Catalog No.
Product Name
Application
Product Information
Citations
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Aurora A PROTAC Degrader
PROTAC Aurora A Degrader-1 is a selective degrader that targets Aurora A, effectively forming a ternary complex with AURKA and CRBN. This compound demonstrates potent biological activity, inducing degradation of AURKA, lowering MYCN levels, and promoting DNA damage and apoptosis in cancer cells. With DC50 values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively, it exhibits significant antiproliferative effects and is valuable for research on neuroblastoma and small cell lung cancer. -
BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-21 is a targeted PROTAC that degrades the BRD4 protein through the induction of ubiquitination, achieving an IC50 of 59 nM. This compound effectively leads to BRD4 degradation via the proteasome pathway, and demonstrates moderate affinity for recombinant HSP90α with an IC50 range of 100-1000 nM. In preclinical studies, PROTAC BRD4 Degrader-21 has been shown to induce apoptosis in cancer cells and inhibit tumor growth in xenograft mouse models, making it a valuable tool for research into acute myeloid leukemia and diffuse large B-cell lymphoma. -
KRASG12D PROTAC Degrader
PROTAC K-Ras Degrader-5 is a cereblon-based PROTAC specifically designed to target KRASG12D, achieving a DC50 of less than 100 nM. This reagent facilitates the recruitment of KRASG12D to the cereblon E3 ubiquitin ligase complex, leading to its ubiquitination and proteasomal degradation. As a result, it effectively reduces pERK levels and inhibits the proliferation of cancer cells. PROTAC K-Ras Degrader-5 also enhances caspase 3/7 activity and cleaved PARP levels, indicative of apoptosis, in pancreatic cancer models. This compound is a valuable tool for researching both pancreatic and colorectal cancer. -
Multiple Target PROTAC
GT19630 is a multiple target PROTAC designed to degrade c-MYC, CK1α, GSPT1, and IKZF1/2/3 proteins. This compound effectively targets and reduces the levels of these proteins in various tumor cell lines, making it a valuable tool for studying diseases characterized by high c-MYC expression, including cancer, cardiovascular disorders, cerebrovascular diseases, and viral infections. Researchers can utilize GT19630 to further investigate the therapeutic potential of protein degradation in relevant biological contexts. -
IKZF2/CK1α Molecule Glue
DEG-35 is a CRBN-dependent dual degrader targeting IKZF2 and CK1α, exhibiting DC50 values of 1.4 nM and 4.4 nM, respectively. This compound activates the p53 apoptosis pathway, highlighting its potential in promoting cell death. DEG-35 serves as a valuable tool for research focused on Acute Myeloid Leukemia (AML), providing insights into targeted degradation strategies for therapeutic applications. -
CK1α molecular glue
dCK1α-2 is an orally active CK1α molecular glue degrader that targets proteins involved in the p53 signaling pathway. This compound demonstrates significant anti-tumor efficacy in preclinical mouse models and promotes the expression of p53-related genes, making it a valuable tool for research on cancer biology and therapeutic interventions aimed at restoring p53 function. Its mechanism of action provides insights into targeted degradation strategies in cancer treatment. -
CK1α Molecular Glue Degrader
QXG-6442 is a CK1α molecular glue degrader that effectively targets and degrades CK1α with a DC50 of 5.7 nM and a Dmax of 90%. This compound demonstrates significant antiproliferative effects in the MOLM-14 cell line, making it a valuable tool for research into the modulation of CK1α activity and its implications in various biological processes and diseases. -
IKZF1/3 And CSNK1A1 Molecular Glue Degrader
MI-2-80 is a molecular glue degrader that specifically targets IKZF1 and IKZF3, as well as CSNK1A1. This compound facilitates the binding of these proteins to the cereblon (CRBN) E3 ubiquitin ligase, promoting their subsequent ubiquitination and proteasomal degradation. MI-2-80 is valuable for research applications focused on understanding the functional roles of IKZF proteins and their involvement in various pathologies, including hematological malignancies. -
HPK1 PROTAC Degrader
PROTAC HPK1 Degrader-5 is a highly potent and orally bioavailable PROTAC that targets HPK1 for degradation (DC50 = 5.0 nM; Dmax ≥ 99%). This compound effectively inhibits SLP76 phosphorylation and promotes ERK pathway activation, leading to increased release of IL-2 and IFN-γ. It demonstrates the capability to counteract immunosuppressive signals induced by PGE2, NECA, or TGF-β. Additionally, PROTAC HPK1 Degrader-5 has shown efficacy in inhibiting tumor growth in MC38 syngeneic mouse models, making it a valuable tool for research in tumor immunotherapy, particularly in colorectal cancer. -
