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suppressed xenograft tumor growth

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-70062
    Pevonedistat
    Maximum Cited Publications
    212 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 .
    Pevonedistat
  • HY-101120
    666-15
    55+ Cited Publications

    		 Epigenetic Reader Domain Cancer
    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 .
    666-15
  • HY-P99275
    Patritumab
    1 Publications Verification

    AMG-888; U3-1287

    		 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 .
    Patritumab
  • HY-148807
    Zavondemstat

    QC8222 free base; TACH 101 free base

    		 Histone Demethylase Apoptosis Cancer
    Zavondemstat (QC8222 free base; TACH 101 free base) is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
    Zavondemstat
  • HY-150190
    F5446
    1 Publications Verification

    		 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 .
    F5446
  • HY-100591
    SirReal2
    2 Publications Verification

    		 Sirtuin Neurological Disease Inflammation/Immunology Cancer
    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 .
    SirReal2
  • HY-10484
    Pevonedistat hydrochloride
    Maximum Cited Publications
    212 Publications Verification

    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 .
    Pevonedistat hydrochloride
  • HY-P99364
    Icrucumab
    1 Publications Verification

    Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1

    		 VEGFR Apoptosis p38 MAPK Akt Endocrinology Cancer
    Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is an IgG1 antibody inhibitor targeting VEGFR-1/FLT1 with anti-tumor activity. By blocking ligand-dependent phosphorylation and downstream signal transduction, Icrucumab reduces the activities of MAPK and Akt in breast cancer xenograft models, inhibits the proliferation and invasion of VEGFR-1-positive tumor cells, and reverses the conversion of M1 macrophages to the pro-tumor M2-like phenotype. Icrucumab also inhibits tumor cell proliferation, promotes apoptosis, and effectively suppresses tumor growth through direct targeting of tumors and host support mechanisms. In addition, Icrucumab exhibits a synergistic effect when combined with chemotherapeutic agents, and it is used in research related to various cancers including advanced solid malignancies, thyroid cancer, melanoma, and lung cancer .
    Icrucumab
  • HY-128341
    ERK5-IN-2

    		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 .
    ERK5-IN-2
  • HY-P991558
    RO-5429083

    RG-7356

    		 Transmembrane Glycoprotein Cancer
    RO-5429083 (RG-7356) is a humanized monoclonal antibody targeting CD44. RO-5429083 binds to the extracellular domain of CD44 and inhibits constitutive EGFR phosphorylation. RO-5429083 suppresses tumor growth in xenograft models and can be used in research related to head and neck squamous cell carcinoma and acute myeloid leukemia .
    RO-5429083
  • HY-155489
    DDO-2728
    2 Publications Verification

    		 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 .
    DDO-2728
  • HY-159579
    CW-3308

    		PROTACs Epigenetic Reader Domain Cancer
    CW-3308 is an orally active BRD9 PROTAC degrader with an DC50 of 92 nM. CW-3308 forms a ternary complex with BRD9 and cereblon to mediate BRD9 degradation. CW-3308 inhibits the viability of synovial sarcoma and rhabdoid tumor cells. CW-3308 reduces BRD9 protein levels in xenograft tumor tissues and suppresses tumor growth in xenograft models. CW-3308 can be used for the research of synovial sarcoma and rhabdoid tumors .
    CW-3308
  • HY-120692
    Cyclanoline chloride

    		JAK STAT Apoptosis Cancer
    Cyclanoline chloride is an alkaloid. Cyclanoline chloride can be isolated from Fangji. Cyclanoline (chloride) inhibits the phosphorylation of JAK2 and STAT3, and induces Apoptosis. Cyclanoline chloride suppresses tumor growth in subcutaneous bladder cancer xenograft models of nude mice. Cyclanoline chloride reverses cisplatin resistance in bladder cancer cells and enhances the efficacy of Cisplatin (HY-17394). Cyclanoline chloride can be used for research related to bladder cancer .
    Cyclanoline chloride
  • HY-12757
    YHO-13177
    2 Publications Verification

    		 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 .
    YHO-13177
  • HY-174979
    Dac590

    		Fat Mass and Obesity-associated Protein (FTO) Apoptosis Inflammation/Immunology Cancer
    Dac590 is an orally active and selective obesity-associated protein (FTO) inhibitor with an IC50 of 6.06 nM. Dac590 shows highly selective over ALKBH5 and ALKBH3. Dac590 suppresses oncogenic FTO signaling, induces myeloid differentiation, G1-phase cell cycle arrest, and apoptosis in acute myeloid leukemia (AML) cells. Dac590 inhibits xenograft tumor growth and prolongs survival in acute myeloid leukemia mouse models with no observed toxicity. Dac590 can be used for the research of AML .
    Dac590
  • HY-178836
    Z56-L23

