Catalog No.
Product Name
Application
Product Information
Citations
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STAT6 PROTAC Degrader
PROTAC STAT6 degrader-3 is a highly potent degrader targeting STAT6, exhibiting a DC50 of less than 1 nM. This compound facilitates the targeted degradation of STAT6, making it a valuable tool for investigating allergic and inflammatory diseases as well as various cancers. Its application in research can provide insights into the role of STAT6 in disease pathways and therapeutic interventions. -
STAT3 PROTAC Degrader
SD-2301 is a selective STAT3 PROTAC degrader that targets and induces the degradation of STAT3 while preserving the expression of other STAT family members such as STAT1, STAT2, STAT4, STAT5, and STAT6. It has demonstrated anti-tumor efficacy in B16F10-bearing mouse models, making it a valuable tool for cancer research. This compound can be utilized in studies focused on the modulation of STAT3 pathways and the development of targeted therapies. -
STAT6 Molecular Glue
STAT6 degrader-1 is a bifunctional molecular glue that specifically targets STAT6 by recruiting E3 ubiquitin ligase, leading to the proteasomal degradation of the protein. This degradation mechanism allows for the modulation of STAT6 activity, making it a valuable tool in the study of cancer biology, inflammatory diseases, and colorectal cancer. Researchers can utilize STAT6 degrader-1 to explore therapeutic strategies aimed at disrupting STAT6 signaling pathways. -
PROTAC STAT6 Degrader
PROTAC STAT6 Degrader-2 is a potent bifunctional degrader that specifically targets signal transducer and activator of transcription 6 (STAT6). It demonstrates high efficiency with a DC50 of 1-10 nM in human peripheral blood mononuclear cells (PBMC) and less than 100 nM in HEK293-HIBiT-STAT6 cells. This compound is ideal for research applications related to STAT6-mediated diseases, facilitating the study of its role in various biological processes. -
STAT6 PROTAC Degrader
PROTAC STAT6 degrader-4 is a potent STAT6 PROTAC degrader with a DC50 of 0.04 nM. It functions by inducing the ubiquitination and subsequent degradation of STAT6, making it an important tool for investigating immune-related diseases. This compound is valuable for researchers studying the role of STAT6 in immune signaling pathways and therapeutic interventions. -
PROTAC STAT3 Degrader
S3D5 is a selective PROTAC degrader specifically targeting STAT3, with a dissociation constant (KD) of 4.35 μM. It effectively induces degradation of the STAT3 protein in HepG2 cells, demonstrating minimal impact on other STAT proteins. This degradation is mediated via the ubiquitin-proteasome system, contributing to its potent anti-proliferative effects in hepatocellular carcinoma by activating the p53 pathway. S3D5 serves as a valuable tool for research focused on the mechanisms underlying hepatocellular carcinoma. -
PROTAC ERK5 Degrader
PPM-3 is a potent and selective PROTAC degrader of ERK5, exhibiting an IC50 of 62.4 nM. While PPM-3 does not directly affect tumor cell proliferation, it modulates tumor development by impacting macrophage differentiation. This compound may serve as a valuable tool for investigating the role of ERK5 degradation in cancer biology and immune modulation. -
BCR-ABL PROTAC Degrader
Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy. -
Ligands for Target Protein for SNIPERs
HG-7-85-01-NH2 is a synthetic ligand designed for use in SNIPER (specific and potent target protein degradation) applications. This compound features the HG-7-85-01 moiety, which inhibits ABL, and is linked to an IAP ligand to facilitate targeted protein degradation. It holds potential for advancing research in targeted therapies and cellular protein regulation. -
BCR-Abl PROTAC Degrader
GMB-805 is a potent BCR-Abl PROTAC degrader, demonstrating a DC50 of 30 nM in K562 cells. It effectively induces antiproliferative activity, making it a valuable tool for studying chronic myeloid leukemia. Additionally, GMB-805 exhibits significant anti-tumor efficacy in vivo, coupled with a favorable safety profile, highlighting its potential for therapeutic development. -
mini-PROTAC BCR-ABL Degrader
Arg-PEG1-Dasa is a mini-PROTAC designed to selectively degrade BCR-ABL, a key oncogenic driver in chronic myeloid leukemia. It demonstrates potent degradation efficacy with an EC50 of 0.85 nM, and exhibits significant antiproliferative activity in K562 cells, with an IC50 of 0.36 nM. This reagent is valuable for research applications focused on targeted therapies for BCR-ABL-driven malignancies. -
PROTAC degrader
