Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
BRD4 PROTAC Degrader
NEP162 is a potent BRD4 PROTAC degrader, demonstrating DC50 values of 1.2 and 1.6 μM in SW480 and U2OS cell lines, respectively. It exhibits significant antiproliferative activity, effectively inhibiting tumor growth and promoting apoptosis in various cancer models. NEP162 is particularly relevant for research applications in osteosarcoma, colorectal cancer, and non-small cell lung cancer. -
AR PROTAC degrader
PROTAC AR-NTD degrader 1 is a protein-targeting chimera designed to selectively target and degrade the N-terminal domain of the Androgen Receptor (AR-V7). This small molecule exhibits significant efficacy in inducing apoptosis in prostate cancer cells, demonstrating a degradation efficiency of 62.2% at 1 μM and 71.1% at 5 μM in VCaP cells. PROTAC AR-NTD degrader 1 is a valuable tool for research focused on androgen receptor signaling and its implications in prostate cancer therapy. -
CRBN Modulator
AG6033 is a novel modulator of the cereblon (CRBN) protein. This compound effectively suppresses various tumor cell lines by influencing the interactions between CRBN and key antitumor target proteins, leading to the degradation of GSPT1 and IKZF1. AG6033 has demonstrated a CRBN-dependent cytotoxic effect, making it a valuable tool for research in cancer biology and the development of targeted therapies. -
PROTAC IRAK4 Degrader
KT-474 hydrochloride is a potent PROTAC degrader targeting IRAK4, exhibiting significant anti-tumor properties. This compound inhibits the cell cycle and induces apoptosis in affected cells, demonstrating tumor regression in xenograft models of MYD88-mutated ABC DLBCL. Additionally, KT-474 features an alkyne group facilitating click chemistry, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for chemical biology research. -
Ligands for E3 Ligase
Thalidomide-NH-(CH2)2-NH-Boc is a Boc-modified thalidomide derivative functioning as a ligand for the E3 ubiquitin ligase Cereblon (CRBN). This compound facilitates the recruitment of CRBN, making it an essential intermediate in the synthesis of PROTAC molecules. The Boc protecting group can be removed under acidic conditions, enabling further functionalization and development of targeted protein degradation strategies in chemical biology research. -
HDAC1-3 PROTAC Degrader
JPS004 is a targeted proteolysis targeting chimera (PROTAC) that degrades histone deacetylases HDAC1-3. By inducing the degradation of these enzymes, JPS004 facilitates histone acetylation, which can promote apoptosis in cancer cells. This compound is valuable for research into cancer biology and therapeutic strategies aimed at modulating epigenetic modifications. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-16 is an effective degrader specifically targeting BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). This compound is known to significantly reduce Cyclin B1 expression, which is associated with G2/M cell cycle progression. Additionally, PROTAC BRD4 Degrader-16 effectively induces apoptosis in MV-4-11 cells, contributing to its potential utility in cancer research and therapeutic applications. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C2-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that features a thalidomide-derived cereblon ligand. This reagent plays a crucial role in PROTAC (proteolysis-targeting chimeras) technology, facilitating targeted protein degradation. It is of significant interest in drug discovery and development research, particularly for studies aimed at modulating protein function and enhancing therapeutic efficacy. -
Ligands for E3 Ligase
Thalidomide-4-NH-PEG2-COO(t-Bu) is a thalidomide derivative that serves as a ligand for the E3 ubiquitin ligase Cereblon (CRBN). The t-Bu protecting group can be cleaved under acidic conditions, facilitating its incorporation into PROTAC (Proteolysis Targeting Chimera) synthesis. This compound is essential for research involving targeted protein degradation and the development of CRBN-based PROTAC molecules. -
Molecular Glue Degrader
Galeterone hydrochloride is a potent molecular glue degrader that targets the androgen receptor (AR) and its splice variants, as well as MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound also acts as a CYP17 inhibitor with an IC50 of 47 nM, promoting cell apoptosis and inhibiting tumor growth in human prostate cancer xenograft models. Galeterone hydrochloride is relevant in the research of castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
Molecular Glue
eEF2K degrader-2 is a molecular glue that targets the eEF2K protein, effectively mediating its degradation. This compound demonstrates significant biological activity by inhibiting proliferation, migration, and invasion, as well as inducing apoptosis in triple negative breast cancer (TNBC) cells. eEF2K degrader-2 exhibits minimal organ toxicity and pathological damage, making it a valuable tool for research applications focused on cancer biology, particularly in breast cancer studies. -
Bcr-AblT315 PROTAC Degrader
PROTAC BCR-ABL Degrader-2 is a selective degrader targeting the Bcr-AblT315 mutant, with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. This compound demonstrates a notable degradation efficacy, achieving degradation rates of 69.89% and 94.23% at concentrations of 100 nM and 300 nM, respectively. Additionally, it shows promising in vivo anti-tumor effects including significant tumor regression and induction of apoptosis in tumor cells, while maintaining a favorable safety profile. PROTAC BCR-ABL Degrader-2 is suitable for research focused on chronic myeloid leukemia (CML). -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 6 is a selective degrader targeting the EGFRDel19 mutant, exhibiting a DC50 value of 45.2 nM in HCC827 cells. This compound effectively induces apoptosis and leads to G1 phase cell cycle arrest in HCC827 cells. Its unique mechanism of action makes it a valuable tool for research focused on EGFR-related pathways and the development of targeted cancer therapies. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-O-C4-NH2 is an E3 ligase ligand-linker conjugate featuring a cereblon ligand derived from thalidomide, combined with a linker utilized in PROTAC technology. This compound is designed to selectively recruit E3 ligases for targeted protein degradation, making it valuable for studies in targeted therapy and drug development. It facilitates the exploration of protein dynamics and functions, contributing to advancements in cancer research and other diseases linked to protein misregulation. -
