Search Result
Results for "
xenograft.
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15766A
-
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NAMPT
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Cancer
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GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
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- HY-15766
-
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NAMPT
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Metabolic Disease
Cancer
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GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
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-
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- HY-153364
-
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PPAR
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Cancer
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FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models .
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-
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- HY-101120
-
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Epigenetic Reader Domain
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Cancer
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666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model .
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- HY-14375
-
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NAMPT
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Cancer
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CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft . CB 300919 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-P99160
-
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Transmembrane Glycoprotein
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Cancer
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Labetuzumab is a humanised anti-carcinoembryonic antigen (CEA) monoclonal antibody that inhibits tumour growth and sensitises human medullary thyroid cancer xenografts to Dacarbazine chemotherapy .
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-
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- HY-141896
-
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RET
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Cancer
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RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
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-
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- HY-168877
-
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MDM-2/p53
Reactive Oxygen Species
Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
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FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer .
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-
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- HY-14833
-
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TP300
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Topoisomerase
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Cancer
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Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
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-
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- HY-103711R
-
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Microtubule/Tubulin
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Cancer
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Estramustine (Standard) is the analytical standard of Estramustine. This product is intended for research and analytical applications. Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].
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- HY-164388
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Z-VAD
4 Publications Verification
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Caspase
Apoptosis
Autophagy
Necroptosis
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Cardiovascular Disease
Cancer
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Z-VAD is a competitive, irreversible pan-caspase inhibitor. Z-VAD inhibits all 10 caspases, except for caspase-2 which is only weakly inhibited. Z-VAD decreases radiation-induced apoptosis. Z-VAD induces both autophagy and necrosis in irradiated MDA-MB-231 and H460 mouse xenografts. Z-VAD with radiation produces a significant tumor growth delay and shows dramatic antiangiogenic effect in cancer xenograft .
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- HY-169422
-
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 16 (Example 83) is an orally available WRN inhibitor. WRN inhibitor 16 did not induce tumor regression in the SW48 xenograft mouse tumor model.
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- HY-169779
-
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p62
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Cancer
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PTX80 is an antagonist of p62 with an IC50 value of 31.18 nM. PTX80 reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model .
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- HY-153521
-
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BCL6
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Cancer
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CCT374705 is an orally active BCL6 inhibitor with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
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- HY-123790
-
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PI3K
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Inflammation/Immunology
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AS2541019 is a PI3Kδ (p110δ) inhibitor. AS2541019 inhibits B cell activation and proliferation, and suppresses xenograft antibody production .
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- HY-147784
-
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Btk
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Cancer
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HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
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-
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- HY-155146
-
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Necroptosis
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Cancer
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Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
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- HY-126730
-
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Phosphatase
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Cancer
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Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts .
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- HY-118269
-
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c-Met/HGFR
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Cancer
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OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
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- HY-136447
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ASP4132
1 Publications Verification
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AMPK
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Cancer
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ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
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- HY-119899
-
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Drug Derivative
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Cancer
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BO-0742, a derivative of AHMA and N-mustard, is a potent anti-cancer agent. BO-0742 significantly suppresses the growth of xenografts of human breast and ovarian cancers in mice .
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- HY-153670
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CCR
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Cancer
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IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research .
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- HY-147402
-
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D-0502
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Estrogen Receptor/ERR
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Cancer
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Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models .
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- HY-P99849
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ABT-806
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EGFR
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Cancer
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Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
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- HY-155079
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EGFR
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Cancer
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DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
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- HY-146615
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TAM Receptor
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Cancer
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Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
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- HY-149539
-
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FLT3
RET
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Cancer
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PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
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- HY-P99925
-
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REGN421
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Notch
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Metabolic Disease
Cancer
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Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
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- HY-148422
-
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Eukaryotic Initiation Factor (eIF)
Apoptosis
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Cancer
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Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .
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- HY-N14738
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Serpin
Autophagy
Apoptosis
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Cancer
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Dutomycin is a SERPINB6 inhibitor with a binding constant (KD) of 1.236 μM. Dutomycin can induce autophagy and apoptosis in cancer cells and inhibit the growth of cancer cells in a zebrafish xenograft model. Dutomycin is promising for research of cancers .
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- HY-146465
-
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Microtubule/Tubulin
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Cancer
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Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model .
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- HY-147402A
-
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D-0502 meglumine
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Estrogen Receptor/ERR
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Cancer
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Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models .
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- HY-164484
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Raf
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Cancer
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IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities .
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- HY-148517
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AZD0095
2 Publications Verification
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Monocarboxylate Transporter
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Cancer
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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) .
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- HY-169928
-
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 14 (compound S35) is an orally active WRN inhibitor with anticancer activity. WRN inhibitor 14 results in tumor growth inhibition in the SW48 xenograft model in BALB/c nude mice .
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- HY-103711
-
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Microtubule/Tubulin
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Cancer
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Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts .
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- HY-15324
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P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
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Syk
Src
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
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Cancer
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PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models . .
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- HY-162892
-
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Epigenetic Reader Domain
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Cancer
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BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model .
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- HY-15323
-
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P505-15 Hydrochloride
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Syk
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
Src
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Cancer
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PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models .
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- HY-126837
-
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Spicamycin VIII
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Antibiotic
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Cancer
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SPM VIII is a dodecanoyl analogue of spicamycin, a nucleoside antibiotic that contains fatty acids of various chain lengths. SPM VIII exhibits potent antitumor activity against the human gastric cancer SC-9 xenograft model .
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- HY-131446
-
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Checkpoint Kinase (Chk)
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Cancer
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Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
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- HY-B2085
-
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Arsthinol; Balarsen
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Others
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Cancer
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Arsthinenol is an orally active antitumor agent, that exhibits cytotoxicity in U87MG cells with an IC50 of 31.6 μM. Arsthinenol forms complex with cyclodextrin, inhibits the tumor growth and improves the survival rates of U87MG xenograft mice .
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- HY-156712
-
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Antibody-Drug Conjugates (ADCs)
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Cancer
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Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) and the cytotoxic agent Monomethyl auristatin E (MMAE). Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR .
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- HY-14815
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Combretastatin A4 phosphate
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Apoptosis
Microtubule/Tubulin
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Cancer
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Fosbretabulin (Combretastatin A4 phosphate) is a vascular disruptor with antitumor activity against atypical thyroid carcinoma (ATC) cell lines and xenografts. Fosbretabulin inhibits tumor growth by inhibiting microtubule polymerization, inducing apoptosis, and suppressing angiogenesis in tumors .
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- HY-168151
-
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EGFR
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Cancer
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EGFR-IN-128 (compund 28) is a potent and selective molecule targeting wild-type EGFR Ex20Ins that demonstrates efficacy in multiple human xenograft models and can cross the blood-brain barrier in preclinical species .
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- HY-163133
-
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PIKfyve
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Cancer
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PIKfyve-IN-3 (compound L22) has a remarkable interaction with PIKfyve kinase with a Kd value of 0.47 nM. PIKfyve-IN-3 has oral activity. PIKfyve-IN-3 inhibits tumor growth in a HeLa xenograft model .
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- HY-170806
-
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Estrogen Receptor/ERR
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Cancer
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ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model .
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-
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- HY-163076
-
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Apoptosis
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Others
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Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
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-
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- HY-N5166
-
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(-)-Ardeemin
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P-glycoprotein
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Cancer
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Ardeemin ((-)-Ardeemin) binds to the P-glycoprotein, preventing anticancer agent from being pumped out of cells. Ardeemin reverses the multidrug resistance phenotype of tumor cells and increases the sensitivity of tumor cells to anticancer agent in mammary carcinoma xenografts .
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-
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- HY-108352
-
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VCE 004
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Topoisomerase
|
Cancer
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HU 331 (HU 331) is a highly specific Topoisomerase II inhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo .
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- HY-124628
-
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Fatty Acid Synthase (FASN)
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Cancer
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IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
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- HY-110201
-
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
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- HY-147208
-
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YAP
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Cancer
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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 .
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- HY-136538
-
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Survivin
|
Cancer
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LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors .
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- HY-P5098
-
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Integrin
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Cancer
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E(c(RGDfK)) is an αvβ3 integrin-specific binding moiety with tumor targeting properties. Increased uptake of E(c(RGDfK)) in human ovarian cancer OVCAR-3 xenograft tumors may be useful in cancer research .
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- HY-158006
-
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MetAP
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Cancer
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SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
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- HY-155251
-
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Apoptosis
Bcl-2 Family
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Cancer
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anti-TNBC agent-3 (compound 3g) is an apoptosis inducer with anti-cancer cell proliferation activity. anti-TNBC agent-3 inhibits tumor growth and metastasis in triple-negative breast cancer (TNBC) xenograft models .
