Search Result
Results for "
DLD-1
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-122312
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Monocarboxylate Transporter
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Cancer
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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].
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- HY-168733
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Lactate Dehydrogenase
Apoptosis
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Cancer
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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].
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- HY-161654
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PROTACs
Ras
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Cancer
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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]
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- HY-120667
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MDM-2/p53
Apoptosis
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Cancer
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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].
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- HY-169652
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Reactive Oxygen Species
AMPK
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Cancer
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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].
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- HY-121619
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Apoptosis
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Inflammation/Immunology
Cancer
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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.
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- HY-156375
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Pyruvate Kinase
PDK-1
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Cancer
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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].
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- HY-168716
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Ras
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Cancer
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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].
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- HY-N13886
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Endogenous Metabolite
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Cancer
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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].
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- HY-163816
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Cytochrome P450
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Cancer
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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].
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- HY-N7305
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P-glycoprotein
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Cancer
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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].
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- HY-119257
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Farnesyl Transferase
Apoptosis
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Cancer
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ABT-100 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].
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- HY-139691
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KLF
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Cancer
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SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells) [1].
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- HY-P2272A
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Wnt
β-catenin
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Cancer
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NLS-StAx-h TFA is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. NLS-StAx-h TFA efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h TFA shows anti-proliferation of cancer cells [1] .
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- HY-158681
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PARP
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Cancer
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PARP1-IN-22 (compound 15) is a potent inhibitor of PARP1, with the IC50 of < 10 nM [1].
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- HY-118829
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Drug Derivative
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Neurological Disease
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3,4-Methylenedioxy PV9 hydrochloride is a Cathinone 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].
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- HY-158680
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PARP
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Cancer
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PARP1-IN-21 (example 16) is a potent inhibitor of PARP1, with the IC50 of < 10 nM [1].
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- HY-161656
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PROTAC Linkers
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Cancer
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PIP-C-3-Azaspiro[5.5]undecane-boc is the linker for PROTAC. PIP-C-3-Azaspiro[5.5]undecane-boc is utilized for synthesis of PROTAC SOS1 degrader-10 (HY-161654) [1].
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- HY-161655
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- HY-126193
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NO Synthase
Apoptosis
Autophagy
Reactive Oxygen Species
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Cancer
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JS-K is a NO donor that reacts with glutathione to generate NO at physiological pH. JS-K induces reactive oxygen species (ROS) to mediate apoptosis. JS-K induces autophagy. JS-K inhibits invasion. JS-K has a broad spectrum anti-proliferative activity in cancer cells. JS-K reduces tumor volume and causes necrosis of implanted tumors in mice [1] .
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- HY-N2493
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Lawsone
1 Publications Verification
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Fungal
Apoptosis
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Infection
Cancer
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Lawsone is an orally active naphthoquinone dye that can be isolated from the leaves of Lawsonia inermis. Lawsone can induce apoptosis. Lawsone has antibacterial, antitumor and antioxidant activities. Lawsone can be used in anti-tumor drug research [1] .
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- HY-122862
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Ras
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Cancer
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RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V [1].
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- HY-B1787
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mTOR
Drug Metabolite
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Cancer
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Sulindac sulfone is an mTORC1 pathway inhibitor and a metabolite of Sulindac. Sulindac sulfone inhibits colon cancer cell growth and induces cell cycle arrest. Sulindac sulfone is used in cancer research [1].
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- HY-146052
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Atg8/LC3
Autophagy
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Cancer
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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 [1].
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- HY-145669
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DIF-3
2 Publications Verification
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CDK
GSK-3
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Infection
Cancer
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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 [1] .
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- HY-136530
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KLF
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Cancer
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SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer [1].
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- HY-149800
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PARP
Apoptosis
Caspase
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Cancer
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PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer [1].
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- HY-13302
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VEGFR
FGFR
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Cancer
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CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy [1].
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- HY-P99041
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ABX-EGF
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EGFR
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Cancer
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Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer [1] .
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- HY-13302B
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VEGFR
FGFR
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Cancer
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CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy [1].
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- HY-13302C
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VEGFR
FGFR
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Cancer
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CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy [1].
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- HY-110088
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MDM-2/p53
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Cancer
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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) [1] .
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- HY-173059
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CDK
|
Cancer
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CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% [1].
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- HY-P99041A
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EGFR
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Cancer
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Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer [1] .
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- HY-136123
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Microtubule/Tubulin
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Cancer
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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 [1].
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- HY-136122
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Microtubule/Tubulin
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Cancer
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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 [1].
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- HY-136121
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Microtubule/Tubulin
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Cancer
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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 [1].
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- HY-169938
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HDAC
Histone Demethylase
Apoptosis
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Cancer
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LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity [1].
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- HY-133537
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Antibiotic
Fungal
ADC Cytotoxin
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Infection
Cancer
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Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity [1] .
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- HY-114657A
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Arp2/3 Complex
|
Inflammation/Immunology
Cancer
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Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis [1].
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- HY-17598
-
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Oxidative Phosphorylation
Parasite
p38 MAPK
Raf
Apoptosis
|
Infection
Cancer
|
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research [1] .
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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2272A
-
|
Wnt
β-catenin
|
Cancer
|
NLS-StAx-h TFA is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. NLS-StAx-h TFA efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h TFA shows anti-proliferation of cancer cells [1] .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99041
-
ABX-EGF
|
EGFR
|
Cancer
|
Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer [1] .
|
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- HY-P99041A
-
|
EGFR
|
Cancer
|
Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer [1] .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-163816
-
|
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].
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