PROTAC HDAC6 Degrader
PROTAC HDAC6 Degrader 1 is a selective compound designed to target and degrade histone deacetylase 6 (HDAC6) through the proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 3.5 nM, this degrader exhibits significant antiproliferative effects, particularly by inducing apoptosis in myeloid leukemia cell lines. It serves as a valuable tool for research on cancer therapies and the modulation of histone deacetylation pathways. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-PEG2-C2-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that features a thalidomide-derived cereblon ligand. This compound is designed to facilitate targeted protein degradation through PROTAC technology, enabling researchers to study protein interactions and dysregulation in various biological contexts. Its unique structure supports the development of novel therapeutic strategies by harnessing the ubiquitin-proteasome system for selective protein modulation. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-4-O-C5-NH2 is an E3 ligase ligand-linker conjugate that utilizes the cereblon ligand derived from Thalidomide, combined with a linker suitable for targeted protein degradation applications. This compound facilitates the design of PROTAC molecules, enabling the selective degradation of target proteins via the ubiquitin-proteasome pathway. Its function in research may enhance studies related to therapeutic modalities in cancer and other diseases through targeted protein regulation. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that targets cereblon, an E3 ubiquitin ligase. This compound is designed for use in PROTAC technology, enabling targeted protein degradation and facilitating the selective modulation of protein levels in cellular systems. It is suitable for research applications focused on protein homeostasis and therapeutic development for various diseases. -
PROTAC c-Met Degrader
PROTAC c-Met Degrader-4 is a potent orally active PROTAC designed to target c-MET for degradation. It exhibits remarkable intracellular degradation potency with a DC50 value of less than 0.5 nM and effectively induces cell cycle arrest and apoptosis while inhibiting cell invasion and migration. This compound is particularly useful in cancer research, demonstrating the ability to suppress proliferation and inhibit the growth of various cancers, including non-small cell lung cancer and gastric cancer. In vivo studies also highlight its effectiveness in reducing tumor growth in Hs746T xenograft models. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C3-NH2 is an E3 ligase ligand-linker conjugate that integrates a thalidomide-derived cereblon ligand with a flexible linker designed for use in PROTAC (proteolysis-targeting chimera) technology. This compound facilitates the targeted ubiquitination and subsequent degradation of specific proteins, thereby allowing researchers to investigate protein function and regulation. Its applications extend to drug discovery and development, particularly in therapies targeting diseases driven by protein misfolding or dysregulation. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-4-NH-PEG1-NH2 TFA is an E3 ligase ligand-linker conjugate that targets Cereblon (CRBN). This compound serves as a critical ligand to recruit the CRBN protein, facilitating the development of proteolysis-targeting chimeras (PROTACs). It plays a significant role in studies focused on targeted protein degradation and E3 ligase modulation in biochemical and pharmacological research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-C7-acid is a synthesized E3 ligase ligand-linker conjugate that utilizes the cereblon ligand derived from Thalidomide. This compound serves as a vital component in the development of PROTAC (proteolysis-targeting chimeras) technology, enabling targeted protein degradation. Thalidomide-O-C7-acid is instrumental for researchers focusing on protein regulation and therapeutic applications in various disease models. -
E3 Ligase Ligand-Linker Conjugate
Deoxy-thalidomide-Pip-C-PIP-boc is a conjugate that functions as an E3 ligase ligand-linker complex, featuring Thalidomide as a critical component. This compound acts as a Cereblon ligand, facilitating the recruitment of the CRBN protein, which is essential for targeted protein degradation. It serves as a vital intermediate in the synthesis of complete PROTAC (Proteolysis Targeting Chimeras) molecules, making it valuable for research in targeted therapeutic strategies and protein homeostasis. -
Ligands for E3 Ligase
Thalidomide-4-O-CH2-COO(t-Bu) is a modified form of Thalidomide that serves as a ligand for the E3 ligase Cereblon (CRBN). It effectively recruits CRBN proteins, facilitating profound biological activity associated with protein degradation pathways. The tert-butyl protecting group can be removed under acidic conditions, enabling its use in the synthesis of PROTAC molecules. This compound is essential for researchers working on CRBN-based PROTAC development. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-PIP-(R)C-pyrrolidine-boc is a conjugate that acts as an E3 ligase ligand-linker complex, incorporating Thalidomide as the enabling component. This compound functions as a Cereblon ligand, facilitating the recruitment of the CRBN protein and serving as a crucial intermediate in the synthesis of PROTAC molecules. Its role in targeted protein degradation makes it a valuable tool for addressing complex biological questions in chemical biology and therapeutic development. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-amido-C5-NH2 is an E3 ligase ligand-linker conjugate featuring a Thalidomide-derived cereblon ligand, designed for applications in PROTAC (Proteolysis Targeting Chimeras) technology. This compound facilitates targeted protein degradation, enabling researchers to investigate proteostasis and elucidate cellular mechanisms. Its use in drug discovery can enhance the development of novel therapeutics by modulating protein levels and activity in complex biological systems. -
Ligands for E3 Ligase
Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified Thalidomide derivative that functions as a ligand for the E3 ubiquitin ligase Cereblon (CRBN). By recruiting CRBN proteins, this compound is a critical intermediate in the development of CRBN-based PROTAC molecules. These PROTACs are engineered to selectively target and degrade the SHP2 protein, making them valuable tools for cancer research and therapeutic applications.
