Catalog No.
Product Name
Application
Product Information
Citations
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TEAD PROTAC Degrader
KG-FP-003 is a potent and selective TEAD PROTAC degrader, demonstrating DC50 values of 6 ± 4 nM for TEAD1, 68 ± 15 nM for TEAD2, 12 ± 5 nM for TEAD3, and 7 ± 5 nM for TEAD4. This compound effectively induces ubiquitination and degradation of TEAD proteins. KG-FP-003 has demonstrated significant anticancer activity against mesothelioma and ovarian cancer, making it a valuable tool for research in cancer biology and therapeutic development targeting TEAD pathways. -
PROTAC TEAD Degrader
PROTAC TEAD degrader-1 is a targeted molecular degrader that selectively promotes the degradation of transcriptional enhanced associate domain (TEAD) proteins via a ubiquitin-proteasome pathway. With a DC50 value of 54.1 nM in 293T cells, it effectively inhibits cell proliferation in NF2-deficient NCI-H226 cells with an IC50 of 0.21 μM. This compound also modulates the expression of yes-associated protein (YAP) target genes, making it a valuable tool for investigating TEAD-related signaling pathways and their implications in various biological processes. -
TEAD1 PROTAC Degrader
PROTAC TEAD degrader-2 is a potent degrader designed to target TEAD1 through the proteolysis-targeting chimera (PROTAC) approach. It effectively disrupts the YAP/TAZ-TEAD interaction, exhibiting a low DC50 of 0.6 nM and an IC50 of 1.8 nM. This compound demonstrates strong selective inhibitory activity against YAP-dependent cancer cell lines and significantly reduces transcriptional activity associated with YAP. PROTAC TEAD degrader-2 serves as a valuable tool for investigating the role of TEAD1 in mesothelioma and glioma research. -
PROTAC GSK-3β Degrader
PROTAC GSK-3β Degrader-1 is a targeted GSK-3β degrader that induces the proteasomal degradation of GSK-3β with an IC50 value of 833 nM. This compound integrates SB-216763, a known GSK-3β inhibitor, a PEG linker, and a CRBN ligand to facilitate E3 ligase-mediated degradation. It has demonstrated efficacy in reducing neurotoxicity induced by Aβ25-35 peptide and CuSO4, making it a valuable tool for researching Alzheimer's disease mechanisms and potential therapeutic interventions. -
GSK3α/GSK3β PROTAC Degrader
PT-65 is a PROTAC degrader targeting GSK3α and GSK3β, exhibiting DC50 values of 28.3 nM and 34.2 nM, respectively. This compound effectively inhibits excessive tau phosphorylation induced by GSK3β, amyloid-beta, and okadaic acid. PT-65 is a valuable tool for research into the pathophysiology of Alzheimer's disease, allowing for further investigation into tau-related mechanisms and potential therapeutic interventions. -
PROTAC ATR Degrader
PROTAC ATR degrader-1 (compound ZS-7) is a potent degrader targeting ataxia telangiectasia and Rad3-related (ATR) proteins, demonstrated by a DC50 of 0.53 μM. This compound facilitates selective degradation of ATR, making it a valuable tool for cancer research and the study of DNA damage response pathways. Its application in cellular models aids in understanding the therapeutic potential of ATR inhibition in various malignancies. -
PROTAC ATR Degrader
Abd110 is a Lenalidomide-based PROTAC that targets and degrades ATR kinase. It selectively reduces levels of ATR and phospho-ATR while sparing related kinases such as ATM and DNA-PKcs. This compound is valuable for research applications focused on ATR-mediated pathways and innate cellular responses to DNA damage. -
Cyclin K Degrader
HQ461 is a molecular glue that facilitates the interaction between CDK12 and DDB1, leading to the targeted degradation of cyclin K. This degradation impairs CDK12 function, which in turn results in reduced phosphorylation of CDK12 substrates, downregulation of DNA damage response genes, and induces apoptosis in affected cells. HQ461 is a valuable tool for research applications focused on the modulation of cell cycle regulation and the DNA damage response pathway. -