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- HY-12401A
-
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Mps1
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Cancer
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Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model .
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- HY-156111
-
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PROTACs
Androgen Receptor
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Cancer
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ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
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- HY-162477
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Cathepsin
Apoptosis
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Cancer
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TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis .
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- HY-161952
-
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SHP2
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Cancer
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JAB-3312 is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. JAB-3312 has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
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- HY-156566
-
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
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- HY-16634
-
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MDM-2/p53
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Cancer
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MI-888 (TFA) is an orally active MDM2-p53 interaction inhibitor with a Ki of 0.44 nM. MI-888 (TFA) can achieve rapid, complete, and sustained tumor regression in a xenograft mouse model of cancer .
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- HY-156244
-
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PROTACs
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Cancer
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PROTAC GDI2 Degrader-1 (compound 21) is a potent PROTAC GDI2 degrader. PROTAC GDI2 Degrader-1 exhibits excellent in vivo antitumor activity in the GDI2-overexpressing pancreatic xenograft models .
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- HY-19981B
-
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ARQ-087 dihydrochloride
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EGFR
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Cancer
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Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models .
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- HY-120394
-
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Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
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TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth .
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- HY-158829
-
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EGFR
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Cancer
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SSOe26 sodium is a 15mer antisense oligonucleotide targeting?HER4. SSOe26 sodium induces exon 26 skipping, leading to the generation of a novel mRNA transcript that excludes exon 26 (CYT2 isoform). SSOe26 sodium decreases tumour growth in mouse xenografts.
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- HY-19981
-
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ARQ-087
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FGFR
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Cancer
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Derazantinib (ARQ-087) is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM). Derazantinib inhibits FGFR phosphorylation. Derazantinib inhibits tumor growth in multiple xenograft models .
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- HY-P3990
-
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VEGFR
Autophagy
Apoptosis
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Cancer
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Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts .
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- HY-163301
-
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Reactive Oxygen Species
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Cancer
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Antitumor agent-139 (compound 9b) is a liver - and mitochondria-targeting gold(I) complexe, and produces reactive oxygen species (ROS) and facilitates DNA excretion. Antitumor agent-139 inhibits tumor growth in a patient-derived xenograft model of hepatocellular carcinoma .
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- HY-W013973
-
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Fungal
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Cancer
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p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
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- HY-W369099
-
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STAT
Apoptosis
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Cancer
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HJC0152 (free base) is an orally active and potent inhibitor of STAT3. HJC0152 (free base) inhibits cell cycle progression and induces apoptosis. HJC0152 (free base) significantly suppresses MDA-MB-231 xenograft tumor growth in mice .
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- HY-135217
-
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Apoptosis
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Cancer
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Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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- HY-122703
-
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Epigenetic Reader Domain
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Cancer
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BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors .
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- HY-117366
-
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PKC
|
Cancer
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PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
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- HY-163743
-
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Salt-inducible Kinase (SIK)
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Cancer
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SIC-19 is a SIK2 inhibitor and promotes SIK2 protein degradation via the ubiquitination pathway. SIC-19 inhibits cancer cell growth and sensitizes cells to PARP inhibitors (Such as Olaparib (HY-10162)), as well as in ovarian cancer organoids and xenograft models .
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- HY-16405
-
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DNA Alkylator/Crosslinker
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Cancer
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PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
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- HY-14688
-
|
|
PARP
|
Cancer
|
|
CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560) .
|
-
- HY-123891
-
|
|
EGFR
|
Cancer
|
|
NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613); EP-100
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-168950
-
|
|
Annexin A
|
Cancer
|
|
ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with cancer cell inhibition activity. ANXA3 degrader 1 displays excellent inhibitory effect in a triple-negative breast cancer (TNBC) tumor xenograft model (TGI=96%) .
|
-
- HY-16406
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
|
-
- HY-131902
-
|
|
MALT1
|
Cancer
|
|
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse .
|
-
- HY-132166
-
|
IDRX-42
|
c-Kit
PDGFR
c-Fms
FLT3
Src
|
Cancer
|
|
M4205 is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. M4205 exhibits antitumor efficacy in xenograft mouse models .
|
-
- HY-163461
-
|
|
PARP
|
Cancer
|
|
4F-DDC is a novel PARP1 inhibitor with an IC50 value of 82 nM. 4F-DDC induces DNA damage and activates the cGAS–STING pathway. 4F-DDC inhibits the growth of HCC-1937-derived tumor xenografts .
|
-
- HY-156681A
-
|
|
PI3K
|
Cancer
|
|
(S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .
|
-
- HY-123020
-
|
BDA-366 analog
|
Bcl-2 Family
|
Cancer
|
|
CYD-2-88 (BDA-366 analog) is a BDA-366 (HY-101083) (Bcl2 BH4 antagonist) analog. CYD-2-88 (20 mg/kg, i.p.) inhibits tumor growth in NSCLC H460 xenografts mice .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-144361
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
|
-
- HY-139109
-
|
ADS 780WS
|
Fluorescent Dye
Apoptosis
|
Others
|
|
IR-783 (ADS 780WS) is a near-infrared (NIR) heptamethine cyanine fluorescent probe. IR-783 significantly inhibits tumour growth and induces apoptosis in MDA-MB-231 xenograft model. IR-783 can be used to study breast cancer .
|
-
- HY-152207
-
|
|
Glutaminase
Apoptosis
|
Cancer
|
|
LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model .
|
-
- HY-153704
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-17 (compound 12) is an orally active CDK4/6 inhibitor with IC50 ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-111965
-
-
- HY-163363
-
|
|
Adrenergic Receptor
|
Cancer
|
|
β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .
|
-
- HY-13589
-
|
LU103793 free base
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer .
|
-
- HY-13589A
-
|
LU103793 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) hydrochloride is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin hydrochloride blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin hydrochloride can be used to research anticancer .
|
-
- HY-155020
-
|
|
Histone Methyltransferase
GLP Receptor
|
Cancer
|
|
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model .
|
-
- HY-155556
-
|
|
ClpP
|
Cancer
|
|
ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
|
-
- HY-170933
-
|
|
SGK
|
Cancer
|
|
SGK1-IN-6 (compound 12f) is a potent SGK1 inhibitor with an IC50 of 0.39 μM. SGK1-IN-6 suppresses tumor growth in the PC3 xenograft model in BALB/c nude mice without inducing any observable toxicity .
|
-
- HY-170565
-
|
|
Mitophagy
Apoptosis
|
Cancer
|
|
CHD-1 is a a hypoxia-activated antitumor prodrug. CHD-1 impairs mitochondrial morphology and membrane potential in hypoxic tumor cells, further triggering excessive mitophagy and inducing apoptosis. CHD-1 inhibits the growth of hypoxic tumor cells in vitro and the growth of HeLa xenograft in vivo .
|
-
- HY-P99922
-
|
|
LAG-3
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
- HY-123334
-
|
|
Porcupine
Wnt
|
Cancer
|
|
GNF-1331 (compound 19) is a potent, selective and orally bioavailable porcupine inhibitor (IC50=12 nM). GNF-1331 blocks Wnt ligand secretion and subsequent Wnt signaling activity, and induces significant antitumor effects in the mouse MMTV-WNT1 xenograft tumor model .
|
-
- HY-155502
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1C3-IN-10 (compound 5r) is a selective AKR1C3 inhibitor (IC50=51 nM). AKR1C3-IN-10 shows good activity in a prostate cancer xenograft model .
|
-
- HY-151808
-
|
|
Btk
|
Cancer
|
|
JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier .
|
-
- HY-156568A
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-13659
-
|
NSC 650426
|
Antibiotic
Bcl-2 Family
Apoptosis
|
Infection
Cancer
|
|
KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice .
|
-
- HY-120663
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
KRCA-0713 is an ALK inhibitor with anti-ALK activity. KRCA-0713 showed promising anti-ALK activity in enzyme and cell-based experiments. KRCA-0713 was shown to effectively inhibit ALK-driven tumor growth in H3122 xenograft model studies, similar to the effect of ceritinib .
|
-
- HY-16214
-
|
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts .
|
-
- HY-157847
-
|
|
STAT
|
Cancer
|
|
Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .
|
-
- HY-145427
-
|
|
DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect .
|
-
- HY-153306
-
|
|
PI3K
|
Cancer
|
|
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
|
-
- HY-156243
-
|
|
ROCK
|
Cancer
|
|
GDI2-IN-1 (compound (+)-37) is a GDP-dissociation inhibitor beta (GDI2) inhibitor with an IC50 of 2.87 μM and a KD of 36 μM. GDI2-IN-1 exhibits excellent in vivo antitumor activity in GDI2-overexpressing pancreatic xenograft models .
