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. -
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. -
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. -
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. -
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. -
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. -
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. -
ASK1 PROTAC Degrader
dASK1 is a selective PROTAC degrader targeting apoptosis signal-regulating kinase 1 (ASK1) through a cereblon (CRBN)-mediated pathway. This compound forms a stable ternary complex with ASK1, promoting its efficient degradation via the ubiquitin-proteasome system. dASK1 exhibits potent activity in degrading ASK1 and serves as a valuable tool in research focused on steatohepatitis and related pathologies. -
CDK9 PROTAC Degrader
KI-CDK9d-32 is a selective and potent degrader designed to target CDK9 through a PROTAC mechanism (DC50: 0.89 nM). It facilitates the ubiquitination and subsequent degradation of CDK9, effectively inhibiting the MYC signaling pathway and disrupting nucleolar homeostasis. This compound demonstrates significant anticancer activity, particularly against acute lymphoblastic leukemia and pancreatic cancer, making it a valuable tool for research in cancer biology and therapeutic development. -
DAPK1 PROTAC Degrader
PROTAC DAPK1 Degrader-1 selectively targets DAPK1 for degradation, exhibiting a DC50 value of 119.6 nM. This compound has been shown to elevate MDM2 protein levels while concurrently decreasing cleaved caspase-3 and cleaved PARP levels in a neurotoxin-induced cell apoptosis model. Its ability to effectively inhibit neuronal apoptosis positions PROTAC DAPK1 Degrader-1 as a valuable tool for investigating neurological disorders, including cerebral ischemia and traumatic brain injury. -
PROTAC Degrader for FKBP12
22-SLF is a PROTAC degrader specifically targeting FK506-binding protein 12 (FKBP12), exhibiting a DC50 of 0.5 µM. This compound forms a ternary complex with C227 and C228 in FBXO22, facilitating FKBP12 degradation in an FBXO22-dependent manner. 22-SLF is a valuable tool for cancer research, serving as a probe to investigate the FBXO22-mediated degradation pathways. -
EZH2 PROTAC
PROTAC EZH2 Degrader-41 is a PROTAC designed to target EZH2 by recruiting cIAP E3 ubiquitin ligase. This compound facilitates the ubiquitination and subsequent proteasomal degradation of EZH2, thereby exerting significant antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 is a valuable tool for investigating the role of EZH2 in lymphoma research and its potential as a therapeutic target. -
PROTAC MDM2 degrader
YX-02-030 is a PROTAC MDM2 degrader that effectively inhibits the MDM2-p53 interaction with an IC50 value of 63 nM, as well as the VHL-HIF1α binding, with an IC50 of 1.35 μM. By binding to MDM2, it recruits the VHL E3 ubiquitin ligase, promoting MDM2 degradation. This compound is particularly relevant in researching therapeutic strategies against p53 mutant or deleted triple-negative breast cancer (TNBC) cells. -
TAF1 PROTAC Degrader
ZS3-046 is a TAF1 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of the TAF1 protein. This compound effectively activates p53, leading to apoptosis in acute myeloid leukemia (AML) cells. In vivo studies have demonstrated its antitumor efficacy in AML tumor xenograft mouse models, making ZS3-046 a valuable tool for researching targeted degradation strategies in cancer therapy. -
MDM2 Degrader
MD-265 is a potent MDM2 degrader utilizing the PROTAC (PROteolysis TArgeting Chimeras) technology. It effectively promotes the degradation of MDM2, resulting in the reactivation of the p53 tumor suppressor pathway in cancer cells with wild-type p53. Preclinical studies demonstrate that MD-265 induces complete tumor regression and enhances long-term survival in leukemia models, making it a valuable tool for cancer research and therapeutic development. -
Hemagglutinin Degrader
PROTAC Hemagglutinin Degrader-1 is a potent degrader specifically targeting influenza hemagglutinin (HA). It exhibits significant biological activity with a median degradation concentration of 1.44 μM, demonstrating broad-spectrum efficacy against influenza viruses. This compound is valuable for research applications focused on viral suppression and the development of antiviral therapeutic strategies. -
HIV-1 Nef Binder, IKZF1 Modulator
FC-14369 is a PROTAC degrader that selectively targets the HIV-1 Nef protein, exhibiting a DC50 value of 160 nM. By engaging both Nef and the Cereblon E3 ubiquitin ligase, FC-14369 facilitates the ubiquitination and subsequent proteasomal degradation of Nef, leading to the restoration of CD4 and MHC-I expression on the cell surface and effectively inhibiting HIV-1 replication. This compound is valuable for research focused on HIV infection and AIDS, advancing understanding of therapeutic strategies in viral infections. -
PROTAC Degrader
FC-14367 is a PROTAC degrader that selectively targets the HIV-1 Nef protein. It facilitates the formation of a ternary complex by simultaneously binding to Nef and Cereblon E3 ubiquitin ligase, leading to the ubiquitination and subsequent proteasomal degradation of Nef. This process restores the surface expression of CD4 and MHC-I molecules while effectively inhibiting HIV-1 replication. FC-14367 is valuable for research focused on HIV infection and AIDS pathogenesis. -
eDHFR PROTAC
PROTAC eDHFR Degrader-2 selectively targets Escherichia coli dihydrofolate reductase (eDHFR) for degradation. By utilizing a PROTAC mechanism, this compound efficiently promotes the degradation of eDHFR-tagged proteins, making it a valuable tool for studies in protein regulation and degradation pathways. Its ability to modulate protein levels can aid in the investigation of various biological processes and contribute to the development of therapeutic strategies. -
