. This compound effectively inhibits the growth, migration, and invasion of cancer cells, making it a valuable tool for research into the therapeutic potential of targeting CYP1B1 in cancer treatment. Its unique mechanism of action offers insights into the modulation of protein levels in various biological contexts. -
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. -
CDK2 Degrader PROTAC
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC that targets cyclin-dependent kinase 2 (CDK2) for degradation. This compound effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine 807/811 by promoting the ubiquitination and proteasomal degradation of CDK2. Demonstrating significant biological activity with EC50 values of 12 nM and 125 nM in human cells, PROTAC CDK2-pRb degrader-1 is particularly useful in research focused on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers, as it inhibits tumor growth and induces tumor stasis in xenograft models. -
PROTAC IRAK4 Degrader
PSP-0119 is a highly selective PROTAC degrader targeting IRAK4, demonstrating an IC50 of 2.83 nM. This compound effectively inhibits IRAK4 kinase activity, NF-κB signaling, and IL-1β-induced IRAK4 phosphorylation. Notably, PSP-0119 induces degradation of IRAK4 specifically in FLT3-mutant acute myeloid leukemia (AML) cell lines while sparing FLT3-wild-type AML cells and normal bone marrow. It serves as a valuable tool for research into the mechanisms underlying AML, particularly in targeting aberrant IRAK4 activity. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4 degrader-40 is a specific degrader targeting SMARCA2 and SMARCA4. It demonstrates potent degradation activity in HeLa cells, with a DC50 value of less than 0.1 nM. This compound is particularly useful for investigating cancers linked to SMARCA2/SMARCA4 abnormalities or mutations within the SWI/SNF complex, facilitating insights into their role in tumorigenesis.