|
-
- HY-162001
-
INX-315
1 Publications Verification
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
|
-
- HY-153834
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-118911
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
|
-
- HY-169074
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-N-methylpiperazine is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-N-methylpiperazine can be used to synthesize PROTAC MLKL Degrader-2 (HY-169072) to exhibit antinecroptotic activity on human cell lines and effectively degrade MLKL in the HT-29 xenograft mouse model .
|
-
- HY-P99282
-
|
VB6-845; Anti-Human EpCAM Recombinant Antibody Fab Fragment, 17-1A
|
Apoptosis
|
Cancer
|
|
Citatuzumab bogatox (VB6-845) is recombinant immunotoxin that composed of Fab fragment of humanized antibody targeting EpCAM and a modified cytotoxin bouganin. Citatuzumab bogatox binds to and selectively induces apoptosis in EpCAM-positive cell lines and shows good activity in EpCAM-positive human tumour xenograft models .
|
-
- HY-160142
-
|
|
Btk
|
Cancer
|
|
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .
|
-
- HY-123952
-
|
TRC-382
|
EGFR
|
Cancer
|
|
RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling .
|
-
- HY-129239
-
|
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice .
|
-
- HY-162985
-
|
|
CDK
|
Cancer
|
|
JHD205 is a CDK4/6 inhibitor that induces apoptosis and DNA damage. JHD205 inhibits DNA repair by upregulating Caspase3 and p-H2AX. JHD205 has superior potency to Abemaciclib (HY-16297A) in a xenograft chick embryo breast cancer model. .
|
-
- HY-N0421
-
|
Cinobufagine
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-122650
-
|
|
Autophagy
|
Cancer
|
|
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
|
-
- HY-153834A
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- HY-168587
-
|
|
Others
|
Cancer
|
|
Antitumor agent-189 (Compound DN4) is a potent antitumor agent. Antitumor agent-189 inhibits A498 cells proliferation, adhesion and invasion with an IC50 of 1.94 μM. Antitumor agent-189 also inhibits angiogenesis and tumor growth in the xenograft model of A498 cells .
|
-
- HY-160084
-
|
|
DNA Methyltransferase
|
Cancer
|
|
2′-Deoxy-4′-thiocytidine (T-dCyd) is a novel epigenetic agent. 2′-Deoxy-4′-thiocytidine administrations led to a significant p21 increase. 2′-Deoxy-4′-thiocytidine can eradicate of tumor cells in the double-mutant xenografts .
|
-
- HY-149982
-
-
- HY-154973
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
AMPK
|
Metabolic Disease
Cancer
|
|
AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
|
-
- HY-42484
-
|
Eribulin intermediate
|
Microtubule/Tubulin
|
Cancer
|
|
ER-076349 (Eribulin intermediate) is an inhibitor of tubulin polymerization, induces G2-M cell cycle arrest, and disrupts mitotic spindles. ER-076349 inhibits cancer cell growth, and inhibits tumor growth in several human tumor xenografts. ER-076349 is an analog of Halichondrin B .
|
-
- HY-119618
-
|
|
Endogenous Metabolite
|
Cancer
|
|
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
|
-
- HY-156784
-
|
DHX9-IN-2
|
DNA/RNA Synthesis
|
Cancer
|
|
ATX968 (example 31) is an orally active, potent and selective inhibitor of ATP-dependent RNA helicase A (DHX9), with the EC50 of 0.054 μM in circBRIP1. ATX968 results in robust and durable tumor growth inhibition or regression in mouse xenograft studies with MSI-H/dMMR colorectal cancer cell lines .
|
-
- HY-12797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
GF 15 is an inhibitor of centrosomal clustering during cell mitosis, with an EC50 value of 900 nM for inducing multipolar spindles. GF???15 is a derivative of griseofulvin that inhibits tubulin polymerization at concentrations above 25 μM. GF 15 inhibits tumor growth and significantly prolongs survival in mouse xenograft models of human colon cancer and multiple myeloma .
|
-
- HY-100765
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis .
|
-
- HY-149631
-
|
|
HDAC
|
Cancer
|
|
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models .
|
-
- HY-126248
-
|
|
PARP
Wnt
|
Cancer
|
|
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .
|
-
- HY-141606
-
|
BAY 94-9343
|
Microtubule/Tubulin
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models .
|
-
- HY-149297
-
|
|
PSMA
|
Cancer
|
|
PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer .
|
-
- HY-122664
-
|
|
BRK
|
Cancer
|
|
XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
|
-
- HY-108713
-
|
SHR1020
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
|
-
- HY-146780
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model .
|
-
- HY-150072
-
|
|
PKA
|
Cancer
|
|
DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC) .
|
-
- HY-170812
-
|
|
Aurora Kinase
|
Cancer
|
|
BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .
|
-
- HY-170936
-
|
|
FAK
Hippo (MST)
YAP
|
Cancer
|
|
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
|
-
- HY-P99493
-
|
IMGN242; huC242-DM4
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 (HY-12454)). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-135217R
-
|
|
Apoptosis
|
Cancer
|
|
Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-156618
-
|
ABSK011
|
FGFR
|
Cancer
|
|
Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .
|
-
- HY-10484
-
|
MLN4924 hydrochloride
|
NEDD8-activating Enzyme
Apoptosis
|
Cancer
|
|
Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice .
|
-
- HY-16706
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-121490
-
|
|
Apoptosis
|
Cancer
|
|
IMM-02 is a DID-DAD binding inhibitor with activity promoting actin assembly and microtubule stabilization. IMM-02 is able to trigger serum response factor-mediated gene expression and lead to cell cycle arrest and apoptosis. IMM-02 has shown the ability to slow tumor growth in a mouse colon cancer xenograft model .
|
-
- HY-118184
-
|
|
PGE synthase
|
Cancer
|
|
AF3485 is a human mPGES-1 inhibitor that exhibits antitumor activity in vitro and in vivo. AF3485 inhibits tumor-associated angiogenesis by reducing PGE2 production, inhibiting EGFR signaling, and decreasing VEGF and FGF-2 expression. AF3485 reduced tumor growth in mice bearing human A431 xenograft tumors by subchronic administration.
|
-
- HY-138364
-
YUM70
2 Publications Verification
|
HSP
Apoptosis
|
Cancer
|
|
YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model .
|
-
- HY-161425
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-149 (Compound 3) is an analogue of Echinomycin (HY-106101). Antitumor agent-149 inhibits HIF-1α-mediated transcription. Antitumor agent-149 induces cancer cell apoptosis. Antitumor agent-149 inhibits tumor growth in SW620 xenograft mice model .
|
-
- HY-144273
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. IDO1-IN-13 has cellular IDO1 inhibition (HeLa EC50= 30 nM). IDO1-IN-13 decreases 51% of the kyn/trp ratio in SK-OV-3 xenograft tumor tissues .
|
-
- HY-116269
-
|
|
Ras
Apoptosis
PAK
ERK
|
Cancer
|
|
AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts .
|
-
- HY-146505
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice .
|
-
- HY-143411
-
|
|
HDAC
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
|
-
- HY-155543
-
|
|
Androgen Receptor
|
Cancer
|
|
Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .
|
-
- HY-132173
-
|
|
Bcl-2 Family
|
Cancer
|
|
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo .
|
-
- HY-70062
-
Pevonedistat
Maximum Cited Publications
157 Publications Verification
MLN4924
|
NEDD8-activating Enzyme
Apoptosis
|
Cancer
|
|
Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice .
|
-
- HY-115514A
-
|
|
BRK
|
Cancer
|
|
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
|
-
- HY-164607
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
YL-5092 is an inhibitor for YT521-B homology (YTH) domain-containing protein 1 (YTHDC1). YL-5092 inhibits acute myeloid leukemia cell with IC50 of 0.28-2.87 μM. YL-5092 exhibits antitumor efficacy in MOLM-13 or U937 xenograft mice .
|
-
- HY-149352
-
|
|
Thymidylate Synthase
|
Cancer
|
|
DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
|
-
- HY-149081
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
|
Cancer
|
|
ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
|
-
- HY-121588
-
|
|
Adrenergic Receptor
|
Cancer
|
|
IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .
|
-
- HY-D2620
-
|
|
Photosensitizer
Reactive Oxygen Species
Ferroptosis
|
Cancer
|
|
CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LDs). CAR-2 exhibits phototoxicity in breast cancer cells with IC50 of 0.01-0.02 μM. CAR-2 exhibits antitumor efficacy in 4T1 xenograft mouse models .