CCND1/CDK4 PROTAC Degrader
CPD-39 is a potent heterobifunctional PROTAC degrader that targets CCND1 and CDK4. This compound effectively induces the degradation of these proteins, demonstrating significant anti-proliferative activity. CPD-39 is intended for research applications focusing on the modulation of cell cycle regulation and cancer therapeutics. -
CDK2 Molecular Glue Degrader
CDK2 degrader 6 is a potent CDK2 molecular glue degrader that functions through binding to cereblon and CDK2, leading to the ubiquitination and proteasomal degradation of CDK2. With a DC50 of 46.5 nM, it effectively modulates the cell cycle and reduces proliferation in breast cancer cells. Additionally, CDK2 degrader 6 demonstrates in vivo antitumor activity in gastric cancer mouse models, making it a valuable tool for research into breast and gastric cancers. -
Molecular Glue Degrader
dCeMM3 is a molecular glue degrader that facilitates the ubiquitination and subsequent degradation of cyclin K. By promoting the interaction of the CDK12-cyclin K complex with the CRL4B ligase complex, dCeMM3 plays a critical role in regulating cell cycle progression. This reagent is particularly useful for research applications focused on targeted protein degradation and the elucidation of CDK12-associated pathways. -
Molecular Glue Degrader
dCeMM2 is a molecular glue degrader that specifically targets cyclin K. It induces ubiquitination and subsequent degradation of cyclin K by facilitating the interaction between CDK12-cyclin K and the CRL4B ligase complex. This compound is valuable for studying the regulation of cell cycle and transcriptional processes, and it serves as a tool in research areas focusing on cancer biology and cell signaling pathways. -
CDK7 PROTAC Degrader
JWZ-5-13 is a potent CDK7 PROTAC degrader that selectively targets cyclin-dependent kinase 7 for ubiquitin-proteasome system-mediated degradation. It exhibits significant antiproliferative effects on various cancer cell lines, making it an essential tool for studying pathways involved in malignancies such as ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia, and non-small cell lung cancer. This compound facilitates the exploration of targeted protein degradation in cancer biology, offering insights into therapeutic strategies. -
CDK2/CDK5 PROTAC Degrader
TMX-2172 is a selective bivalent PROTAC that targets CDK2 and CDK5, inducing their proteasomal degradation with IC50 values of 6.5 nM and 6.8 nM, respectively. This compound demonstrates notable selectivity for CDK2 and CDK5, while sparing other cyclin-dependent kinases such as CDK1, CDK4, CDK6, CDK7, and CDK9. TMX-2172 effectively inhibits the enzymatic activity of CDK2 and CDK5, leading to a reduction in ASCL1 protein levels, induction of cancer cell death, and antiproliferative effects. This reagent is applicable in research focused on ovarian cancer and small cell lung cancer. -
CDK12/7/9 Degrader
BSJ-5-63 is a potent PROTAC degrader targeting CDK12, CDK7, and CDK9. It effectively reduces protein expression levels of these kinases as well as RNAPII and Cyclin K, resulting in decreased mRNA expression of BRCA1 and BRCA2. This compound exhibits significant anticancer activity and is particularly relevant for research focused on prostate cancer. -
CDK12/CDK13 PROTAC Degrader
ZLC491 is a PROTAC degrader that selectively targets CDK12 and CDK13, utilizing cereblon- and proteasome-dependent mechanisms for degradation. This compound effectively inhibits the transcription and expression of long genes, particularly those involved in DNA damage response pathways. ZLC491 demonstrates anti-proliferative effects in various triple-negative breast cancer cell lines, making it a valuable tool for research into targeted therapies for this aggressive cancer subtype. -
PROTAC/CDK2 Degrader
