Catalog No.
Product Name
Application
Product Information
Citations
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Molecular Glue
(R)-CR8 trihydrochloride is a potent inhibitor of CDK1, CDK2, CDK5, CDK7, and CDK9, functioning as a molecular glue degrader that targets cyclin K. With inhibitory activity characterized by low nanomolar IC50 values, it effectively induces apoptosis while exhibiting neuroprotective properties. This compound is suitable for research applications in cancer biology and neurodegenerative disease studies. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-PEG4-NHS ester is a PEG-based linker designed for the synthesis of PROTACs (Proteolysis Targeting Chimeras). It functions as a ligand for E3 ligases, facilitating targeted protein degradation. This compound is instrumental in chemical biology research aimed at exploring pathways involved in protein turnover and has applications in developing therapeutics for diseases driven by dysregulated protein levels. -
Molecular Glues
(S)-Thalidomide is the S-enantiomer of Thalidomide, functioning as a molecular glue. It exerts significant biological activities, including immunomodulation, anti-inflammation, antiangiogenesis, and pro-apoptosis. This compound induces teratogenic effects through its interaction with cereblon (CRBN), making it a valuable tool for research into cell signaling pathways and developmental biology. -
E3 Ligase Ligand-Linker Conjugate
Biotin-Thalidomide is a biotinylated derivative of Thalidomide designed to selectively bind to the cereblon (CRBN) E3 ubiquitin ligase. This compound serves as a crucial ligand-linker conjugate for the development of proteolysis-targeting chimeras (PROTACs). Biotin-Thalidomide facilitates targeted proteasomal degradation of specific proteins, making it a valuable tool for research in targeted protein degradation and molecular biology. Its utility extends to applications in drug discovery and therapeutic development. -
CDK4/6 PROTAC Degrader
PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies. -
CDK12/CCNK Molecular Glue
NCT02 is a molecular glue degrader that targets CDK12 through the E3 ubiquitin ligase DDB1, resulting in the ubiquitination and subsequent proteasomal degradation of its partner protein CCNK. This mechanism leads to the downregulation of CDK12, inhibiting its downstream signaling pathways. NCT02 exhibits significant biological activity by inducing apoptosis in tumor cells, arresting the cell cycle, and selectively inhibiting the proliferation of colorectal cancer cells with TP53 mutations or belonging to the CMS4 molecular subtype. Additionally, NCT02 demonstrates potential in suppressing tumor growth in both in vitro and in vivo models. -
PROTAC Linkers
Thalidomide-O-amido-PEG4-azide is a PEG-based linker designed for the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound possesses an azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with alkyne-containing molecules. Additionally, it can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with DBCO or BCN functionalized compounds. This makes Thalidomide-O-amido-PEG4-azide a versatile tool in targeted protein degradation applications and chemical biology research. -
CCND1/CDK4 PROTAC Degrader
CPD-10 is a targeted CCND1 and CDK4 PROTAC degrader that effectively promotes the degradation of these proteins. Exhibiting significant anti-proliferative activity, CPD-10 induces apoptosis in cancer cell lines. It decreases the expression levels of cyclin D1, cyclin D3, CDK4, and phosphorylated Rb at serines 5807 and 811 in a dose-dependent manner, making it a valuable tool for research in cancer biology and therapeutic applications targeting cell cycle regulation. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 9 is a CRBN-based PROTAC designed to specifically target and degrade the mutant forms of the epidermal growth factor receptor (EGFR), particularly EGFRL858R/T790M/C797S. It demonstrates potent degradation activity with a DC50 of 10.2 nM and a Kd of 240.2 nM, effectively eliminating EGFR mutants while leaving wild-type EGFR unaffected. This compound serves as a valuable tool in cancer research, particularly in studies focused on targeted therapies for EGFR-driven malignancies. -
Androgen Receptor PROTAC Degrader
PROTAC AR Degrader-8 is an androgen receptor (AR) PROTAC degrader that effectively induces degradation of full-length AR (AR-FL) with DC50 values of 0.018 μM in 22Rv1 cells and 0.14 μM in LNCaP cells, as well as degrading the AR-V7 variant with a DC50 of 0.026 μM in 22Rv1 cells. This compound exhibits potent inhibition of cancer cell proliferation, with IC50 values of 0.038 μM and 1.11 μM in 22Rv1 and LNCaP cells, respectively. PROTAC AR Degrader-8 induces G2/M cell cycle arrest and promotes apoptosis in 22Rv1 cells, demonstrating significant anticancer efficacy in both murine and zebrafish models. It is a valuable tool for investigating mechanisms underlying prostate cancer and castration-resistant prostate cancer. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-PEG2-C2-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that features a Thalidomide-derived cereblon ligand combined with a two-unit polyethylene glycol (PEG) linker. This compound is designed for use in proteolysis-targeting chimera (PROTAC) applications, facilitating targeted protein degradation by promoting the interaction between the target protein and the E3 ubiquitin ligase. Its unique structure enables researchers to explore novel therapeutic strategies in cellular and molecular biology studies. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-O-PEG4-azide is an E3 ligase ligand-linker conjugate featuring a Thalidomide-based cereblon ligand. It serves as an essential component in PROTAC technology, facilitating targeted protein degradation. This compound is a versatile click chemistry reagent, containing an azide group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules, as well as strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN moieties. These properties make it valuable for various bioconjugation applications in chemical biology and therapeutic research. -