    		Drug-Linker Conjugates for ADC Ras Cancer
    Z56-L23 is a conjugate of RAS-targeting ADC cytotoxic payload-linker with anti-tumor activity. Z56-L23 can be conjugated with HER3 antibody, EGFR antibody or EGFRxHER3 bispecific antibody to form intact antibody-drug conjugates (ADCs). ADC molecules related to Z56-L23 effectively inhibit the proliferation of tumor cells and also significantly suppress tumor growth in xenograft mouse models. Z56-L23 can be used in the research of pancreatic cancer .
    Z56-L23
  • HY-149433
    BWA-522

    		PROTACs Androgen Receptor Apoptosis Cancer
    BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .
    BWA-522
  • HY-N0475
    Triptophenolide

    Hypolide; (+)-Triptophenolide

    		 Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis Inflammation/Immunology Cancer
    Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
    Triptophenolide
  • HY-P11228
    FPP29

    		PROTACs Apoptosis DNA/RNA Synthesis Cancer
    FPP29 is a potent peptide-based FOXM1 PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494)) .
    FPP29
  • HY-P3990
    Coibamide A

    		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 .
    Coibamide A
  • HY-170824
    SMD-3236

    		PROTACs SWI/SNF Complex Epigenetic Reader Domain Cancer
    SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia .
    SMD-3236
  • HY-132173
    GL0388

    		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 .
    GL0388
  • HY-165245
    SBI-183

    		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 .
    SBI-183
  • HY-175652
    AZD9750

    		PROTACs Adenosine Receptor Cancer
    AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .
    AZD9750
  • HY-N6651
    Isocryptotanshinone

    		STAT Phosphatase Apoptosis Autophagy p38 MAPK EGFR JAK Bcl-2 Family Survivin Akt mTOR PARP Caspase Atg8/LC3 CDK Cancer
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation [1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC .
    Isocryptotanshinone
  • HY-116269
    AZA197

    		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. AZA197 can be used for the study of colon cancer .
    AZA197
  • HY-170933
    SGK1-IN-6

    		SGK Cancer
    SGK1-IN-6 is a selective SGK1 inhibitor with an IC50 of 0.39 μM, showing selectivity over SGK2/3. SGK1-IN-6 inhibits cancer cell migration and invasion, improves SGK1 protein thermal stability. SGK1-IN-6 decreases SGK1 protein levels in tumor tissues, suppresses tumor growth in mouse xenograft models. SGK1-IN-6 can be used for the research of prostate cancer .
    SGK1-IN-6
  • HY-177332
    SLC-391

    		TAM Receptor SARS-CoV Akt Infection Cancer
    SLC-391 is an orally active AXL kinase inhibitor with an IC50 of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer .
    SLC-391
  • HY-175208
    MST3-IN-1

    		Hippo (MST) Caspase Bcl-2 Family Apoptosis Cancer
    MST3-IN-1 is a selective and orally active MST3 inhibitor, with an IC50 of 122.4 nM. MST3-IN-1 shows antiproliferative activity against HepG2 cell. MST3-IN-1 effectively induces apoptosis in HepG2 cells, and halts the cell cycle at the G2/M transition. MST3-IN-1 significantly suppressed tumor growth in HepG2 xenograft mice. MST3-IN-1 can be used for the study of liver cancer .
    MST3-IN-1
  • HY-162938
    Skp2 inhibitor 3

    		E1/E2/E3 Enzyme Cancer
    Skp2 inhibitor 3 is an orally active inhibitor of the Skp2-Cks1 complex, with an IC50 of 4.86 μM. Skp2 inhibitor 3 reduces Skp2 protein expression while upregulating the expression of p21 and p27. Skp2 inhibitor 3 inhibits colony formation and migration of cancer cells, and induces cell cycle arrest at the S phase. Skp2 inhibitor 3 suppresses tumor growth in xenograft mice. Skp2 inhibitor 3 can be used in the research of gastric cancer and prostate cancer .
    Skp2 inhibitor 3
  • HY-172614
    RK-0080552

    RK-552

    		 Histone Methyltransferase Apoptosis Cancer
    RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .
    RK-0080552
  • HY-W369099
    HJC0152 free base

    		STAT Apoptosis Cancer
    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 .
    HJC0152 free base
  • HY-177750
    TD-522

    		Molecular Glues Apoptosis Cancer
    TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .
    TD-522
  • HY-124067
    EC-70124

    		IKK JAK STAT NF-κB Cancer
    EC-70124 is an orally active multikinase inhibitor targeting IKKβ and JAK2. EC-70124 blocks IkB phosphorylation and STAT3 (Tyr705) activation, suppressing NF-κB nuclear translocation and STAT3 transcriptional activity. EC-70124 reduces tumor growth and cancer stem cell (CSC) populations in prostate cancer cells and xenograft models. EC-70124 is promising for research of prostate cancer .
    EC-70124
  • HY-122703
    BETi-211

