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proteasomal

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63

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1

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1

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1

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7

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8

Isotope-Labeled Compounds

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-156437
    NBI-961

    		Apoptosis Ser/Thr Protease NEKs Mitosis Cancer
    NBI-961 is a potent NEK2 inhibitor that inhibits proteasomal degradation. NBI-961 induces G2/mitosis arrest and apoptosis in diffuse large B cell lymphoma (DLBCL) cells .
    NBI-961
  • HY-147174
    PROTAC_ERRα

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker .
    PROTAC_ERRα
  • HY-111518
    JH-XI-10-02
    1 Publications Verification

    		 PROTACs CDK Cancer
    JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19 .
    JH-XI-10-02
  • HY-10969
    Obatoclax Mesylate
    10+ Cited Publications

    GX15-070 Mesylate

    		 Bcl-2 Family Autophagy Parasite Infection Cancer
    Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
    Obatoclax Mesylate
  • HY-163814
    CDK2 degrader 1

    		PROTACs CDK Cancer
    CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker) .
    CDK2 degrader 1
  • HY-108553
    Dihydroeponemycin

    		Proteasome Apoptosis Cancer
    Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis .
    Dihydroeponemycin
  • HY-P10007
    Z-Gly-Pro-Phe-Leu-CHO

    Z-GPFL-CHO

    		 Proteasome Cancer
    Z-Gly-Pro-Phe-Leu-CHO (Z-GPFL-CHO) is a tetrapeptide aldehyde that acts as a highly selective and potent proteasomal inhibitor (Ki = 1.5 µM for branched chain amino acid preferring, 2.3 µM for small neutral amino acid preferring, and 40.5 µM for chymotrypsin-like activities; IC50 = 3.1 µM for peptidyl-glutamyl peptide hydrolyzing activity) .
    Z-Gly-Pro-Phe-Leu-CHO
  • HY-P3414
    Proteasome-activating peptide 1

    		Proteasome Neurological Disease
    Proteasome-activating peptide 1 is a peptide, which increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis .
    Proteasome-activating peptide 1
  • HY-10969A
    Obatoclax

    GX15-070

    		 Bcl-2 Family Autophagy Parasite Infection Cancer
    Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
    Obatoclax
  • HY-151886
    NU223612

    		PROTACs Indoleamine 2,3-Dioxygenase (IDO) Neurological Disease Cancer
    NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB) .
    NU223612
  • HY-164487
    JBJ-08-178-01

    		Proteasome Cancer
    JBJ-08-178-01 is a mutant-selective tyrosine kinase inhibitor against human epidermal growth factor receptor 2 (HER2) with an antitumoral activity. JBJ-08-178-01 reduces both the kinase activity and protein levels of HER2 by inducing proteasomal degradation of the receptor in lung cancer. JBJ-08-178-01 is promising for research of non-small-cell lung cancer .
    JBJ-08-178-01
  • HY-P3414A
    Proteasome-activating peptide 1 TFA
    1 Publications Verification

    		 Proteasome Neurological Disease
    Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis .
    Proteasome-activating peptide 1 TFA
  • HY-W181530
    NCT02

    		Molecular Glues CDK Apoptosis Ligands for E3 Ligase Cancer
    NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
    NCT02
  • HY-P4348
    MeOSuc-Gly-Leu-Phe-AMC

    		Proteasome Others
    MeOSuc-Gly-Leu-Phe-AMC is a peptide substrate of proteasomal .
    MeOSuc-Gly-Leu-Phe-AMC
  • HY-10585
    Valproic acid
    Maximum Cited Publications
    43 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. Valproic acid 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 epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
    Valproic acid
  • HY-10585A
    Valproic acid sodium
    Maximum Cited Publications
    43 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-10585AG
    Valproic acid (sodium)

    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-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-10585AR
    Valproic acid sodium (Standard)

    		Organoid HDAC Autophagy Mitophagy HIV Notch Apoptosis Endogenous Metabolite Infection Neurological Disease Metabolic Disease Cancer
    Valproic acid (sodium) (Standard) is the analytical standard of Valproic acid (sodium). This product is intended for research and analytical applications. 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 (Standard)
  • HY-128577
    NIC3

    		BTB/POZ Family Cancer
    NIC3 is a selective nucleus accumbens-associated protein-1 (NAC1) inhibitor, binds to the conserved Leu-90 of NAC1, prevents its homodimerization, and leads to proteasomal NAC1 degradation. Anti-cancer activity .
    NIC3
  • HY-130800
    Eragidomide
    2 Publications Verification