P19As is a PROTAC degrader that targets the BCR-ABL fusion protein, exhibiting a DC50 value of approximately 200 nM for wild-type BCR-ABL. This compound effectively degrades the T315I mutant variant and demonstrates potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cell lines. P19As serves as a valuable tool for investigating therapeutic strategies in chronic myeloid leukemia and acute lymphoblastic leukemia. -
BCR-ABL PROTAC Degrader
P19P is a BCR-ABL PROTAC degrader that demonstrates a DC50 value of approximately 20 nM for wild-type BCR-ABL protein. It effectively degrades various drug-resistant mutants, including T315I, E255K, H396R, and V468F, and exhibits significant anti-proliferative activity in BaF3-BCR-ABL (T315I) cells, with an IC50 of 13.1 nM against ABL (T315I). P19P is suitable for research applications related to chronic myeloid leukemia and acute lymphoblastic leukemia while showing no inhibition of vascular lumen formation in HUVEC cells. -
BCR-ABL PROTAC Degrader
SIAIS100 is a potent BCR-ABL PROTAC degrader, exhibiting a DC50 value of 2.7 nM. This compound facilitates the targeted degradation of the BCR-ABL fusion protein, making it an important tool in the study of chronic myeloid leukemia (CML). Its ability to induce proteolytic degradation offers valuable insights for therapeutic development and understanding disease mechanisms associated with CML. -
BCR-ABL PROTAC Degrader
SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia. -
BCR-ABL PROTAC Degrader
P22D is a BCR-ABL PROTAC degrader designed for targeted protein degradation, exhibiting a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. This compound effectively inhibits the proliferation of K562 cells harboring the wild-type BCR-ABL, but does not exhibit activity against BaF3-BCR-ABL (T315I) cells. P22D is valuable for research on chronic myeloid leukemia and acute lymphocytic leukemia, offering insights into the mechanisms of resistance and targeted therapies. -
BCR-ABL PROTAC Degrader
Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, demonstrating a DC50 value of 1.56 nM. This compound utilizes phenylalanine as the E3 ligase ligand and triggers the N-end rule pathway to facilitate the degradation of target proteins. Phe-PEG1-Dasa effectively suppresses the proliferation of K562 leukemia cells, making it a valuable tool for research into leukemia treatment strategies. -
PROTAC FLT3-ITD Degrader
PF15 is a PROTAC designed to target FLT3 kinase through its ligands linked with CRBN. This highly selective FLT3-ITD degrader exhibits a DC50 of 76.7 nM, effectively inhibiting the proliferation of FLT3-ITD-positive cells. PF15 down-regulates the phosphorylation of FLT3 and STAT5, demonstrating significant anti-tumor activity in mouse models, making it a valuable tool for leukemia research. -
LCK PROTAC Degrader
SJ11646 is a LCK-targeting PROTAC degrader based on Dasatinib, exhibiting a DC50 of 0.00838 pM. This compound demonstrates potent cytotoxic effects against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, effectively prolonging LCK signaling suppression and inducing apoptosis in T-ALL. Additionally, SJ11646 binds with high affinity to 51 human kinases, including ABL1, KIT, and DDR1, and shows enhanced antileukemic efficacy in T-ALL mouse models, making it a valuable tool for research into novel therapeutic strategies for leukemia. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate, featuring a Thalidomide-based cereblon ligand integrated with a flexible linker tailored for PROTAC (Proteolysis Targeting Chimera) applications. This compound demonstrates the capacity to facilitate targeted protein degradation by recruiting E3 ligases to specific substrates, thereby enhancing the control of protein levels in cellular systems. It is valuable for research in targeted therapy and protein regulation studies. -
Ligands for E3 Ligase
Thalidomide-5-NH-CH2-COO(t-Bu) serves as a ligand for the E3 ubiquitin ligase Cereblon (CRBN). This derivative of Thalidomide features a t-Bu protecting group, which can be removed under acidic conditions, facilitating the development of proteolysis-targeting chimeras (PROTACs). Thalidomide-5-NH-CH2-COO(t-Bu) is crucial for synthesizing CRBN-based PROTACs, enabling targeted protein degradation for various biological research applications. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-4-NH-PEG1-COOH TFA functions as an E3 Ligase Ligand-Linker Conjugate that targets Cereblon (CRBN). This compound selectively recruits the CRBN protein, facilitating targeted protein degradation pathways. Thalidomide-4-NH-PEG1-COOH TFA is a critical intermediate in the synthesis of CRBN-based PROTAC molecules, making it valuable for research into novel therapeutic strategies in cancer and other diseases. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-PEG1-C2-NH2 is an E3 ligase ligand-linker conjugate designed for use in targeted protein degradation applications. This compound features a Thalidomide-derived cereblon ligand that facilitates the recruitment of specific substrates to the ubiquitin-proteasome system. Its linker component is compatible with PROTAC technology, making it a valuable tool for researchers investigating therapeutic strategies aimed at modulating protein levels within cells. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-NH-C8-NH2 is a synthetic E3 ligase ligand-linker conjugate that features a Thalidomide-based cereblon ligand. This compound serves as a valuable tool in PROTAC (Proteolysis Targeting Chimera) technology, facilitating targeted degradation of specific proteins in cellular systems. It is widely utilized in studies focusing on protein homeostasis, disease modeling, and therapeutic development in various fields including cancer research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C8-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that combines the Thalidomide-derived cereblon ligand with a C8 amido linker. This compound is specifically designed for use in PROTAC technology, facilitating targeted protein degradation by recruiting E3 ligases to specific substrates. Its biochemical properties make it suitable for investigating protein modulation and therapeutic applications in cellular research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-PEG2-C2-NH2 is a conjugate designed for E3 ligase targeting, featuring a Thalidomide-derived cereblon ligand combined with a polyethylene glycol (PEG) linker. This compound facilitates targeted protein degradation by engaging E3 ligases through PROTAC technology. It is suitable for research applications aimed at exploring protein regulation and therapeutic interventions in various diseases. -
PROTAC CDK4/6/9 Degrader
PROTAC CDK4/6/9 Degrader 1 is a targeted protein degradation agent that specifically degrades cyclin-dependent kinases CDK4, CDK6, and CDK9. This compound effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells by inducing G1 phase arrest, promoting apoptosis, and suppressing cellular migration and invasion. PROTAC CDK4/6/9 Degrader 1 serves as a valuable tool for studying the role of these kinases in TNBC and may support the development of novel therapeutic strategies aimed at this aggressive cancer subtype. -
Molecular Glue Degrader
VNPP433-3β hydrochloride functions as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants, as well as MAP kinase-interacting serine/threonine protein kinases Mnk1 and Mnk2. This compound promotes apoptosis in cancer cells and has demonstrated efficacy in inhibiting tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride is suitable for research applications focused on castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
E3 ligase ligand-Linker Conjugate
Thalidomide-NH-PEG1-NH2 is an E3 ligase ligand-linker conjugate that combines a Thalidomide-derived cereblon ligand with a polyethylene glycol (PEG) linker, designed for proteolysis-targeting chimera (PROTAC) applications. This compound facilitates the recruitment of E3 ligases, enabling targeted degradation of specific proteins within cellular environments. It is instrumental in the development of novel therapeutic strategies for modulating protein levels in research studies. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-O-PEG4-Boc is an E3 ligase ligand-linker conjugate that combines a Thalidomide-derived cereblon ligand with a PEG4 linker. This compound is designed for use in PROTAC technology, facilitating targeted protein degradation. It exhibits key biological activity by modulating the E3 ligase pathways, making it a valuable tool in the study of protein homeostasis and therapeutic applications in disease models. -
PROTAC USP7 Degrader
XM-U-14 is a selective PROTAC degrader targeting USP7, demonstrating a DC50 of 0.74 nM for inducing USP7 degradation in the RS4;11 cell line. This compound effectively upregulates p53 and p21 levels and exhibits significant inhibition of acute lymphoblastic leukemia (ALL) cell proliferation, with IC50 values of 0.5 nM and 8.3 nM for RS4;11 and Reh cells, respectively. Additionally, XM-U-14 induces apoptosis and cell cycle arrest, ultimately inhibiting tumor growth, making it a valuable tool for cancer research and therapeutic exploration. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-amide-C5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that targets cereblon via its Thalidomide component. This compound is designed for use in PROTAC (proteolysis-targeting chimeras) technology, facilitating the targeted degradation of specific proteins within various biological pathways. Its application in chemical research allows for enhanced studies in protein regulation and therapeutic interventions. -
