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Results for "

DLD1

" in MedChemExpress (MCE) Product Catalog:

45

Inhibitors & Agonists

1

Peptides

8

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-122312
    BAY-8002
    4 Publications Verification

    Monocarboxylate Transporter Cancer
    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity [1].
    BAY-8002
  • HY-177512

    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 [1].
    MSC778
  • HY-12794
    Vps34-PIK-III
    Maximum Cited Publications
    12 Publications Verification

    PI3K Autophagy Neurological Disease Cancer
    Vps34-PIK-III is an orally active and selective VPS34 inhibitor (IC50=18 nM). Vps34-PIK-III effectively inhibits autophagy and can be used as a molecular tool. vps34-PIK-III is also a PI3K inhibitor that inhibits the expression of genes in liver cancer stem cells (CSCs) [1] .
    Vps34-PIK-III
  • HY-N0447
    8-Gingerol
    5 Publications Verification

    TRP Channel Bacterial Apoptosis Autophagy STAT PERK EGFR PI3K Akt mTOR Caspase MMP Infection Cardiovascular Disease Inflammation/Immunology Cancer
    8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC50 value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.
    8-Gingerol
  • HY-148740

    DNA/RNA Synthesis Cancer
    Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity [1].
    Werner syndrome RecQ helicase-IN-3
  • HY-159480

    Src ATM/ATR Apoptosis mTOR AMPK Cancer
    AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC50: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases [1].
    AD1058
  • HY-46866

    Apoptosis Caspase PARP Metabolic Disease Inflammation/Immunology Cancer
    Isoegomaketone is an orally active apoptosis inducer and radiosensitizer. Isoegomaketone regulates multiple key signaling pathways such as PI3K/AKT/mTOR, NF-κB, MAPK, cleaves Caspase family proteins and PARP, and modulates Bax, AIF and endoplasmic reticulum stress proteins. Isoegomaketone also induces autophagy and keratinocyte proliferation, effectively reduces the levels of inflammatory factors and oxidative stress, inhibits adipocyte differentiation, and resensitizes TRAIL-resistant cancer cells. Isoegomaketone can be applied to research related to colorectal cancer, melanoma, lung cancer, prostate cancer, liver cancer, as well as rheumatoid arthritis and obesity [1] .
    Isoegomaketone
  • HY-157334
    DEG-77
    1 Publications Verification

    Molecular Glues Casein Kinase IKZF Family Bcl-2 Family CDK Apoptosis Cancer
    DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC50 values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.
    DEG-77
  • HY-139691

    KLF Cancer
    SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells) [1].
    SR15006
  • HY-161430

    DNA/RNA Synthesis Apoptosis Cancer
    RTx-161 is an allosteric Polθ polymerase inhibitor with an IC50 value of 4.1 nM. RTx-161 selectively kills HR-deficient cancer cells and suppresses PARP inhibitor (PARPi) resistance in multiple genetic backgrounds, including HR-proficient cells. Additionally, RTx-161 can induce apoptosis [1].
    RTx-161
  • HY-P10810

    Wnt β-catenin Cancer
    QPH-FR is a LGR5 inhibitor. QPH-FR competitively binds to LGR5 and prevents the formation of the LGR5/RSPO1 complex. QPH-FR promotes RNF43/ZNRF3-mediated ubiquitination of FZD receptors, inhibits the Wnt β-catenin signaling pathway, and reduces the stemness of colorectal cancer cells. QPH-FR is applicable to relevant research on colorectal cancer [1].
    QPH-FR
  • HY-114977

    DNA/RNA Synthesis Apoptosis Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    Avenanthramide A is an orally active phytoalexin that targets the RNA helicase DDX3 with a KD of 8.8 μM. Avenanthramide A induces mitochondrial swelling and increased ROS production, and triggers apoptosis in CRC cells. Avenanthramide A inhibits smooth muscle cell proliferation and enhances nitric oxide production. Avenanthramide A can be used in research on colorectal cancer and atherosclerosis [1] .
    Avenanthramide A
  • HY-109963

