Catalog No.
Product Name
Application
Product Information
Citations
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HDAC3/8 PROTAC degrader
YX968 is a potent and selective PROTAC degrader targeting histone deacetylases HDAC3 and HDAC8, with DC₅₀ values of 1.7 nM and 6.8 nM, respectively. By inducing degradation of these epigenetic regulators, YX968 promotes apoptosis and exhibits significant antitumor activity, representing a promising therapeutic strategy for cancers driven by aberrant HDAC3/8 activity. -
PROTAC AR degrader
ARD-1676 is an orally bioavailable PROTAC degrader of the androgen receptor (AR), composed of an AR-binding ligand and a cereblon-recruiting moiety. It effectively induces AR degradation both in vitro and in vivo, and demonstrates significant antitumor activity by inhibiting VCaP prostate cancer xenograft growth in mouse models. ARD-1676 represents a promising therapeutic strategy for targeting AR-driven malignancies. -
PROTAC GSPT1 degrader
MI-389 is a PROTAC degrader targeting the translation termination factor GSPT1. Its activity relies on recruitment of the CRL4^CRBN E3 ubiquitin ligase complex to induce selective degradation of GSPT1. MI-389 effectively disrupts a critical dependency shared across multiple acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines, making it a promising therapeutic candidate for hematologic malignancies characterized by GSPT1 dependence. -
PROTAC CDK12-Cyclin K degrader
PP-C8 is a potent and selective PROTAC degrader targeting the CDK12–Cyclin K complex. It induces efficient degradation of CDK12 and Cyclin K with DC₅₀ values of 416 nM and 412 nM, respectively. In preclinical models, PP-C8 exhibits strong synergistic antiproliferative effects when combined with PARP inhibitors, particularly in triple-negative breast cancer (TNBC), highlighting its potential as a therapeutic strategy for enhancing DNA damage response–targeted treatments. -
PROTAC BRD4 degrader
dBET23 is a highly potent and selective PROTAC degrader targeting the bromodomain-containing protein BRD4. It exhibits a DC₅₀ of approximately 50 nM at 5 hours for the BRD4 bromodomain 1 (BRD4^BD1) protein, effectively promoting its ubiquitination and proteasomal degradation. dBET23 serves as a valuable chemical tool for studying BRD4-dependent transcriptional regulation and holds potential for therapeutic applications in BRD4-driven cancers. -
PROTAC AR degrader
ARD-61 is a highly potent and selective PROTAC degrader of the androgen receptor (AR), also capable of degrading progesterone receptors (PR) in AR-positive cancer cell lines. It induces apoptosis and demonstrates significant antitumor efficacy in vivo, effectively inhibiting tumor growth in the MDA-MB-453 xenograft mouse model. Additionally, ARD-61 is equipped with an alkyne functional group, enabling its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, facilitating conjugation and functionalization for chemical biology applications. -
EGFR PROTAC degrader
SJF-1521 is a selective PROTAC degrader targeting the epidermal growth factor receptor (EGFR). It incorporates lapatinib, a known EGFR inhibitor, as the targeting ligand and promotes proteasomal degradation of EGFR. SJF-1521 effectively induces EGFR degradation in OVCAR8 ovarian cancer cells, offering a promising strategy for disrupting EGFR signaling in EGFR-driven malignancies. -
PROTAC ERα Degrader
PROTAC ERα Degrader-1 is a bifunctional molecule composed of an estrogen receptor-alpha (ERα) ligand, a linker, and an E3 ubiquitin ligase-recruiting moiety. Derived from compound P1 in patent WO2017201449A1, it functions as a targeted protein degrader that promotes ubiquitination and subsequent proteasomal degradation of ERα. PROTAC ERα Degrader-1 represents a novel approach for modulating estrogen receptor signaling in hormone-dependent cancers. -
PROTAC BET degrader
SJ995973 is a highly potent PROTAC (proteolysis-targeting chimera) designed to selectively degrade bromodomain and extra-terminal domain (BET) family proteins, including BRD2, BRD3, and BRD4. By inducing targeted proteasomal degradation, SJ995973 enables efficient disruption of BET protein function, offering a powerful approach for investigating BET-related transcriptional regulation and for the development of novel anticancer therapies. -
G9a/GLP PROTAC degrader