IRAK4 PROTAC Degrader
PROTAC IRAK4 degrader-14 is an orally active degrader targeting IRAK4 with a DC50 of 2.4 nM. It functions by selectively degrading IRAK4, thereby inhibiting pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. This compound has significant relevance in research focused on inflammatory diseases, particularly psoriasis. -
DcpS PROTAC degrader
JCS-1 is a highly potent DcpS PROTAC degrader that facilitates the targeted degradation of the DcpS enzyme through non-covalent binding via a RG3039-based warhead, while recruiting the E3 ligase VHL. This compound effectively promotes ubiquitination and subsequent degradation of DcpS at nanomolar concentrations, demonstrating a DC50 value of 87 nM in MOLM-14 cells. JCS-1 is a valuable tool for investigating acute myeloid leukemia (AML) and other genetic disorders associated with DcpS dependency. -
PTPN2 PROTAC Degrader
PROTAC PTPN2 degrader-2 TFA is a highly potent PTPN2 degrader with a DC50 of less than 50 nM. This compound facilitates targeted protein degradation, providing a valuable tool for investigating the role of PTPN2 in cancer and metabolic disorders, including colon cancer. Its application in research can enhance understanding of disease mechanisms and therapeutic interventions. -
PTPN2 PROTAC Degrader
PROTAC PTPN2 Degrader-2 is a selective PTPN2 degrader that effectively induces targeted degradation of the PTPN2 protein, demonstrating a DC50 of less than 50 nM. This compound is instrumental for exploring cellular mechanisms within cancer and metabolic disorders, particularly in the context of colon cancer research. Its utility in protein knockdown enables innovative studies into therapeutic strategies for disease intervention. -
STAT6 PROTAC Degrader
PROTAC STAT6 degrader-1 is a targeted protein degradative compound designed to modulate STAT6 activity through the recruitment of E3 ligase CRBN. With a DC50 of less than 1 nM, this PROTAC showcases potent efficacy in STAT6 degradation. It is particularly relevant for research on inflammation and various cancer types, providing a valuable tool for exploring STAT6's role in pathophysiology and therapeutic responses. -
STAT3 PROTAC Degrader
SD-436 is a selective and potent degrader of STAT3, functioning through the PROTAC mechanism with a DC50 of 0.5 μM and an IC50 of 19 nM for STAT3. It promotes the ubiquitination and subsequent degradation of STAT3, leading to significant tumor regression. This reagent is applicable in cancer research, including studies focused on leukemia and lymphoma. -
PTP1B/TC-PTP PROTAC Degrader
DU-14 is a potent dual degrader targeting PTP1B and TC-PTP via the PROTAC mechanism. It demonstrates remarkable selectivity with IC50 values of 24.2 nM and 30.1 nM for PTP1B and TC-PTP phosphatase activity, respectively. DU-14 enhances interferon-gamma signaling, promotes T cell activation, and exhibits anti-tumor properties, making it a valuable tool for cancer immunology research and the study of immune modulation. -
STAT6 PROTAC Degrader
PROTAC STAT6 degrader-3 is a highly potent degrader targeting STAT6, exhibiting a DC50 of less than 1 nM. This compound facilitates the targeted degradation of STAT6, making it a valuable tool for investigating allergic and inflammatory diseases as well as various cancers. Its application in research can provide insights into the role of STAT6 in disease pathways and therapeutic interventions. -
STAT3 PROTAC Degrader
SD-2301 is a selective STAT3 PROTAC degrader that targets and induces the degradation of STAT3 while preserving the expression of other STAT family members such as STAT1, STAT2, STAT4, STAT5, and STAT6. It has demonstrated anti-tumor efficacy in B16F10-bearing mouse models, making it a valuable tool for cancer research. This compound can be utilized in studies focused on the modulation of STAT3 pathways and the development of targeted therapies. -
STAT6 Molecular Glue
STAT6 degrader-1 is a bifunctional molecular glue that specifically targets STAT6 by recruiting E3 ubiquitin ligase, leading to the proteasomal degradation of the protein. This degradation mechanism allows for the modulation of STAT6 activity, making it a valuable tool in the study of cancer biology, inflammatory diseases, and colorectal cancer. Researchers can utilize STAT6 degrader-1 to explore therapeutic strategies aimed at disrupting STAT6 signaling pathways. -
PROTAC STAT6 Degrader
PROTAC STAT6 Degrader-2 is a potent bifunctional degrader that specifically targets signal transducer and activator of transcription 6 (STAT6). It demonstrates high efficiency with a DC50 of 1-10 nM in human peripheral blood mononuclear cells (PBMC) and less than 100 nM in HEK293-HIBiT-STAT6 cells. This compound is ideal for research applications related to STAT6-mediated diseases, facilitating the study of its role in various biological processes. -