    Histone Methyltransferase Cancer
    PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies [1].
    PR5-LL-CM01
  • HY-119257
    ABT-100
    1 Publications Verification

    Farnesyl Transferase Apoptosis Cancer
    ABT-100, a chemical probe, is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity [1].
    ABT-100
  • HY-106789

    CS-684

    Bacterial Infection Inflammation/Immunology Cancer
    Plaunotol is an orally active acyclic diterpene alcohol. Plaunotol has antibacterial activity against Helicobacter pylori which causes peptic ulcer [1]. Plaunotol inhibits tumor angiogenesis and cell proliferation. Plaunotol induces apoptosis by activation of caspase 8 and caspase 9 pathways. Plaunotol is a potential anticancer agent against colon cancer .
    Plaunotol
  • HY-W587878

    Cytochrome P450 Pyruvate Kinase Fungal Apoptosis Insecticide Infection Cancer
    Thujopsene is the inhibitor for cytochrome P450, that inhibits CYP2B6, CYP3A4, CYP2C19, CYP2C8, CYP2C9 with IC50s of 1.3, 12.6, 13.6, 29.8, and 44.9 μM, respectively. Thujopsene binds to PKM2, inhibits the metabolism pathway of cancer cell, induces apoptosis in MKN45, thereby exhibiting antitumor efficacy. Thujopsene exhibits anti-termite and antifungal activities through autoxidation [1] .
    Thujopsene
  • HY-148741

    DNA/RNA Synthesis Cancer
    Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity [1].
    Werner syndrome RecQ helicase-IN-4
  • HY-161654

    SOS1 PROTACs Ras Cancer
    PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500)) [1]
    PROTAC SOS1 degrader-10
  • HY-120667

    MDM-2/p53 Apoptosis Cancer
    DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice [1].
    DS-5272
  • HY-165606

    Oct3/4 c-Myc Apoptosis Cancer
    SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133 +/CD44 + cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers [1] .
    SB-T-1214
  • HY-176701

    Histone Methyltransferase Cancer
    PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma [1].
    PRMT5-MTA-IN-4
  • HY-N7305

    P-glycoprotein Cancer
    Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR) [1].
    Jatrophane 5
  • HY-168733

    Lactate Dehydrogenase Apoptosis Cancer
    LDHA-IN-9 (Compound 1g) is an inhibitor for LDH-A with an IC50 of 25 nM. LDHA-IN-9 inhibits the proliferation of DLD-1 cell (GI50 of 27 μM) through apoptosis induction. LDHA-IN-9 exhibits antitumor activity in mouse model without significant toxicity (25 mg/kg) [1].
    LDHA-IN-9
  • HY-121619

    Apoptosis Inflammation/Immunology Cancer
    Jacaric acid is a conjugated linolenic acid, which inhibits viability in cells PC-3 (IC50 is 11.8 μM), LNCaP (IC50 is 2.2 μM) and DLD-1, induces apoptosis and necrosis [1]. Jacaric acid exhibits anticaner activity against prostate cancer and adenocarcinoma . Jacaric acid exhibits immunomodulating activity in murine peritoneal macrophages as an immunopotentiator . Jacaric acid is orally active.
    Jacaric acid
  • HY-169652

    Reactive Oxygen Species (ROS) AMPK Cancer
    NPC26 is a small molecule mitochondrial disruptor with anti-tumor activity. NPC-26 shows significant anti-proliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 can damage mitochondrial function, leading to the opening of the mitochondrial permeability transition pore (mPTP) and the production of reactive oxygen species, ultimately inducing cell death. NPC-26 can kill CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway [1].
    NPC26
  • HY-156375

    Pyruvate Kinase PDK-1 Cancer
    PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) [1].
    PKM2 activator 6
  • HY-168716