MS8709 (compound 10) is a first-in-class PROTAC degrader targeting the histone methyltransferases G9a and GLP, with potential anticancer activity. Engineered from the G9a/GLP inhibitor UNC0642, MS8709 recruits the von Hippel–Lindau (VHL) E3 ubiquitin ligase to promote the selective ubiquitination and proteasomal degradation of G9a/GLP proteins. This targeted degradation approach offers a novel therapeutic strategy for disrupting epigenetic dysregulation in cancer. -
PIK3CG PROTAC degrader
ARM165 is a heterobifunctional PROTAC molecule that targets and degrades PIK3CG (PI3Kγ), effectively inhibiting the PI3Kγ-Akt signaling pathway. It exhibits potent antileukemic activity, suppressing the proliferation of acute myeloid leukemia (AML) cells with an IC₅₀ of less than 1 μM. ARM165 is a promising tool for investigating PI3Kγ-driven signaling and developing targeted therapies for leukemia. -
MYC-MAX degrader
MDEG-541 is a potent PROTAC degrader targeting the MYC-MAX complex, derived from the MYC-MAX dimerization inhibitor 10058-F4 (28RH) and thalidomide as the cereblon-recruiting ligand. It exhibits strong antiproliferative activity and reduces the expression of key oncogenic and regulatory proteins, including GSPT1, MYC, GSPT2, and PLK1. MDEG-541 is a valuable tool for studying MYC-driven cancers and targeted protein degradation strategies. -
PROTAC SOS1 degrader
PROTAC SOS1 Degrader-1 (TFA) is a potent PROTAC molecule targeting SOS1, with a DC₅₀ of 98.4 nM. It exhibits antiproliferative activity in cancer cells harboring various KRAS mutations and demonstrates antitumor efficacy with low toxicity, making it a promising candidate for targeted cancer therapy research. -
PRC1 PROTAC degrader
MS181 (Compound 1) is a potent PROTAC degrader that targets components of the polycomb repressive complex 1 (PRC1) by recruiting cereblon (CRBN) and binding EED. It effectively reduces the expression of key PRC1 and PRC2 components, including EED, EZH2, SUZ12, BMI1, and RING1B. MS181 exhibits significant antiproliferative activity, making it a valuable tool for studying epigenetic regulation and potential cancer therapeutics. -
PRC1 PROTAC degrader
MS9715 is a potent and selective PROTAC degrader targeting NSD3, designed by conjugating the NSD3 PWWP1 domain binder BI-9321 to a von Hippel-Lindau (VHL) E3 ligase ligand. It effectively induces degradation of NSD3 and holds significant potential for research in NSD3-dependent cancers, offering a novel approach to target epigenetic drivers in oncology. -
PROTAC CDK12/13 Degrader
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective dual degrader targeting CDK12 and CDK13, with DC₅₀ values of 2.2 nM and 2.1 nM, respectively. It exhibits potent anti-proliferative activity and serves as a valuable tool for investigating transcriptional regulation and therapeutic strategies in breast cancer research. -
PROTAC pirin degrader
CCT367766 formic is a third-generation, cereblon-based heterobifunctional PROTAC and pirin-targeting protein degradation probe (PDP). It effectively depletes pirin protein expression at low concentrations. CCT367766 formic demonstrates moderate affinity for the CRBN–DDB1 complex (IC₅₀ = 490 nM) and strong binding affinity for recombinant pirin and CRBN, with K_d values of 55 nM and 120 nM, respectively. This compound serves as a valuable chemical tool for exploring the biological roles of the largely understudied protein pirin. -
PROTAC EZH2 Degrader
PROTAC EZH2 Degrader-2 (Compound E-3P-MDM2) is a PROTAC molecule designed by linking the EZH2 inhibitor Tazemetostat (EPZ6438) to an E3 ligase ligand. It induces dose-dependent degradation of EZH2 in SU-DHL-6 cells, suppresses H3K27me3 expression, and concurrently degrades PRC2 components EED and SUZ12 without altering their mRNA levels. PROTAC EZH2 Degrader-2 exhibits strong anti-cancer and anti-proliferative activity, making it a valuable tool for epigenetic and oncology research. -
PROTAC ALK/EGFR degrader
SIAIS164018 hydrochloride is a PROTAC-based dual degrader targeting ALK and EGFR, with IC₅₀ values of 2.5 nM for ALK and 6.6 nM for the ALK G1202R mutant. It effectively suppresses cancer cell migration and invasion, induces G1 phase cell cycle arrest, and promotes apoptosis, making it a promising candidate for targeted cancer therapy research. -
PROTAC Aurora A degrader
dAURK-4 hydrochloride is a potent and selective PROTAC degrader targeting Aurora A kinase (AURKA), derived from the AURKA inhibitor Alisertib. It effectively induces AURKA degradation and exhibits notable anticancer activity, making it a valuable agent for studying AURKA-driven oncogenic pathways and therapeutic development. -
