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Folding

" in MedChemExpress (MCE) Product Catalog:

1356

Inhibitors & Agonists

3

Screening Libraries

11

Fluorescent Dye

122

Biochemical Assay Reagents

63

Peptides

2

MCE Kits

3

Inhibitory Antibodies

28

Natural
Products

1

Recombinant Proteins

39

Isotope-Labeled Compounds

11

Click Chemistry

4

Oligonucleotides

4

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16578
    GW9662
    205+ Cited Publications

    		 PPAR Cancer
    GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
    GW9662
  • HY-12750
    AZD3965
    75+ Cited Publications

    		 Monocarboxylate Transporter Cancer
    AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, showing 6-fold selectivity over MCT2.
    AZD3965
  • HY-15150
    Bemcentinib
    60+ Cited Publications

    R428; BGB324

    		 TAM Receptor Cancer
    Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer .
    Bemcentinib
  • HY-50094
    Pictilisib
    65+ Cited Publications

    GDC-0941

    		 PI3K Autophagy Apoptosis Cancer
    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
    Pictilisib
  • HY-13271A
    Tubastatin A
    35+ Cited Publications

    		 Beta-lactamase HDAC Autophagy Apoptosis Cancer
    Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
    Tubastatin A
  • HY-103456
    PHTPP
    25+ Cited Publications

    		 Estrogen Receptor/ERR Cancer
    PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα .
    PHTPP
  • HY-19522
    Seladelpar
    1 Publications Verification

    MBX-8025; RWJ-800025

    		 PPAR Metabolic Disease
    Seladelpar (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM. Seladelpar shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar can be used for the study of primary biliary cholangitis .
    Seladelpar
  • HY-139609
    Camonsertib
    2 Publications Verification

    RP-3500; ATR inhibitor 4

    		 ATM/ATR mTOR Cancer
    Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
    Camonsertib
  • HY-15224
    PCI-34051
    25+ Cited Publications

    		 HDAC Apoptosis Cancer
    PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.
    PCI-34051
  • HY-12661A
    AMG PERK 44
    5+ Cited Publications

    		 PERK Autophagy Cancer
    AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy .
    AMG PERK 44
  • HY-100256
    Trifarotene

    CD5789

    		 RAR/RXR Autophagy Inflammation/Immunology
    Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ～65-fold and ～16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively .
    Trifarotene
  • HY-122882
    HOIPIN-8
    4 Publications Verification

    		 E1/E2/E3 Enzyme Inflammation/Immunology
    HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC .
    HOIPIN-8
  • HY-13271
    Tubastatin A Hydrochloride
    35+ Cited Publications

    Tubastatin A HCl; TSA HCl

    		 Beta-lactamase HDAC Autophagy Apoptosis Cancer
    Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
    Tubastatin A Hydrochloride
  • HY-111925
    BI-749327
    15+ Cited Publications

    		 TRP Channel Cardiovascular Disease
    BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
    BI-749327
  • HY-12076
    BMS 777607
    10+ Cited Publications

    BMS 817378

    		 c-Met/HGFR TAM Receptor Cancer
    BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases .
    BMS 777607
  • HY-10889
    Preladenant
    5+ Cited Publications

    SCH-420814

    		 Adenosine Receptor Neurological Disease Cancer
    Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
    Preladenant
  • HY-50098
    Mardepodect
    3 Publications Verification

    PF-2545920

    		 Phosphodiesterase (PDE) Neurological Disease Cancer
    Mardepodect is a potent, selective orally active, and brain-penetrant PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs .
    Mardepodect
  • HY-18705
    Azoramide
    5+ Cited Publications

    		 Apoptosis Reactive Oxygen Species (ROS) Caspase Bcl-2 Family Mitochondrial Metabolism Endocrinology
    Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity .
    Azoramide
  • HY-112724
    Ivarmacitinib

    SHR0302

    		 JAK Apoptosis Inflammation/Immunology Cancer
    Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
    Ivarmacitinib
  • HY-15245
    GSK2636771
    5+ Cited Publications

    		 PI3K Cancer
    GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
    GSK2636771
  • HY-136557A
    AFM32a hydrochloride
    2 Publications Verification

    PAD2-IN-1 hydrochloride

    		 Protein Arginine Deiminase Inflammation/Immunology Cancer
    AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .
    AFM32a hydrochloride
  • HY-16997
    Itacitinib
    20+ Cited Publications

    INCB039110

    		 JAK Cancer
    Itacitinib (INCB039110) is an orally active and selective inhibitor of JAK1 with an IC50 of 2 nM for human JAK1. Itacitinib shows >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis .
    Itacitinib
  • HY-136979
    RBN012759
    10+ Cited Publications

    		 PARP Inflammation/Immunology Cancer
    RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants .
    RBN012759
  • HY-13227
    SD-208
    5+ Cited Publications

    		 TGF-β Receptor Cancer
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
    SD-208
  • HY-15797
    UNC2250
    4 Publications Verification

    		 TAM Receptor Cancer
    UNC2250 is a potent and selective Mer inhibitor with an IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
    UNC2250
  • HY-126666
    PNU-159682 carboxylic acid