|
-
- HY-172108
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. TGFβRI-IN-7 inhibits SMAD2/3 phosphorylation and H22 cell viability with IC50 values of 12 and 65 nM, respectively. TGFβRI-IN-7 shows anti-tumor efficacy in a xenograft model of H22 cells, with TGI of 79.6 % .
|
-
- HY-W013973R
-
|
|
Fungal
|
Cancer
|
|
p-Terphenyl (Standard) is the analytical standard of p-Terphenyl. This product is intended for research and analytical applications. p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
|
-
- HY-125158
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
HOI-07 is a selective Aurora B kinase inhibitor. HOI-07 blocks phosphorylation of histone H3 on Ser10 in
lung cancer cells. HOI-07 induces cell-cycle arrest, and apoptosis. HOI-07 has antitumor activity, and suppresses the tumor growth of A549, 143B and KHOS xenografts .
|
-
- HY-10254
-
|
PD0325901; PD325901
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
|
-
- HY-168934
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR137 is a WRN degrader, with an IC50 of 8 nM. KWR137 exhibits good anti-proliferative activity against MSI-H cells, with a GI50 of 509 nM in SW48 cells and a GI50 of 824 μM in HCT116 cells. It also demonstrates anti-tumor growth effects in xenograft mouse models. KWR137 can be used for cancer research .
|
-
- HY-400685
-
|
|
Drug Intermediate
|
Cancer
|
|
SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-145388
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
|
-
- HY-168043
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-35 is a STAT3 inhibitor that binds to SH2 domain. STAT3-IN-35 inhibits the phosphorylation of STAT3 and possesses antiproliferative activities against triple-negative breast cancer (TNBC) cell lines. STAT3-IN-35 also has a toxicity and potent antitumor activity in a TNBC xenograft model .
|
-
- HY-108696
-
GNE-781
3 Publications Verification
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .
|
-
- HY-119062
-
|
|
MetAP
|
Cardiovascular Disease
Cancer
|
|
A-800141 is an orally active and selective MetAP2 inhibitor with an IC50 of 12 nM. A-800141 has weak inhibitory activity for MetAP1 (IC50 : 36 μM). GAPDH can be used as a biomarker to monitor the MetAP2 inhibition of A-800141. A-800141 has antiangiogenic and anticancer activity in a variety of xenograft tumor models .
|
-
- HY-120638
-
|
|
Topoisomerase
|
Cancer
|
|
BMS-250749 is a topoisomerase I (Top I) inhibitor of the fluoroglycosyl-3,9-difluoroindolecarbazole class. BMS-250749 exhibits potent cytotoxicity and selectivity, and shows curative antitumor activity against Lewis lung cancer. BMS-250749 exhibits broad-spectrum antitumor activity superior to CPT-11 in certain preclinical xenograft models. .
|
-
- HY-P10759
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
- HY-12098
-
|
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
|
-
- HY-157210
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-26 (compound 36) is an orally active CDK7 inhibitor (IC50: 7.4 nM). CDK7-IN-26 potently inhibits the growth of triple-negative breast cancer (TNBC) cell line-derived xenograft (CDX) tumors in vivo and inhibits MDA-MB-453 cells in vitro with an IC50 of 0.15 μM .
|
-
- HY-150082
-
|
|
CDK
DNA/RNA Synthesis
|
Cancer
|
|
CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila .
|
-
- HY-165421
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
|
-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-B0942
-
|
|
nAChR
Bacterial
Apoptosis
Caspase
|
Infection
Neurological Disease
Cancer
|
|
Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo .
|
-
- HY-143905
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-161338
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-61 (Compound 9a) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-61 destroys the microtubule skeleton, blocks the cell cycle in G2/M phase, induces Apoptosis, and inhibits cancer cell migration and colony formation. Tubulin polymerization-IN-61 shows antitumor activity in vivo against 4T1 xenograft model .
|
-
- HY-156568
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models .
|
-
- HY-156112
-
|
|
Ser/Thr Protease
|
Cancer
|
|
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
|
-
- HY-19925
-
|
|
HIV
|
Infection
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-143904
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-16706A
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-134901
-
WM-3835
4 Publications Verification
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice .
|
-
- HY-162010
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile.
MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors treatment research .
|
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-150190
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 methyltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo .
|
-
- HY-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-172454
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-36 (Compound B8) is an allosteric inhibitor of SHP2, with an IC50 value of 9.0 nM. In addition, its IC50 for p-ERK is 40 nM. SHP2-IN-36 also exhibited significant antitumor activity in the KYSE520 xenograft mouse model. SHP2-IN-36 can be used for research in the field of anti-tumor .
|
-
- HY-139104
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis .
|
-
- HY-125858
-
MI-1061
1 Publications Verification
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-139795
-
|
|
HDAC
|
Cancer
|
|
ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC50s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model .
|
-
- HY-128355A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Others
Cancer
|
|
(R)-IDO/TDO-IN-1 (compound 25) is an indoleamine-2,3-dioxygenase (IDO) inhibitor, with good pharmacokinetic properties. (R)-IDO/TDO-IN-1 exhibits anti-tumor activity in MC38 xenograft model. (R)-IDO/TDO-IN-1 shows synergistic effect with anti-PD-1 monoclonal antibody (SHR-1210) .
|
-
- HY-164427
-
|
|
SHP2
ERK
|
Cancer
|
|
SHP2-IN-31 is a SHP2 inhibitor, with IC50s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models .
|
-
- HY-160005
-
|
NSC 781517
|
Topoisomerase
|
Cancer
|
|
LMP517 (NSC 781517) a indenoisoquinoline, is a potent a dual TOP1 and TOP2 inhibitor. LMP517 shows better antitumor activity than its parent compound LMP744 (HY-U00248) against H82 (Small Cell Lung Cancer) xenografts. LMP517 induces TOP1 cleavage complexes (TOP1ccs) and TOP2ccs .
|
-
- HY-151462
-
RP-6685
1 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
|
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-169037
-
|
HU-336; Δ8-THCQ
|
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Δ8-Tetrahydrocannabinoquinone (HU-336) is a potent antiangiogenic agent. Δ8-Tetrahydrocannabinoquinone inhibits angiogenesis by directly inducing apoptosis of vascular endothelial cells without changing the expression of pro- and antiangiogenic cytokines and receptors. Δ8-Tetrahydrocannabinoquinone is highly effective against tumor xenografts in nude mice .
|
-
- HY-149495
-
|
|
PROTACs
CDK
|
Cancer
|
|
CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer .
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-
- HY-N0421R
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
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-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- HY-155542
-
|
|
ROR
|
Cancer
|
|
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells .
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-
- HY-108713A
-
|
SHR1020 malate
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer .
|
-
- HY-169310
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
|
-
- HY-156633
-
|
PC14586
|
MDM-2/p53
|
Cancer
|
|
Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation .
|
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-155991
-
|
|
Apoptosis
|
Cancer
|
|
RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity .
|
-
- HY-129163
-
HJ-PI01
1 Publications Verification
10-Acetylphenoxazine
|
Pim
|
Cancer
|
|
HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research .
|
-
- HY-161957
-
|
|
Topoisomerase
|
Cancer
|
|
Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models .
|
-
- HY-172175
-
|
|
mTOR
Akt
PI3K
Apoptosis
Autophagy
|
Cancer
|
|
HYS-072 is an orally active derivative of chrysin (HY-14589) with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-125858A
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-165245
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
|
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-167876
-
|
|
PI3K
|
Cancer
|
|
PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors .
|
-
- HY-108713R
-
|
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (Standard) is the analytical standard of Famitinib. This product is intended for research and analytical applications. Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
|
-
- HY-15160A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-146114
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity .
|
-
- HY-15160B
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-121372
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
|
-
- HY-13440
-
AMG 511
2 Publications Verification
|
PI3K
|
Cancer
|
|
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
|
-
- HY-169937
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
|
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-110077
-
API-1
1 Publications Verification
|
Akt
Apoptosis
Caspase
PARP
|
Cancer
|
|
API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC50 = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model .
|
-
- HY-162881
-
|
|
EGFR
|
Cancer
|
DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
|
-
- HY-155532
-
|
|
Apoptosis
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-146462
-
|
|
Apoptosis
ROS Kinase
|
Cancer
|
|
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
|
-
- HY-116447
-
|
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
|
-
- HY-131328
-
|
LOXO-305
|
Btk
|
Cancer
|
|
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
|
-
- HY-144256
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties .
|
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-110354
-
|
G28UCM
|
Fatty Acid Synthase (FASN)
Bacterial
Antibiotic
|
Infection
Cancer
|
|
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
|
-
- HY-170764
-
|
|
YAP
|
Cancer
|
|
M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .
|
-
- HY-P10788
-
|
|
Complement System
|
Cancer
|
|
CK3 peptide is an NRP-1 targeting peptide with the amino acid sequence CLKADKAKC. The CK3 peptide specifically binds to NRP-1 to target breast cancer cells. Single-photon emission computed tomography (SPECT) and near-infrared fluorescence (NIRF) imaging show significant accumulation of CK3 peptide in xenograft tumors in nude mice. CK3 peptide can be used for molecular imaging studies of breast cancer.
|
-
- HY-W998345
-
|
|
PROTACs
PDK-1
Akt
|
Cancer
|
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
|
-
- HY-155489
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4 11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
|
-
- HY-P10793
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
|
-
- HY-16999
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
|
-
- HY-168035
-
|
|
Histone Methyltransferase
|
Cancer
|
|
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
|
-
- HY-103441
-
|
|
EGFR
|
Cancer
|
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
|
-
- HY-149398
-
|
|
Apoptosis
PARP
CDK
|
Cancer
|
|
PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .
|
-
- HY-12757
-
|
|
BCRP
|
Cancer
|
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
|
-
- HY-153190A
-
|
|
Ferroptosis
STAT
|
Cancer
|
|
W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNA damage response, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway .
|
-
- HY-P10816
-
|
Ac-(DLeu)LLLRVK-Amba
|
Bacterial
|
Infection
Cancer
|
|
PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
|
-
- HY-169078
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
|
-
- HY-P99272
-
|
BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
|
CXCR
|
Cancer
|
|
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
|
-
- HY-128341
-
|
|
ERK
|
Cardiovascular Disease
Cancer
|
|
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
|
-
- HY-148278
-
|
|
Ras
|
Cancer
|
|
BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
|
-
- HY-15186
-
|
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-13072B
-
|
AS-703569 benzoate; R-763 benzoate
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-161629
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
|
-
- HY-168899
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model .
|
-
- HY-147136
-
|
|
YAP
|
Cancer
|
|
MYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC50 of 11 nM. The IC50 values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model .
|
-
- HY-155313
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
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β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
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![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](//file.medchemexpress.eu/product_pic/hy-155313.gif)
- HY-157317
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Apoptosis
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Cancer
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Antitumor agent-126 (Compound II4) is a photoactive (IC50= 0.149) anticancer agent with significant near-infrared fluorescence emission at 650-760 nm. Antitumor agent-126 has antiproliferative activity and can induce apoptosis after laser irradiation. Antitumor agent-126 effectively inhibits tumor growth in mouse xenograft models exposed to 650 nm laser irradiation. Antitumor agent-126 can be used in cancer research .
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- HY-15186C
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GDC-0068 tosylate; RG7440 tosylate
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Organoid
Akt
Apoptosis
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Cancer
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Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
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- HY-169120
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Telomerase
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Cancer
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FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
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- HY-115908
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CDK
Apoptosis
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Cancer
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ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
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- HY-P99623
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MGD006; S80880
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CD3
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Cancer
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Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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- HY-143402
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Topoisomerase
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Cancer
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Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
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- HY-133541
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GLUT
ADC Cytotoxin
Apoptosis
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Cancer
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Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts .
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- HY-139061
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LPL Receptor
ROCK
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Cancer
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Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
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- HY-124727
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JAK
Apoptosis
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Cancer
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ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
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- HY-117938
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Aminoacyl-tRNA Synthetase
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Cancer
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T-3861174 is an inhibitor of prolyl-tRNA synthetase (PRS, Aminoacyl-tRNA Synthetase) without completely inhibiting its translation process. T-3861174 activates the GCN2-ATF4 pathway and induces death in multiple tumor cell lines, including SK-MEL-2. T-3861174 demonstrated significant antitumor activity in multiple xenograft models without significantly affecting body weight .
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- HY-103019E
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BAY-1251152; VIP152
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CDK
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Others
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Enitociclib (VIP152; BAY-1251152) is a selective CDK9 inhibitor. Known for its unique benzyl sulfoxide moiety, VIP152 has demonstrated promising efficacy and tolerability both in vitro and in vivo, including in mouse and rat xenograft models via weekly intravenous infusions Highly effective and well tolerated. VIP152 shows promising long-term single-agent inhibitory activity against double-click refractory diffuse large B-cell lymphoma .
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- HY-10819
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Antifolate
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Cancer
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AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a Km of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED .
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- HY-15160C
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Polo-like Kinase (PLK)
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Cancer
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TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
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- HY-168300
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Reactive Oxygen Species
Apoptosis
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Inflammation/Immunology
Cancer
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Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
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- HY-173065
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CDK
Apoptosis
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Cancer
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CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model .
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- HY-169002
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Phosphatase
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Cancer
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PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
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- HY-153190
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Oxidative Phosphorylation
STAT
Ferroptosis
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Cancer
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W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
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- HY-161515
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NAMPT
Epigenetic Reader Domain
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Cancer
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BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
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- HY-170027
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HIF/HIF Prolyl-Hydroxylase
AMPK
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Cancer
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LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
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- HY-106963
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LGD1550
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RAR/RXR
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Cancer
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ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
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- HY-151155
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
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- HY-160962
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Caspase
Apoptosis
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Cancer
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SM1044 is a dihydroartemisinin (DHA) dimer. SM1044 activates caspase, induces apooptosis in RL95-2 and KLE cells. SM1044 inhibits proliferations of cancer cells RL95-2, KLE, HEC-50, HEC-1-A, HEC-1-B, AN3CA, with IC50 < 3.6 μM . SM1044 inhbits tumor growth in RL95-2 xenograft mouse model .
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- HY-150562
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CDK
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Cancer
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CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
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- HY-161630
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Toll-like Receptor (TLR)
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Cancer
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TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
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- HY-101144
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TCD-717
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Others
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Cancer
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RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
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- HY-149695
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EGFR
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Cancer
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EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
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- HY-101117
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Histone Methyltransferase
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Cancer
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EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
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- HY-162679
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c-Met/HGFR
Apoptosis
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Cancer
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c-Met degrader-1 (Compound H11) is an orally active c-Met degrader (through the ubiquitin proteasome system). c-Met degrader-1 has anti-hepatocellular carcinoma activity (HCC) and inhibits tumor growth in MHCC97H xenografts. c-Met degrader-1 inhibits HCC cell growth, arrests cell cycle, and induces apoptosis. c-Met degrader-1 may overcome resistance to type Ib inhibitors .
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- HY-137849
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PARP
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Cancer
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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 .
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- HY-161628
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Topoisomerase
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Cancer
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Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
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- HY-161631
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Toll-like Receptor (TLR)
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Cancer
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TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
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- HY-149677
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Mitochondrial Metabolism
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Cancer
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ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
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- HY-144777
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FLT3
Apoptosis
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Cancer
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FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
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- HY-146494
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
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- HY-163983
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Microtubule/Tubulin
Apoptosis
PARP
Caspase
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Cancer
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Tubulin polymerization-IN-68 (compound 32) is a tubulin inhibitor that can inhibit tubulin polymerization and destroy the cellular microtubule network. Tubulin polymerization-IN-68 can upregulate the expression of PARP-1 and caspase-3 and induce cell apoptosis, and has anticancer activity. Tubulin polymerization-IN-68 can effectively inhibit HepG2 (IC50=93 nM) and significantly inhibit the growth of HepG2 xenograft tumors in nude mice by oral administration .
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- HY-100591
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Sirtuin
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Neurological Disease
Inflammation/Immunology
Cancer
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SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
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- HY-173075
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RIP kinase
Mixed Lineage Kinase
Necroptosis
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Cancer
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Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models .
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- HY-164576
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NODA-Bz-SCN
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Radionuclide-Drug Conjugates (RDCs)
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Cancer
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NCS-MP-NODA (NODA-Bz-SCN) is a bifunctional chelator that can be used to bind to the labeled peptide DK222 with high specificity for PD-L1. The corresponding fluorinated radioactive is synthesized by the aluminum fluoride method, and NCS-MP-NODA targets DK222 to obtain the radioactive analog [18/19F]DK222. [18F]DK222 can quantify PD-L1 in vivo via PET tracking in xenograft models of multiple cancer types.
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- HY-170951
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Androgen Receptor
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Cancer
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AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC50 of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer .
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- HY-162688
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Telomerase
G-quadruplex
Apoptosis
Ferroptosis
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Others
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Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model .
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- HY-115552
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PARP
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Cancer
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Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .
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- HY-148813
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PROTACs
STAT
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Cancer
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AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-149948
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
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- HY-164689
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Proteasome
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Cancer
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Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
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- HY-149208
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HDAC
Apoptosis
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Cancer
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HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
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- HY-13208
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AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
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IAP
Apoptosis
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Cancer
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Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
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- HY-146755
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Trk Receptor
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Cancer
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TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
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- HY-169075
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HDAC
CDK
Apoptosis
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Cancer
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CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
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- HY-151263
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HDAC
G-quadruplex
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Cancer
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G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer .
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- HY-146461
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Apoptosis
Caspase
ROS Kinase
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Cancer
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Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
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- HY-156077
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Apoptosis
DNA/RNA Synthesis
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Cancer
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anti-TNBC agent-2 (3j) an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research .
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- HY-139659
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PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
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Cancer
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ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-151153
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HDAC
Microtubule/Tubulin
Caspase
Apoptosis
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Cancer
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HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice .
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-
- HY-123045
-
|
|
CDK
|
Cancer
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|
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
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-
- HY-155226
-
|
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FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
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-
- HY-117707
-
|
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Raf
|
Cancer
|
|
EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
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-
- HY-158783
-
|
|
Ceramidase
Bcl-2 Family
LPL Receptor
Apoptosis
|
Neurological Disease
|
|
SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .
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-
- HY-12965B
-
|
|
TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
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-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
|
-
- HY-146432
-
|
|
Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
|
Cancer
|
|
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
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-
- HY-146323
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-58 (Compound C18) is an anti-tumor agent. Antitumor agent-58 effectively inhibits colony formation and cell migration of MGC-803 cells. Antitumor agent-58 induces apoptosis of MGC-803 cells through activation of the p38 and JNK signaling pathways. Antitumor agent-58 induces mitochondrial dysfunction of MGC-803 cells. Antitumor agent-58 effectively inhibits tumor growth of xenograft model bearing MGC-803 cells .
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-
- HY-162873
-
|
|
MEK
Raf
|
Cancer
|
|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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-
- HY-155356
-
|
|
PROTACs
Ras
|
Cancer
|
|
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
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-
- HY-170855A
-
|
|
PROTACs
RET
|
Cancer
|
|
YW-N-7 (TFA) is a PROTAC that targets both the inhibition and degradation of RET kinase, with a DC50 of 88 nM. YW-N-7 (TFA) exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse tumor model and can be used in the area of cancer (Structure: red part represents the target protein ligand: HY-170856; blue part represents the E3 ligase ligand: HY-1708557; black part represents the linker; E3 ligase ligand + linker: HY-170858) .
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-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
|
-
- HY-157169
-
|
AMU302
|
Pim
mTOR
Akt
PI3K
|
Cancer
|
|
IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629) .
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-
- HY-169019
-
|
|
PI3K
Apoptosis
|
Cancer
|
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
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-
- HY-116522
-
-
- HY-146293
-
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|
HDAC
HSP
|
Cancer
|
|
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
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-
- HY-173048
-
|
|
ClpP
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC50 of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC50 of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models .
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-
- HY-156124
-
|
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Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
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-
- HY-111790
-
M3258
1 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
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-
- HY-156002
-
|
Paluratide
|
Ras
ERK
|
Cancer
|
|
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
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-
- HY-P10761
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P990027
-
|
|
ADC Antibody
|
Cancer
|
|
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
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-
- HY-111077
-
|
|
JAK
STAT
|
Inflammation/Immunology
Cancer
|
|
INCB16562 is an orally active and selective inhibitor against JAK1/2 markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma .
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-
- HY-170947
-
|
|
STAT
Quinone Reductase
|
Cancer
|
|
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
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-
- HY-139815
-
|
|
HDAC
|
Cancer
|
|
ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
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-
- HY-123237
-
|
|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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-
- HY-144638
-
|
|
Apoptosis
|
Cancer
|
|
JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity .
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-
- HY-151799
-
|
|
p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
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-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
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-
- HY-163510
-
|
|
Androgen Receptor
|
Cancer
|
|
AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
|
-
- HY-W276819
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-9 (Compound M2) is an inhibitor for polo-like kinase 1 (PLK1), that inhibits PLK proteins modified with peptides 1010pT, cdc25c and PBIP, with IC50s of 1.6, 0.8 and 1.4 μM, respectively. PLK1-IN-9 inhibits proliferations of cancer cells HeLa, HL60, SNU387/499, HepG2, exhibits cytotoxicity and induces apoptosis. PLK1-IN-9 inhibits tumor growth in HepG2 xenograft mouse model .
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-
- HY-143471
-
|
PLK1/BRD4-IN-1
|
Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
Androgen Receptor
c-Myc
|
Cancer
|
|
WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .
|
-
- HY-170574
-
|
|
Molecular Glues
Ser/Thr Kinase
Apoptosis
|
Cancer
|
|
CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC50 value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model .
|
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
-
- HY-125858B
-
|
|
Drug-Linker Conjugates for ADC
MDM-2/p53
|
Others
|
|
(S,R,S)-MI-1061 is the isomer of MI-1061(HY-125858). (S,R,S)-MI-1061 can used to synthesize Antibody-Drug Conjugates (ADCs). MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .
|
-
- HY-P99361
-
|
PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
|
Cancer
|
|
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
|
-
- HY-153221
-
|
|
CDK
|
Cancer
|
|
QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC50 values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer .
|
-
- 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 .
|
-
- HY-168102
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
|
-
- HY-155066
-
|
|
PI3K
mTOR
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
|
-
- HY-168081
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-52 (Compound III-5) is an orally active PD-1/PD-L1 inhibitor that blocks the interaction between PD-1 and PD-L1, with an IC50 of 109.9 nM. PD-1/PD-L1-IN-52 exhibits antitumor activity in a C57BL/6 mouse xenograft model implanted with human PD-1-expressing MC38 colon cancer cells, with a TGI of 49.6% .
|
-
- HY-172209
-
|
|
p38 MAPK
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
PPIA-IN-1 (Compound 20b) is the inhibitor for peptidylprolyl isomerase A (PPIA) with a KD of 0.52 μM. PPIA-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for HCT116 is 0.69 μM), arrests the cell cycle at G0/G1 phase, and exhibits anti-metastatic effect in cell HCT116. PPIA-IN-1 increases ROS, causes DNA damage, ER stress and mitochondrial dysfunction, inducing apoptosis in HCT116 through MAPK pathway. PPIA-IN-1 exhibits antitumor activity in mouse CT26 xenograft models .
|
-
- HY-106031
-
|
|
Topoisomerase
|
Cancer
|
|
F-14512 is a targeted cytotoxic compound that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 combines an epipodophyllotoxin core that targets topoisomerase II with a spermine group that acts as a cell delivery vehicle, with improved selectivity for tumor cells. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and demonstrates high potency in multiple human cell lines (median IC50=0.18 μM). In the MX1 breast tumor xenograft model, F-14512 exhibits potent antitumor activity .
|
-
- HY-10812
-
|
|
PI3K
mTOR
|
Cancer
|
|
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
|
-
- HY-149433
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
|
-
- HY-172399
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
|
Cancer
|
|
FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC50 of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC50 for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models .
|
-
- HY-W087187
-
|
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
|
Cancer
|
|
DOTAGA-anhydride is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide drug conjugates (RDCs). DOTAGA-anhydride can be used to label monoclonal antibodies (mAbs) such as trastuzumab (targeting HER2/neu receptor with an affinity of 5.5 nM) under mild conditions (PBS pH 7.4, 25 °C, 30 minutes) after chelation with indium-111. [111In-DOTAGA]-trastuzumab showed a tumor uptake of 65% ID/g in mice bearing breast cancer BT-474 xenografts 72 hours after injection, which is valuable for SPECT/CT imaging and biodistribution studies.
|
-
- HY-157295
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC50 values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .
|
-
- HY-162103
-
|
|
TAM Receptor
Apoptosis
|
Cancer
|
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Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
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- HY-118119
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PGE synthase
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Cancer
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CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
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- HY-P10744
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Radionuclide-Drug Conjugates (RDCs)
PSMA
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Cancer
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BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-156792
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Ser/Thr Kinase
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Cancer
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RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
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- HY-169830
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Drug Derivative
Apoptosis
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Cancer
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2-(Cyclohexylmethyl)-plumbagin is a derivative of the naphthoquinone compound Plumbagin (HY-N1497). Under nutrient-deprived conditions, 2-(Cyclohexylmethyl)-plumbagin selectively exhibits cytotoxicity against PANC-1 human pancreatic cancer cells (PC50 = 0.11 µM) and reduces the phosphorylation of Akt and mTOR in PANC-1 cells. 2-(Cyclohexylmethyl)-plumbagin also induces apoptosis (Apoptosis) in PANC-1 cells at a concentration of 1 µM. Additionally, 2-(Cyclohexylmethyl)-plumbagin reduces tumor volume and weight in a xenograft MiaPaCa-2 pancreatic cancer mouse model .
