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Gi

" in MedChemExpress (MCE) Product Catalog:

107

Inhibitors & Agonists

1

Fluorescent Dye

2

Biochemical Assay Reagents

12

Peptides

1

Inhibitory Antibodies

8

Natural
Products

9

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2

Isotope-Labeled Compounds

3

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1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W013712

    Potassium Channel Neurological Disease
    GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
    <em>GI</em>-530159
  • HY-19956
    GI254023X
    5+ Cited Publications

    Gi4023; SRI028594

    MMP Cancer
    GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
    <em>GI</em>254023X
  • HY-13670

    Gi147211; OSI-211

    Topoisomerase Cancer
    Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects .
    Lurtotecan
  • HY-11076

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
    <em>GI</em> 181771
  • HY-105074

    Gi262570; Gi262570X

    PPAR Metabolic Disease
    Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.
    Farglitazar
  • HY-13613
    Dutasteride
    2 Publications Verification

    GG 745; Gi 198745

    5 alpha Reductase Apoptosis Cancer
    Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
    Dutasteride
  • HY-13613R

    GG 745 (Standard); Gi 198745 (Standard)

    5 alpha Reductase Apoptosis Cancer
    Dutasteride (Standard) is the analytical standard of Dutasteride. This product is intended for research and analytical applications. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
    Dutasteride (Standard)
  • HY-101703

    Gi4747

    MMP Inflammation/Immunology
    Ro 31-9790 is a synthetic metalloproteinase (MMP) inhibitor.
    Ro 31-9790
  • HY-13613S

    GG 745-13C6; Gi 198745-13C6

    Apoptosis 5 alpha Reductase Cancer
    Dutasteride- 13C6 is the 13C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].
    Dutasteride-13C6
  • HY-137788

    nAChR Neurological Disease
    α-Conotoxin GI has high affinity for nAChR.α-Conotoxin GI is a short peptide toxin that can be isolated from the venom of Conus geographus.α-Conotoxin GI has the similar activity with neuromuscular blocking agent .
    α-Conotoxin <em>GI</em>
  • HY-156025

    Others Inflammation/Immunology
    HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
    HCAR2 agonist 1
  • HY-P1376

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
    G-Protein antagonist peptide
  • HY-P1376A

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
    G-Protein antagonist peptide TFA
  • HY-152136

    Bacterial Fungal Infection
    Antituberculosis agent-6 (compound 9g) is a potent antimycobacterial agent. Antituberculosis agent-6 shows significant activity against M. tuberculosis, with a MIC of 3.49 μM. Antituberculosis agent-6 also shows good antifungal activity against A. niger, with a MIC of 62.50 μM. Antituberculosis agent-6 shows high GI absorption .
    Antituberculosis agent-6
  • HY-146210

    EGFR Cancer
    EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
    EGFR-IN-50
  • HY-14427
    4E1RCat
    2 Publications Verification

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC50 an of ∼4 μM.
    4E1RCat
  • HY-149896

    Biochemical Assay Reagents Cancer
    Antitumor agent-107 (compound 5h) is an anticancer agent that shows excellent inhibitory activity against leukemia cell lines (GI50=0.32-1.34 μM). Antitumor agent-107 also shows antitumor activity against various other human cancer cell lines (GI50 range 0.35-9.43 μM) .
    Antitumor agent-107
  • HY-118762

    Cathepsin Cancer
    KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM . KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines .
    KGP94
  • HY-145266

    PARP Cancer
    OM-1700 is a potent tankyrase inhibitor with IC50s of 127 and 14 nM for tankyrase 1 and tankyrase 2, respectively. OM-1700 reduces cell growth in the colon cancer cell line COLO 320DM (GI50=650 nM) .
    OM-1700
  • HY-151426

    Apoptosis Cancer
    Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI50 value of 0.15 mM. Anticancer agent 83 reduces mitochondrial membrane potential and induces DNA damage to induces leukemia cells apoptosis .
    Anticancer agent 83
  • HY-N10307

    Fungal Bacterial Endogenous Metabolite Infection Cancer
    Anserinone B is an antifungal and antibacterial benzoquinone. Anserinone B causes radial growth reductions of 50% and 37% against S.fimicola and A. furfuraceus, respectively. Anserinones B also displays moderate cytotoxicity in the NCI’s 60 human tumor cell line panel (GI50=4.4 µg/mL) .
    Anserinone B
  • HY-143883

    Akt Cancer
    MS143 is a potent AKT degrader (DC50=46 nM and GI50=0.8 µM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth .
    MS143
  • HY-144872

    Others Cancer
    RJ-34, an aristolactam analogue, exhibits potent antitumor activities against a broad array of cancer cell lines with GI50 values in the subnanomolar range (GI50 <0.1 nM for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells) .
    RJ-34
  • HY-150204

