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Gi Inhibitors

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65

Inhibitors & Agonists

1

Biochemical Assay Reagents

5

Peptides

3

Natural
Products

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-118762
    KGP94

    		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-146210
    EGFR-IN-50

    		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-145266
    OM-1700

    		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
    Anticancer agent 83

    		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-150550
    COX-2-IN-26

    		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-19956
    GI254023X
    Maximum Cited Publications
    10 Publications Verification

    Gi4023; SRI028594

    		 MMP Cancer
    GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
    GI254023X
  • HY-13670
    Lurtotecan

    Gi147211; OSI-211

    		 Topoisomerase Cancer
    Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects .
    Lurtotecan
  • 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/BRAF-IN-1

    		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
    DA5-HTL

    		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-151872
    HDAC-IN-48

    		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-137849
    RK-582

    		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-B0790
    TAI-1

    		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-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-145864
    VEGFR-2-IN-12

    		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-153738
    ERK1/2 inhibitor 9

    		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 <em>inhibitor</em> 9
  • HY-131339
    SP-96

    		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
    DX3-213B

    		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-B1714A
    NSC 601980

    		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-P1376
    G-Protein antagonist peptide

    		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-161385
    Topoisomerase I inhibitor 16

    		Topoisomerase Cancer
    Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
    Topoisomerase I <em>inhibitor</em> 16
  • HY-147032
    USP8-IN-1

    		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-110156
    YZ9

    		Others Cancer
    Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM. Y29 also inhibits the HeLa cell growth with a GI50 of 2.7 µM .
    YZ9
  • HY-156378
    Aurora A inhibitor 3

    		Aurora Kinase Cancer
    Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC50 value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI50 values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively .
    Aurora A <em>inhibitor</em> 3
  • HY-B1714
    NSC 601980 analog

    		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
    SSE15206

    		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-149901
    USP8-IN-2

    		Deubiquitinase Cancer
    USP8-IN-2 (Compd U52) is a deubiquitinase USP8 inhibitor with an IC50 value of 6.0 μM. USP8-IN-2 also inhibits the proliferation of H1957 cells with an GI50 value of 24.93 μM, respectively .
    USP8-IN-2
  • HY-N3443
    Jolkinol A

    		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-112779
    Pertussis Toxin

    		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
  • HY-128602
    c-Kit-IN-2

    		c-Kit Cancer
    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively .
    c-Kit-IN-2
  • HY-149902
    USP8-IN-3

    		Deubiquitinase Cancer
    USP8-IN-3 (Compd U51) is a deubiquitinase USP8 inhibitor with an IC50 value of 4.0 μM. USP8-IN-3 also inhibits the proliferation of GH3 and H1957 cells with GI50s of 37.03 μM and 6.01 μM, respectively .
    USP8-IN-3
  • HY-N7654
    (-)-Epipodophyllotoxin

    		Apoptosis Cancer
    (-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro .
    (-)-Epipodophyllotoxin
  • HY-152524
    Androgen receptor antagonist 7

    		Androgen Receptor Cancer
    Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM .
    Androgen receptor antagonist 7
  • HY-149361
    VEGFR2-IN-4

    		VEGFR Inflammation/Immunology
    VEGFR2-IN-4 (compound 25) is a potent and selective VEGFR2 kinase inhibitor, with a GI50 of 0.7 nM. VEGFR2-IN-4 shows anti-angiogenic effect. VEGFR2-IN-4 can be used for the research of rheumatoid arthritis .
    VEGFR2-IN-4
  • HY-157850
    BP-M345

    		Others Cancer
    BP-M345 (compound 5) is a potent, cancer cell-targeting antiproliferative agent that exhibits low toxicity to non-tumor cells. BP-M345 inhibits cancer cell proliferation with a GI50 value ranging from 0.17 to 0.45 μM .
    BP-M345
  • HY-101122
    LX2761

    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract .
    LX2761
  • HY-P3839
    Nocistatin

    		Opioid Receptor Neurological Disease
    Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
    Nocistatin
  • HY-153811
    YAP-TEAD-IN-3

    		YAP Cancer
    YAP-TEAD-IN-3 (compound 155) is a YAP/TAZ-TEAD inhibitor. YAP-TEAD-IN-3 inhibits Avi-humanTEAD 4217-434 with an IC50 value of 9 nM. YAP-TEAD-IN-3 also inhibits NCI-H2052 with an GI50 of 0.048 μM (cell proliferation)，and an IC50 of 0.048 μM (YAP reporter gene expression)，respsectively .
    YAP-TEAD-IN-3
  • HY-163278
    Lck-IN-2

    		Src Apoptosis Cancer
    Lck-IN-2 (compound 12a) is an inhibitor of Lymphocyte-specific protein tyrosine kinase (Lck) with IC50 of 10.6 nM. Lck-IN-2 reveals efficacy in colon cancer cells with GI50s of 0.24-1.26 μM. Lck-IN-2 exhibits an apoptotic effect in Colo201 cells .
    Lck-IN-2
  • HY-157871
    TAK1-IN-5

    		MAP3K Cancer
    TAK1-IN-5 (Compound 26) is an inhibitor of the transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. TAK1-IN-5 can inhibit the growth of MPC-11 and H929 cells with a GI50 lower than 30 nM. TAK1-IN-5 can be used in the study of multiple myeloma .
    TAK1-IN-5
  • HY-145426
    MPT0B390

    		HDAC Cancer
    MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
    MPT0B390
  • HY-160613
    EGFR/HER2-IN-11

    		EGFR Cancer
    EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM .
    EGFR/HER2-IN-11
  • HY-P1376A
    G-Protein antagonist peptide TFA

    		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-156003
    HDAC-IN-64

    		HDAC Cancer
    HDAC-IN-64 (Compound 13) is a HDAC inhibitor. HDAC-IN-64 inhibits HDAC4/5/6/7/9 with IC50s of 24, 45, 85, 31, 37 nM. HDAC-IN-64 has anti-proliferative activity and anti-migration properties on prostate cancer (PCA) cells. HDAC-IN-64 inhibits LNCaP and RWPE-1 cell growth with GI50 of 0.32 and 1.1 μM respectively .
    HDAC-IN-64
  • HY-103712A
    Samuraciclib hydrochloride
    5 Publications Verification

    CT7001 hydrochloride; ICEC0942 hydrochloride

    		 CDK Apoptosis Cancer
    Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
    Samuraciclib hydrochloride
  • HY-103712B
    Samuraciclib hydrochloride hydrate
    5 Publications Verification

    CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate

    		 CDK Apoptosis Cancer
    Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
    Samuraciclib hydrochloride hydrate
  • HY-103712
    Samuraciclib

    CT7001; ICEC0942

    		 CDK Apoptosis Cancer
    Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects .
    Samuraciclib

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