Catalog No.
Product Name
Application
Product Information
Citations
-
PROTAC FGFR2 Degrader
LC-MB12 is an orally active PROTAC compound that targets FGFR2 degradation, with a DC₅₀ of 11.8 nM. It consists of the FGFR2 inhibitor BGJ398, a PROTAC linker, and a cereblon (CRBN) ligand. LC-MB12 effectively inhibits FGFR2 signaling in gastric cancer cells and exhibits antitumor activity. -
PROTAC Wee1 degrader
Pomalidomide-C3-adavosertib is a rapid and selective PROTAC degrader of Wee1, with an IC₅₀ of 3.58 nM. It exhibits anti-proliferative activity against cancer cells and induces apoptosis. -
Kinases PROTAC/Nek9 Inhibitor
DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity. -
ENL PROTAC Degrader
MS41 is a selective PROTAC degrader of eleven-nineteen leukemia (ENL), with DC₅₀ values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). MS41 effectively inhibits the proliferation of ENL-dependent leukemia cells, induces G1 phase cell cycle arrest, and promotes apoptosis. It reduces chromatin occupancy of the ENL-associated transcription elongation complex, thereby suppressing oncogenic gene expression and leukemia progression. -
CDK12/CDK13 PROTAC degrader
YJ1206 is an orally active and selective PROTAC degrader targeting CDK12 and CDK13, with an IC50 of 12.55 nM in VCaP cells. It induces DNA damage, promotes apoptosis, and leads to tumor regression in orthotopic WA74 patient-derived xenograft (PDX) models of resistant prostate cancer. Additionally, YJ1206 enhances antitumor efficacy when used in combination with AKT pathway inhibitors, highlighting its potential for combination therapy in advanced prostate cancer. -
PROTAC AKT degrader
INY-05-040 is a potent and selective PROTAC degrader targeting all three isoforms of AKT (AKT1, AKT2, and AKT3). It induces rapid proteasomal degradation of AKT, effectively inhibiting downstream signaling pathways such as PI3K/AKT/mTOR, which are critical for cancer cell survival and proliferation. INY-05-040 demonstrates broad antiproliferative activity across 288 cancer cell lines, highlighting its potential as a powerful therapeutic agent for targeting AKT-driven malignancies. -
PROTAC AR/AR-V7 degrader
PROTAC AR/AR-V7 Degrader-1 (27c) is a PROTAC-based dual degrader targeting both full-length androgen receptor (AR) and its splice variant AR-V7, which is implicated in resistance to androgen deprivation therapies. It exhibits DC₅₀ values of 2.67 μM for AR and 2.64 μM for AR-V7, effectively promoting their proteasomal degradation. By eliminating both isoforms, compound 27c induces apoptosis in AR-driven cancer cells, making it a promising therapeutic candidate for castration-resistant prostate cancer (CRPC) and other AR/AR-V7–dependent malignancies. -
EGFR degrader
MS-39 is a highly potent and selective PROTAC degrader specifically engineered to target mutant forms of the epidermal growth factor receptor (EGFR). It is constructed by conjugating the EGFR inhibitor gefitinib to a von Hippel–Lindau (VHL) E3 ligase ligand via a tailored linker. MS-39 exhibits strong binding affinity and efficient degradation of mutant EGFR proteins, offering a promising strategy for overcoming resistance in EGFR-driven cancers. Its design enables targeted proteasomal degradation rather than mere kinase inhibition, providing a novel approach to cancer therapy. -
multi-kinase PROTAC degrader
SB1-G-187 is a multifunctional PROTAC designed as a multi-kinase degrader, capable of inducing the selective degradation of multiple kinase targets through the ubiquitin–proteasome system. In addition to its targeted degradation activity, SB1-G-187 features an alkyne functional group, enabling its use as a click chemistry reagent. It can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, allowing for versatile applications in chemical biology, such as probe development, conjugation, and target identification. -
PROTAC JAK2 Degrader