    LPL Receptor Inflammation/Immunology
    ONO-0740556 is a potent Gi-coupled human lysophosphatidic acid receptor 1 (LPA1) agonist with an EC50 value of 0.26 nM .
    ONO-0740556
  • HY-10340
    Tirbanibulin
    5+ Cited Publications

    KX2-391; KX-01

    Src Microtubule/Tubulin Cancer
    Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
    Tirbanibulin
  • HY-10340A
    Tirbanibulin dihydrochloride
    5+ Cited Publications

    KX2-391 dihydrochloride; KX-01 dihydrochloride

    Src Microtubule/Tubulin Cancer
    Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
    Tirbanibulin dihydrochloride
  • HY-10340B
    Tirbanibulin Mesylate
    5+ Cited Publications

    KX2-391 Mesylate; KX01 Mesylate

    Src Microtubule/Tubulin Cancer
    Tirbanibulin Mesylate (KX2-391 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
    Tirbanibulin Mesylate
  • HY-115933

    EGFR Raf Cancer
    EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAF V600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity .
    EGFR/BRAF-IN-1
  • HY-157497

    Bcr-Abl Src Autophagy Apoptosis Cancer
    DA5-HTL is a compound combined dasatinib with HaloTag system efficiently inhibits the growth of the cancer cells with GI50 of 1.923 nM .
    DA5-HTL
  • HY-145864

    VEGFR Cancer
    VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent VEGFR-2 inhibitor with an IC50 of 0.037 µM. VEGFR-2-IN-12 shows high growth inhibition against MCF-7 cells (GI50=1.6 µM). VEGFR-2-IN-12 has antitumor activity .
    VEGFR-2-IN-12
  • HY-131339

    Aurora Kinase Cancer
    SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC) .
    SP-96
  • HY-144310

    Oxidative Phosphorylation Mitochondrial Metabolism Cancer
    DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer .
    DX3-213B
  • HY-151872

    HDAC Ferroptosis Cancer
    HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HDAC-IN-48
  • HY-B0790

    Apoptosis Cancer
    TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells .
    TAI-1
  • HY-137849

    PARP Cancer
    RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
    RK-582
  • HY-B1714A

    Others Cancer
    NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
    NSC 601980
  • HY-101213
    OSW-1
    1 Publications Verification

    OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.
    OSW-1
  • HY-P5358

    Protease Activated Receptor (PAR) Others
    YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
    YFLLRNP
  • HY-160129

    ML-970; AS-I-145; NSC 716970

    Nucleoside Antimetabolite/Analog Cancer
    Centanamycin (ML-970; AS-I-145; NSC 716970) is a novel DNA-binding agent, and shows cytotoxic activity, with an average GI50 of 34 nM in NCI-60 cell line screening .
    Centanamycin
  • HY-150550

    COX Inflammation/Immunology
    COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile .
    COX-2-IN-26
  • HY-100816
    Rbin-1
    2 Publications Verification

    Ribozinoindole-1

    Phosphatase Metabolic Disease
    Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
    Rbin-1
  • HY-153738

    ERK Cancer
    ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
    ERK1/2 inhibitor 9
  • HY-B1714

    Others Cancer
    NSC 601980 analog is the analog of the NSC601980, NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
    NSC 601980 analog
  • HY-111425

    Microtubule/Tubulin Apoptosis Cancer
    SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells .
    SSE15206
  • HY-149986

    Parasite Infection
    Antitrypanosomal agent 13 (compound 4b) is a potent antitrypanosomal agent. Antitrypanosomal agent 13 has trypanocidal and cytotoxic activity with GI50 values of 0.18 and 8.4 μM for T. brucei and HL-60, respectively .
    Antitrypanosomal agent 13
  • HY-110202

    Adenosine Receptor Neurological Disease Inflammation/Immunology
    MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis .
    MRS5698
  • HY-147032

    Deubiquitinase Cancer
    USP8-IN-1 is a USP8 inhibitor with an IC50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI50 of 82.04 μM (CN111138358A; U10) .
    USP8-IN-1
  • HY-N3443

    Others Cancer
    Jolkinol A is a natural product that can be found in Euphorbia pubescens. Jolkinol A inhibits cell growth with GI50s of 95.3, 57.3, >100 µM for MCF-7, NCI-460, SF-268 cells, respectively .
    Jolkinol A
  • HY-N12200

    Others Cancer
    Mollicellin I (compound 1) is a depsidone. The growth inhibitory activity of Mollicellin I on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines is not significant, with GI50s >10 μg/mL .
    Mollicellin I
  • HY-112779

    Others Infection
    Pertussis Toxin is a protein-based AB5-type exotoxin produced by the bacterium Bordetella pertussis, which causes whooping cough. Pertussis Toxin inhibits G protein-coupled receptor (GPR) signaling through Gi proteins .
    Pertussis Toxin

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