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PI3Kα,PC-3 cells,22RV1 cells,MDA-MB-231 cells,MDA-MB-453 cells,MDA-MB-453 cells

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製品番号 製品名 Target 研究分野 構造式
  • HY-159852

    PI3K Ras Akt Cancer
    BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
    BBO-10203
  • HY-158113

    Histone Acetyltransferase PROTACs Cancer
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
    CBPD-409
  • HY-173405

    Ras PI3K Akt Cancer
    VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer .
    VVD-699
  • HY-174461

    PROTACs PI3K Cancer
    PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)) .
    PROTAC PI3Kα degrader-1
  • HY-16596

    PI3K Cancer
    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
    CNX-1351
  • HY-170329

    PROTACs Androgen Receptor Apoptosis Cancer
    PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer .
    PROTAC AR Degrader-8
  • HY-145479
    PROTAC AR-V7 degrader-1
    1 Publications Verification

    PROTACs Androgen Receptor Cancer
    PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC50 of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer .(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))
    PROTAC AR-V7 degrader-1
  • HY-100385
    Brevianamide F
    2 Publications Verification

    Cyclo(L-Pro-L-Trp)

    PI3K Bacterial Infection
    Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F shows potent PI3Kα inhibitory activity with an IC50 of 4.8 μM .
    Brevianamide F
  • HY-143275

    PROTACs PI3K Akt Cancer
    HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)) .
    HL-8
  • HY-126076A

    DNA/RNA Synthesis Cancer
    VPC-80051 is an inhibitor of hnRNP A1 splicing activity. VPC-80051 directly interacts with hnRNP A1 RBD and reduces AR-V7 messenger levels in 22Rv1 CRPC cell line. VPC-80051 can be used in prostate cancer research .
    VPC-80051
  • HY-133045

    Ligands for E3 Ligase Cancer
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
    VHL Ligand 8
  • HY-131972

    PI3K Cancer
    PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy .
    PF-06843195
  • HY-13440
    AMG 511
    5 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 .
    AMG 511
  • HY-101272
    GDC-0326
    1 Publications Verification

    PI3K Cancer
    GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
    GDC-0326
  • HY-158432

    Histone Demethylase PROTACs Cancer
    GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
    GT-653
  • HY-173177

    Apoptosis MDM-2/p53 Cancer
    PSF-IN-2 (Compound (C)-30) is a PSF inhibitor with an IC50 value of 0.005 pM. PSF-IN-2 exhibits anti-cancer activity, and its IC50 value for inhibiting the proliferation of 22Rv1 cells is 0.5 μM. PSF-IN-2 activates the p53 signaling pathway by inhibiting the binding of PSF to RNA, inducing the expression of related genes, promoting apoptosis, and inhibiting the cell cycle. PSF-IN-2 can be used in cancer research .
    PSF-IN-2
  • HY-133020

    PROTACs Androgen Receptor Cancer
    ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-266
  • HY-B1550

    DL-Benzoin; Desyl alcohol; (±)-2-Hydroxy-2-phenylacetophenone

    PI3K Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Benzoin (DL-Benzoin) is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116) .
    Benzoin
  • HY-118712

    mTOR Cancer
    WYE-23 is a mTOR inhibitor, and IC50 is 0.45 nM. It is selective to PI3Kα and IC50 is 661 nM. WYE-23 has antitumor activity .
    WYE-23
  • HY-143404
    PI3K-IN-30
    3 Publications Verification

    PI3K Cancer
    PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC50s of 5.1, 136, 30.7 and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively .
    PI3K-IN-30
  • HY-13864
    PF-4989216
    1 Publications Verification

    PI3K Apoptosis Cancer
    PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
    PF-4989216
  • HY-174798

    PI3K Ligands for Target Protein for PROTAC Cancer
    PI3Kα Ligand-1 is the ligand for PI3Kα that can be used for synthesis of PROTACs, such as PI3Kα degrader-1 (HY-174461) .
    PI3Kα Ligand-1
  • HY-150618
    PI3Kα-IN-9
    1 Publications Verification

    PI3K Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research .
    PI3Kα-IN-9
  • HY-164373

    Androgen Receptor Apoptosis Cancer
    SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
    SC428
  • HY-150268

    BET-IN-16

    Epigenetic Reader Domain Cancer
    Zavabresib (BET-IN-16) (Compound I) is a BET inhibitor. BET-IN-16 shows anticancer activity. Zavabresib inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively .
    Zavabresib
  • HY-131345

