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tumor growth promoting

" in MedChemExpress (MCE) Product Catalog:

47

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1

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3

Peptides

1

Inhibitory Antibodies

5

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Products

3

Isotope-Labeled Compounds

1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W021040
    Fludioxonil

    CGA-173506

    		 Fungal Apoptosis Infection Cancer
    Fludioxonil (CGA-173506) is a phenylpyrrole-type fungicide with oral activity that can inhibit the growth of S. sclerotiorum. Fludioxonil promotes tumor growth and metastasis, and induces cardiac toxicity. Fludioxonil causes cytoskeletal disruption, DNA damage, and apoptosis in mouse glioma cells .
    Fludioxonil
  • HY-160768
    OTUB2-IN-1

    		Deubiquitinase Inflammation/Immunology Cancer
    OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) .
    OTUB2-IN-1
  • HY-P99746
    Murlentamab

    3C23K; GM102

    		 TGF-β Receptor Inflammation/Immunology Cancer
    Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming .
    Murlentamab
  • HY-19356A
    Didesmethylrocaglamide

    		Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity .
    Didesmethylrocaglamide
  • HY-111614
    Melengestrol acetate

    		Progesterone Receptor Metabolic Disease Cancer
    Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity . Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research .
    Melengestrol acetate
  • HY-N1381
    Periplocin
    3 Publications Verification

    		 Apoptosis Inflammation/Immunology Cancer
    Periplocin is a cardiotonic steroid isolated from root-bark Periploca sepium Bunge. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase .
    Periplocin
  • HY-111614S2
    Melengestrol acetate-d3

    		Isotope-Labeled Compounds Progesterone Receptor Metabolic Disease Cancer
    Melengestrol acetate-d3 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity[1]. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research[2].
    Melengestrol acetate-d3
  • HY-159154
    PSS-II

    		Biochemical Assay Reagents Cancer
    PSS-II promotes the production of ROS under light, thereby killing cancer cells and inhibiting tumor growth without damaging important organs of the body .
    PSS-II
  • HY-149886
    HIF-2α-IN-9

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-9 (compound 35r) is an inhibitor ofHIF-2α. HIF-2α-IN-9 inhibits VEGF-A (IC50=305 nM), and regulates growth-promoting genes in tumor cells, reactivates macrophage-mediated tumor immunity .
    HIF-2α-IN-9
  • HY-111614S
    Melengestrol acetate-d6

    		Progesterone Receptor Metabolic Disease Cancer
    Melengestrol acetate-d6 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity[1]. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research[2].
    Melengestrol acetate-d6
  • HY-111614R
    Melengestrol acetate (Standard)

    		Progesterone Receptor Metabolic Disease Cancer
    Melengestrol acetate (Standard) is the analytical standard of Melengestrol acetate. This product is intended for research and analytical applications. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity . Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research .
    Melengestrol acetate (Standard)
  • HY-111614S1
    Melengestrol acetate-d2

    		Progesterone Receptor Metabolic Disease Cancer
    Melengestrol acetate-d2 is the deuterium labeled Melengestrol acetate. Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity[1]. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research[2].
    Melengestrol acetate-d2
  • HY-N10502
    Colletofragarone A2

    		MDM-2/p53 HSP Cancer
    Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo .
    Colletofragarone A2
  • HY-N1381R
    Periplocin (Standard)

    		Apoptosis Inflammation/Immunology Cancer
    Periplocin (Standard) is the analytical standard of Periplocin. This product is intended for research and analytical applications. Periplocin is a cardiotonic steroid isolated from root-bark Periploca sepium Bunge. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase .
    Periplocin (Standard)
  • HY-142683
    SCP1-IN-2

    		Phosphatase Neurological Disease Cancer
    SCP1-IN-2 (Compound SH T-65) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-2 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-2 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
    SCP1-IN-2
  • HY-142682
    SCP1-IN-1

    		Phosphatase Neurological Disease Cancer
    SCP1-IN-1 (compound SH T-62) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-1 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-1 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
    SCP1-IN-1
  • HY-101780A
    Tinostamustine hydrochloride

    EDO-S101 hydrochloride; NL-101 hydrochloride

    		 HDAC Cancer
    Tinostamustine hydrochloride (EDO-S101 hydrochloride) is a compound with anti-multiple myeloma activity and the ability to promote CD38 expression. Tinostamustine hydrochloride enhances the sensitivity of tumor cells to the anti-CD38 monoclonal antibody daratumumab by increasing the acetylation level of histone H3. Tinostamustine hydrochloride can increase the expression of MICA and MICB, thereby activating NK cells. Tinostamustine hydrochloride can significantly delay tumor growth and improve the survival rate of mice .
    Tinostamustine hydrochloride
  • HY-149092
    Anticancer agent 109

