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Selective TβRII degrader

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9873

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162014
    WDR5 degrader-1

    		PROTACs WDR5 Cancer
    WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 .
    WDR5 degrader-1
  • HY-146349
    PROTAC EGFR degrader 4

    		PROTACs EGFR Autophagy Cancer
    PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR del19 and EGFR L858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .
    PROTAC EGFR degrader 4
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    		PROTACs PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
    PROTAC PD-1/PD-L1 degrader-1
  • HY-158342
    PROTAC TEAD degrader-1

    		PROTACs YAP Cancer
    PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
    PROTAC TEAD degrader-1
  • HY-162608
    PROTAC JAK1 degrader 1

    		PROTACs Cancer
    PROTAC JAK1 degrader 1 degrader 1 (compound 10c) is an effective and selective PROTAC JAK1 degrader with a DC50 of 214 nM. PROTAC JAK1 degrader 1 has antitumor activity. (Structure Note: PINK, JAK1 ligand 1 (HY-10961); Blue, VHL ligand Thalidomide (HY-14658); Black, linker) .
    PROTAC JAK1 degrader 1
  • HY-171140
    PROTAC HDAC6 degrader 3

    		PROTACs HDAC Cancer
    PROTAC HDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader for HDAC6 with an IC50 of 686 nM and a DC50 of 171 nM. PROTAC HDAC6 degrader 3 promotes the acetylation of α-tubulin . (Pink: ligand for target protein (HY-171141); Blue: ligand for E3 ligase VHL (HY-150803))
    PROTAC HDAC6 degrader 3
  • HY-161692
    ERα degrader 8

    		Estrogen Receptor/ERR Cancer
    ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC50 value of 0.15 μM .
    ERα degrader 8
  • HY-161398
    TGFβRII-IN-3

    		TGF-β Receptor TGF-beta/Smad Cancer
    TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research .
    TGFβRII-IN-3
  • HY-168099
    ERα degrader 10

    		Estrogen Receptor/ERR Cancer
    ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer .
    ERα degrader 10
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1

    		Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
    PROTAC BRD2/BRD4 degrader-1
  • HY-123971
    HDAC6 degrader-4

    		HDAC PROTACs Cancer
    HDAC6 degrader-4 is a PROTAC and a selective HDAC6 degrader consists of a non-selective HDAC inhibitor and thalidomide-type E3 ligase ligand. HDAC6 degrader-4 can be used for cancer research .
    HDAC6 degrader-4
  • HY-168101
    ERα degrader 11

    		Estrogen Receptor/ERR Cancer
    ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells .
    ERα degrader 11
  • HY-155492
    ERα degrader 7

    		Estrogen Receptor/ERR Cancer
    ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research .
    ERα degrader 7
  • HY-146267
    ERα degrader 5

    		Estrogen Receptor/ERR Cancer
    ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .
    ERα degrader 5
  • HY-139185
    PROTAC ERRα Degrader-3

    		PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins .
    PROTAC ERRα Degrader-3
  • HY-111594
    Homo-PROTAC cereblon degrader 1
    1 Publications Verification

    		 PROTACs Cancer
    Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3 .
    Homo-PROTAC cereblon degrader 1
  • HY-163757
    PROTAC PD-L1 degrader-1

    		PROTACs PD-1/PD-L1 Inflammation/Immunology Cancer
    PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)) .
    PROTAC PD-L1 degrader-1
  • HY-132194
    ERα degrader-2

    		Estrogen Receptor/ERR Cancer
    ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER + breast cancer research .
    ERα degrader-2
  • HY-115997
    PROTAC HSP90 degrader BP3

    		PROTACs HSP Cancer
    PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC HSP90 degrader BP3
  • HY-162723
    FOSL1 degrader 1

    		PROTACs AP-1 Cancer
    FOSL1 degrader 1 (4) is a T-5224-PROTAC, potently degrade FOSL1 (AP-1) to suppress cancer stemness gene expression in HNSCC. FOSL1 degrader 1 (4) effectively eliminate HNSCC cancer stem cells to inhibit tumor growth through degrading FOSL1. FOSL1 degrader 1 (4) displays around 30- to 100-fold increased potency over T-5224 (Pink: T-5224 (HY-12270); Black: Linker (HY-130200); Blue: Pomalidomide (HY-10984)) .
    FOSL1 degrader 1
  • HY-172882
    IKZF2-degrader 1

