Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PROTAC KDM4 Degrader
PROTAC KDM4 Degrader-1 is a potent proteolysis targeting chimera (PROTAC) designed to selectively degrade KDM4A-C while sparing KDM4D. This compound demonstrates significant antiproliferative effects in esophageal cancer cells, inducing apoptosis and cell cycle arrest. Additionally, PROTAC KDM4 Degrader-1 effectively inhibits histone H3 lysine demethylation, making it a valuable tool for research into cancer biology and epigenetic regulation. -
IRAK4 PROTAC Degrader
PROTAC IRAK4 degrader-13 is a selective IRAK4-directed PROTAC degrader that effectively targets IRAK4 with DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes, respectively. This compound significantly activates TIR signaling and reduces the expression of proinflammatory cytokines in an Imiquimod-induced psoriasis mouse model. PROTAC IRAK4 degrader-13 is applicable in research focused on TLR- and IL-1R-driven inflammatory diseases, including hidradenitis suppurativa and atopic dermatitis. -
Ligands for E3 Ligase
XB2M54 is a selective antagonist of X-linked inhibitor of apoptosis protein (XIAP), functioning as a ligand for E3 ligases. It effectively inhibits NOD2-mediated inflammatory signaling pathways, making it a valuable tool in inflammation research. Additionally, XB2M54 can be employed in the synthesis of PROTAC ERα Degrader-1, facilitating studies on targeted protein degradation and its implications in therapeutic applications. -
PD-L1 PROTAC Degrader
PROTAC PD-L1 degrader-2 is a selective degrader targeting PD-L1. It demonstrates a potent inhibitory effect with an IC50 of 197.4 nM and a binding affinity characterized by a Kd of 301 nM. This compound facilitates the internalization and subsequent degradation of PD-L1 through both proteasomal and lysosomal pathways, thereby enhancing immune system activation. Its efficacy has been validated in MC38 C57BL/6 mouse models, underscoring its potential for antitumor applications. -
Ligands for Target Protein for PROTAC
(Rac)-BMS-1 is a racemic compound that serves as a ligand for target proteins in the development of proteolysis-targeting chimeras (PROTACs). It plays a crucial role in synthesizing D5B PROTAC, facilitating targeted protein degradation. This compound is valuable for researchers investigating protein regulation and therapeutic applications in cancer and other diseases. -
Ligands for Target Protein for PROTAC
SHP2-IN-43 is a potent inhibitor of SHP2, demonstrating an IC50 of 98.7 nM. This compound serves as a valuable ligand for targeted protein degradation (PROTAC) applications, facilitating the synthesis of SHP2-D26. Researchers can utilize SHP2-IN-43 to explore the therapeutic potential of modulating SHP2 activity in various biological contexts. -
PROTAC VEGFR2 Degrader
PROTAC VEGFR-2 Degrader-1 is a targeted protein degradation compound designed to selectively degrade VEGFR-2. It demonstrates minimal VEGFR-2 inhibition with an IC50 exceeding 1 μM, and exhibits limited anti-proliferative activity against EA.hy926 cells, with an IC50 greater than 100 μM. This reagent is valuable for research applications focused on the regulation of VEGFR-2 and its role in vascular biology and related disease mechanisms. -
PROTAC VEGFR2 Degrader
PROTAC VEGFR-2 Degrader-2 primarily targets the vascular endothelial growth factor receptor 2 (VEGFR-2) for degradation through the PROTAC mechanism. This compound displays minimal inhibition of VEGFR-2 activity with an IC50 exceeding 1 μM and demonstrates anti-proliferative effects in EA.hy926 cells, with an IC50 greater than 100 μM. It serves as a valuable tool for studies focused on targeted protein degradation and the modulation of signaling pathways related to angiogenesis. -
LCK PROTAC Degrader
SJ45566 is a potent PROTAC-based degrader targeting LCK with a DC50 of 1.21 nM. This compound is designed for the selective degradation of LCK, providing a valuable tool for investigating T-Cell Acute Lymphoblastic Leukemia. Its efficacy in modulating LCK levels makes it applicable in studies aimed at understanding T-cell signaling pathways and cancer biology. -
Lck Molecular Glue Degrader
LCK degrader-2 is a Lck molecular glue degrader designed to selectively target and degrade the Lck protein. This compound demonstrates potent biological activity in disrupting Lck-mediated signaling pathways, making it a valuable tool for studying acute lymphoblastic leukemia (ALL) and other Lck-dependent malignancies. Its application in cancer research provides insights into therapeutic strategies for Lck-related diseases. -
Molecular Glue
Lck degrader-1 is a molecular glue degrader that targets lymphocyte-specific protein tyrosine kinase (LCK) with a DC50 of 23.1 nM. This compound plays a significant role in the degradation of LCK, making it a valuable tool for studying T-cell acute lymphoblastic leukemia (T-ALL). Researchers can utilize Lck degrader-1 to explore the molecular mechanisms underlying T-ALL and investigate potential therapeutic strategies. -
TRK PROTAC Degrader
CG428 is a potent CRBN-dependent PROTAC degrader specifically targeting tropomyosin receptor kinase (TRK). It effectively reduces levels of the TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells with a DC50 of 0.36 nM and inhibits downstream PLCγ1 phosphorylation with an IC50 of 0.33 nM. CG428 demonstrates higher binding affinity for TRKA (Kd = 1 nM) compared to TRKB and TRKC, making it a valuable tool for research into colorectal carcinoma. -
Ligands for Target Protein for PROTAC