    		ADC Payload Inflammation/Immunology Cancer
    PNU-159682 carboxylic acid (Compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response .
    PNU-159682 carboxylic acid
  • HY-16978
    TG6-10-1
    5+ Cited Publications

    		 5-HT Receptor Prostaglandin Receptor Neurological Disease Endocrinology
    TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors .
    TG6-10-1
  • HY-177512
    MSC778

    		FLAP Cancer
    MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib (HY-10619) to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer .
    MSC778
  • HY-N2229
    Rhapontigenin
    3 Publications Verification

    		 Cytochrome P450 Fungal Bacterial Infection Inflammation/Immunology Cancer
    Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50  = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively .
    Rhapontigenin
  • HY-15557
    AZ20
    5+ Cited Publications

    		 ATM/ATR Cancer
    AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
    AZ20
  • HY-13260
    CCT128930
    5+ Cited Publications

    		 Akt Autophagy Apoptosis Cancer
    CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity.
    CCT128930
  • HY-10251
    BMS-599626
    3 Publications Verification

    AC480

    		 EGFR Cancer
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
    BMS-599626
  • HY-14339
    Intepirdine
    2 Publications Verification

    SB-742457; GSK-742457; RVT-101

    		 5-HT Receptor Neurological Disease
    Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.
    Intepirdine
  • HY-20180
    Pictilisib dimethanesulfonate
    65+ Cited Publications

    GDC-0941 dimethanesulfonate ; GDC-0941 (2 MeSO3H salt)

    		 PI3K Autophagy Apoptosis Cancer
    Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
    Pictilisib dimethanesulfonate
  • HY-10472
    LY2811376
    10+ Cited Publications

    		 Beta-secretase Neurological Disease
    LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
    LY2811376
  • HY-107625A
    SNAP 94847 hydrochloride
    2 Publications Verification

    		 MCHR1 (GPR24) Neurological Disease
    SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
    SNAP 94847 hydrochloride
  • HY-15555
    EPZ005687
    5 Publications Verification

    		 Histone Methyltransferase Cancer
    EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
    EPZ005687
  • HY-13531
    AS-604850
    1 Publications Verification

    		 PI3K Cancer
    AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
    AS-604850
  • HY-119939
    CHDI-390576
    1 Publications Verification

    CHDI00390576

    		 HDAC Cancer
    CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
    CHDI-390576
  • HY-10871
    Otenabant
    2 Publications Verification

    CP-945598

    		 Cannabinoid Receptor Metabolic Disease
    Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.
    Otenabant
  • HY-W040230
    Acrylodan

    		Fluorescent Dye Others
    Acrylodan, reacted with thiols, is sensitive to the local environmental dipolarity and dynamics within the binding pocket surrounding Cys 34 .
    Acrylodan
  • HY-50094R
    Pictilisib (Standard)

    GDC-0941 (Standard)

    		 PI3K Autophagy Apoptosis Reference Standards Cancer
    Pictilisib (Standard) is the analytical standard of Pictilisib. This product is intended for research and analytical applications. Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
    Pictilisib (Standard)
  • HY-152153
    GRP78-IN-3

    		HSP Cancer
    GRP78-IN-3 (Compound 8) is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM) .
    GRP78-IN-3
  • HY-12010
    BMS-599626 Hydrochloride
    3 Publications Verification

    AC480 Hydrochloride

    		 EGFR Cancer
    BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
    BMS-599626 Hydrochloride
  • HY-19522A
    Seladelpar sodium
    1 Publications Verification

    MBX-8025 sodium; RWJ-800025 sodium

    		 PPAR Metabolic Disease Inflammation/Immunology
    Seladelpar (MBX-8025) sodium salt is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM. Seladelpar sodium salt shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar sodium salt hydrochloride can be used for the study of primary biliary cholangitis .
    Seladelpar sodium
  • HY-P1029
    MLCK inhibitor peptide 18
    5+ Cited Publications

    		 Myosin CaMK Autophagy Others
    MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC50 of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations.
    MLCK inhibitor peptide 18
  • HY-12845
    UNC2400

    		Histone Methyltransferase Autophagy Cancer
    UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies .
    UNC2400
  • HY-109562A
    CCG258208 hydrochloride
    1 Publications Verification

    GRK2-IN-1 hydrochloride

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research .
    CCG258208 hydrochloride
  • HY-133998
    SIRT-IN-3
    1 Publications Verification

    		 Sirtuin Cancer
    SIRT-IN-3 is a potent SIRT inhibitor, with an IC50 of 17 μM for SIRT1. SIRT-IN-3 shows about 4-fold and 14-fold selectivity for SIRT1 over SIRT2 and SIRT3, respectively (IC50 of 74 μM and 235 μM for SIRT2 and SIRT3, respectively) .
    SIRT-IN-3
  • HY-139826
    CuATSP

    		Ferroptosis Neurological Disease
    CuATSP, a potent inhibitor of ferroptotic cell death, is almost 20-fold more potent than CuATSM.
    CuATSP

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