STAT6 PROTAC Degrader
PROTAC STAT6 degrader-4 is a potent STAT6 PROTAC degrader with a DC50 of 0.04 nM. It functions by inducing the ubiquitination and subsequent degradation of STAT6, making it an important tool for investigating immune-related diseases. This compound is valuable for researchers studying the role of STAT6 in immune signaling pathways and therapeutic interventions. -
PROTAC STAT3 Degrader
S3D5 is a selective PROTAC degrader specifically targeting STAT3, with a dissociation constant (KD) of 4.35 μM. It effectively induces degradation of the STAT3 protein in HepG2 cells, demonstrating minimal impact on other STAT proteins. This degradation is mediated via the ubiquitin-proteasome system, contributing to its potent anti-proliferative effects in hepatocellular carcinoma by activating the p53 pathway. S3D5 serves as a valuable tool for research focused on the mechanisms underlying hepatocellular carcinoma. -
PROTAC ERK5 Degrader
PPM-3 is a potent and selective PROTAC degrader of ERK5, exhibiting an IC50 of 62.4 nM. While PPM-3 does not directly affect tumor cell proliferation, it modulates tumor development by impacting macrophage differentiation. This compound may serve as a valuable tool for investigating the role of ERK5 degradation in cancer biology and immune modulation. -
PROTAC GPX4 Degrader
PROTAC GPX4 degrader-5 is a selective degrader targeting GPX4, with a DC50 of 28 nM. This compound effectively induces ferroptosis and enhances reactive oxygen species (ROS) levels while exhibiting low toxicity to normal cells. PROTAC GPX4 degrader-5 demonstrates significant anti-proliferative effects in various tumor cell lines, making it a valuable tool for cancer research. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-35 is a selective degrader targeting SMARCA2 with a DC50 potency of less than 0.1 μM. This compound exhibits significant anticancer activity by regulating cell proliferation and growth, primarily through mechanisms of cell cycle arrest and inhibition of DNA replication in SMARCA4-deleted cancer cells. It is a valuable tool for research focused on targeted protein degradation and its implications in cancer therapy. -
Molecular Glue
OPB-171775 is an orally active molecular glue that targets phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). This compound induces SLFN12-mediated RNase activity, leading to subsequent cell death. Additionally, OPB-171775 activates the GCN2 signaling pathway associated with SLFN12, showcasing its significant efficacy in combating gastrointestinal stromal tumors. Researchers can utilize OPB-171775 to explore pathways in cancer biology and investigate the therapeutic potential of molecular glues in tumor treatment. -
FKBP51 Degrader, VHL Binder
SelDeg51 is a selective PROTAC degrader targeting FKBP51 with a Kd value of 18 nM and a maximum degradation efficacy (Dmax) of 90%. It facilitates the proteasomal degradation of FKBP51 through the formation of a ternary complex with FKBP51 and VHL, effectively reactivating glucocorticoid receptor signaling. SelDeg51 is particularly relevant for research in stress-related mental disorders, chronic pain, and obesity. -
FKBP12F36V PROTAC Degrader
dTAGV-1 is a selective proteolysis-targeting chimera (PROTAC) degrader designed to target FKBP12F36V-tagged proteins. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studying protein turnover and function. Its application is particularly relevant in cellular and molecular biology research, facilitating the investigation of protein interactions and therapeutic targets. -
PROTAC FKBP12 Degrader
10-SLF is a PROTAC FKBP12 degrader that facilitates the formation of a ternary complex between FKBP12 and the mutant E3 ligase FBXW7-R465C. This compound promotes the FBXW7-R465C-mediated proteasomal degradation of FKBP12, selectively lowering FKBP12 levels in cells harboring the FBXW7-R465C mutation. 10-SLF is valuable for studying protein degradation pathways and the role of FKBP12 in various biological contexts. -
Nucleoprotein PROTAC Degrader
KB03-SLF is an electrophilic PROTAC degrader targeting DCAF16 to facilitate the degradation of the nuclear protein FKBP12. This compound serves as a valuable tool in cancer research, enabling the investigation of protein homeostasis and degradation pathways. KB03-SLF’s unique structure incorporates specific ligands that enhance its efficacy as a degradative agent, making it a significant asset for studies focused on targeted protein elimination. -
FKBP12 PROTAC Degrader
