Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.
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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
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 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.
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.
BTX161 is a thalidomide analog that functions as an effective degrader of CKIα. This compound promotes the degradation of CKIα in human acute myeloid leukemia (AML) cells, leading to enhanced activation of the DNA damage response (DDR) and p53 while simultaneously stabilizing the p53 antagonist MDM2. BTX161 serves as a valuable tool for studying the role of CKIα in cancer biology and potential therapeutic strategies targeting the DDR pathway.
(R,R)-BMS-986397 is a potent CK1α degrader, exhibiting a degradation concentration (DC50) range of 0.1-0.5 pM. This compound is instrumental in studying the role of CK1α in cellular processes and has applications in anti-leukemia research, enabling insights into targeted therapeutic strategies. Its ability to specifically degrade CK1α makes it a valuable tool for investigating CK1α-related signaling pathways in cancer biology.
TGFβRII-IN-3 is a selective degrader of the TGFβ type II receptor (TGFβ RII), exhibiting an IC50 of 4.1 μM. This compound disrupts TGFβ signaling pathways by promoting the proteolytic degradation of TGFβ RII, leading to the inhibition of endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 is a valuable tool in cancer research, offering insights into the modulation of TGFβ-mediated biological processes.
NF764 is a selective degrader of β-catenin (CTNNB1) that induces its degradation through a proteasome-dependent mechanism. By effectively lowering CTNNB1 protein levels, NF764 serves as a valuable tool for investigating the role of β-catenin in various cancer signaling pathways. This compound is essential for research aimed at understanding tumorigenesis and developing targeted cancer therapies.
Synonyms: JB301
SK2187 is a selective degrader of Aurora kinase A (AURKA) utilizing the PROTAC technology, exhibiting a DC50 of approximately 10 nM. This compound demonstrates significant growth inhibition of NGP neuroblastoma cells, with an IC50 value of 101.5 nM. SK2187 is particularly relevant for research on MYCN-amplified neuroblastoma, enabling exploration of targeted degradation pathways in cancer therapy.
dAurAB2 is a dual-targeting PROTAC designed to degrade Aurora-A and Aurora-B, demonstrating potent efficacy with DC50 values of 59 nM and 39 nM, respectively. This compound effectively reduces N-Myc protein levels in MYCN-amplified IMR32 neuroblastoma cells, making it a valuable tool for neuroblastoma research. The unique design incorporates a specific Aurora ligand and an E3 ligase ligand connected by a tailored linker, facilitating targeted degradation and advancing studies in cancer biology.
AurAP14 is a PROTAC degrader specifically targeting Aurora A, with a DC50 of 120 nM. This compound exhibits potent inhibitory effects on various tumor cell lines, showing IC50 values of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis while effectively arresting A549 cells in the S and G2/M phases of the cell cycle. Additionally, AurAP14 demonstrates significant anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR, making it a valuable tool for research focused on treating Aurora A-overexpressing non-small cell lung cancer (NSCLC).
dAURK-4 is a potent and selective degrader of Aurora A kinase (AURKA) utilizing the PROTAC (proteolysis-targeting chimera) approach. This compound induces the degradation of AURKA, leading to significant antitumor activity. dAURK-4 is ideal for research applications focused on cancer biology, particularly in studies exploring the role of AURKA in tumorigenesis and therapeutic resistance.
Out of stock
All 3 sizes
JB300 is a highly selective degrader of Aurora A, utilizing PROTAC technology with a DC50 of 30 nM. This compound demonstrates significant potential for tumor research by promoting targeted degradation of the Aurora A protein through the recruitment of E3 ligase. JB300 comprises the PROTAC target protein ligand MK-5108, an E3 ligase ligand Thalidomide-O-COOH, and a linker, enabling the efficient conjugation necessary for effective protein degradation. It is a valuable tool for investigating the role of Aurora A in cancer biology and for the development of targeted therapeutics.
PROTAC AURKA Degrader 2 is a selective degrader targeting Aurora Kinase A (AURKA), with an IC50 of 3.58 nM. It demonstrates significant selectivity for AURKA over Aurora Kinase B (AURKB), showing an IC50 of 77.2 nM. This compound effectively depletes AURKA from the mitotic spindle, making it a valuable tool for investigating the role of AURKA in cell division and for potential therapeutic applications in cancer research.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
Synonyms: Phx-3
Questiomycin A is a potent GRP78 degrader, targeting the cytoprotective endoplasmic reticulum chaperone to promote enhanced anticancer activity, particularly in conjunction with Sorafenib. Additionally, Questiomycin A exhibits antimicrobial properties and is derived from the metabolite of Pseudomonas chlororaphis HT66. This compound is valuable for research in the biological control of both cancer and plant diseases, providing insights into therapeutic strategies and molecular mechanisms.
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.
Out of stock
All 3 sizes
Dovitinib-RIBOTAC is an RNA-targeting RIBOTAC degrader that specifically binds to and facilitates the degradation of pre-miR-21. This compound exhibits significant anti-tumor activity and inhibits metastasis in breast cancer models. It serves as a valuable tool for studying the role of miR-21 in cancer biology and therapeutic development.
TDP-43 degrader-1 is a targeted degrader of TDP-43, effective in modulating its cellular distribution. This compound reduces the aggregation of TDP-43-positive HuR stress granules and facilitates the relocalization of aberrantly distributed TDP-43 from the cytoplasm to the nucleus. TDP-43 degrader-1 is a valuable tool in the research of neurodegenerative diseases, including amyotrophic lateral sclerosis and Alzheimer's disease.
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.
Out of stock
All 3 sizes
GSPT1 degrader-2 is a potent molecular glue degrader that targets GSPT1, demonstrating a DC50 of less than 30 nM. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to selectively degrade GSPT1 offers insights into the mechanisms of tumor biology and therapeutic potential in an array of malignancies.
Out of stock
All 3 sizes
And1 Degrader 1 is a targeted degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), promoting its degradation in non-small cell lung cancer (NSCLC) cells. At a concentration of 5 μM, And1 Degrader 1, in conjunction with Olaparib at 1 μM, effectively inhibits the proliferation of A549 and H460 cell lines. This compound serves as a valuable tool in cancer research, facilitating the study of And1's role in tumor progression and therapy resistance.
di-Ellipticine-RIBOTAC is a RNase recruiting chimera (RIBOTAC) that selectively targets and degrades expanded G4C2 RNA repeats (r(G4C2)exp). It binds specifically to the three-dimensional structure of r(G4C2)exp, facilitating the recruitment of endogenous ribonucleases to cleave the RNA. This compound effectively degrades the mutant C9orf72 allele, thereby reducing the production of toxic dipeptide repeat proteins (DPRs) associated with amyotrophic lateral sclerosis and frontotemporal dementia. di-Ellipticine-RIBOTAC serves as a valuable tool for investigating the molecular mechanisms underlying c9ALS/FTD pathologies.
Out of stock
All 3 sizes
di-Ellipticine-RIBOTAC TFA is a RNase recruiting chimera (RIBOTAC) degrader targeting the expanded G4C2 RNA repeat (r(G4C2)exp). It selectively binds to the three-dimensional structure of r(G4C2)exp, recruiting endogenous ribonuclease to induce cleavage and degradation of this RNA. This compound effectively reduces the levels of the toxic dipeptide repeat proteins derived from the C9orf72 allele, thereby alleviating pathological phenotypes associated with amyotrophic lateral sclerosis and frontotemporal dementia in cellular and murine models. di-Ellipticine-RIBOTAC TFA is valuable for research into ALS and FTD.
Out of stock
All 3 sizes