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- HY-156457
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EGFR
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Cancer
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EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
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- HY-148409
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Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
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Cancer
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MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
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- HY-173047
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Ras
ERK
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Cancer
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KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRAS G12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRAS G12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models .
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- HY-114162B
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Epigenetic Reader Domain
Apoptosis
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Cancer
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VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
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- HY-159891
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Microtubule/Tubulin
Apoptosis
Caspase
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Cancer
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Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective antitumor compound targeting microtubule protein. Microtubule destabilizing agent-2 destabilizes microtubule proteins and inhibits microtubule polymers. Microtubule destabilizing agent-2 arrests the G0/G1 phase in human tumor cells. Microtubule destabilizing agent-2 induces Apoptosis by activating the cascade pathway of caspases. Microtubule destabilizing agent-2 has anti-inflammatory activity, as inhibiting TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 reduces tumors growth in xenograft mice .
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- HY-173060
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ERK
Apoptosis
Autophagy
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Cancer
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ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
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- HY-N9174
-
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Others
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Cancer
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5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
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- HY-163434
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EGFR
Histone Methyltransferase
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Cancer
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PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
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- HY-150613
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Epigenetic Reader Domain
PARP
Apoptosis
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Cancer
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PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
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- HY-143881
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FGFR
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Cancer
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FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-164411
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c-Met/HGFR
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Cancer
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KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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- HY-149521
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PI3K
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Cancer
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PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
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- HY-168936
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))
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- HY-172256
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PI4K
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Cancer
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PI4KIII beta inhibitor 5 is a PI4KIIIβ inhibitor with an IC50 of 19 nM. PI4KIII beta inhibitor 5 can induce cancer cell apoptosis (Apoptosis), cell cycle arrest at the G2/M phase, and autophagy (Autophagy) by inhibiting the PI3K/AKT pathway. PI4KIII beta inhibitor 5 has also demonstrated significant antitumor activity in the H446 xenograft model of small cell lung cancer. PI4KIII beta inhibitor 5 can be used for research in the field of cancer therapy .
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- HY-149508
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Keap1-Nrf2
Reactive Oxygen Species
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Cancer
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Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin .
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- HY-160777
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Galeterone 3β-imidazole
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Molecular Glues
Androgen Receptor
MNK
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Cancer
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VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
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- HY-121081
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CDK
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Cancer
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BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
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- HY-172217
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DNA Methyltransferase
Apoptosis
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Cancer
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DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
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- HY-158156
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NF-κB
Apoptosis
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Cancer
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NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
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- HY-156086
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Trk Receptor
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Cancer
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TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA G595R, TRKA G667C and TRKA F589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM .
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- HY-P5520
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Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
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Cancer
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GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
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- HY-173182
-
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Microtubule/Tubulin
P-glycoprotein
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Cancer
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Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor. By binding to the colchicine site of tubulin, it causes G2/M cell cycle arrest and generates reactive oxygen species (ROS). Antitumor agent-200 exhibits significant inhibitory activity against MCF7/ADR and KBV200 cell lines with overexpression of P-glycoprotein (P-gp), with drug resistance indices (DRI) of 0.83 and 0.58 respectively. In the MCF-7 xenograft model, Antitumor agent-200 (25 mg/kg, intraperitoneal injection) can achieve a tumor growth inhibition rate of 57.2%. Antitumor agent-200 can be used in the research of the anti-cancer field .
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- HY-123929
-
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MDM-2/p53
Wnt
IKK
Apoptosis
Caspase
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Cancer
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PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
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- HY-168715
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SHP2
Apoptosis
MAPKAPK2 (MK2)
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Cancer
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SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
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- HY-121365
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Bacterial
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Infection
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Forphenicinol is an immunomodulator and a derivative of the bacterial metabolite forphenicine. It increases the phagocytosis of yeast by peritoneal macrophages isolated from thioglycolate-stimulated mice. Forphenicinol (100 μg/animal) prevents cyclophosphamide-induced suppression of delayed-type hypersensitivity (DTH), as well as enhances DTH in response to the hapten oxazolone or sheep red blood cells in mice. It enhances the bactericidal activity of macrophages against P. aeruginosa in mice when administered at a dose of 0.5 mg/kg.2 Forphenicinol (15.6-1,000 μg/animal) increases survival in a mouse model of P. aeruginosa infection. It also inhibits tumor growth in S180 sarcoma and IMC carcinoma mouse xenograft models when administered at doses ranging from 0.05 to 5 mg/kg per day.
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- HY-170921
-
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Deubiquitinase
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Cancer
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USP1-IN-11 (compound 38-P2) is a selective, reversible, and noncompetitive USP1 (Ubiquitin-specific protease 1) inhibitor. USP1-IN-11 activates the DDR (DNA damage repair) pathway, induces cell cycle arrest and cell Apoptosis, and inhibits cell survival. USP1-IN-11 enhances the sensitivity of Olaparib (HY-10162)-resistant cells to Olaparib (HY-10162) and shows a synergetic effect with Andrographolide (HY-N0191) in BRCA-proficient cancer cells. USP1-IN-11 displays significant, dose-dependent antitumor efficacy in the MDA-MB-436 xenograft model .
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- HY-P10819
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Histone Demethylase
Apoptosis
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Cancer
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S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
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- HY-173320
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Wee1
HSP
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Cancer
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|
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .
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- HY-157228
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PROTACs
Ras
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Cancer
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ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
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- HY-168135
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PROTACs
c-Met/HGFR
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Cancer
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PROTAC c-Met degrader-1 (Compound Met-DD4) is an orally active PROTAC degrader for c-Met with a DC50 of 6.21 nM. PROTAC c-Met degrader-1 inhibits the proliferation of c-Met-addicted cell MKN-45 with an IC50 of 4.37 nM, and arrests the cell cycle at G0/G1 phase. PROTAC c-Met degrader-1 exhibits antitumor efficacy in MKN-45 xenograft mouse models . (Pink: Ligand for target protein (HY-13404); Blue: Ligand for E3 ligase (HY-W087383); Black: Linker (HY-W074901))
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- HY-168555
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CDK
PROTACs
Apoptosis
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Cancer
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YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
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- HY-159577
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PI3K
mTOR
Akt
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Cancer
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Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
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- HY-156110
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Insulin Receptor
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Cancer
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IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
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- HY-158726
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Fluorescent Dye
Apoptosis
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Cancer
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Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model .
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- HY-170968
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EGFR
Apoptosis
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Cancer
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EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
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- HY-151563A
-
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Deubiquitinase
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Cancer
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OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .
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- HY-172200
-
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PD-1/PD-L1
HDAC
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Cancer
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PD-L1/HDAC6-IN-1 (Compound HP29) is the inhibitor for PD-L1 and HDAC6 that inhibits the PD-L1/PD-1 interaction and HDAC6 with an IC50 of 26.8 nM and 69 nM. PD-L1/HDAC6-IN-1 enhances the killing ability of Jurkat T cells against HepG2 cells with an IC50 of 3.4 μM. PD-L1/HDAC6-IN-1 exhibits good pharmacokinetics characteristics in rats with a drug exposure of 871.62 ng·h/mL, and exhibits antitumor activity in mouse B16-F10 xenograft models .
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- HY-173147
-
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CDK
|
Cancer
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CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer .
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- HY-159912
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YAP
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Cancer
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pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
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- HY-145836
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FGFR
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Cancer
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FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
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-
- HY-155046
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FGFR
|
Cancer
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|
FGFR4-IN-14 (Compound 27i) is a FGFR4 inhibitor (IC50: 2.4 nM. FGFR4-IN-14 inhibits the proliferation of V550L and N535K mutant strains, with IC50s of 21 nM, 2.5 nM, 171 nM against huh7, BaF3/ETV6-FGFR4-V550L and BaF3/ETV6-FGFR4-N535K cells respectively. FGFR4-IN-14 has potent antitumor efficacy in the Huh7 xenograft model. FGFR4-IN-14 can be used for research of hepatocellular carcinoma (HCC) .
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-
- HY-164445
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STAT
|
Cancer
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STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
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-
- HY-146095
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
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Cancer
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|
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
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-
- HY-171509
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Drug-Linker Conjugates for ADC
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Cancer
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Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
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-
- HY-P1925A
-
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PI3K
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
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-
- HY-126287
-
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Trk Receptor
Apoptosis
|
Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
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-
- HY-117991
-
|
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VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
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-
- HY-159922
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
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-
- HY-170978
-
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PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
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-
- HY-153321
-
|
BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
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-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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-
- HY-N6972
-
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Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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-
- HY-P10914
-
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MDM-2/p53
Autophagy
|
Inflammation/Immunology
Cancer
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|
D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
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- HY-163709
-
|
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PROTACs
FAK
|
Cancer
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PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
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-
- HY-167854
-
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Aurora Kinase
Apoptosis
IGF-1R
|
Cancer
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KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
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-
- HY-170852
-
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PROTACs
RET
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Cancer
|
|
QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854) .
