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Active Degraders Inhibitors

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40

Inhibitors & Agonists

1

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1

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5

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2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108619
    Gisadenafil besylate

    UK 369003-26

    		 Phosphodiesterase (PDE) Neurological Disease
    Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP) .
    Gisadenafil besylate
  • HY-10213
    SNX-5422

    PF-04929113

    		 HSP Cancer
    SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
    SNX-5422
  • HY-137449
    Rintodestrant

    G1T48

    		 Estrogen Receptor/ERR CDK Cancer
    Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor .
    Rintodestrant
  • HY-127026
    Quinaprilat

    		Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat is an orally active non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat acts as anti-hypertensive agent and vasodilator .
    Quinaprilat
  • HY-14841
    Gisadenafil

    UK-369003

    		 Phosphodiesterase (PDE) Neurological Disease
    Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP) .
    Gisadenafil
  • HY-155666
    YXG-158

    		Androgen Receptor Cancer
    YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer .
    YXG-158
  • HY-136185
    Atorvastatin Epoxy Tetrahydrofuran Impurity

    		Drug Metabolite Others
    Atorvastatin Epoxy Tetrahydrofuran Impurity is an impurity isolated oxidative degradation products of Atorvastatin (HY-B0589) . Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
    Atorvastatin Epoxy Tetrahydrofuran Impurity
  • HY-127026A
    Quinaprilat hydrate

    		Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat hydrate is a non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat hydrate specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat hydrate acts as anti-hypertensive agent and vasodilator .
    Quinaprilat hydrate
  • HY-100898
    OGT 2115
    2 Publications Verification

    		 Others Cancer
    OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity .
    OGT 2115
  • HY-123058
    Vps34-IN-4

    		PI3K Autophagy Cancer
    Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components .
    Vps34-IN-4
  • HY-147088
    TEAD-IN-2

    		YAP Cancer
    TEAD-IN-2 is a novel, orally active inhibitor of transcriptional enhancer associate domain (TEAD) and modulates TEAD by ubiquitination and/or degradation by compounds. TEAD-IN-2 can be used for the research of a variety of diseases, disorders or conditions associated with TEAD .
    TEAD-IN-2
  • HY-N7454
    Anhydroerythromycin A

    		Antibiotic Bacterial Infection
    Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
    Anhydroerythromycin A
  • HY-141550
    BPK-25

    		Others Inflammation/Immunology
    BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .
    BPK-25
  • HY-15578
    McMMAF
    4 Publications Verification

    Maleimidocaproyl monomethylauristatin F

    		 Drug-Linker Conjugates for ADC Cancer
    McMMAF is a protective group (maleimidocaproyl)-conjugated MMAF, which is a potent tubulin polymerization inhibitor. McMMAF can be used as a agent-linker for antibody-drug conjugates (ADC). McMMAF is uncleavable, and must be internalized and degraded within a cell, releasing cysteine-McMMAF as the active agent .
    McMMAF
  • HY-153386
    CPD-1224

    		Anaplastic lymphoma kinase (ALK) Cancer
    CPD-1224 is an orally active derivative of ALK inhibitors to cereblon ligands. CPD-1224 targets to EML4-ALK oncogenic fusions, and degrades ALK and mutant L1196M/G1202R .
    CPD-1224
  • HY-127026S
    Quinaprilat-d5

    		Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].
    Quinaprilat-d5
  • HY-160506
    PRO-6E

    		PROTACs c-Met/HGFR Apoptosis
    PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .
    PRO-6E
  • HY-13822
    SKI II
    2 Publications Verification

    		 SphK Wnt Apoptosis Cancer
    SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation .
    SKI II
  • HY-153357
    NRX-0492

    		Btk Cancer
    NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex .
    NRX-0492
  • HY-149843
    LC-MB12

    		FGFR PROTACs Cancer
    LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity .
    LC-MB12
  • HY-12486
    FL118

    10,11-(Methylenedioxy)-20(S)-camptothecin

    		 Survivin Apoptosis IAP Cancer
    FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer .
    FL118
  • HY-138050
    Nyasol

    (-)-Nyasol; (Z)-Hinokiresinol; cis-Hinokiresinol

    		 NO Synthase Bacterial Fungal Parasite Leukotriene Receptor Infection Inflammation/Immunology
    Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells .
    Nyasol
  • HY-15578G
    McMMAF

