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Pathways Recommended: Stem Cell/Wnt Cell Cycle/DNA Damage
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DLD-1 cells

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40

Inhibitors & Agonists

1

Inhibitory Antibodies

5

Natural
Products

1

Isotope-Labeled Compounds

Targets Recommended:
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 .
    BAY-8002
  • 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-164561
    TASIN-30
    1 Publications Verification

    		 Emopamil Binding Protein Ferroptosis Apoptosis Cancer
    TASIN-30 is a selective EBP inhibitor with an EC50 of 0.097 μM. TASIN-30 blocks the production of 7-dehydrocholesterol (7-DHC) and downstream cholesterol biosynthesis processes. TASIN-30 depletes downstream sterols, disrupts the integrity of lipid rafts in tumor cells, accelerates intracellular cholesterol consumption, and inhibits tumor cell proliferation. TASIN-30 induces ferroptosis and apoptosis by reducing 7-DHC levels and increasing phospholipid peroxidation. TASIN-30 achieves tumor suppression in nude mice with osteosarcoma. TASIN-30 can be used in cancer-related research such as colorectal cancer and osteosarcoma .
    TASIN-30
  • HY-145669
    DIF-3
    Maximum Cited Publications
    8 Publications Verification

    		 Wnt CDK GSK-3 Infection Cancer
    DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo .
    DIF-3
  • HY-110088
    SCH529074
    3 Publications Verification

    		 MDM-2/p53 Cancer
    SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
    SCH529074
  • HY-139691
    SR15006

    		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) .
    SR15006
  • HY-146052
    Autophagy inducer 3
    1 Publications Verification

    		 Atg8/LC3 Autophagy Cancer
    Autophagy inducer 3 has autophagy induced activity. Autophagy inducer 3 possesses robust autophagic cell death in diverse cancer cells sparing normal counterpart. Autophagy inducer 3 induces lethal autophagy by formation of characteristic autophagic vacuoles, LC3 puncta formation, upregulation of signature autophagy markers like Beclin and Atg family proteins .
    Autophagy inducer 3
  • HY-N13009
    MO-2097

    		Raf HIF/HIF Prolyl-Hydroxylase ERK MEK Reactive Oxygen Species (ROS) Apoptosis Caspase Cancer
    MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer .
    MO-2097
  • HY-158346
    RP-2119

    		DNA/RNA Synthesis Cancer
    RP-2119 is an orally bioactive Polymerase Theta (Polθ) inhibitor, with an IC50 of 0.7 nM against human Polθ ATPase. RP-2119 reduces Polθ activity and exerts antiproliferative effects in BRCA2-deficient cancer cells. RP-2119 exhibits antitumor activity in BRCA2-deficient cancer cell xenograft mouse models . RP-2119 can be used for the research of cancer and homologous recombination-deficient cancers, including brca1/brca2-mutant cancers and shld2-mutant cancers .
    RP-2119
  • 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 .
    ABT-100
  • HY-136121
    Tubulin inhibitor 6

    		Microtubule/Tubulin Cancer
    Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM .
    Tubulin inhibitor 6
  • HY-161654
    PROTAC SOS1 degrader-10

    		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))
    PROTAC SOS1 degrader-10
  • HY-120667
    DS-5272

    		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 .
    DS-5272
  • HY-165606
    SB-T-1214

    		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 .
    SB-T-1214
  • HY-176701
    PRMT5-MTA-IN-4

    		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 .
    PRMT5-MTA-IN-4
  • HY-169652
    NPC26

    		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 .
    NPC26
  • HY-121619
    Jacaric acid

    		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 . 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-N7305
    Jatrophane 5

    		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) .
    Jatrophane 5
  • HY-16491
    Tesetaxel

    DJ-927

    		 Microtubule/Tubulin Cancer
    Tesetaxel (DJ-927) is an orally active and brain-penetrant taxane tubulin inhibitor. Tesetaxel inhibits tubulin depolymerization with an IC50 of 0.44 μM. Tesetaxel inhibits cancer cells proliferation and shows potent antitumor activity against P-glycoprotein-positive cancer cells. Tesetaxel can be used for the research of cancer, such as solid tumors, liver metastasis, and advanced breast cancer .
    Tesetaxel
  • HY-168733
    LDHA-IN-9

    		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) .
    LDHA-IN-9
  • HY-156375
    PKM2 activator 6

    		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) .
    PKM2 activator 6
  • HY-168716
    SOS1-IN-17

    		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 .
    SOS1-IN-17
  • HY-163816
    Antiproliferative agent-53-d3

    		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 .
    Antiproliferative agent-53-d3
  • HY-158681
    PARP1-IN-22

    		PARP Cancer
    PARP1-IN-22 (compound 15) is a potent inhibitor of PARP1, with the IC50 of ＜ 10 nM .
    PARP1-IN-22
  • HY-158680
    PARP1-IN-21