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-
- HY-163985
-
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|
PROTACs
FGFR
Apoptosis
|
Cancer
|
|
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
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-
- HY-139062
-
|
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
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-
- HY-157213
-
|
|
Apoptosis
PROTACs
FLT3
|
Cancer
|
|
LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
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-
- HY-164490
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
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-
- HY-N6972R
-
|
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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-
- HY-136765
-
|
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PI3K
|
Cancer
|
|
PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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-
- HY-159803
-
|
6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin
|
Endogenous Metabolite
|
Cancer
|
|
IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitory activity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitory activity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
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-
- HY-164392
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .
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-
- HY-170824
-
|
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .
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-
| Cat. No. |
Product Name |
Type |
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- HY-D2620
-
|
|
Fluorescent Dyes/Probes
|
|
CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LDs). CAR-2 exhibits phototoxicity in breast cancer cells with IC50 of 0.01-0.02 μM. CAR-2 exhibits antitumor efficacy in 4T1 xenograft mouse models .
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-
- HY-158726
-
|
|
Fluorescent Dyes/Probes
|
|
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model .
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| Cat. No. |
Product Name |
Type |
-
- HY-W013973
-
|
|
Biochemical Assay Reagents
|
|
p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
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-
- HY-139109
-
|
ADS 780WS
|
Indicators
|
|
IR-783 (ADS 780WS) is a near-infrared (NIR) heptamethine cyanine fluorescent probe. IR-783 significantly inhibits tumour growth and induces apoptosis in MDA-MB-231 xenograft model. IR-783 can be used to study breast cancer .
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-
- HY-W013973R
-
|
|
Biochemical Assay Reagents
|
|
p-Terphenyl (Standard) is the analytical standard of p-Terphenyl. This product is intended for research and analytical applications. p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-164388
-
Z-VAD
4 Publications Verification
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is a competitive, irreversible pan-caspase inhibitor. Z-VAD inhibits all 10 caspases, except for caspase-2 which is only weakly inhibited. Z-VAD decreases radiation-induced apoptosis. Z-VAD induces both autophagy and necrosis in irradiated MDA-MB-231 and H460 mouse xenografts. Z-VAD with radiation produces a significant tumor growth delay and shows dramatic antiangiogenic effect in cancer xenograft .
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-
- HY-P5098
-
|
|
Integrin
|
Cancer
|
|
E(c(RGDfK)) is an αvβ3 integrin-specific binding moiety with tumor targeting properties. Increased uptake of E(c(RGDfK)) in human ovarian cancer OVCAR-3 xenograft tumors may be useful in cancer research .
|
-
- HY-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
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-
- HY-P3990
-
|
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613); EP-100
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
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-
- HY-13589
-
|
LU103793 free base
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer .
|
-
- HY-13589A
-
|
LU103793 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Cemadotin (LU103793) hydrochloride is a water-soluble synthetic analogue of Dolastatin 15 (HY-P1126) that inhibits cell proliferation in vitro and the growth of tumor xenografts in mice. Cemadotin hydrochloride blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin hydrochloride can be used to research anticancer .
|
-
- HY-P10759
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
- HY-P10788
-
|
|
Complement System
|
Cancer
|
|
CK3 peptide is an NRP-1 targeting peptide with the amino acid sequence CLKADKAKC. The CK3 peptide specifically binds to NRP-1 to target breast cancer cells. Single-photon emission computed tomography (SPECT) and near-infrared fluorescence (NIRF) imaging show significant accumulation of CK3 peptide in xenograft tumors in nude mice. CK3 peptide can be used for molecular imaging studies of breast cancer.
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-
- HY-P10793
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
|
-
- HY-P10816
-
|
Ac-(DLeu)LLLRVK-Amba
|
Bacterial
|
Infection
Cancer
|
|
PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
|
-
- HY-156002
-
|
Paluratide
|
Ras
ERK
|
Cancer
|
|
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
|
-
- HY-P10761
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P10744
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P5520
-
|
|
Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
-
- HY-P10819
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
|
-
- HY-P1925A
-
|
|
PI3K
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
|
-
- HY-P10914
-
|
|
MDM-2/p53
Autophagy
|
Inflammation/Immunology
Cancer
|
|
D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99160
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Labetuzumab is a humanised anti-carcinoembryonic antigen (CEA) monoclonal antibody that inhibits tumour growth and sensitises human medullary thyroid cancer xenografts to Dacarbazine chemotherapy .
|
-
- HY-P99849
-
|
ABT-806
|
EGFR
|
Cancer
|
|
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-P99922
-
|
|
LAG-3
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
- HY-P99493
-
|
IMGN242; huC242-DM4
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 (HY-12454)). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-111965
-
-
- HY-P99282
-
|
VB6-845; Anti-Human EpCAM Recombinant Antibody Fab Fragment, 17-1A
|
Apoptosis
|
Cancer
|
|
Citatuzumab bogatox (VB6-845) is recombinant immunotoxin that composed of Fab fragment of humanized antibody targeting EpCAM and a modified cytotoxin bouganin. Citatuzumab bogatox binds to and selectively induces apoptosis in EpCAM-positive cell lines and shows good activity in EpCAM-positive human tumour xenograft models .
|
-
- HY-141606
-
|
BAY 94-9343
|
Microtubule/Tubulin
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models .
|
-
- HY-P99272
-
|
BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
|
CXCR
|
Cancer
|
|
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
- HY-P990027
-
|
|
ADC Antibody
|
Cancer
|
|
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
|
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
-
- HY-P99361
-
|
PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
|
Cancer
|
|
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-135217
-
-
-
- HY-N0421
-
-
-
- HY-N14738
-
-
-
- HY-N5166
-
-
-
- HY-135217R
-
-
-
- HY-139104
-
-
-
- HY-N0421R
-
|
|
Structural Classification
Animals
Source classification
Steroids
|
Apoptosis
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
-
- HY-N12044
-
-
-
- HY-133541
-
|
|
Classification of Application Fields
Disease Research Fields
Cancer
|
GLUT
ADC Cytotoxin
Apoptosis
|
|
Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts .
|
-
-
- HY-N9174
-
|
|
Structural Classification
Flavonoids
Flavones
Source classification
Plants
Moraceae
Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat
|
Others
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
-
- HY-N6972
-
-
-
- HY-N6972R
-
|
|
Structural Classification
Alkaloids
Stephania cepharantha Hayata
Plants
Isoquinoline Alkaloids
Menispermaceae
Stephania japonica (Thunb.) Miers
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-157029S
-
|
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
-
- HY-157031S
-
|
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-14375
-
|
|
|
Alkynes
|
|
CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft . CB 300919 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-157029S
-
|
|
|
Alkynes
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-157031S
-
|
|
|
Alkynes
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-139659
-
|
|
|
PROTAC Synthesis
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-157411
-
|
|
|
Alkynes
|
|
anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-158829
-
|
|
|
Antisense Oligonucleotides
|
|
SSOe26 sodium is a 15mer antisense oligonucleotide targeting?HER4. SSOe26 sodium induces exon 26 skipping, leading to the generation of a novel mRNA transcript that excludes exon 26 (CYT2 isoform). SSOe26 sodium decreases tumour growth in mouse xenografts.
|
-
- HY-153834
-
|
|
|
Aptamers
|
|
GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-164185
-
|
|
|
Aptamers
|
|
P12FR2 sodium is an aptamer targeting human pancreatic adenocarcinoma up-regulated factor (PAUF). P12FR2 specifically binds to human PAUF with an estimated apparent KD of 77 nM. P12FR2 inhibits PAUF-induced PANC-1 cell migration and pancreatic cancer xenograft growth.
|
-
- HY-153834A
-
|
|
|
Aptamers
|
|
GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-158830
-
|
|
|
Antisense Oligonucleotides
|
|
MDM4-targeting ASO sodium is a 25mer antisense oligonucleotide targeting?MDM4. MDM4-targeting ASO sodium induced exon 6 skipping, leading to nonsense-mediated decay of the mRNA transcript that excludes exon-6. In multiple human melanoma cell lines and in melanoma patient-derived xenograft (PDX) mouse models, MDM4-targeting ASO-mediated skipping of exon 6 decreased MDM4 abundance, inhibited melanoma growth, and enhanced sensitivity to MAPK-targeting therapeutics.
|
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