    CC-90009

    		 Ligands for E3 Ligase Molecular Glues Apoptosis Inflammation/Immunology Cancer
    Eragidomide (CC-90009) is a first-in-class GSPT1-selective cereblon (CRBN) E3 ligase modulator, acts as a molecular glue. Eragidomide coopts the CRL4 CRBN to selectively target GSPT1 for ubiquitination and proteasomal degradation .
    Eragidomide
  • HY-176070
    HRG038

    		Epigenetic Reader Domain Cancer
    HRG038 is a selective covalent BRD4 degrader. HRG038 binds covalently to the E3 ubiquitin ligase CUL4 DCAF16, recruiting it to BRD4, leading to the ubiquitination and subsequent proteasomal degradation of BRD4. HRG038 is promising for research of cancers .
    HRG038
  • HY-173097
    (S,R,S)-AHPC-Boc derivative 1

    VH032-Boc derivative 1

    		 MALT1 Cancer
    (S,R,S)-AHPC-Boc derivative 1 (Compound 80-9; VH032-Boc derivative 1) is a selective proteasomal degrader targeting MALT1, which recruits the E3 ubiquitin ligase CRBN to form a ternary complex with MALT1, leading to ubiquitination and subsequent proteasomal degradation of MALT1. (S,R,S)-AHPC-Boc derivative 1 inhibits the NF-κB signaling pathway by disrupting the CBM complex, demonstrating potential for inducing apoptosis in ABC-DLBCL cells. (S,R,S)-AHPC-Boc derivative 1 is promising for research of MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL) .
    (S,R,S)-AHPC-Boc derivative 1
  • HY-130257
    CP5V

    		PROTACs Cancer
    CP5V is a PROTAC connected by ligands for von Hippel-Lindau and CDK, which specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation. CP5V induces mitotic inhibition and suppresses cancer cell proliferation .
    CP5V
  • HY-13822
    SKI II
    5 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-W054146
    RAMB4
    1 Publications Verification

    		 Proteasome Cancer
    RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity .
    RAMB4
  • HY-157439
    SARS-CoV-2-IN-72

    		SARS-CoV Infection
    SARS-CoV-2-IN-72 (compound 12) is a potent allosteric inhibitor of the SARS-COV-2 papain-like protease domain that can trigger the degradation of NSP3 .
    SARS-CoV-2-IN-72
  • HY-19979
    RCM-1
    4 Publications Verification

    		 DNA/RNA Synthesis Cancer
    RCM-1 is a forkhead box M1 (FOXM1) inhibitor with an EC50 of 0.72 μM in U2OS cells. RCM-1 blocks the nuclear localization and increased the proteasomal degradation of FOXM1. RCM-1 can be used for asthma and other chronic airway diseases research .
    RCM-1
  • HY-W014507
    9,10-Phenanthrenequinone

    		Claudin Cancer
    9,10-Phenanthrenequinone is an inhibitor of claudin-5/CLDN5 that induces apoptosis via a NO synthase/ROS-dependent mechanism. 9,10-Phenanthrenequinone also promotes endothelial barrier dysfunction by promoting caspase activation and DNA fragmentation, and reducing CLDN5 expression and proteasomal proteolysis .
    9,10-Phenanthrenequinone
  • HY-123587
    PR-924

    		Proteasome Apoptosis Cancer
    PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities .
    PR-924
  • HY-172595
    Apoptotic agent-5

    		Apoptosis E1/E2/E3 Enzyme Cancer
    Apoptotic agent-5 (5d) is an apoptotic agent. Apoptotic agent-5 inhibits the growth of triple-negative breast cancer cells. Apoptotic agent-5 attenuates proteasomal degradation via the ubiquitin-proteasome pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic .
    Apoptotic agent-5
  • HY-10585AS1
    Valproic acid-d14 sodium

    Sodium Valproate-d14 sodium

    		 Isotope-Labeled Compounds HDAC Autophagy Mitophagy HIV Notch Endogenous Metabolite Cancer
    Valproic acid-d14 (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an 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 salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
    Valproic acid-d14 sodium
  • HY-10585AS
    Valproic acid-d7 sodium

    Sodium Valproate-d7(sodium)

    		 Isotope-Labeled Compounds HDAC Autophagy Mitophagy HIV Notch Endogenous Metabolite Cancer
    Valproic acid-d7 (sodium) is the deuterium labeled Valproic acid (sodium salt). Valproic acid sodium salt (Sodium Valproate) is an 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 salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
    Valproic acid-d7 sodium
  • HY-P10714
    Ub4ix

    		Proteasome Apoptosis Deubiquitinase Cancer
    Ub4ix is a DUB/26S proteasome inhibitor. Ub4ix can protect K48-linked Ub chains from being chopped up by deubiquitinating enzymes (DUBs) and prevent the proteasomal degradation of Ub-tagged proteins. Ub4ix can reduce the viability of Hela cells and induce apoptosis, with an IC50 value of 1.6 μM .
    Ub4ix
  • HY-146237
    Golcadomide