PROTAC JAK2 degrader
SJ1008030 (Compound 8) formic is a selective PROTAC degrader of JAK2, designed to target and eliminate JAK2 protein via the ubiquitin–proteasome pathway. It effectively inhibits the growth of MHH–CALL-4 leukemia cells with an IC₅₀ of 5.4 nM. SJ1008030 formic is a valuable tool for leukemia research and the study of JAK2-driven signaling pathways. -
PROTAC HPK1 degrader
SS47 TFA is a PROTAC-based degrader targeting hematopoietic progenitor kinase 1 (HPK1), an immunosuppressive regulatory kinase. It induces proteasome-mediated degradation of HPK1 and significantly enhances the antitumor efficacy of BCMA CAR-T cell therapy in vivo. In addition to its biological function, SS47 TFA is also a click chemistry reagent containing an alkyne group, allowing it to participate in copper-catalyzed azide–alkyne cycloaddition (CuAAC) with azide-functionalized molecules. This dual functionality makes SS47 TFA a valuable tool in both cancer immunotherapy research and chemical biology applications. -
PROTAC NCOA4 degrader
PROTAC NCOA4 Degrader-1 (Compound V3) is a highly potent PROTAC targeting NCOA4, with a DC₅₀ of 3 nM in HeLa cells. It functions as a ferroptosis inhibitor by reducing NCOA4 levels and lowering intracellular ferrous iron (Fe²⁺) concentrations. PROTAC NCOA4 Degrader-1 has demonstrated protective effects in a CCl₄-induced acute liver injury model, making it a valuable tool for studying ferroptosis and liver disease therapeutics. -
AKT PROTAC degrader
MS15 TFA is a potent and selective PROTAC degrader targeting AKT isoforms. It inhibits the activity of AKT1, AKT2, and AKT3 with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively. MS15 TFA serves as a valuable tool for studying AKT signaling and its role in cancer and metabolic diseases. -
PROTAC CDK8-cyclin C dual degrader
LL-K8-22 is a potent, selective, and durable PROTAC degrader targeting the CDK8–cyclin C complex, with DC₅₀ values of 2.52 μM and 2.64 μM, respectively. It suppresses STAT1 Ser727 phosphorylation and inhibits E2F- and MYC-driven oncogenic transcriptional programs. LL-K8-22 shows potential for use in triple-negative breast cancer (TNBC) research and related therapeutic studies. -
Protac smarca2 degrader
SMD-3040 formate is a potent and selective PROTAC degrader targeting SMARCA2, a core ATPase subunit of the SWI/SNF chromatin remodeling complex. It exhibits strong in vivo antitumor activity, making it a promising candidate for cancer research involving epigenetic regulation and synthetic lethality strategies. -
PROTAC EGFR degrader
MS9427 TFA is a potent PROTAC degrader targeting EGFR, with binding affinities (K_d) of 7.1 nM for wild-type EGFR and 4.3 nM for the EGFR L858R mutant. It selectively degrades the mutant EGFR via both the ubiquitin–proteasome system (UPS) and autophagy–lysosome pathways. MS9427 TFA effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and is a valuable tool for anticancer research focused on EGFR-driven malignancies. -
PROTAC c-Src kinase degrader
DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase, acting through CRBN-mediated ubiquitination. It effectively reduces c-Src levels and inhibits proliferation in c-Src-dependent cancer cell lines, making it a useful tool for targeted protein degradation research. -
β-catenin PROTAC degrader
xStAx-VHLL is a PROTAC degrader targeting β-catenin, promoting its ubiquitination and proteasomal degradation. It effectively inhibits the Wnt/β-catenin signaling pathway and suppresses proliferation of colon cancer cells, demonstrating anti-tumor activity. -
PROTAC CBP/p300 Degrader
CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy. -
PROTAC CRBN Degrader
CRBN-6-5-5-VHL is a potent and selective VHL-based PROTAC degrader targeting cereblon (CRBN), with a DC₅₀ of 1.5 nM. It selectively degrades CRBN without affecting neo-substrates IKZF1 and IKZF3. -
PROTAC IRAK4 degrader
PROTAC IRAK4 Degrader-1 is a cereblon-based PROTAC targeting IRAK4, derived from US patent US20190192668A1 (Compound I-210). It induces IRAK4 degradation in OCI-LY-10 cells with <20% at 0.01 μM, >20–50% at 0.1 μM, and >50% at 1 μM. -
FKBP12F36V Degrader
dTAG-47 is a heterobifunctional degrader that selectively targets FKBP12^F36V-tagged proteins for degradation. By binding FKBP12^F36V, which acts as a degradation tag (dTAG), dTAG-47 enables conditional and selective protein degradation. It is a valuable tool for studying protein function in models such as basal-like breast cancer (BBC). -