    		PARP Cancer
    PARP1-IN-21 (example 16) is a potent inhibitor of PARP1, with the IC50 of ＜ 10 nM .
    PARP1-IN-21
  • HY-118829
    3,4-Methylenedioxy PV9 hydrochloride

    		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) .
    3,4-Methylenedioxy PV9 hydrochloride
  • HY-N13886
    Anicequol

    		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 .
    Anicequol
  • HY-174442
    PARP1-IN-40

    		PARP Cancer
    PARP1-IN-40 is a highly selectively and orally active PARP1 inhibitor (IC50: 0.19 nM for PARP1, 26 nM for PARP2). PARP1-IN-40 kills tumor cells by inhibiting PARP1, leading to accumulation of DNA damage. PARP1-IN-40 has high antitumor activity against BRCA mutant MDA-MB-436 cells. PARP1-IN-40 can be used in combination with chemotherapy for cancer-related research .
    PARP1-IN-40
  • HY-136123
    Tubulin inhibitor 8

    		Microtubule/Tubulin Cancer
    Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM .
    Tubulin inhibitor 8
  • HY-136122
    Tubulin inhibitor 7

    		Microtubule/Tubulin Cancer
    Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM .
    Tubulin inhibitor 7
  • HY-177967
    Antitumor agent-209

    		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 .
    Antitumor agent-209
  • HY-W098807
    4-Chloro-7-ethoxyquinoline

    		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 .
    4-Chloro-7-ethoxyquinoline
  • HY-179413
    Polθ-IN-9

    		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 .
    Polθ-IN-9
  • HY-175762
    Z118298144

    		Others Cancer
    Z118298144 is a Fascin inhibitor. Z118298144 has a strong binding capacity to fascin and inhibits Actin bundling. Z118298144 significantly reduces proliferation and impairs migration of CRC cells. Z118298144 can be used for cancer, especially colorectal cancer (CRC) research .
    Z118298144
  • HY-181807
    SOS1/KRAS-IN-2

    		SOS1 Ras Apoptosis Cancer
    SOS1/KRAS-IN-2 (Compound 20) is a SOS1::KRAS G12C protein-protein interaction inhibitor with a IC50 of 4.11 nM. SOS1/KRAS-IN-2 blocks the interaction between SOS1 and KRAS G12C. SOS1/KRAS-IN-2 induces cell Apoptosis. SOS1/KRAS-IN-2 exhibits anticancer activity against colorectal cancer and tongue squamous cell carcinoma .
    SOS1/KRAS-IN-2
  • HY-W695425
    Creatine transporter-IN-1

    		Amino acid Transporter Cancer
    Creatine transporter-IN-1 is a synthetic creatine transporter (CT1/SLC6A8) inhibitor. Creatine transporter-IN-1 inhibits creatine uptake and shows anticancer activity against cancer cells .
    Creatine transporter-IN-1
  • HY-W1129940
    p-SCN-Macropa

    		Radionuclide-Drug Conjugates (RDCs) Cancer
    p-SCN-Macropa is a bifunctional macrocyclic chelator featuring macrocyclic polyamine skeletons and thiocyanate (-SCN) reactive moieties. p-SCN-Macropa can conjugate with monoclonal antibodies including Nimotuzumab (HY-P9968), Rituximab (HY-P9913) and Trastuzumab (HY-P9907)-PEG6-DM1 for 225Ac radiolabeling to construct radioimmunoconjugates. p-SCN-Macropa is applicable for the research of colorectal cancer, HER2-positive breast cancer, TROP-2-positive cancers, and PSMA-positive cancers .
    p-SCN-Macropa
  • HY-P991980
    H2Mab-139

    H2Mab-141, H2Mab-19

    		 EGFR Cancer
    H2Mab-139 (H2Mab-141;H2Mab-19) is an anti-HER2 monoclonal antibody. H2Mab-139 specifically binds to HER2 on various cancer cells. H2Mab-139 can detect HER2 overexpression in colorectal cancer via flow cytometry and immunohistochemical analysis. H2Mab-139 exhibits anti-tumor activity in mouse oral cancer and breast cancer xenografts. H2Mab-139 is applicable to research related to multiple cancers including colon cancer, oral cancer, and breast cancer .
    H2Mab-139
  • HY-N17588
    9-O-Angeloyl-8-methoxythymol

    		Others Cancer
    9-O-Angeloyl-8-methoxythymol is a thymol derivative and cytotoxin, with a IC50 value of 13.1 μg/mL against human myeloid leukemia cells, a IC50 value of 31.8 μg/mL against human lymphoblastic leukemia cells, and a IC50 >40 μg/mL against colon cancer and lymphoma cells. 9-O-Angeloyl-8-methoxythymol is applicable to leukemia-related research .
    9-O-Angeloyl-8-methoxythymol
  • HY-183630
    AZD4956

    		DNA/RNA Synthesis Cancer
    AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC50 value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors .
    AZD4956

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