    		TAM Receptor Cancer
    Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
    Anticancer agent 109
  • HY-P4322
    H-Ile-Lys-Val-Ala-Val-OH
    1 Publications Verification

    		 ERK Akt Neurological Disease Cancer
    H-Ile-Lys-Val-Ala-Val-OH is one of the most potent active sites of laminin-1. H-Ile-Lys-Val-Ala-Val-OH promotes cell adhesion, neurite outgrowth, and tumor growth. H-Ile-Lys-Val-Ala-Val-OH stimulates BMMSC population growth and proliferation by activating MAPK/ERK1/2 and PI3K/Akt signalling pathways .
    H-Ile-Lys-Val-Ala-Val-OH
  • HY-163719
    PARP7-IN-22

    		PARP Cancer
    PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy .
    PARP7-IN-22
  • HY-10180A
    MLN8054 sodium

    		Aurora Kinase Cancer
    MLN8054 sodium is an Aurora A inhibitor with radiosensitivity-enhancing activity. MLN8054 sodium can activate the DNA double-strand break reaction of prostate cancer cells in in vitro experiments. The application of MLN8054 sodium is closely related to accumulation in the G2/M phase of the cell cycle and polyploid formation. In vivo experiments show that MLN8054 sodium can significantly delay the growth of prostate cancer tumors and promote tumor cell apoptosis when used in combination with radiotherapy .
    MLN8054 sodium
  • HY-160421
    TREM2-IN-1

    		Apoptosis Inflammation/Immunology Cancer
    TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206 + and CX3CR1 + immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells .
    TREM2-IN-1
  • HY-N5112B
    β,β-Dimethylacrylshikonin
    1 Publications Verification

    Isoarnebin I

    		 HIF/HIF Prolyl-Hydroxylase Apoptosis Notch NO Synthase Bcl-2 Family Cancer
    β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
    β,β-Dimethylacrylshikonin
  • HY-147082
    GA-017
    2 Publications Verification

    		 YAP Cancer
    GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids .
    GA-017
  • HY-121490
    IMM-02

    		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 .
    IMM-02
  • HY-15578
    McMMAF
    5 Publications Verification

    Maleimidocaproyl monomethylauristatin F

    		 Drug-Linker Conjugates for ADC Apoptosis Cancer
    McMMAF (Maleimidocaproyl monomethylauristatin F) is an active molecule linker for ADC, made by coupling the powerful microtubule inhibitor Monomethyl auristatin F (MMAF) with the protecting group maleimidocaproyl. McMMAF can be conjugated with anti-BCMA antibodies to form J6M0-mcMMAF, promoting apoptosis and inhibiting tumor growth .
    McMMAF
  • HY-155068
    FC-116

    		Reactive Oxygen Species Apoptosis Microtubule/Tubulin Cancer
    FC-11 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. FC-11 can also induce endoplasmic reticulum (ER) stress to generate excess reactive oxygen species (ROS), leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-11 can be used in cancer research .
    FC-116
  • HY-N15340
    1-Oleoyl-2-linoleoyl-sn-glycerol

    		PKC Cancer
    1-Oleoyl-2-linoleoyl-sn-glycerol is a diacylglycerol (DG). 1-Oleoyl-2-linoleoyl-sn-glycerol can activate protein kinase C (PKC), thus triggering downstream signaling cascades and promoting tumor growth. 1-Oleoyl-2-linoleoyl-sn-glycerol is promising for research of breast cancer .
    1-Oleoyl-2-linoleoyl-sn-glycerol
  • HY-157793
    SMU-L11

    		Toll-like Receptor (TLR) NF-κB MAPKAPK2 (MK2) Inflammation/Immunology Cancer
    SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4 + T and CD8 + T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases .
    SMU-L11
  • HY-149398
    PARP-1/2-IN-2

    		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 .
    PARP-1/2-IN-2
  • HY-18343
    CP-31398

    		MDM-2/p53 Apoptosis Cancer
    CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
    CP-31398
  • HY-157055
    PD-1-IN-25

    		PD-1/PD-L1 Cancer
    PD-1-IN-25 (compound 43) is a potent PD-1/PD-L1 interaction inhibitor with an IC50 value of 10.2 nM in the HTRF assay. PD-1-IN-25 can promote CD8+ T cell activation through inhibiting PD-1/PD-L1 cellular signaling. PD-1-IN-25 delays the tumor growth .
    PD-1-IN-25
  • HY-P10388
    TAX2 peptide