    SOS1 Ras Cancer
    SOS1-IN-17 (Compound 8d) is an orally active inhibitor for SOS1-KRASG12C interaction with an IC50 of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC50 of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC50 of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model [1].
    SOS1-IN-17
  • HY-156502

    MAP4K Cancer
    TINK-IN-1 (Compound 9) is a potent and selective Traf2- and Nck-interacting kinase (TNIK) inhibitor with an IC50 of 8 nM. TINK-IN-1 inhibits colorectal cancer cells viability [1].
    TINK-IN-1
  • HY-114977R

    Reference Standards Apoptosis DNA/RNA Synthesis Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    Avenanthramide A (Standard) is the analytical standard of Avenanthramide A. This product is intended for research and analytical applications. Avenanthramide A is an orally active phytoalexin that targets the RNA helicase DDX3 with a KD of 8.8 μM. Avenanthramide A induces mitochondrial swelling and increased ROS production, and triggers apoptosis in CRC cells. Avenanthramide A inhibits smooth muscle cell proliferation and enhances nitric oxide production. Avenanthramide A can be used in research on colorectal cancer and atherosclerosis [1] .
    Avenanthramide A (Standard)
  • HY-163816

    Cytochrome P450 Cancer
    Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice [1].
    Antiproliferative agent-53-d3
  • HY-N13886

    Endogenous Metabolite Cancer
    Anicequol, a microbial secondary metabolites, is an anchorage-independent growth of tumor cells inhibitor. Anicequol inhibits the anchorage-independent growth of human colon cancer DLD-1 cells with the IC50 of 1.2 μM [1].
    Anicequol
  • HY-153332

    PARP Cancer
    Tankyrase-IN-5 (Compound 30f), an analogue of MSC2504877 (HY-123851), is a tankyrase TNKS1 and TNKS2 inhibitor with IC50s of 2.3 nM and 7.9 nM, respectively [1].
    Tankyrase-IN-5
  • HY-177967

    Drug Derivative Cancer
    Antitumor agent-209 (Compound 10g), a quinolone derivative, is an antitumor agent. Antitumor agent-209 can inhibit proliferation of HCT-116, RKO, DLD1, HepG2, BGC-823, NCI-H1650 and SK-OV-3 cells with IC50 values of 0.37, 0.58, 0.81, 0.79, 0.89, 0.78 and 0.89 μM [1].
    Antitumor agent-209
  • HY-118829

    Drug Derivative Neurological Disease
    3,4-Methylenedioxy PV9 hydrochloride is a drug derivative. 3,4-Methylenedioxy PV9 hydrochloride shows toxicity against BEAS-2B, human aortic endothelia, HASM, SK-N-SH, A172, HepG2, MKN45, and DLD1cells (LC50=12.8-67.5 μM) [1].
    3,4-Methylenedioxy PV9 hydrochloride
  • HY-W098807

    Drug Derivative Cancer
    4-Chloro-7-ethoxyquinoline (Compound 9a), a quinolone derivative, is an anticancer agent. 4-Chloro-7-ethoxyquinoline can inhibit proliferation of HCT-116, RKO, DLD1, HepG2, BGC-823, NCI-H1650 and SK-OV-3 cells with IC50 values of 3.16, 3.87, 2.75, 2.66, 3.91, 3.34 and 3.46μM [1].
    4-Chloro-7-ethoxyquinoline
  • HY-144794

    Apoptosis EGFR FAK Cancer
    EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis [1].
    EGFR-IN-46
  • HY-N16557

    Apoptosis EGFR STAT PERK Cancer
    (Rac)-8-Gingerol is a non-volatile component. (Rac)-8-Gingerol can be extracted from ginger. (Rac)-8-Gingerol enhances Apoptosis. (Rac)-8-Gingerol decreases the level of phosphorylated EGFR and, accordingly, the phosphorylation levels of its downstream effectors, STAT3 and ERK. (Rac)-8-Gingerol exhibits anticancer activity against colorectal cancer [1].
    (Rac)-8-Gingerol
  • HY-176727