    		Molecular Glues IKZF Family Cancer
    IKZF2-degrader 1 (Compound 31) is a IKZF2 molecular glue degrader, with an DC50 of 0.5 nM. IKZF2-degrader 1 has minimal CK1α degradation activity relatively (DC50: 210 nM). IKZF2-degrader 1 can be used for research of IKZF2-dependent cancers .
    IKZF2-degrader 1
  • HY-144605
    PROTAC EGFR degrader 3

    		EGFR PROTACs Cancer
    PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .
    PROTAC EGFR degrader 3
  • HY-111866
    PROTAC RIPK degrader-2

    		PROTACs RIP kinase Metabolic Disease Cancer
    PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .
    PROTAC RIPK degrader-2
  • HY-144624
    PROTAC Axl Degrader 1

    		PROTACs TAM Receptor Cancer
    PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .
    PROTAC Axl Degrader 1
  • HY-144627
    PROTAC Axl Degrader 2

    		PROTACs TAM Receptor Cancer
    PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 μM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .
    PROTAC Axl Degrader 2
  • HY-153023
    PROTAC STAT3 degrader-2

    		PROTACs STAT Cancer
    PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research . PROTAC STAT3 degrader-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC STAT3 degrader-2
  • HY-155021
    PROTAC α-synuclein degrader 5

    		α-synuclein Neurological Disease
    PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC50 of 7.51 μM and the highest degradation rate Dmax of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research .
    PROTAC α-synuclein degrader 5
  • HY-162960
    pan-KRAS degrader 1

    		Ras Cancer
    pan-KRAS degrader 1 (Compound 1) is a panKRAS degrader with a surface plasmon resonance (SPR) dissociation constant Ki value of 25 nM for KRAS G12V .pan-KRAS degrader 1 has antitumor activity .
    pan-KRAS degrader 1
  • HY-163820
    WIZ degrader 4

    		Histone Acetyltransferase Others
    WIZ degrader 4 (Example 1) is a WIZ degrader with an AC50 value of 160 nM. WIZ degrader 4 can be used to investigate sickle cell disease (SCD) and thalassemia .
    WIZ degrader 4
  • HY-155197
    ER degrader 7

    		Microtubule/Tubulin Estrogen Receptor/ERR Cancer
    ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth .
    ER degrader 7
  • HY-163824
    WIZ degrader 7

    		Histone Acetyltransferase Others
    WIZ degrader 7 (Example 16) is a WIZ degrader with an IC50 value of < 0.01 μM. WIZ degrader 7 can be used to investigate sickle cell disease (SCD) and thalassemia .
    WIZ degrader 7
  • HY-169077
    IKZF3 degrader 1

    		Molecular Glues IKZF Family Cancer
    IKZF3 degrader 1 (compound 19a) is a molecular glue degrader of IKZF3 (EC50=0.012 μM). IKZF3 degrader 1 promotes the binding of IKZF3 to Cereblon (CRBN), leading to the ubiquitination and degradation of IKZF3 .
    IKZF3 degrader 1
  • HY-168518
    PROTAC CDK9 degrader-9

    		PROTACs CDK Cancer
    PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research .
    PROTAC CDK9 degrader-9
  • HY-156153
    CARM1 degrader-2

    		Histone Methyltransferase Cancer
    PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
    CARM1 degrader-2
  • HY-156152
    CARM1 degrader-1

    		Histone Methyltransferase Cancer
    PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC50=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
    CARM1 degrader-1
  • HY-163822
    WIZ degrader 5

    		Histone Acetyltransferase Others
    WIZ degrader 5 (compound 41) is a WIZ degrader and induces the degradation of WIZ with maximum degradation of 88.6% in 293T cells. WIZ degrader 5 can be used for study of sickle cell disease .
    WIZ degrader 5
  • HY-137488
    PROTAC BRAF-V600E degrader-2