CDK2 Degrader 2 is a potent PROTAC targeting cyclin-dependent kinase 2 (CDK2), facilitating its degradation in MKN1 cells with a DC50 value of less than 100 nM. This compound employs a novel design, integrating a ligand for the target protein along with a linker and a ligand for the E3 ligase cereblon (CRBN). CDK2 Degrader 2 is valuable for research applications focused on the regulation of cell cycle progression and the exploration of targeted protein degradation mechanisms. -
Molecular Glue Degrader
dCeMM4 is a molecular glue degrader that targets cyclin K by inducing its ubiquitination and subsequent degradation. It facilitates the interaction between CDK12-cyclin K and the CRL4B ligase complex, leading to effective protein degradation. This compound is useful for research applications investigating cell cycle regulation and the ubiquitin-proteasome system. -
PROTAC CDK9 Degrader
PROTAC CDK9 degrader-9 is a selective and potent degrader designed to target cyclin-dependent kinase 9 (CDK9) via PROTAC technology. This compound facilitates the targeted degradation of CDK9, thereby modulating transcriptional regulation and influencing cell proliferation. It is particularly useful in anti-cancer research, where the inhibition of CDK9 can lead to suppression of oncogenic pathways. -
PROTAC CDK9 degrader
PROTAC CDK9 degrader-2, a selective degrader of cyclin-dependent kinase 9 (CDK9), utilizes a PROTAC mechanism involving a natural product ligand, Wogonin, which targets the ubiquitin E3 ligase Cereblon (CRBN). With an IC50 of 17 μM in MCF-7 cell lines, this compound demonstrates potent activity in the degradation of CDK9, making it a valuable reagent for research applications focused on CDK9-related pathways in cancer biology and therapeutic development. -
CDK2 Degrader
(R)-CDK2 Degrader 6 is a cereblon-based molecular glue degrader specifically targeting cyclin-dependent kinase 2 (CDK2). It functions by inducing ubiquitination and subsequent proteasomal degradation of CDK2, with a DC50 value of 27 nM. This compound is suitable for cancer research applications, providing a valuable tool for studying CDK2-related pathways and therapeutic interventions. -
CDK2 Molecular Glue Degrader
(S)-CDK2 degrader 6 selectively targets cyclin-dependent kinase 2 (CDK2) as a molecular glue degrader. With a DC50 of 166.7 nM over 24 hours, this compound effectively promotes the degradation of CDK2, thereby modulating cell cycle progression. It holds significant potential for applications in breast cancer research, enabling the exploration of therapeutic strategies that involve the regulation of CDK2 activity. -
Ligands for Target Protein for PROTAC
FN-1501-propionic acid is a ligand targeting cyclin-dependent kinases 2 and 9 (CDK2/9), utilized in the development of PROTAC (proteolysis targeting chimeras) for targeted protein degradation. This compound can be combined with a CRBN ligand to facilitate the design of PROTAC-based CDK2/9 degraders, enabling selective degradation of these kinases. Its application in research enhances the study of cellular processes regulated by CDK2 and CDK9, making it a valuable tool for investigating therapeutic strategies against diseases associated with dysregulated kinase activity. -
CDK9 PROTAC Degrader
PROTAC CDK9 degrader-11 is an orally active PROTAC degrader that specifically targets CDK9, demonstrating a DC50 value of 1.09 nM. This compound shows cytotoxicity in various small cell lung cancer cell lines with an IC50 in the nanomolar range. PROTAC CDK9 degrader-11 effectively induces cell cycle arrest at the G0/G1 phase and reduces invasion in DMS114 and DMS53 cells. Additionally, it exhibits significant antitumor efficacy in NCI-H446 xenograft mouse models, making it a valuable tool for cancer research and therapeutic development. -
CDK4/6 PROTAC Degrader