    		CD47 TGF-β Receptor Cancer
    TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
    TAX2 peptide
  • HY-146452
    Anticancer agent 57

    		Apoptosis Cancer
    Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) .
    Anticancer agent 57
  • HY-162772
    IDH1/2-IN-1

    		Isocitrate Dehydrogenase (IDH) Apoptosis Cancer
    IDH1/2-IN-1 (Compound 6b) serves as a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC50 values of 0.22 μM and 1.6 μM, respectively. IDH1/2-IN-1 effectively inhibits tumor growth by suppressing tumor cell proliferation and enhancing host defense through the activation of antioxidant enzymes. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating robust antitumor activity. IDH1/2-IN-1 holds potential for research in leukemia .
    IDH1/2-IN-1
  • HY-151153
    HDAC1-IN-5

    		HDAC Microtubule/Tubulin Caspase Apoptosis Cancer
    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 .
    HDAC1-IN-5
  • HY-168555
    YJ1206

    		CDK PROTACs Apoptosis Cancer
    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) .
    YJ1206
  • HY-143616
    EZH2-IN-7

    		Histone Methyltransferase Cancer
    EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .
    EZH2-IN-7
  • HY-169431
    VEGFR-2/AKT-IN-2

    		VEGFR Akt Caspase Bcl-2 Family Apoptosis Cancer
    VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells .
    VEGFR-2/AKT-IN-2
  • HY-157693
    C18:1 Cyclic LPA

    		Endogenous Metabolite Cancer
    C18:1 Cyclic LPA is a naturally occurring analog of the growth factor-like phospholipid mediator, lysophosphatidic acid (LPA), characterized by the formation of a 5-membered ring between its sn-2 hydroxy group and the sn-3 phosphate. This unique structure allows C18:1 Cyclic LPA to influence a variety of cellular functions, such as inhibiting cell cycle progression, promoting the formation of stress fibers, curtailing tumor cell invasiveness and metastasis, and modulating the differentiation and survival of neuronal cells. Notably, many of these cellular effects elicited by C18:1 Cyclic LPA appear to counter those induced by LPA, despite the activation of seemingly similar receptor populations.
    C18:1 Cyclic LPA
  • HY-144088
    ZYF0033

    HPK1-IN-22

    		 MAP4K Inflammation/Immunology Cancer
    ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
    ZYF0033
  • HY-123929
    PAWI-2

    		MDM-2/p53 Wnt IKK Apoptosis Caspase Cancer
    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 .
    PAWI-2
  • HY-164476
    ES-072

    		EGFR GSK-3 PD-1/PD-L1 Cancer
    ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
    ES-072
  • HY-170620
    PROTAC PARP1 degrader-4

    		PROTACs PARP Cancer
    PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PROTAC PARP1 degrader-4 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PROTAC PARP1 degrader-4 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)) .
    PROTAC PARP1 degrader-4
  • HY-168996
    LA-CB1

    		CDK Apoptosis Cancer
    LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
    LA-CB1
  • HY-167854
    KW-2450 free base

    		Aurora Kinase Apoptosis IGF-1R Cancer
    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.
    KW-2450 free base
  • HY-170872
    PT-129

    		PROTACs DNA/RNA Synthesis Cancer
    PT-129 is an RPOTAC degrader targeting the NTF2 domain (protein-RNA interaction site) of G3BP1/2, which mediates the disassembly of intracellular stress granules. PT-129 can inhibit the formation of stress granules in stressed cells and disassemble existing stress granules, and can disrupt the transmission of ATF4, thereby inhibiting the proliferation of cancer cells. Stress granules (SGs) are membrane-less cytoplasmic compartments formed under stress stimuli. SGs promote the transmission of ATF4 from fibroblasts to tumor cells through a migratory effect, mediating fibroblast-related tumor growth. And G3BP1/2 is a central protein of the SGs network, and the inhibition of G3BP1/2 may reduce the stress resistance of cancer cells in the tumor microenvironment. PT-129 is composed of a target protein ligand (red part) G3BP1/2-Targeting ligand-1 (HY-170873), an E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a PROTAC linker (black part) Amino-PEG3-C2-acid (HY-W040165); among them, the E3 ligase ligand + linker form a complex Thalidomide-NH-PEG3-propionic acid (HY-136166) .
    PT-129

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