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antitumor potency

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36

Inhibitors & Agonists

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Natural
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1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12202
    MEK inhibitor
    2 Publications Verification

    		 MEK Cancer
    MEK inhibitor is a potent MEK inhibitor with antitumor potency.
    MEK inhibitor
  • HY-115568
    BETd-246
    2 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity .
    BETd-246
  • HY-15958
    VBY-825
    1 Publications Verification

    		 Cathepsin Inflammation/Immunology Cancer
    VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects .
    VBY-825
  • HY-139590
    Zeteletinib

    BOS-172738; DS-5010

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
    Zeteletinib
  • HY-155303
    DCLK1-IN-2

    		Ser/Thr Protease Cancer
    DCLK1-IN-2 (compound I-5) is a potent DCLK1 inhibitor with an IC50 of 171.3  nM. DCLK1-IN-2 shows remarkable antiproliferative effects on SW1990 cell lines (IC50 of 0.6 μM) and in vivo antitumor potency .
    DCLK1-IN-2
  • HY-169075
    CDK/HDAC-IN-4

    		HDAC CDK Apoptosis Cancer
    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 .
    CDK/HDAC-IN-4
  • HY-162594
    Antitumor agent-164

    		Microtubule/Tubulin Cancer
    Antitumor agent-164 (compound 60c) is a colchicine-binding site inhibitor (CBSI) with potency against taxane-sensitive TNBC. Antitumor agent-164 is a next-generation derivative of VERU-111 .
    Antitumor agent-164
  • HY-168097
    Ferroptosis inducer-6

    		Ferroptosis Reactive Oxygen Species Cancer
    Ferroptosis inducer 6 (6d) is a ferroptosis inducer with high potency for type I/-II photodynamic therapy by inducing ROS generation, oxidative stress and mitochondrial damage. Ferroptosis inducer 6 has anti-tumor activity .
    Ferroptosis inducer-6
  • HY-144232
    Anticancer agent 28

    		Others Cancer
    Anticancer agent 28 shows good antitumor activity in H22 allogeneic mice in vivo. Anticancer agent 28 has inhibitory potency in K562 cells of 50 times than oridonin, and its IC50 value is 0.09 μM.
    Anticancer agent 28
  • HY-139590A
    Zeteletinib hemiadipate

    BOS-172738 hemiadipate; DS-5010 hemiadipate

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
    Zeteletinib hemiadipate
  • HY-12457
    Rachelmycin

    CC-1065; NSC 298223

    		 Antibiotic DNA/RNA Synthesis Infection Cancer
    Rachelmycin (CC-1065) is an antitumor antibiotic and a DNA-alkylating agent. Rachelmycin has cytotoxic potency that can be used as a cytotoxin to synthesis ADC. Rachelmycin effectively inhibits DNA synthesis. Rachelmycin can be used for cancer and infection research .
    Rachelmycin
  • HY-146438
    PPARγ agonist 3

    		PPAR Cancer
    PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
    PPARγ agonist 3
  • HY-170906S
    MAT2A-IN-23

    		Methionine Adenosyltransferase (MAT) Cancer
    MAT2A-IN-23 (compound 39) is a MAT2A inhibitor, with an IC50 of 4 nM. MAT2A-IN-23 inhibits SAM in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 3 and 2 nM, respectively. MAT2A-IN-23 inhibits SDMA in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 2 and >3000 nM, respectively. MAT2A-IN-23 inhibits HCT-116 (MTAP −/−) cell proliferation with with an IC50 of 47 nM .
    MAT2A-IN-23
  • HY-168122
    Apoptosis inducer 29

    		Apoptosis Cancer
    Apoptosis inducer 29 (compund Y9) is an apoptosis inducer that exhibits antitumor effects in non-small cell lung cancer. Apoptosis inducer 29 selectively acidifies lysosomes and induces lysosomal dysfunction, with superior potency to Gboixn (HY-111651) in vitro and in vivo. .
    Apoptosis inducer 29
  • HY-146439
    PPARγ agonist 4