CST651 is a selective proteolysis-targeting chimera (PROTAC) degrader specifically designed to target cyclin-dependent kinases CDK4 and CDK6. This compound effectively degrades CDK4 and CDK6 in MM.1S cells, exhibiting DC50 values of 20 nM and 5.1 nM, respectively. CST651 demonstrates the ability to inhibit cancer cell proliferation and migration, making it a valuable tool for research into various cancers, including acute lymphoblastic leukemia. -
PROTAC Degrader
PROTAC CDK2 Degrader-1 is a selective PROTAC degrader designed to target cyclin-dependent kinase 2 (CDK2). This compound effectively induces degradation of CDK2 and inhibits phosphorylation of the retinoblastoma (RB) protein in the CDK2-dependent OVCAR3 cell line, with an IC50 range of 100-500 nM. It serves as a valuable tool for investigating the biological functions of CDK2 in cancer research and therapeutic applications. -
Molecular Glues
CDK12 ligand-3 is a molecular glue that effectively targets and degrades the CDK12 protein, with a DC50 of 35 nM. This compound also influences the degradation of CDK13 and its regulatory partner, Cyclin K, while inhibiting serine 2 phosphorylation of the RNA polymerase II CTD. CDK12 ligand-3 demonstrates significant anti-proliferative effects on Jurkat cells and is applicable in cancer research, particularly in the study of leukemia. -
CDK9 Degrader
PROTAC CDK9 degrader-8 is a potent degrader targeting CDK9, exhibiting an IC50 value of 0.01 μM. This compound effectively induces the degradation of CDK9, making it a valuable tool for investigating the role of CDK9 in cancer biology and therapeutic resistance. It is suitable for use in studies aimed at understanding the mechanisms of tumor progression and exploring potential treatment strategies. -
CDK12/CDK13 Inhibitor/CycK Molecular Glue Degrader
SR-5037 is an orally active inhibitor of CDK12 and CDK13, with an IC50 of 31 nM, and functions as a molecular glue degrader for CycK, demonstrating a DC50 of 30 nM and Dmax exceeding 98%. By inhibiting the enzymatic activity of the CDK12/CycK and CDK13/CycK complexes, SR-5037 facilitates the recruitment of DDB1, leading to proteasome-mediated degradation of CycK. This compound has shown efficacy in degrading active CycK in mouse models of triple-negative breast cancer and is a valuable tool for investigating treatment options in such malignancies. -
CDK2/4/6 PROTAC Degrader
PROTAC CDK2/4/6 Degrader-1 is a potent orally bioavailable degrader targeting CDK2, CDK4, and CDK6 through the proteolysis-targeting chimera (PROTAC) mechanism. This compound functions by facilitating the ubiquitination and degradation of these cyclin-dependent kinases, thereby inhibiting their activity. Its applications extend to the study of malignant melanoma, providing valuable insights into tumor biology and potential therapeutic interventions. This degrader is synthesized as a prodrug from PROTAC CDK2/4/6 Degrader-2, enabling enhanced functionality in biological systems. -
CDKs PROTAC Degrader
TMX-2138 is a potent CDKs PROTAC degrader that achieves IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. This compound facilitates the ubiquitination and subsequent degradation of cyclin-dependent kinases (CDKs), making it a valuable tool for investigating their roles in cellular processes. TMX-2138 is particularly relevant for research focused on ovarian cancer, enabling the study of CDK-targeted therapies and their potential therapeutic implications. -
CDK9 Degrader/Ligands for Target Protein for PROTAC
(R)-PROTAC CDK9 ligand-1 is a potent degrader targeting cyclin-dependent kinase 9 (CDK9), a key regulator of transcription and cell cycle progression. This compound facilitates the synthesis of PROTACs (proteolysis-targeting chimeras), which exhibit antitumor activity by promoting the degradation of CDK9. Research applications include investigations into cancer biology and therapeutic strategies aimed at modulating CDK9 levels for improved treatment outcomes. -
PROTAC USP7 Degrader