    		Epigenetic Reader Domain Cancer
    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 .
    BETi-211
  • HY-14815
    Fosbretabulin

    Combretastatin A4 phosphate

    		 Apoptosis Microtubule/Tubulin Cancer
    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 .
    Fosbretabulin
  • HY-175017
    Survivin-IN-2

    		Survivin Cancer
    Survivin-IN-2 is a survivin inhibitor. Survivin-IN-2 shows cytotoxicity in cells with IC50s of 0.53 μM (C4-2 cells) and 1.06 μM (PC-3 cells). Survivin-IN-2 effectively suppresses xenograft tumor growth without apparent toxicity and eliminates survivin in the tumors. Survivin-IN-2 can be used for the study of prostate cancer .
    Survivin-IN-2
  • HY-70062R
    Pevonedistat (Standard)

    MLN4924 (Standard)

    		 NEDD8-activating Enzyme Apoptosis Reference Standards Cancer
    Pevonedistat (Standard) is the analytical standard of Pevonedistat. This product is intended for research and analytical applications. 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 .
    Pevonedistat (Standard)
  • HY-175253
    YZ-35

    		STAT Apoptosis Cancer
    YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer .
    YZ-35
  • HY-148807A
    Zavondemstat L-lysine

    QC8222; TACH 101

    		 Apoptosis Histone Demethylase Cancer
    Zavondemstat (QC8222; TACH 101) L-lysine is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat L-lysine induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat L-lysine suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat L-lysine can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
    Zavondemstat L-lysine
  • HY-177796
    TMLB-C16

    		Apoptosis CDK Caspase PARP Cancer
    TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a KD of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC50 = 6.53 μM) and HCCLM3 cells (IC50 = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research .
    TMLB-C16
  • HY-P991243
    MP-RM-1

    		EGFR Akt Cancer
    MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells .
    MP-RM-1
  • HY-179468
    STAT3-IN-49

    		STAT Cancer
    STAT3-IN-49 (compound B16) is a potent and selective STAT3 inhibitor. STAT3-IN-49 binds to the SH2 domain of STAT3, thereby suppressing its phosphorylation and nuclear translocation. STAT3-IN-49 inhibits triple-negative breast cancer (TNBC) cell migration, invasion, and colony formation. STAT3-IN-49 inhibits tumor growth in an MDA-MB-231 xenograft mouse model. STAT3-IN-49 can be used for TNBC research .
    STAT3-IN-49
  • HY-175291
    Cystatin B agonist 1

    		MMP Cadherin Cancer
    Cystatin B agonist 1 is an orally active MMP-2/9 inhibitor. Cystatin B agonist 1 exhibits inhibitory effects with IC50 values of 3.95 and 3.43 μM against U87 and T98G cells, respectively. Cystatin B agonist 1 induces the cell-cycle arrest at S phase, inhibits angiogenesis, and suppresses migration and invasion of MG cells. Cystatin B agonist 1 inhibits tumor growth in U87 MG xenograft model. Cystatin B agonist 1 can be used for the study of malignant glioma (MG) .
    Cystatin B agonist 1
  • HY-178343
    Aurora A-IN-5

    		Aurora Kinase Apoptosis Cancer
    Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
    Aurora A-IN-5
  • HY-175208A
    MST3-IN-1 TFA

    		Hippo (MST) Caspase Bcl-2 Family Apoptosis Cancer
    MST3-IN-1 TFA (Compound LD-1) is a selective and orally active MST3 inhibitor, with an IC50 of 122.4 nM. MST3-IN-1 TFA shows antiproliferative activity against HepG2 cell. MST3-IN-1 TFA effectively induces Apoptosis in HepG2 cells, and halts the cell cycle at the G2/M transition. MST3-IN-1 TFA significantly suppressed tumor growth in HepG2 xenograft mice. MST3-IN-1 TFA can be used for the study of liver cancer .
    MST3-IN-1 TFA
  • HY-164445
    STAT3-IN-32

    		STAT c-Myc CDK Cancer
    STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a Kd of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 suppresses pancreatic cancer cell proliferation. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer .
    STAT3-IN-32
  • HY-179382
    HSB401

    		FLT3 Apoptosis Cancer
    HSB401 is an orally active FLT3 inhibitor (IC50: 28, 5, 72, 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, FLT3-ITD, respectively). HSB401 downregulates FLT3 signaling and induces cell cycle arrest and apoptosis. HSB401 spares c-KIT inhibition, thereby reducing the risk of myelosuppression. HSB401 significantly suppresses tumor growth in the MV4-11 xenograft mouse model. HSB401 can be used for the research of acute myeloid leukemia .
    HSB401
  • HY-162892
    BRD4-IN-9

    		Epigenetic Reader Domain Cancer
    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 .
    BRD4-IN-9
  • HY-146780
    TGFβRI-IN-4

    		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 .
    TGFβRI-IN-4

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