Ligands for E3 Ligase
Thalidomide-5-O-CH2-COO(t-Bu) is a thalidomide derivative that functions as a ligand for cereblon (CRBN), facilitating the recruitment of the CRBN protein. The tert-butyl protecting group can be cleaved under acidic conditions, enabling its use in the synthesis of proteolysis-targeting chimeras (PROTACs). This compound serves as a critical intermediate in the development of CRBN-based PROTAC molecules for targeted protein degradation research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C2-NH2 is a synthetic E3 ligase ligand-linker conjugate designed to target cereblon, a substrate receptor for the ubiquitin-proteasome system. This compound plays a crucial role in PROTAC technology, facilitating targeted protein degradation by linking a specific protein of interest to the E3 ligase for ubiquitination. Its application enhances the study of protein function and regulation in cellular processes, making it valuable for research in drug development and disease modulation. -
E3 Ligase Ligand
Thalidomide-5-propoxyethanamine is an E3 ligase ligand specifically designed to target cereblon (CRBN). This compound enhances the recruitment of the CRBN protein, playing a crucial role in modulating protein homeostasis and ubiquitin-proteasome pathways. It is useful for research applications involving targeted protein degradation and the study of CRBN-related signaling pathways. -
RET PROTAC Degrader
RD-23 is a selective RET PROTAC degrader that functions through the promotion of ubiquitination and subsequent degradation of the RETG810C mutation, exhibiting a DC50 value of 11.7 nM. This compound effectively inhibits downstream Shc signaling pathways and induces apoptosis in RET-related cancer models. RD-23 is a valuable tool for investigating the biological roles and therapeutic targeting of RET in oncology research. -
Ligands for E3 Ligase
Thalidomide 4'-ether-PEG1-azide is a Thalidomide-derived ligand that specifically targets cereblon (CRBN), facilitating its recruitment for protein degradation. This compound is utilized in the development of proteolysis-targeting chimeras (PROTACs) to enhance targeted protein removal in cellular systems. Its unique structure promotes effective binding and functional interactions in E3 ligase-mediated pathways, supporting studies in protein regulation and therapeutic discovery. -
E3 Ligase Ligand
Thalidomide-NH-CH2-COOH TFA is a thalidomide-derived ligand targeting the E3 ligase cereblon (CRBN). This compound facilitates the recruitment of CRBN, making it a valuable tool in the design of PROTACs for targeted protein degradation research. Its application in the development of bifunctional molecules allows for enhanced modulation of protein levels and contributes significantly to the study of protein homeostasis and therapeutic strategies. -
Ligands for E3 Ligase
Thalidomide-4-NH-PEG1-NH-Boc is a Boc-modified derivative of Thalidomide that serves as a ligand for the E3 ubiquitin ligase, Cereblon (CRBN). This compound is integral in PROTAC (proteolysis-targeting chimera) synthesis, allowing for efficient recruitment of CRBN to target proteins for degradation. The Boc protecting group can be removed under acidic conditions, facilitating further chemical modifications required in PROTAC development. Thalidomide-4-NH-PEG1-NH-Boc is an essential intermediate for researchers exploring targeted protein degradation and related therapeutic strategies. -
EML4-ALK PROTAC Degrader
Pro-PEG3-BA is a targeted PROTAC degrader that specifically degrades EML4-ALK and EGFR mutants, with DC50 values of 0.42 μM and 13.50 μM, respectively. It effectively inhibits proliferation and induces cell cycle arrest and apoptosis in non-small cell lung cancer (NSCLC) cell lines in vitro. In vivo studies reveal that Pro-PEG3-BA rewires the ubiquitin-proteasome system, leading to a reduction in EML4-ALK protein levels while demonstrating a favorable safety profile. This reagent is suitable for research focused on non-small cell lung cancer treatments. -
Molecular Glue Degrader
VNPP433-3β dihydrochloride is a potent molecular glue degrader that targets the androgen receptor (AR), AR splice variants (AR-Vs), and MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound induces apoptosis in cancer cells and has been shown to inhibit tumor growth in CWR22Rv1 xenograft mouse models. VNPP433-3β dihydrochloride is valuable for research in castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