    		PROTACs Raf Cancer
    PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .
    PROTAC BRAF-V600E degrader-2
  • HY-172827
    PROTAC BRD4 Degrader-30

    		PROTACs Epigenetic Reader Domain
    PROTAC BRD4 degrader-30 is an ISOX-DUAL-Based PROTAC degrader selectively targeting BRD4 (IC50 = 65 nM). PROTAC BRD4 degrader-30 can be used for research of c-Myc oncoprotein and cancer cell pathophysiology. (Pink: BRD4 ligand (HY-172828); Blue: CRBN ligand (HY-103596); Black: linker (HY-Y0139); CRBN ligand+linker: HY-138847) .
    PROTAC BRD4 Degrader-30
  • HY-144306
    ERα degrader 4

    		Estrogen Receptor/ERR Apoptosis Cancer
    ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
    ERα degrader 4
  • HY-174135
    PROTAC HPK1 Degrader-4

    		PROTACs MAP4K Cancer
    PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC50 of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355); Blue: ligand for E3 ligase CRBN (HY-45808); Black: Linker (HY-174356); Target protein ligand-linker Conjugate (HY-174357)) .
    PROTAC HPK1 Degrader-4
  • HY-163152
    PROTAC BRM degrader-1

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRM degrader-1 (compound 17) is a PROTAC-based BRM and BRG1 degrader, with DC50 values of 93 pM and 4.9 nM, respectively .
    PROTAC BRM degrader-1
  • HY-156591
    PROTAC MLKL Degrader-1

    		PROTACs Mixed Lineage Kinase Others
    PROTAC MLKL Degrader-1 (Compound 36) is a PROTAC degrader of MLKL, with a Dmax ＞90%. PROTAC MLKL Degrader-1 contains modified CRBN ligands, linker and Lenalidomide (HY-A0003)-linker fragments. PROTAC MLKL Degrader-1 abrogates cell death in a TSZ model of necroptosis.
    PROTAC MLKL Degrader-1
  • HY-155361
    PROTAC BRD9 Degrader-7

    		PROTACs Cancer
    PROTAC BRD9 Degrader-7 is an orally active and selective degrader of BRD9 with a DC50 of 1.02 nM. PROTAC BRD9 Degrader-7 has superior oral activity with a Cmax of 3436.95 ng/mL .
    PROTAC BRD9 Degrader-7
  • HY-161108
    PROTAC Chk1 degrader-1

    		PROTACs Checkpoint Kinase (Chk) Cancer
    PROTAC Chk1 degrader-1 (Compound PROTAC-2 ) is a potent PROTAC-targeted degrader of Chk1 with a DC50 of 1.33 μM. PROTAC Chk1 degrader-1 can be used in cancer research .
    PROTAC Chk1 degrader-1
  • HY-145073
    PROTAC ER Degrader-10

    		PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
    PROTAC ER Degrader-10
  • HY-160531
    IKZF1-degrader-1

    		Molecular Glues IKZF Family Cancer
    IKZF1-degrader-1 (Compound 9-B) is a IKZF1 molecular glue degrader with the DC50 value of 0.134 nM. IKZF1-degrader-1 can be used to degrader tumors .
    IKZF1-degrader-1
  • HY-162331
    STING Degrader-1

    		Molecular Glues STING Inflammation/Immunology Cancer
    STING Degrader-1 (compound 2), a molecular glue, is a potent STING degrader that covalently binds to STING and E3 ligase. STING Degrader-1 exhibits a "hook effect", that degrades 75% STING protein at 10 μM, and degrades ca. 30% STING protein at 30 μM .
    STING Degrader-1
  • HY-162318
    MYC degrader 1

    		Molecular Glues c-Myc Cancer
    MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
    MYC degrader 1
  • HY-158325
    PROTAC FLT-3 degrader 4

    		PROTACs FLT3 Apoptosis Cancer
    PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor) .
    PROTAC FLT-3 degrader 4
  • HY-153901
    PROTAC EGFR degrader 8

    		EGFR PROTACs Cancer
    PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC50 of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC50s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC .
    PROTAC EGFR degrader 8

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