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NCI

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110

Inhibitors & Agonists

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1

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-156060

    Toll-like Receptor (TLR) Inflammation/Immunology
    NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases .
    NCI126224
  • HY-U00095

    NCI 329680; ZINC01574758

    Others Cancer
    Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
    Hepsulfam
  • HY-156215

    HCV Infection
    NCI-B16 is a small molecule RNA binder and inhibits HCV viral replication .
    NCI-B16
  • HY-D1161

    NCI 240899

    Fluorescent Dye Neurological Disease
    True Blue (NCI 240899) is a fluorescent dye, as neuronal retrograde tracer (excitation wavelength 395-425 nm, barrier filter 450 nm). True Blue can label neuron and has no effects on neuronal survival .
    True Blue
  • HY-U00155

    NSC172112; NSC268497

    DNA Alkylator/Crosslinker Cancer
    NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
    NCI172112
  • HY-N0840
    Bruceantin
    1 Publications Verification

    (-)-Bruceantin; NCI165563; NSC165563

    Others Cancer
    Bruceantin(NSC165563) is first isolated from Brucea javanica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
    Bruceantin
  • HY-157522

    Phosphodiesterase (PDE) Cancer
    NCI-14465 is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP1) inhibitor with an IC 50 of 26.4 μM. NCI-14465 can be used in cancer research .
    NCI-14465
  • HY-123597

    DDUG; NCI C04808

    Autophagy Checkpoint Kinase (Chk) Cancer
    NSC 109555 (DDUG; NCI C04808) is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM). NSC 109555 also inhibits Brk, c-Met, IGFR, and LCK with IC50 values ??of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM), and also inhibits the growth of L1210 leukemia cells and induces autophagy in vitro. NSC 109555 enhances Gemcitabine (HY-17026)-induced reactive oxygen species (ROS) production in MIA PaCa-2 cells.
    NSC 109555
  • HY-163000

    EGFR Cancer
    EGFR-IN-129 (Compound 10b) is a potent and selective EGFR inhibitor, with an IC50 of 51.2 nM. EGFR-IN-129 exhibits broadest-spectrum antiproliferative activity against the NCI-tumor panel .
    EGFR-IN-129
  • 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-N8900

    Others Cancer
    Vernolide-B has cytoxicity (ED50s: 3.78, 5.88, 6.42 μg/mL for KB, NCI-661, and HeLa cells respectively). Vernolide B is sesquiterpene lactone that can be isolated from Vernonia cinerea .
    Vernolide B
  • 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-147728

    Microtubule/Tubulin Cancer
    Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
    Microtubule inhibitor 7
  • HY-147724

    Microtubule/Tubulin Cancer
    Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
    Microtubule inhibitor 3
  • HY-19797

    p97 Cancer
    ML241 is a potent, selective and competitive p97 ATPase inhibitor with an IC50 of 0.11 μM. ML241 can be used for the research of cancer .
    ML241
  • HY-125730

    Others Cancer
    Kibdelone A is a type of natural compound from the flavonoid family, and it has potential value as an anti-proliferative agent .
    Kibdelone A
  • HY-168093

    Ferroptosis Cancer
    Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
    Cetzole
  • 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-164384

    PI3K Akt mTOR Apoptosis Cancer
    DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
    DFX117
  • HY-101130
    PNU-74654
    Maximum Cited Publications
    10 Publications Verification

    Wnt β-catenin Apoptosis Cancer
    PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
    PNU-74654
  • HY-151394

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-33 is an inhibitor of [1,2]oxazoloisoindoles tubulin polymerization, exhibits high antiproliferative activity against the NCI panel .
    Tubulin polymerization-IN-33
  • HY-N2039

    Others Cancer
    20(R)-Ginsenoside Rg2 shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities .
    20(R)-Ginsenoside Rg2
  • HY-162787

    Adenosine Receptor Cancer
    Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .
    Adenosine receptor antagonist 5
  • HY-169476

    Drug Derivative Cancer
    Pyrrolidine linoleamide is a derivative of linoleic acid amide with anticancer activity. Pyrrolidine linoleamide exhibits antiproliferative activity against a range of cancer cell lines, with IC50 values of 12.0, 27.5, 7.7, 21.9, 36.6, 32.6, and 33.9 μg/mL against U251, MCF-7, NCI-ADR/RES, 786-0, NCI-H460, PC-3, and OVCAR-3 cell lines, respectively .
    Pyrrolidine linoleamide
  • HY-143296

    SphK Cancer
    SphK1-IN-1 (compound 48) is a SphK1 inhibitor with effective antitumor activity. SphK1-IN-1 inhibits SphK1 ATPase with an IC50 value of 4.02 μM. SphK1-IN-1 can be used for the research of cancer .
    SphK1-IN-1
  • HY-N12004

    Others Cancer
    19-Hydroxy-10-deacetylbaccatin III (compound 13) is a taxane with potential antitumor activity. 19-Hydroxy-10-deacetylbaccatin III has weak cytotoxicity against A498 and NCI-H226 cell lines. The study found that the inhibition rates of 30 μg/mL 19-Hydroxy-10-deacetylbaccatin III on A498, NCI-H226 and PC-3 were 16.6% and 32% respectively .
    19-Hydroxy-10-deacetylbaccatin III
  • HY-169299

