Catalog No.
Product Name
Application
Product Information
Citations
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RIPK1 PROTAC Degrader
LD4172 is a selective RIPK1 PROTAC degrader that exhibits a Ki of 4.8 nM. It facilitates RIPK1 protein degradation through the formation of a ternary complex with RIPK1 and VHL E3 ligase, leading to ubiquitination and proteasomal degradation. LD4172 effectively inhibits TNF-induced classical NF-κB signaling in TRAF2-deficient cells, significantly reducing IκBα phosphorylation and IL-8 production. Additionally, it promotes apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy, making it a valuable chemical probe for studying RIPK1-related functions in melanoma and colon cancer research. -
CDK2/4/6 PROTAC Degrader
PROTAC CDK2/4/6 Degrader-2 is a targeted protein degradator specifically designed to degrade cyclin-dependent kinases CDK2, CDK4, and CDK6. This compound effectively inhibits cell proliferation and induces cell cycle arrest and apoptosis in malignant melanoma cells. Its application extends to cancer research, particularly in investigating the role of CDK2/4/6 in tumor biology. The compound can also be converted into its prodrug form, enabling versatile utilization in various assays related to cancer therapeutics. -
BRD4 Degrader
PROTAC BRD4 Degrader-6 is a potent small-molecule degrader that targets BRD4, exhibiting an IC50 value of 2.7 nM for the BRD4 BD1 domain. This compound effectively degrades BRD4 protein and leads to the downregulation of c-Myc expression. In vitro studies demonstrate its capacity to inhibit proliferation and induce apoptosis in the pancreatic cancer cell line BxPC3, making it a valuable tool for research in human pancreatic cancer biology. -
PROTAC Ferritin Degrader
DeFer-2 is a PROTAC degrader targeting ferritin, with a Kd of 17.1 μM. By inducing ferritin degradation, DeFer-2 leads to caspase 3-GSDME-mediated pyroptosis in cancer cells, driven by an accumulation of free iron and elevated reactive oxygen species (ROS). This compound demonstrates significant tumor growth inhibition and extends survival in mouse models bearing B16F10 subcutaneous tumors, making it a valuable tool for research in melanoma. -
AURKA PROTAC Degrader
SK2188 is a potent and selective PROTAC degrader that targets Aurora Kinase A (AURKA) with a DC50 of 3.9 nM. It induces DNA damage and promotes apoptosis in cancer cells, effectively leading to the degradation of MYCN. SK2188 serves as a valuable tool for investigating tumor cell proliferation and exploring therapeutic strategies in MYCN-amplified neuroblastoma. -
SMARCA2 Degrader
A947 is a selective SMARCA2 proteolysis-targeting chimera (PROTAC) that functions as a potent degrader of SMARCA2. It exhibits a binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM, establishing its effectiveness in mediating targeted protein degradation. This compound has significant applications in cancer research, facilitating studies on the role of SMARCA2 in tumorigenesis and potential therapeutic interventions. -
HCK/BTK PROTAC Degrader
DFCI-002-06 is an orally active PROTAC degrader targeting both HCK and BTK, demonstrating DC₅₀ values of 1.3 nM and 4.5 nM, respectively. This compound exhibits superior anti-tumor activity compared to a dual-target inhibitor, promoting apoptosis in cancer cells, particularly in MYD88 mutant B-cell malignancies. DFCI-002-06 serves as a valuable tool for researching mechanisms underlying these specific cancer types. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-17 is a potent protein degrader targeting bromodomain-containing protein 4 (BRD4). It exhibits IC50 values of 29.54 nM for BRD4 (BD1) and 3.82 nM for BRD4 (BD2). This compound effectively inhibits G2/M cell cycle progression, leading to decreased expression of Cyclin B1, and significantly induces apoptosis in MV-4-11 cells. PROTAC BRD4 Degrader-17 is valuable for research applications focused on cancer cell biology and the development of targeted degraders in therapeutic strategies. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 5 is a targeted protein degradation agent that effectively degrades the EGFRDel19 variant in HCC827 cells, exhibiting a DC50 of 34.8 nM. This compound significantly induces apoptosis and leads to G1 phase cell cycle arrest in HCC827 cells, making it a valuable tool for studying EGFR-related signaling pathways and potential therapeutic interventions in lung cancer research. -
FLT3-PROTAC Degrader
PROTAC FLT-3 degrader 4 is a CRBN-based degrader that selectively targets FLT3-ITD mutants by harnessing the ubiquitin-proteasome system for degradation. This compound demonstrates potent activity against FLT3-ITD mutant acute myeloid leukemia (AML) cells, offering a focused approach for research applications in cancer therapeutics. Its oral bioavailability positions it as a valuable tool for investigating FLT3-related signaling pathways and potential treatment strategies in AML. -
p53 Stabilizer/MDM2 PROTAC Degrader
Seldegamadlin is a selective p53 stabilizer and an MDM2 PROTAC degrader with a DC50 of 0.4 nM. It effectively inhibits the proliferation of RS4;11 cancer cells, demonstrating an IC50 of 0.3 nM, and induces cell cycle arrest at the G2/M phase while promoting apoptosis. By upregulating p53 activity, Seldegamadlin overcomes the p53-MDM2 feedback loop, making it a valuable tool for research in hematologic and solid tumors, including acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). -
AR-FL/AR-V7 PROTAC Degrader
BWA-522 is an orally active PROTAC degrader that targets the full-length androgen receptor (AR-FL) and its splice variant AR-V7. By antagonizing the N-terminal domain of the androgen receptor, BWA-522 effectively suppresses downstream signaling pathways and induces apoptosis in cancer cells. Furthermore, this compound has demonstrated significant inhibition of tumor growth in LNCaP xenograft mouse models, making it a valuable tool for prostate cancer research. -
PROTAC
Luxdegalutamide (ARV-766) is an orally active proteolysis-targeting chimera (PROTAC) designed to selectively degrade the androgen receptor (AR), including clinically relevant resistance-associated mutants such as T878A, H875Y, and L702H. By inducing AR ubiquitination and proteasomal degradation, Luxdegalutamide effectively suppresses AR signaling and exhibits potent antitumor activity. It is a promising therapeutic agent and research tool for studying castration-resistant prostate cancer (CRPC) and mechanisms of AR-driven oncogenesis. -
BTK/GSPT1 Degrader
GBD-9 is a dual-action degrader that targets both BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It acts as a PROTAC to promote BTK degradation and functions as a molecular glue to induce GSPT1 degradation. GBD-9 exhibits significant antiproliferative activity in cancer cells, making it a promising candidate for cancer research. -
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.