GNF-8625 is a potent TRK inhibitor that functions by targeting TRK receptor tyrosine kinases, specifically TRKA, TRKB, and TRKC, with IC50 values of 0.8 nM, 22 nM, and 5.4 nM, respectively. This compound can be utilized in conjunction with Thalidomide to create a PROTAC degrader, enabling targeted protein degradation. GNF-8625 is valuable in research applications investigating TRK-mediated pathways and offers potential in therapeutic strategies for cancers involving aberrant TRK signaling. -
RET PROTAC Degrader
PROTAC RET Degrader 1 is an orally bioavailable RET PROTAC degrader that effectively crosses the blood-brain barrier. It demonstrates remarkable potency with DC50 values for various RET mutations, including 1.7 nM for RET (WT) and 3 nM for RET (G810S). PROTAC RET Degrader 1 exhibits strong anti-proliferative effects in cancer cell lines harboring oncogenic RET fusions and mutations, and shows significant anti-tumor efficacy in patient-derived xenograft mouse models. This reagent is valuable for investigating RET-positive cancers and their therapeutic targeting. -
TLR4 Inhibitor/PROTAC Linker
TLR4-IN-C34-C2-COOH is a TLR4 inhibitor that serves as a PROTAC linker. It demonstrates significant potential in the modulation of inflammatory responses, particularly in studies involving acute myocardial injury. By targeting TLR4 in enterocytes and macrophages, TLR4-IN-C34-C2-COOH effectively reduces systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis, making it a valuable tool for research in inflammation-related pathways. -
PROTAC Aurora-A/Aurora-B Degrader
dAurAB5 is a dual PROTAC degrader targeting Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM). It effectively induces the degradation of these kinases, leading to reduced N-Myc levels and decreased viability in IMR32 neuroblastoma cells. dAurAB5 also downregulates AAK1, PTK2, GAK, and TTK, making it a valuable tool for investigating the molecular mechanisms in neuroblastoma and related cancers. -
FAK PROTAC degrader
FAK PROTAC B5 is a potent degrader targeting focal adhesion kinase (FAK) with an IC50 of 14.9 nM. This compound exhibits significant FAK degradation capabilities along with antiproliferative effects. Furthermore, it demonstrates notable plasma stability and moderate membrane permeability, effectively inhibiting cell migration and invasion. FAK PROTAC B5 is suitable for research applications focused on cancer biology and cellular signaling pathways. -
PROTAC FAK Degarder
BSJ-04-146 is a selective PROTAC that targets focal adhesion kinase (FAK) for degradation, exhibiting an IC50 of 26 nM. It demonstrates rapid and robust degradation of FAK in cancer cells while maintaining high specificity across the proteome, and it induces prolonged degradation in murine models. The activity of BSJ-04-146 relies on the ubiquitin-proteasome system, making it a valuable tool for investigating pathways associated with pancreatic cancer and triple-negative breast cancer. -
PTK2/FAK PROTAC Degrader
BI-0319 is a selective PROTAC degrader targeting PTK2/FAK, effectively promoting the degradation of these proteins. This compound has demonstrated the ability to reduce cancer cell viability, inhibit cellular proliferation, and curtail invasion, making it a valuable tool for cancer research, particularly in studies related to liver cancer. BI-0319 provides insights into therapeutic strategies focused on protein degradation in oncology. -
c-Met PROTAC Degrader
PROTAC c-Met degrader-1 is a selective and orally active degrader targeting c-Met, exhibiting a DC50 of 6.21 nM. This compound promotes CRBN-dependent ubiquitination and subsequent proteasomal degradation of c-Met, effectively inducing G0/G1 phase arrest in c-Met-dependent cancer cells. Furthermore, PROTAC c-Met degrader-1 demonstrates significant anticancer activity by killing c-Met-dependent cells and inhibiting tumor growth in animal models, making it a valuable tool for research in gastric cancer. -
PROTAC c-Met Degrader
PROTAC c-Met degrader-2 is a PROTAC-based degrader that selectively targets c-Met for degradation through the ubiquitin-proteasome pathway, exhibiting a DC50 of 50 nM. This compound employs a unique linkage incorporating a CRBN ligand derived from Thalidomide, facilitating targeted protein degradation. It serves as a valuable tool for researching c-Met-related pathways and their implications in various cancers, enhancing the understanding of therapeutic strategies involving c-Met modulation. -
PROTAC BTK Degrader
PROTAC BTK Degrader-1 is an innovative PROTAC-based compound designed for the selective degradation of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 34.51 nM for wild-type BTK and 64.56 nM for the BTK-481S mutant. This compound effectively lowers BTK protein levels, thereby inhibiting tumor growth. Additionally, PROTAC BTK Degrader-1 features an alkyne group facilitating its application in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for advanced chemical research and targeted therapies. -
PROTAC
L18I is a PROTAC designed to target Bruton’s tyrosine kinase (Btk), facilitating the degradation of this protein and thereby mitigating inflammation associated with autoimmune diseases, such as lupus erythematosus induced by BM12 splenocytes. This compound comprises the IBT6A ligand, a linker moiety (Propargyl-PEG3-alcohol), and an E3 ubiquitin ligase ligand (Lenalidomide-Br), effectively promoting the destruction of Btk. L18I serves as a valuable tool for investigating Btk's role in autoimmunity and offers potential pathways for therapeutic intervention.