PROTAC CDK4/6 Degrader
XY028-133 (Example 14) is a PROTAC-based degrader targeting CDK4/6, composed of ligands for von Hippel-Lindau (VHL) and CDK. It induces selective degradation of CDK4/6 and exhibits anti-tumor activity, making it a useful tool for cell cycle and cancer research. -
PROTAC ALK Degrader
TL13-112 is a potent and selective PROTAC degrader targeting ALK, with an IC₅₀ of 0.14 nM for ALK inhibition. In addition to ALK, TL13-112 also induces degradation of Aurora A (IC₅₀: 8550 nM), FER (42.4 nM), PTK2 (25.4 nM), and RPS6KA1 (677 nM), supporting its utility in kinase signaling and cancer research. -
PROTAC AR Degrader
ARD-2128 is a highly potent, orally bioavailable PROTAC degrader targeting the androgen receptor (AR). It efficiently reduces AR protein levels, downregulates AR-regulated gene expression in tumor tissues, and inhibits tumor growth without observable toxicity. ARD-2128 is a promising tool for prostate cancer research. -
PROTAC RIPK degrader
PROTAC RIPK Degrader-2 is a non-peptidic, VHL-based PROTAC that selectively targets the serine/threonine kinase RIPK2 for degradation. It promotes cancer cell death and ion channel activation, while also inhibiting key protein interactions involved in disease pathways, including those related to cancer and diabetes. - PROTAC IRAK3 Degrader-1 (Compound 23) is a potent and selective PROTAC molecule targeting IRAK3, with an IC₅₀ of 5 nM. It enables efficient degradation of IRAK3, providing a valuable tool for studying innate immune signaling and inflammatory pathways.
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USP7 PROTAC Degrader
U7D-1 is a first-in-class, potent, and selective PROTAC degrader of USP7 (ubiquitin-specific protease 7), with a DC₅₀ of 33 nM in RS4;11 cells. It exhibits anticancer activity and induces apoptosis in Jeko-1 cells, supporting its utility in cancer research targeting deubiquitinating enzymes. -
PROTAC CDK4/6 Degrader
BSJ-03-204 triTFA is a potent and selective PROTAC degrader targeting CDK4/6, constructed using ligands for cereblon and CDK. Based on Palbociclib, it exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and shows anti-cancer activity, making it a valuable tool for cell cycle and oncology research. -
HDAC Degrader
JPS016 is a benzamide-based PROTAC that recruits the Von Hippel-Lindau (VHL) E3 ligase to selectively degrade class I histone deacetylases (HDACs). It is a potent degrader of HDAC1/2, leading to broad transcriptional changes and enhanced apoptosis in HCT116 cells, supporting its application in epigenetic and cancer research. -
BCR-ABL PROTAC Degrader
SIAIS100 TFA is a potent PROTAC degrader targeting BCR-ABL, with a DC₅₀ of 2.7 nM. It is a valuable tool for studying BCR-ABL signaling and therapeutic strategies in chronic myeloid leukemia (CML). -
FOSL1 degrader
FOSL1 Degrader 1 (4) is a potent T-5224-based PROTAC that selectively degrades FOSL1 (AP-1), suppressing cancer stemness gene expression in head and neck squamous cell carcinoma (HNSCC). It effectively inhibits tumor growth and eliminates cancer stem cells, showing 30–100 times greater efficacy than T-5224. -
MYC RIBOTAC
MYC-RIBOTAC is a ribonuclease-targeting chimera (RIBOTAC) designed to degrade MYC mRNA by targeting its internal ribosome entry site (IRES). It combines a MYC mRNA-binding moiety with a small molecule that recruits and activates RNase L1. MYC-RIBOTAC reduces MYC mRNA and protein levels, induces apoptosis, and holds promise for antitumor research. -
PROTAC CDK12/13 Degrader
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective dual degrader of CDK12 and CDK13, with DC₅₀ values of 2.2 nM and 2.1 nM, respectively. It exhibits strong antiproliferative activity and is a valuable tool for investigating cell cycle regulation and therapeutic strategies in breast cancer research. -
PROTAC PIKfyve degrade
PIK5-12d is a potent PROTAC degrader targeting PIKfyve, with a DC₅₀ of 1.48 nM. It induces extensive cytoplasmic vacuolization, disrupts autophagic flux, and inhibits proliferation in multiple prostate cancer cell lines. PIK5-12d exhibits notable anti-tumor activity, supporting its use in cancer research. -
PROTAC CBP/p300 degrader
JET-209 is a potent PROTAC degrader targeting CBP and p300, with DC₅₀ values of 0.05 nM and 0.2 nM, respectively. It is composed of lenalidomide, a linker, and the bromodomain inhibitor GNE-207. JET-209 is a valuable tool for cancer research involving epigenetic regulation.