E3 ligase ligand-Linker Conjugate
Thalidomide-NH-PEG1-NH2 diTFA is a synthesized E3 ligase ligand-linker conjugate designed to target cereblon, a substrate receptor for the E3 ubiquitin ligase complex. This compound facilitates the development of PROTAC (proteolysis-targeting chimera) technology, enabling targeted protein degradation in various biological research applications. Its unique structure is instrumental in studying protein interactions and modulation within cellular pathways. -
Ligands for E3 Ligase
Thalidomide-4-NH-PEG1-COO(t-Bu) functions as a ligand for E3 ligase, specifically targeting the Cereblon (CRBN) protein. This compound features a t-Bu protecting group, which can be cleaved under acidic conditions, enabling the synthesis of proteolysis-targeting chimeras (PROTACs). It serves as a crucial intermediate in the development of CRBN-based PROTAC molecules, facilitating targeted protein degradation for research applications in cancer and other diseases. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-PEG3-C2-NH2 is an E3 ligase ligand-linker conjugate designed for targeted protein degradation applications. This compound features a cereblon ligand derived from Thalidomide, coupled with a PEG3 linker, facilitating the development of proteolysis-targeting chimeras (PROTACs). Its primary utility lies in modulating protein levels within cellular systems, enabling researchers to investigate protein function and potential therapeutic interventions. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that targets cereblon through its Thalidomide-derived component. This compound is designed for applications in PROTAC technology, facilitating targeted protein degradation. Its structure combines a specific ligand with a functional linker, making it a valuable tool for research in cellular signaling and protein modulation. -
AR PROTAC Degrader
ITRI-90 is an orally bioavailable androgen receptor (AR) PROTAC degrader that facilitates the degradation of both full-length AR (AR-FL) and the splice variant AR-V7 through the ubiquitin-proteasome pathway. This mechanism effectively reduces AR transcriptional activity and downregulates target gene expression. ITRI-90 has shown significant antitumor effects by inhibiting the proliferation of prostate cancer cells, including those resistant to Enzalutamide, and promoting apoptosis. Additionally, it possesses favorable pharmacokinetic properties, making it a valuable tool for research in prostate cancer. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-PEG8-Ts is a synthesized E3 ligase ligand-linker conjugate that combines the Thalidomide-derived cereblon ligand with an eight-unit polyethylene glycol (PEG) linker. This compound is essential in the development of PROTAC (Proteolysis Targeting Chimeras) technology, enabling targeted degradation of specific proteins through the recruitment of E3 ligases. Its applications include research in targeted protein degradation, with potential implications in various therapeutic areas, including cancer and neurodegenerative diseases. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-O-PEG4-amine TFA is an E3 ligase ligand-linker conjugate that combines a Thalidomide-derived cereblon ligand with a PEG4 linker for use in proteolysis-targeting chimera (PROTAC) applications. This compound facilitates targeted protein degradation by promoting the interaction between E3 ligases and specific substrate proteins. It serves as a valuable tool for researchers investigating cellular protein regulation and therapeutic interventions in various disease models. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride is an E3 ligase ligand-linker conjugate designed to incorporate a thalidomide-based cereblon ligand with a polyethylene glycol (PEG) linker. This compound facilitates targeted protein degradation through PROTAC technology, enhancing specificity and efficacy in research applications. It serves as a valuable tool for studying the role of E3 ligases in cellular processes and for developing novel therapeutic strategies through targeted modulation of protein levels. -
PROTAC Linker
Thalidomide-NH-C5-NH2 serves as a PROTAC linker, facilitating the recruitment of E3 ligases through its thalidomide-based cereblon ligand. This compound enables targeted protein degradation, making it a valuable tool in drug discovery and development. Its application in the design of bifunctional degraders enhances the specificity and efficacy of therapeutic strategies aimed at modulating protein functions in various biological contexts.