RAFKBP12 is a PROTAC degrader that specifically targets FKBP12, utilizing the CAP-TAC strategy to facilitate proteasome-dependent degradation. This compound operates independently of E3 ubiquitin ligases and protein ubiquitination, demonstrating its innovative mechanism of action. RAFKBP12 serves as a valuable tool for research in protein degradation pathways and therapeutic applications related to FKBP12 modulation. -
LRRK2 PROTAC Degrader
PROTAC LRRK2 Degrader-1 is a targeted protein degrader that selectively engages leucine-rich repeat kinase 2 (LRRK2), exhibiting an IC50 value of less than 10 nM. This compound is designed for the study of LRRK2-mediated pathways and offers significant potential for advancing research on Parkinson's disease. Its ability to induce targeted degradation makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders associated with LRRK2 dysregulation. -
LRRK2 PROTAC Degrader
ROTAC LRRK2 degrader-1 is a potent PROTAC degrader targeting LRRK2, a protein associated with neurodegenerative diseases. This compound facilitates the targeted degradation of LRRK2, which is implicated in the pathogenesis of Parkinson’s Disease. ROTAC LRRK2 degrader-1 can be utilized in research to investigate LRRK2-related biological pathways and therapeutic interventions for Parkinson’s Disease and other associated disorders. -
LRRK2 PROTAC Degrader
PROTAC LRRK2 Degrader-2 is designed to target LRRK2 through a PROTAC mechanism, exhibiting a DC50 of 0.14 nM. This compound effectively recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, facilitating targeted ubiquitination and subsequent proteasomal degradation of LRRK2. It serves as a valuable tool for research focused on Parkinson's disease and the study of LRRK2-related pathways. -
ADC/PROTAC Linkers
Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br serves as a versatile drug-linker conjugate for antibody-drug conjugate (ADC) applications. This reagent enables the synthesis of conjugates targeting the CD40 antigen, facilitating the development of targeted therapies. Its unique structure supports the design of PROTACs and other innovative bio-conjugates, contributing to advances in cancer research and immunotherapy. -
Chk1 PROTAC Degrader
PROTAC Chk1 degrader-1 is a selective Chk1-targeting PROTAC that facilitates the recruitment of the Cereblon E3 ligase to promote ubiquitination and subsequent proteasomal degradation of Chk1. This compound effectively induces Chk1 degradation in malignant melanoma cells, demonstrating a robust biological activity without exhibiting a hook effect. PROTAC Chk1 degrader-1 is suitable for research applications focused on understanding the role of Chk1 in malignant melanoma and exploring targeted degradation strategies in cancer therapy. -
Molecular Glue BRD4 Degrader
BRD4 degrader-1 is a monovalent, covalent molecular glue that specifically targets BRD4, a key regulator in various cellular processes. By engaging DCAF16, an E3 ubiquitin ligase, this compound facilitates the degradation of both long and short isoforms of BRD4 within the cellular context. Its mechanism of action makes BRD4 degrader-1 a valuable tool for research applications aimed at understanding and manipulating BRD4-related pathways in cancer and other diseases. -
BRD4 Degrader
MMH1 is a novel BRD4 molecular glue degrader that effectively recruits the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2). This targeted degradation mechanism allows for the selective reduction of BRD4 levels, which is crucial for studying its role in various biological processes. MMH1 is particularly useful in research applications focusing on cancer biology and epigenetic regulation, enabling the exploration of therapeutic strategies targeting BRD4-associated pathways. -
BRD4 Degrader
BRD4 degrader-3 is a selective bromodomain-containing protein 4 (BRD4) degrader, showcasing potent activity with IC50 values of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. This compound employs the PROTAC technology to facilitate targeted degradation of BRD4. Additionally, it features an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for chemical biology applications in studying BRD4-related pathways and functions. -
BRD9 PROTAC Degrader
dBRD 9-A is a selective BRD9 PROTAC degrader that targets the E3 ubiquitin ligase CRBN for the near-complete degradation of BRD9. This compound disrupts BRD9 chromatin binding on a genome-wide scale, leading to downregulation of oncogenic transcriptional programs driven by SS18-SSX and the depletion of GBAF complex members from SS18-SSX complexes. dBRD 9-A also induces cell cycle arrest and promotes apoptosis in synovial sarcoma cells, making it a valuable tool for research focused on synovial sarcoma. -
PROTAC BRD4 Degrader