Molecular Glue Degrader
VNPP433-3β is an orally active molecular glue degrader that targets androgen receptor (AR) and its splice variants (AR-Vs), as well as MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound induces apoptosis in cells and demonstrates significant inhibition of tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β is a valuable tool for investigating mechanisms in castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
PROTAC CDK4/6 degrader
HEMTAC CDK4/6 degrader 1 is a PROTAC designed to target CDK4 and CDK6 through a dual-ligand approach involving HSP90. This compound effectively induces the degradation of CDK4/6 in B16F10 melanoma cells, leading to cell cycle arrest at the G0/G1 phase and subsequent apoptosis. It serves as a vital tool for cancer research, particularly in elucidating mechanisms of CDK4/6 regulation and their role in tumor progression. Additionally, HEMTAC CDK4/6 degrader 1 features an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds for advanced applications in chemical biology. -
PROTAC ERα Degrader
PROTAC ERα Degrader-4 is a selective degrader targeting estrogen receptor alpha (ERα) through the PROTAC mechanism. It exhibits potent inhibitory activity with a Ki value of 5.08 μM, effectively leading to the degradation of ERα in both Tamoxifen-sensitive and resistant ER+ breast cancer cells, as well as in ERα-mutated breast cancer cell lines. Additionally, PROTAC ERα Degrader-4 induces apoptosis, making it a valuable tool for cancer research aimed at understanding and combating ERα-driven malignancies. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-Piperazine 5-fluoride is a synthesized compound that functions as an E3 ligase ligand-linker conjugate, featuring the Thalidomide-derived cereblon ligand. This reagent is designed for applications in PROTAC (Proteolysis Targeting Chimeras) technology, facilitating targeted protein degradation. Its unique structure allows for effective modulation of protein levels in experimental settings, making it a valuable tool in the study of cellular processes and therapeutic development. -
PROTAC HDAC8 Degrader
SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation. -
E3 ligase ligand-linker conjugate
Thalidomide-4-O-C6-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that plays a critical role in the targeted protein degradation (PROTAC) system, specifically in dTAG-13 applications. This compound is utilized for its ability to degrade FKBP12F36V and bromodomain and extraterminal (BET) proteins, facilitating the modulation of various cellular processes. Its utility in research allows for advancements in understanding protein function and the development of therapeutic strategies. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-NH-PEG3-propionic acid is an E3 ligase ligand-linker conjugate that combines the thalidomide-derived cereblon ligand with a three-unit polyethylene glycol (PEG) linker. This compound is utilized in PROTAC technology to facilitate targeted protein degradation by engaging E3 ligases. Its design enables efficient delivery of the cereblon ligand to specific cellular targets, making it valuable for research in protein homeostasis and therapeutic applications in cancer and other diseases. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-NH-PEG4-COOH is an E3 ligase ligand-linker conjugate designed to facilitate the synthesis of dCBP-1. This compound acts as a potent and selective heterobifunctional degrader targeting the p300/CBP proteins, enabling targeted protein degradation for research applications in cellular processes, epigenetics, and cancer biology. Researchers can utilize this conjugate to explore pathways and mechanisms regulated by p300/CBP, advancing the understanding of transcriptional regulation and related therapeutic strategies. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-C6-COOH is an E3 ligase ligand-linker conjugate that combines the Thalidomide-derived cereblon ligand with a carbon chain linker, facilitating the development of PROTAC (Proteolysis Targeting Chimera) molecules. This compound engages the cereblon protein, effectively modulating protein degradation pathways. Thalidomide-O-C6-COOH is suitable for research applications focused on targeted protein degradation and exploring the therapeutic potential of PROTAC-based strategies in various diseases. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-4-O-C5-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that utilizes the Thalidomide-based cereblon ligand in conjunction with a specialized linker designed for PROTAC (Proteolysis Targeting Chimeras) applications. This compound facilitates targeted protein degradation, enabling the selective modulation of protein levels within cells. It is valuable for researchers investigating protein homeostasis, targeted therapy mechanisms, and the development of novel therapeutic strategies. -
PROTAC eEF2K Degrader
PROTAC eEF2K degrader-1 is a small molecule designed to target and induce degradation of the elongation factor 2 kinase (eEF2K). This compound has been shown to effectively promote apoptosis in MDA-MB-231 cancer cells, demonstrating its potential in cancer research. The mechanism of action involves the targeted elimination of eEF2K, providing a valuable tool for studying the role of this kinase in cellular processes and therapeutic applications. -
CCNK Molecular Glue Degrader