PROTAC USP7 Degrader-2 targets the ubiquitin-specific protease 7 (USP7) and functions as a selective degrader. Demonstrating a DC50 of 1.91 μM in TE-12 cells, this compound effectively inhibits the migration of upper gastrointestinal tract cancer cells, although its anti-proliferative activity is relatively modest. PROTAC USP7 Degrader-2 is valuable for research focused on metastatic upper gastrointestinal cancer, aiding in the exploration of therapeutic strategies targeting USP7. -
MNK1 PROTAC Degrader
PROTAC MNK1 degrader-1 is a selective degrader that targets MNK1, exhibiting a DC50 of 11.92 nM and a Dmax exceeding 96% in MV4-11 cells. This compound effectively reduces phosphorylated eIF4E levels (IC50: 22.07 nM), triggers apoptosis, and causes G1 phase cell cycle arrest. With demonstrated potent antitumor activity, PROTAC MNK1 degrader-1 also shows robust antileukemic efficacy in MV4-11 xenograft mouse models while maintaining acceptable drug safety profiles. -
SARS-CoV-2 Mpro PROTAC degrader
HP211206 is a PROTAC degrader targeting the main protease (Mpro) of SARS-CoV-2, designed to selectively degrade both the protease and its drug-resistant variants. This compound demonstrates an IC50 of 181.9 nM and a DC50 of 621 nM, reflecting its potency in disrupting viral replication. HP211206 also exhibits antiviral activity, making it a valuable tool for research aimed at understanding and combating SARS-CoV-2 infections. -
SARS-CoV-2 Mpro PROTAC Degrader
PROTAC SARS-CoV-2 Mpro degrader-2 is a highly effective PROTAC degrader targeting the main protease (Mpro) of SARS-CoV-2. This compound exhibits significant antiviral activity against various coronaviruses, including EC50 values of 10.8 μM for SARS-CoV-2, 1.6 μM for HCoV-OC43, and 6.5 μM for HCoV-229E. In Calu-3 cells, it demonstrates potent efficacy with an EC50 of 0.89 μM, making it a valuable tool for research focused on coronavirus biology and potential therapeutic interventions. -
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. -
IDO1 PROTAC Degrader
NU227326 is a potent IDO1 PROTAC degrader designed to penetrate the blood-brain barrier, exhibiting a DC50 of 4.5 nM in HiBiT degradation assays. It effectively degrades IDO1 in human glioblastoma cell lines U87 and GBM43, with DC50 values of 7.1 nM and 11.8 nM, respectively, as demonstrated in Western blot assays. This compound is valuable for research into various malignancies, including glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer. -
PROTAC IDO1 Degrader
NU223612 is a selective PROTAC designed to target and degrade indoleamine 2,3-dioxygenase 1 (IDO1) through CRBN-mediated proteasomal degradation, exhibiting a Kd of 640 nM. With a binding affinity for CRBN of 290 nM, NU223612 effectively reduces IDO1 protein levels, making it a valuable tool in the study of immune modulation and tumor microenvironments. Additionally, NU223612 demonstrates the ability to cross the blood-brain barrier, enhancing its potential utility in neurobiological research. -
PROTAC Linkers
DSPE-PEG-Biotin, MW 2000 is a polyethylene glycol (PEG) based linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs). This compound facilitates the conjugation of biotin to target proteins, enhancing their recognition and degradation by the cellular proteasome. Its application in PROTAC technology supports the development of novel therapeutics by enabling targeted protein modulation in cellular research. -
PROTAC linker
DSPE-PEG8-Mal is a PEG-based linker designed for use in PROTAC (proteolysis-targeting chimera) synthesis. This compound facilitates the development of PROTACs by enhancing their solubility and stability. Its primary mechanism involves forming a covalent bond with target proteins, thus enabling targeted degradation. DSPE-PEG8-Mal is essential for researchers investigating novel therapeutic strategies via targeted protein degradation. -
PROTAC TG2 degrader