    Maleimidocaproyl monomethylauristatin F

    		 Drug-Linker Conjugates for ADC Cancer
    McMMAF GMP is a GMP grade McMMAF (HY-15578). McMMAF is a protective group (maleimidocaproyl)-conjugated MMAF, which is a potent tubulin polymerization inhibitor. McMMAF can be used as a agent-linker for antibody-drug conjugates (ADC). McMMAF is uncleavable, and must be internalized and degraded within a cell, releasing cysteine-McMMAF as the active agent .
    McMMAF
  • HY-142686
    SGK1-IN-3

    		SGK Inflammation/Immunology
    SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis .
    SGK1-IN-3
  • HY-10585A
    Valproic acid sodium
    Maximum Cited Publications
    33 Publications Verification

    Sodium Valproate sodium

    		 Organoid HDAC Autophagy Mitophagy HIV Notch Apoptosis Endogenous Metabolite Infection Neurological Disease Metabolic Disease Cancer
    Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
    Valproic acid sodium
  • HY-10585
    Valproic acid
    Maximum Cited Publications
    33 Publications Verification

    Dipropylacetic Acid

    		 Organoid HDAC Autophagy Mitophagy HIV Notch Apoptosis Endogenous Metabolite Infection Neurological Disease Metabolic Disease Cancer
    Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
    Valproic acid
  • HY-103238
    RSVA405

    		AMPK STAT Autophagy Neurological Disease Metabolic Disease Inflammation/Immunology
    RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity .
    RSVA405
  • HY-149480
    ERD-3111

    		PROTACs Estrogen Receptor/ERR Cancer
    ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
    ERD-3111
  • HY-10585B
    Valproic acid (sodium)(2:1)

    VPA (sodium)(2:1); 2-Propylpentanoic Acid (sodium)(2:1)

    		 HDAC Autophagy Mitophagy HIV Notch Apoptosis Endogenous Metabolite Infection Neurological Disease Metabolic Disease Cancer
    Valproic acid (VPA) sodium (2:1) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
    Valproic acid (sodium)(2:1)
  • HY-144761
    TOPK-p38/JNK-IN-1

    		JNK Cancer
    TOPK-p38/JNK-IN-1 (Compound B12) is an orally active TOPK-p38/JNK signaling pathway inhibitor with the IC50 value of 2.14 µM for NO production. TOPK-p38/JNK-IN-1 shows anti-inflammatory activities. TOPK-p38/JNK-IN-1 also inhibits phosphorylate downstream related proteins and avoids degradation of TOPK .
    TOPK-p38/JNK-IN-1
  • HY-13001
    Quizartinib
    25+ Cited Publications

    AC220

    		 FLT3 Ligands for Target Protein for PROTAC Apoptosis Autophagy Cancer
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
    Quizartinib
  • HY-103352
    L-006235

    L-235

    		 Cathepsin Metabolic Disease
    L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss .
    L-006235
  • HY-A0003
    Lenalidomide
    30+ Cited Publications

    CC-5013

    		 Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
    Lenalidomide
  • HY-A0003B
    Lenalidomide hemihydrate
    30+ Cited Publications

    CC-5013 hemihydrate

    		 Ligands for E3 Ligase Molecular Glues Apoptosis Cancer
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
    Lenalidomide hemihydrate
  • HY-A0003A
    Lenalidomide hydrochloride

    CC-5013 hydrochloride

    		 Ligands for E3 Ligase Molecular Glues Inflammation/Immunology Cancer
    Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
    Lenalidomide hydrochloride
  • HY-158113
    CBPD-409

    		Histone Acetyltransferase PROTACs Cancer
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
    CBPD-409
  • HY-158105
    ARV-393

    		PROTACs BCL6 Cancer
    ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. ARV-393 consists of ligand conjugates targeting BCL6 and the E3 ligase cereblon, respectively. ARV-393 has DC50 and GI50 values of <1 nM in multiple cell lines of diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL). ARV-393 also demonstrated considerable tumor suppressor activity in tumor xenograft models. ARV-393 is being studied to inhibit non-Hodgkin lymphoma.
    ARV-393
  • HY-10214
    SNX-2112
    2 Publications Verification

    PF-04928473

    		 HSP Autophagy Cancer
    SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively .
    SNX-2112
  • HY-A0003S
    Lenalidomide-d5

    CC-5013-d5

    		 Isotope-Labeled Compounds Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
    Lenalidomide-d5
  • HY-141645
    IMM-H007

    WS070117

    		 AMPK TGF-β Receptor NF-κB JNK AP-1 Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis .
    IMM-H007

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