    CC-99282

    		 Ligands for E3 Ligase Molecular Glues Cancer
    Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL) .
    Golcadomide
  • HY-161779
    PLX-3618

    		Molecular Glues Epigenetic Reader Domain Apoptosis Cancer
    PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models .
    PLX-3618
  • HY-173274
    CB039

    		Molecular Glues Cancer
    CB039 is a selective a molecular glue degrader that targets RBM39 (RNA-binding protein 39). CB039 promotes the formation of a ternary complex between RBM39 and the E3 ubiquitin ligase CUL4-DCAF15, leading to proteasomal degradation of RBM39. CB039 is promising for research of cancers with RBM39 dependency, such as acute myeloid leukemia (AML) and ovarian cancer .
    CB039
  • HY-N6769
    Radicicol
    3 Publications Verification

    Monorden

    		 HSP Bacterial Antibiotic Parasite Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
    Radicicol
  • HY-10585S3
    Valproic acid-d4 sodium

    VPA-d4 sodium; 2-Propylpentanoic Acid-d4 sodium

    		 Isotope-Labeled Compounds HDAC Autophagy Mitophagy HIV Notch Endogenous Metabolite Cancer
    Valproic acid-d4 (sodium) is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an 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 sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
    Valproic acid-d4 sodium
  • HY-10585S4
    Valproic acid-d4-1

    VPA-d4-1; 2-Propylpentanoic Acid-d4-1

    		 Isotope-Labeled Compounds HDAC Autophagy Mitophagy HIV Notch Endogenous Metabolite Cancer
    Valproic acid-d4-1 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an 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 sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
    Valproic acid-d4-1
  • HY-10585S2
    Valproic acid-d15

    VPA-d15; 2-Propylpentanoic Acid-d15

    		 HDAC Autophagy Mitophagy HIV Notch Endogenous Metabolite Cancer
    Valproic acid-d15 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an 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 sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
    Valproic acid-d15
  • HY-123587A
    (R)-PR-924

    		Apoptosis Cancer
    (R)-PR-924 is the isomer of PR-924 (HY-123587), and can be used as an experimental control. PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities .
    (R)-PR-924
  • HY-10585S
    Valproic acid-d4
    1 Publications Verification

    VPA-d4; 2-Propylpentanoic Acid-d4

    		 HDAC Autophagy Mitophagy HIV Notch Endogenous Metabolite Cancer
    Valproic acid-d4 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an 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 sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
    Valproic acid-d4
  • HY-10585S1
    Valproic acid-d6

    VPA-d6; 2-Propylpentanoic Acid-d6

    		 HDAC Autophagy Mitophagy HIV Notch Endogenous Metabolite Cancer
    Valproic acid-d6 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an 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 sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
    Valproic acid-d6
  • HY-110078
    Eeyarestatin I
    5 Publications Verification

    		 p97 Apoptosis Cancer
    Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects .
    Eeyarestatin I
  • HY-P5910
    Azurin p28 peptide

    		MDM-2/p53 Apoptosis Cancer
    Azurin p28 peptide is a tumor-penetrated antitumor peptide. Azurin p28 peptide redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide induces apoptosis or cell cycle arrest. Azurin p28 peptide inhibits p53-positive tumor growths. Azurin p28 peptide shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
    Azurin p28 peptide
  • HY-16591
    Birinapant
    30+ Cited Publications

    TL32711

    		 IAP Apoptosis HIV Cancer
    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
    Birinapant
  • HY-P5910A
    Azurin p28 peptide TFA

    		MDM-2/p53 Apoptosis Cancer
    Azurin p28 peptide TFA is a tumor-penetrated antitumor peptide. Azurin p28 peptide TFA redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide TFA induces apoptosis or cell cycle arrest. Azurin p28 peptide TFA inhibits p53-positive tumor growths. Azurin p28 peptide TFA shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
    Azurin p28 peptide TFA
  • HY-125593
    Dasminapant

    APG-1387

    		 IAP Apoptosis Cancer
    Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma .
    Dasminapant
  • HY-171830
    MS105

    YX39-105

    		 PROTACs Tyrosinase Apoptosis Cancer
    MS105 is an orally active and selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. MS105 recruits VHL E3 ligase via the VHL ligand moiety to promote PTK6 ubiquitination and proteasomal degradation, inhibiting breast cancer cell proliferation, migration, and inducing apoptosis. MS105 is promising for research of breast cancer. (Pink: BRK inhibitor P21d hydrochloride (HY-115514); Black: linker (HY-W105727); Blue: (S,R,S)-AHPC (HY-125845)) .
    MS105

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