ZLY025 is a potent CCNK molecular glue degrader with a DC50 of 42.7 nM. This compound demonstrates significant antiproliferative effects across a range of tumor cell lines, exhibiting IC50 values between 0.08 and 2.45 μM. ZLY025 is capable of inducing apoptosis and causing G1 phase cell cycle arrest, making it a valuable tool for cancer research, particularly in the study of lung cancer. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that targets cereblon, a substrate receptor in the CRL4 ubiquitin-proteasome system. This compound facilitates the development of proteolysis-targeting chimeras (PROTACs), offering a novel approach for selective protein degradation in various biological research applications. Its unique structure allows for the effective modulation of protein levels, making it a valuable tool in cellular biology and therapeutic research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-C5-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that combines a Thalidomide-derived cereblon ligand with a specialized linker utilized in PROTAC technology. This compound facilitates selective protein degradation by engaging the E3 ubiquitin ligase pathway, making it a valuable tool for investigating targeted protein modulation and therapeutic applications in cancer research and other diseases. Its structural design enhances its potential in developing targeted protein degradation strategies. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-C10-COOH is an E3 ligase ligand-linker conjugate that features a Thalidomide-derived CRBN ligand. This compound is designed for use in PROTAC (proteolysis-targeting chimera) technology, enabling selective degradation of target proteins. Its biological activity is critical for research applications focused on targeted protein degradation and cellular modulation in various therapeutic contexts. -
PROTAC XPO1 Degrader
PROTAC XPO1 degrader-1 is a targeted protein degrader designed to selectively promote the degradation of XPO1. This compound demonstrates significant anti-proliferative effects, induces apoptosis, inhibits NF-κB signaling, and causes cell cycle arrest at the G1 phase. It is an important tool for researching hematological malignancies, offering insights into therapeutic strategies by modulating XPO1 levels. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4 degrader-38 is a dual-targeted PROTAC degrader designed to promote the ubiquitination and subsequent degradation of the SMARCA2 and SMARCA4 proteins. With DC50 values of 3.0 nM and 4.0 nM for SMARCA2 and SMARCA4 respectively, this compound effectively blocks the G0/G1 cell cycle phase and induces apoptosis in cancer cells. It has significant potential for use in research focused on acute myeloid leukemia (AML) and other malignancies involving these chromatin remodeling factors. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-C2-amido-C2-COOH is a ligand-linker conjugate targeting the CRBN E3 ubiquitin ligase. This compound is designed for the development of proteolysis-targeting chimeras (PROTACs), specifically facilitating the degradation of CDK2/9. It serves as a valuable tool in research focused on protein degradation pathways and the modulation of cellular processes through targeted protein elimination. -
PROTAC JAK2 Degrader
SJ1008030 is a PROTAC compound designed to selectively degrade Janus kinase 2 (JAK2). This compound exhibits potent inhibitory activity against MHH–CALL-4 cell growth, with an IC50 of 5.4 nM. SJ1008030 is valuable for research applications focusing on leukemia, facilitating the study of JAK2-related pathways and therapeutic interventions. -
PROTAC FLT3/JAK2/BRD4 Degrader
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a potent PROTAC degrader that simultaneously targets FLT3, JAK2, and BRD4, exhibiting DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It demonstrates significant antiproliferative activity against MV4;11 cells with an IC50 of 0.79 nM, inducing apoptosis in these cells. Additionally, PROTAC FLT3/JAK2/BRD4 Degrader-1 shows marked anti-tumor efficacy in MV4;11 xenograft models in NOD SCID mice. This compound is valuable for research into acute myeloid leukemia (AML). -
Target Protein Ligand-Linker Conjugates
Baricitinib 4-aminobenzoic acid TFA is a Target Protein Ligand-Linker Conjugate that features a ligand for JAK2 alongside a PROTAC linker designed to facilitate the recruitment of E3 ligases. This compound serves as a critical component in the synthesis of the PROTAC JAK2 degrader SJ1008030, enabling targeted degradation of the JAK2 protein. It is particularly relevant for research focused on JAK2-related pathways and potential therapeutic strategies against related diseases. -
Target Protein Ligand-Linker Conjugates
Baricitinib 4-aminobenzoic acid is a targeted protein ligand-linker conjugate designed for use in PROTAC (Proteolysis Targeting Chimera) applications. It features a ligand for JAK2 along with a PROTAC linker that facilitates the recruitment of E3 ligases, enabling degradation of target proteins. This compound is valuable for synthesizing PROTAC JAK2 degrader SJ1008030, advancing research in targeted protein degradation and related therapeutic strategies. -
PROTAC FGFR1/2 Degrader
DGY-09-192 is a PROTAC degrader targeting FGFR1 and FGFR2, demonstrating DC50 values of 4.35 nM and 70 nM, respectively. This compound selectively degrades both wild-type FGFR1/2 and various FGFR2 fusion proteins, such as FGFR2-PHGDH and FGFR2-OPTN. By suppressing downstream FGFR signaling, DGY-09-192 effectively reduces the phosphorylation of key targets including FRS2 Y196 and ERK1/2 T202/Y204, making it a valuable tool for investigating FGFR-driven malignancies in both in vitro and in vivo studies. -
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. -
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.