SJ1008030 (compound 8) TFA is a selective JAK2-targeting PROTAC that promotes proteasomal degradation of Janus kinase 2 (JAK2). It exhibits potent antiproliferative activity in MHH–CALL-4 leukemia cells, with an IC₅₀ of 5.4 nM. By effectively eliminating JAK2 protein rather than merely inhibiting its activity, SJ1008030 TFA represents a promising therapeutic strategy for JAK2-driven hematologic malignancies, particularly in leukemia research. -
PROTAC degrader
SJF-8240 (PROTAC 7) is a proteolysis-targeting chimera (PROTAC) designed to selectively degrade the receptor tyrosine kinase c-Met. It induces polyubiquitination and subsequent proteasomal degradation of c-Met, leading to effective inhibition of downstream signaling. SJF-8240 exhibits potent antiproliferative activity in GTL16 gastric cancer cells, with an IC₅₀ of 66.7 nM, making it a promising tool for targeted cancer therapy and c-Met–driven tumor research. -
IRAK4 degrader
KTX-582 is a potent heterobifunctional PROTAC degrader that targets interleukin-1 receptor–associated kinase 4 (IRAK4) and the transcription factor Ikaros, with DC₅₀ values of 4 nM and 5 nM, respectively. It induces apoptosis in MYD88^L265P-mutant diffuse large B-cell lymphoma (DLBCL) cells, a subtype characterized by constitutive IRAK4 signaling. In preclinical lymphoma models, KTX-582 effectively drives in vivo tumor regression, highlighting its therapeutic potential for MYD88-mutant hematologic malignancies. -
STING PROTAC degrader
Anti-inflammatory agent 70 (N-Me-SP23) is a PROTAC-based degrader targeting the STING (stimulator of interferon genes) protein, a key regulator of innate immune and inflammatory responses. By promoting STING degradation, N-Me-SP23 effectively inhibits the STING signaling pathway, leading to reduced downstream inflammatory cytokine production. This compound exhibits notable anti-inflammatory activity and holds potential for therapeutic research in STING-associated autoimmune and inflammatory disorders. -
PROTAC EGFR degrader
MS9449 is a potent PROTAC-based degrader of the epidermal growth factor receptor (EGFR), exhibiting strong binding affinities with K\_d values of 17 nM for wild-type EGFR and 10 nM for the L858R mutant. It effectively induces degradation of mutant EGFR proteins via both the ubiquitin–proteasome system (UPS) and the autophagy–lysosome pathway, enabling dual-pathway clearance. MS9449 shows strong antiproliferative activity in non-small cell lung cancer (NSCLC) cells, making it a valuable compound for anticancer research, particularly in EGFR-driven tumors. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-12 (compound 9c) is a bifunctional molecule designed to target and degrade the bromodomain-containing protein BRD4 by recruiting the von Hippel–Lindau (VHL) E3 ubiquitin ligase. It functions as a highly potent degrader, with a DC₅₀ of 0.39 nM and 0.24 nM when conjugated to STEAP1 and CLL1 antibodies, respectively, enabling targeted delivery and degradation of BRD4 in PC3 prostate cancer cells. -
PROTAC YAP degrader
PROTAC YAP degrader-1 (compound YZ-6) is a bifunctional molecule designed to selectively degrade Yes-associated protein (YAP), a key effector of the Hippo signaling pathway involved in cell proliferation, survival, and tumorigenesis. In addition to promoting proteasomal degradation of YAP, it also inhibits YAP's nuclear localization, thereby impairing its transcriptional co-activator functions.YZ-6 is composed of two main components:Target protein ligand: NSC682769 and E3 ubiquitin ligase recruiter with linker: (R,S,R)-AHPC-PEG2-C2-Boc which recruits the VHL E3 ligase complex. The linker used in the PROTAC design is Acid-PEG2-C2-Boc, facilitating optimal spatial orientation for ternary complex formation. The demethylated analog Demethyl-NSC682769 serves as a target ligand activity control. PROTAC YAP degrader-1 represents a novel tool for functional YAP inhibition and offers potential therapeutic applications in YAP-driven cancers and fibrotic diseases. -
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.