    		PPAR Cancer
    PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
    PPARγ agonist 4
  • HY-147656
    NAMPT degrader-1

    		ATTECs NAMPT Autophagy Cancer
    NAMPT degrader-1 (Compound A3), an autophagosome-tethering compound (ATTEC), is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency .
    NAMPT degrader-1
  • HY-B0305A
    Roxatidine Acetate Hydrochloride

    HOE 760

    		 Histamine Receptor Metabolic Disease Inflammation/Immunology Cancer
    Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity .
    Roxatidine Acetate Hydrochloride
  • HY-B0305
    Roxatidine acetate

    		Histamine Receptor Metabolic Disease Inflammation/Immunology Cancer
    Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity .
    Roxatidine acetate
  • HY-109189
    Rezivertinib
    1 Publications Verification

    BPI-7711

    		 EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
    Rezivertinib
  • HY-15656A
    Ceritinib dihydrochloride
    Maximum Cited Publications
    32 Publications Verification

    LDK378 dihydrochloride

    		 Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Endocrinology Cancer
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency .
    Ceritinib dihydrochloride
  • HY-15656
    Ceritinib
    Maximum Cited Publications
    32 Publications Verification

    LDK378

    		 Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Endocrinology Cancer
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
    Ceritinib
  • HY-15812
    Aurora kinase-IN-5

    		Aurora Kinase Cancer
    Aurora kinase-IN-5 (compound 1) is an Aurora kinase (Aurora Kinase) inhibitor with anti-tumor activity that promotes paclitaxel (HY-B0015) induced cell death. Aurora kinase-IN-5 exhibits high selectivity and potency against Aurora A, B, and C kinases, with IC50 values of 5.6, 18.4, and 24.6 nM, respectively .
    Aurora kinase-IN-5
  • HY-139795
    ZYJ-25e

    		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 .
    ZYJ-25e
  • HY-15656R
    Ceritinib (Standard)

    		Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R Endocrinology Cancer
    Ceritinib (Standard) is the analytical standard of Ceritinib. This product is intended for research and analytical applications. Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
    Ceritinib (Standard)
  • HY-118899
    XR5944

    		Endogenous Metabolite Cancer
    XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
    XR5944
  • HY-151453
    Topoisomerase IIα-IN-4

    		Topoisomerase Apoptosis Cancer
    Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .
    Topoisomerase IIα-IN-4
  • HY-146755
    TIY-7

    		Trk Receptor Cancer
    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 .
    TIY-7
  • 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 .
    M3258
  • HY-139815
    ZYJ-34c

    		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 .
    ZYJ-34c
  • HY-149878
    BD-9136

    		PROTACs Epigenetic Reader Domain Cancer
    BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity .(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))
    BD-9136
  • HY-106031
    F-14512

    		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 .
    F-14512
  • HY-145836
    FGFR4-IN-8

    		FGFR Cancer
    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 .
    FGFR4-IN-8
  • HY-158029
    PI3Kα-IN-21

    		PI3K Apoptosis Cancer
    PI3Kα-IN-21 (compound 8) is a PI3Kα inhibitor, and its selectivity for PI3Kα is 10.41/16.99/37.53 times higher than PI3Kβ/γ/δ respectively (IC50: 96.89/568.24/397.48 nM ). PI3Kα-IN-21 inhibits cancer cell activity, proliferation, and migration, and induces mitochondrial apoptosis through the PI3K/Akt/mTOR pathway. PI3Kα-IN-21 exhibits in vivo antitumor potency in a mouse model of non-small cell lung cancer .
    PI3Kα-IN-21
  • HY-15334
    CEP-5214

    		VEGFR Cancer
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
    CEP-5214
  • HY-12875
    BQU57

    		Ras Cancer
    BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .
    BQU57
  • HY-170926
    CQ1373

    		RET Apoptosis Cancer
    CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .
    CQ1373

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