PROTAC TG2 degrader-1 is a von Hippel-Lindau (VHL)-based PROTAC designed to specifically target tissue transglutaminase (TG2) with a dissociation constant (KD) of 68.9 μM. This compound effectively induces the degradation of TG2 in ovarian cancer cells through a proteasome-dependent mechanism. It serves as a valuable tool for research investigating the role of TG2 in cancer biology and potential therapeutic applications. -
PROTAC HPK1 Degrader
PROTAC HPK1 Degrader-1 is a selective HPK1 degrader that exhibits a DC50 value of 1.8 nM, demonstrating its potency in degrading HPK1. This compound effectively inhibits the phosphorylation of the SLP76 protein, with an IC50 of 496.1 nM. PROTAC HPK1 Degrader-1 serves as a valuable tool for investigating HPK1's role in T cell receptor (TCR) signaling pathways. -
PROTAC HPK1 Degrader
SS47 is a PROTAC-based HPK1 degrader that facilitates proteasome-mediated degradation of the HPK1 protein. By targeting HPK1 for destruction, SS47 significantly enhances antitumor efficacy, making it a valuable tool for cancer research. Its applications include investigating the role of HPK1 in tumorigenesis and evaluating the efficacy of targeted protein degradation strategies in oncology. -
PROTAC HPK1 Degrader
PROTAC HPK1 Degrader-2 targets HPK1 for degradation via a proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 23 nM in human peripheral blood mononuclear cells (PBMC), this compound is instrumental in elucidating HPK1's functions in cancer biology. The selectivity and potency of PROTAC HPK1 Degrader-2 make it a valuable tool for cancer research applications, enabling the study of targeted protein degradation and its implications in therapeutic strategies. -
PROTAC HPK1 Degrader
HPK1-IN-47 is a selective HPK1 ligand designed for the synthesis of PROTACs, specifically serving as a precursor for PROTAC HPK1 Degrader-2. It exhibits potential in targeting HPK1, which plays a significant role in various HPK1-mediated diseases, particularly cancer. This compound is valuable for research applications focused on elucidating the therapeutic potential of HPK1 degradation in cancer treatment. -
PROTAC HPK1 Degrader
PROTAC HPK1 Degrader-6 is a potent PROTAC compound designed to selectively target and degrade the HPK1 protein, exhibiting an IC50 of less than 50 nM. This compound facilitates the investigation of HPK1's role in leukemia and other related disorders. By employing the dual binding mechanism to HPK1 and the E3 ligase CRBN, it serves as a valuable tool for researchers exploring targeted protein degradation as a therapeutic strategy. -
PROTAC HPK1 Degrader
DD205-291 is an orally active PROTAC HPK1 degrader that exhibits a DC50 value of 5.3 nM. Its primary mechanism involves the targeted degradation of HPK1, leading to the inhibition of SLP-76 phosphorylation. This modulation subsequently results in the enhanced expression of key cytokines such as IL-2 and IFN-γ, making DD205-291 a valuable reagent for studies in immune signaling and related therapeutic applications. -
Ligands for Target Protein for PROTAC
PD0325901-O-C2-dioxolane is a derivative of the MEK inhibitor PD0325901, designed as a ligand for targeted protein degradation in conjunction with VHL or CRBN E3 ligases. This compound facilitates the synthesis of MEK1/2 degraders, enabling the selective degradation of MEK proteins in experimental studies. Its application in research provides critical insights into MEK-related signaling pathways and their role in various diseases, particularly in cancer biology. -
MEK1/2 PROTAC Degrader
MS910 is a potent and selective PROTAC degrader targeting MEK1 and MEK2 kinases. It demonstrates effective degradation of MEK1 and MEK2 in various cancer cell lines, with reported DC50 values of 118 nM for MEK1 and 55 nM for MEK2 in HT-29 cells, and 94 nM for MEK1 and 38 nM for MEK2 in SK-MEL-28 cells. MS910 is primarily utilized in cancer research to explore the therapeutic potential of targeted protein degradation.