TD-428 is a potent PROTAC designed to target and degrade the BRD4 protein via its connection to Cereblon ligands. With a DC50 value of 0.32 nM, TD-428 exhibits high specificity for BRD4 degradation. This compound combines TD-106, a ligand for CRBN, with JQ1, a BET inhibitor, facilitating effective degradation of BET proteins. TD-428 is valuable for research applications involving cancer biology and epigenetic regulation. -
BRD4 PROTAC Degrader
L1BC8 is a BRD4 PROTAC degrader that exhibits significant anticancer activity through targeted degradation of the BRD4 protein. This compound functions as a drug-linker conjugate for antibody-drug conjugates (ADCs), enabling the synthesis of BRD4-degrader antibody conjugates. The resulting conjugates demonstrate potent, antigen-dependent BRD4 degradation and antiproliferative effects in cellular assays, making L1BC8 a valuable tool for cancer research and therapeutic development. -
Molecular Glue
AMPTX-1 is a molecular glue that functions as a selective, reversibly covalent degrader of BRD9, promoting its recruitment to the E3 ubiquitin ligase DCAF16. This compound exhibits significant activity in inducing proteasomal degradation of BRD9, making it a valuable tool for research involving chromatin regulation and cellular signaling pathways. AMPTX-1 can be utilized in studies focused on targeted protein degradation and the modulation of BRD9-related biological processes. -
BRD9 Degrader
PROTAC BRD9 Degrader-7 is a selective BRD9-targeting PROTAC that induces BRD9 degradation through the ubiquitin-proteasome pathway, demonstrating a DC50 of 1.02 nM. This compound effectively inhibits cell proliferation in MV4-11 acute myeloid leukemia cells, making it a valuable tool for research in hematologic malignancies and related disorders. Its capacity to modulate BRD9 levels positions it as a promising candidate for studies aimed at understanding the role of this protein in cancer biology. -
SMARCA2/SMARCA4 Degrader
G-6599 is a monovalent degrader targeting SMARCA2 and SMARCA4, known for its role in regulating chromatin remodeling. This compound covalently binds to a specific cysteine residue in the E3 ligase FBXO22, facilitating the formation of a ternary complex with SMARCA2 and SMARCA4, leading to their efficient degradation through the ubiquitin-proteasome pathway. G-6599 is relevant for research in androgen-dependent prostate cancer and mutant non-small cell lung cancer, providing valuable insights into therapeutic interventions. -
SMARCA2 Degrader
YDR1 is a potent SMARCA2 degrader that functions as a PROTAC, exhibiting a DC50 of 7.7 nM. This compound is particularly relevant for research into SMARCA4 mutant cancers, facilitating targeted degradation of SMARCA2. It offers valuable insights into the molecular mechanisms underlying these cancers and aids in the development of novel therapeutic strategies. -
PROTAC BRD4 Degrader
CCW 28-3 is a PROTAC that specifically targets BRD4 for degradation through a proteasome- and RNF4-dependent mechanism. This compound facilitates the targeted removal of BRD4, a critical regulator of gene expression linked to various cancers. Its application in research includes studying the role of BRD4 in transcriptional regulation and therapeutic interventions aimed at modulating oncogenic pathways. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-9 is a bifunctional degrader targeting the BRD4 protein through a ligase-dependent mechanism using von Hippel-Lindau. It exhibits potent biological activity, effectively degrading BRD4 in PC3 prostate cancer cells with a DC50 of 0.86 nM when conjugated with STEAP1 antibodies and 7.6 nM with CLL1 antibodies. This compound is valuable for research into targeted protein degradation and therapeutic strategies against BRD4-mediated oncogenic processes. -
CBP/p300 PROTAC Degrader
Thalidomide-NH-CBP/p300 ligand 2 is a PROTAC-based degrader that targets the CBP and p300 proteins. This compound facilitates the selective degradation of these transcriptional coactivators, which are implicated in various cancers and other diseases. Its application in research includes the elucidation of the roles of CBP and p300 in transcriptional regulation and therapeutic development for conditions influenced by these proteins. -
PROTAC ERRα Degrader
PROTAC_ERRα is a targeted degrader of the estrogen-related receptor alpha (ERRα), employing a proteolysis-targeting chimera (PROTAC) mechanism for enhanced specificity. This compound induces over 80% proteasomal degradation of ERRα in MCF-7 cells, with a DC50 value of 100 nM. PROTAC_ERRα serves as a valuable tool for investigating the biological functions of ERRα in cancer research and for therapeutic development aimed at ERRα-related pathways.