    PARP Topoisomerase Apoptosis Cancer
    TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines .
    TOPOI/PARP-1-IN-2
  • HY-164033

    Ramnodigin

    Apoptosis Cancer
    HOE 689 (Ramnodigin) is an analog of Digitoxin (HY-B1357). HOE 689 exhibits cytotoxicity to lung cancer cells and induces apoptosis in cancer cell NCI-H460 with an IC50 of 52 nM .
    HOE 689
  • HY-148517
    AZD0095
    1 Publications Verification

    Monocarboxylate Transporter Cancer
    AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .
    AZD0095
  • HY-N10877

    Others Cancer
    Chlorajapolide F is a nature product that could be isolated from the aerial part of Chloranthus japonicas. Chlorajapolide F has low cytotoxic activity against NCI-H460 and SMMC-7721 cell lines .
    Chlorajapolide F
  • HY-N12231

    Antibiotic Bacterial Lipoxygenase Infection Cancer
    Carbazomycin B is a bacterial metabolite and can be isolated from Streptomyces. Carbazomycin B is an antifungal and antibacterial agent. Carbazomycin B inhibits 5-lipoxygenase (5-LO) activity in extract from RBL-1 cell with the IC50 Of 1.5 µM sup>[2]sup>[3]sup>[4].
    Carbazomycin B
  • HY-100555

    HSP Infection Cancer
    CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
    CH5138303
  • HY-139882

    Others Cancer
    Anticancer agent 16 exhibits good cytotoxic activity against HCT-116, NCI-H460, and SKOV3 cell lines with IC50 8.55 μΜ, 5.41 μΜ, and 6.4 μΜ, respectively.
    Anticancer agent 16
  • HY-147726

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
    Microtubule inhibitor 5
  • HY-147208

    YAP Cancer
    MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
    MSC-4106
  • HY-N10562

    P-glycoprotein Cancer
    Mutabilol (compound 1) is a potent p-glycoprotein (P-gp) regulator. Mutabilol is a nature product could be isolated from Plectranthus mutabilis leaves. Mutabilol increases the P-gp expression in NCI-H460/R cells .
    Mutabilol
  • HY-N7302

    Others Cancer
    Anthracophyllone is an aristolane sesquiterpene that can be isolated from the mushroom Anthracophyllum. Anthracophyllone has cytotoxicity against MCF-7, KB, NCI-H187, Vero cells (IC50: 32.97, 18.02, 15.17, 18.06 μM) .
    Anthracophyllone
  • HY-161173

    PROTACs Ras Cancer
    PROTAC SOS1 degrader-5 (compound 4) is a potent PROTAC SOS1 degrader, with the DC50 of 13 nM. PROTAC SOS1 degrader-5 strongly inhibits NCI-H358 cells proliferation with an IC50 of 5 nM .
    PROTAC SOS1 degrader-5
  • HY-147858A

    PROTACs Cancer
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
    PROTAC EGFR degrader 7 diTFA
  • HY-147703

    Aurora Kinase Cancer
    Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
    Aurora kinase inhibitor-9
  • HY-101567
    BMS-986158
    2 Publications Verification

    Epigenetic Reader Domain Cancer
    BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
    BMS-986158
  • HY-157085

    HSP Cancer
    BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice .
    BX-2819
  • HY-144337

    DNA Alkylator/Crosslinker Cancer
    DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
    DNA crosslinker 4 dihydrochloride
  • HY-115949

    Others Cancer
    Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively .
    Antitumor agent-47
  • HY-161614

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 44 (Compound 26r) is an inhibitor for tubullin. Tubulin inhibitor 44 exhibits cytotoxicity in cancer cells NCI-H460, BxPC-3 and HT-29, with IC50s of 0.96, 0.66 and 0.61 nM, respectively .
    Tubulin inhibitor 44
  • HY-W560574

    Xanthine Oxidase Cancer
    Xanthine oxidase-IN-14 (Compound 3f) is an inhibitor for xanthine oxidase, with IC50 >100 μM. Xanthine oxidase-IN-14 inhibits proliferations of cancer cells MCF-7, NCI-H460 and SF-268, with IC50 greater than 150 μM .
    Xanthine oxidase-IN-14
  • HY-157319

    PI3K Cancer
    PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
    PI3Kα-IN-15
  • HY-14389

    Microtubule/Tubulin Cancer
    LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM . LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research .
    LP-261
  • HY-145379

    Parasite Endogenous Metabolite Infection
    Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacterium tuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
    Miaosporone A
  • HY-157888

    SHP2 Phosphatase Cancer
    SHP2-IN-26 (Compound 4b) is a highly selective SHP2 allosteric inhibitor with a IC50 value of 3.2 nM. SHP2-IN-26 inhibits the phosphorylation of ERK and AKT in NCI-H358 cells. SHP2-IN-26 has antitumor activity .
    SHP2-IN-26

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