    DNA/RNA Synthesis Cancer
    WRN inhibitor 19 (Compound 40) is a WRN helicase inhibitor (IC50: 3.7 nM). WRN inhibitor 19 exhibits selective antiproliferative activity in WRN-dependent cancer cells. WRN inhibitor 19 inhibits WRN helicase function by competitively binding to the ATP site and induces DNA damage and cell cycle arrest. WRN inhibitor 19 can be used in the study of WRN-dependent cancers [1].
    WRN inhibitor 19
  • HY-172617

    BMI1 Microtubule/Tubulin Apoptosis Cancer
    APD-94 is a dual inhibitor targeting tubulin and Bmi-1. APD-94 interfers tubulin normal polymerization. APD-94 suppresses the expression of Bmi-1. APD-94 causes cell cycle arrest at the G2/M phase in cancer cells and induces apoptosis, thus inhibiting cancer cell proliferation. APD-94 represses the growth of HT29 cell xenografts in NOD/SCID mice. APD-94 can be used for colorectal cancer study [1].
    APD-94
  • HY-179413

    DNA/RNA Synthesis Cancer
    Polθ-IN-9 is an orally active Polθ polymerase inhibitor (IC50 = 9.6 nM, Kd = 47.5 nM). Polθ-IN-9 shows remarkable selectivity with no inhibitory activity against other human DNA polymerases, including Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. Polθ-IN-9 exhibits strong antiproliferative activity in DLD1 BRCA2 KO cells (IC50 = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC50 = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib (HY-10162), in the MDA-MB-436 xenograft model. Polθ-IN-9 can be used for the research of homologous recombination (HR)-deficient cancers such as breast cancer [1].
    Polθ-IN-9
  • HY-180304

    Kinesin Cancer
    CCT369834 is an ATP-competitive HSET inhibitor with an IC50 of 39 nM. CCT369834 is a trans-cyclooctene-tagged probe. CCT369834 and HSET specifically co-localize on mitotic spindles. CCT369834 can be used for the research of cancer [1].
    CCT369834
  • HY-114943

    PARP Wnt β-catenin Cancer
    TNKS-IN-1 is a selective and potent tankyrase (TNKS1/TNKS2) inhibitor with IC50 values of 7.9 nM and 8.7 nM. TNKS-IN-1 induces axin2 accumulation with an EC50 of 1500 nM. TNKS-IN-1 can antagonize the Wnt signal transduction pathway by stabilizing axin proteins and promoting β-catenin degradation. TNKS-IN-1 can be used for the research of colorectal cancer [1].
    TNKS-IN-1
  • HY-182322

    DNA/RNA Synthesis Cancer
    POLQ-IN-1 is a DNA polymerase θ (POLQ) inhibitor with a pIC50 of 8.2. POLQ-IN-1 inhibits the proliferation of homologous recombination-deficient cells. POLQ-IN-1 is used for the research of homologous recombination-deficient tumors [1].
    POLQ-IN-1
  • HY-185459

    PARP Epigenetic Reader Domain Cancer
    PCIP-1 is a PARP2 inhibitor. PCIP-1 recruits BET proteins to PARP2 to inhibit DNA repair, acts via event-driven pharmacology, and does not inhibit PARP-catalyzed PARylation. PCIP-1 inhibits DNA repair, thereby inducing synthetic lethality in homologous recombination-deficient cancer cells and increasing the sensitivity of PARP1-knockout cells. PCIP-1 can be used in the research of homologous recombination-deficient cancers, T-cell acute lymphoblastic leukemia, and BRCA-mutant cancers [1].
    PCIP-1
  • HY-181557

    DNA Alkylator/Crosslinker DNA/RNA Synthesis Apoptosis Cancer
    SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC50=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC50=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors [1].
    SY-589

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