CCR2 PROTAC Degrader
LUF7996 is a potent CCR2 PROTAC degrader that selectively targets and degrades CCR2 with a DC50 value of 2.6 μM. This compound effectively engages with the E3 ligase cereblon, promoting sustained and concentration-dependent degradation of CCR2 via the lysosomal pathway. LUF7996 is particularly valuable for research applications involving the inhibition of monocyte migration in vitro, facilitating studies in inflammation and immune response modulation. -
α1A-AR Degrader
α1A-AR Degrader 9c is a selective, reversible degrader specifically targeting the α1A-adrenergic receptor (α1A-AR) through the proteasomal degradation pathway. It demonstrates significant biological activity, inhibiting the proliferation of PC-3 cells with an IC50 value of 6.12 μM. This compound is valuable for research applications in prostate cancer, providing insights into the therapeutic potential of α1A-AR degradation in oncology studies. -
PROTAC BRD4 Degrader
L134 is a potent PROTAC BRD4 degrader that targets BRD4 for ubiquitination and subsequent degradation via the ubiquitin-proteasome pathway, demonstrating a DC50 value of 7.36 nM. This compound operates in a DCAF11-dependent manner, making it a valuable tool for studying BRD4-related signaling and therapeutic applications in cancer and other diseases. As a versatile reagent, L134 supports research in targeted protein degradation and the modulation of gene expression pathways. -
p300/CBP Degrader
MJP6412 is a selective degrader of the histone acetyltransferases p300 and CBP, exhibiting DC50 values of 1.6 nM and 1.2 nM, respectively. This compound effectively induces degradation of these proteins, thereby modulating acetylation levels in cells. MJP6412 is particularly relevant in cancer research, providing insights into the role of p300 and CBP in oncogenic processes and potential therapeutic interventions. -
PROTAC KDM5B Degrader
GT-653 is a PROTAC degrader targeting lysine-specific demethylase 5B (KDM5B). It efficiently induces degradation of KDM5B by 68.35% at a concentration of 10 μM through a ubiquitin proteasome-dependent mechanism. This compound elevates H3K4me3 levels and activates type-I interferon signaling pathways in prostate cancer cells, specifically in the 22RV1 cell line. Research applications include studying KDM5B's role in cancer biology and evaluating potential therapeutic strategies that involve epigenetic modulation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-12 is a CRBN-recruiting PROTAC designed to selectively degrade the EZH2 protein, exhibiting an IC50 of 3.90 nM for EZH2 and an IC50 of 5.24 μM for EZH1. This compound facilitates targeted protein degradation, making it a valuable tool for research focused on epigenetic regulation and cancer biology. Its ability to modulate the expression of key oncogenic factors positions it as a significant reagent for therapeutic investigations targeting EZH2-dependent pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-24 is an innovative molecule designed to target EZH2 by utilizing a PROTAC-mediated degradation mechanism. This compound exhibits potent EZH2 methyltransferase inhibitory activity, facilitating the selective degradation of the EZH2 protein. Research applications include studies on epigenetic regulation and therapeutic strategies for cancers with aberrant EZH2 activity. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-30 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2) with an IC50 of 6.22 μM in SU-DHL-6 cells. This compound is instrumental in research applications focusing on diffuse large B-cell lymphoma by promoting the degradation of EZH2 and thereby modulating epigenetic regulation. The inclusion of ligands for both EZH2 and MDM2, coupled with a linker, facilitates targeted protein degradation and offers a valuable tool for investigating therapeutic strategies in cancer biology. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-43 is a targeted PROTAC protein degrader that specifically degrades the EZH2 protein, exhibiting an IC50 of 21.73 μM in SU-DHL-6 cells. This compound is valuable for investigating the role of EZH2 in lymphoma research and understanding its mechanistic function in histone methylation. The dual ligand design incorporates a histone methyltransferase ligand and a VHL ligand, promoting efficient substrate recognition and recruitment for proteasomal degradation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-17 is a selective protein degrader that targets the enhancer of zeste homolog 2 (EZH2). This compound demonstrates significant antiproliferative activity, with an IC50 of 18.32 μM in lymphoma cell lines. PROTAC EZH2 Degrader-17 is a valuable tool for investigating EZH2-related pathologies and provides insights into the therapeutic potential of protein degradation in cancer research. -
EZH2 Ligand
EZH2 ligand-3 functions as a ligand targeting the Enhancer of Zeste Homolog 2 (EZH2) protein. This compound plays a crucial role in the synthesis of PROTAC EZH2 Degrader-35, facilitating the selective degradation of EZH2 in cellular models. It is valuable for research applications focused on epigenetic regulation and targeted protein degradation strategies. -
EZH2 PROTAC
PROTAC EZH2 Degrader-26 is a targeted proteolysis-targeting chimera (PROTAC) designed to specifically degradation of the enhancer of zeste homolog 2 (EZH2). This compound demonstrates a potent inhibitory activity with an IC50 of 5.80 nM against EZH2, alongside micromolar-level activity against EZH1, with an IC50 of 0.06 μM. PROTAC EZH2 Degrader-26 is suitable for research applications involving epigenetic regulation, cancer biology, and studies aimed at understanding histone methylation processes.