    PI3K Cancer
    PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity .
    PI3Kα-IN-4
  • HY-147419

    PI3K Cancer
    Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity .
    Vulolisib
  • HY-156681A

    (S)-STX-478; (S)-STX-478-101; (S)-LY4064809

    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 .
    (S)-Tersolisib
  • HY-100470
    NSC781406
    2 Publications Verification

    PI3K mTOR Cancer
    NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
    NSC781406
  • HY-128333

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer .
    PI3K/mTOR Inhibitor-4
  • HY-P10781

    Radionuclide-Drug Conjugates (RDCs) PSMA Cancer
    PSMA-D5 has a binding affinity for PSMA with a Ki of 0.21 nM and can be used for PSMA tracing after radiolabeling. PSMA-D5 ([68Ga]-labeled) contains a DOTA chelator, allowing convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. PSMA-D5 ([68Ga]-labeled) shows excellent pharmacokinetic properties, exhibiting remarkable tumor uptake in 22Rv1 tumors . PSMA-D5 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    PSMA-D5
  • 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 .
    CP-07
  • HY-176128

    PROTACs Androgen Receptor Apoptosis PARP Caspase Cancer
    BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
    BWA-6047
  • HY-131345A

    PI3K Cancer
    (S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer .
    (S)-PI3Kα-IN-4
  • HY-163281

    Fluorescent Dye Cancer
    FSY-OSO2F shows an uptake in MCF-7 cells through the regulation of L-Tyr, ASC, and ASC2 transporters. FSY-OSO2F can be used as a PET tracer, when labeled with 18F, and exhibits good uptake and good contrast in MCF-7 and 22Rv1 subcutaneous tumors .
    FSY-OSO2F
  • HY-N16066

    CHNQD-0803

    AMPK Apoptosis NF-κB TNF Receptor Inflammation/Immunology
    Candidusin A (CHNQD-0803) (Compound 4) is a AMPK activator with a KD of 47.28 nM. Candidusin A can be isolated from marine fungus Aspergillus candidus. Candidusin A has cytotoxic activity and induces apoptosis in human prostate cancer cells (22Rv1, PC-3 and LNCaP cells). Candidusin A reduces adipogenesis genes expression and fat deposition, negatively regulates the NF-κB-TNFα inflammatory axis to suppress inflammation, and ameliorates liver injury and fibrosis. Candidusin A can be used for non-alcoholic steatohepatitis (NASH) research .
    Candidusin A
  • HY-179056

    PROTACs PSMA Androgen Receptor HSP Apoptosis Cancer
    Psa-AR is a PROTAC degrader targeting PSMA, with a Kd of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer .
    Psa-AR
  • HY-163938

    PROTACs Cancer
    PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)) .
    PROTAC erf3a Degrader-1
  • HY-175454

    DNA/RNA Synthesis PDGFR Oxidative Phosphorylation Mitochondrial Metabolism Cancer
    YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibits tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research .
    YH-0623
  • 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 .
    AR/AR-V7-IN-1
  • HY-143235

    Epigenetic Reader Domain Apoptosis Bcl-2 Family Caspase c-Myc Cancer
    BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
    BRD4 Inhibitor-15
  • HY-149914

    Androgen Receptor Cancer
    WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell) .
    WCA-814
  • HY-176281

    PI3K CDK Cancer
    PI3Kα-IN-26 (Compound 11e) is a PI3Kα inhibitor with an IC50 of 75.31 nM. PI3Kα-IN-26 has a broad-spectrum anticancer activity, such as leukemia, colon and breast cancer, without significant cytotoxic effect on the normal Vero cells (mean IC50s of 2.74, 3.50, 3.34 and 85.29 μM, respectively) .
    PI3Kα-IN-26
  • HY-143403

    PI3K Cancer
    PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects .
    PI3K-IN-31
  • HY-123849

    PI3K mTOR Cancer
    SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects .
    SN32976
  • HY-15960A

    VDC-597; SN33597

    PI3K mTOR Apoptosis Cancer
    PWT-33597 (VDC-597) is a dual inhibitor of PI3Kα and mTOR, which can effectively block the signaling downstream of PI3K and mTOR. PWT-33597 is capable of inducing tumor cell apoptosis and inhibiting tumor growth. PWT-33597 has anti-tumor activity and can be used in the research of tumors such as renal cell carcinoma .
    PWT-33597
  • HY-147767

    PI3K Apoptosis Reactive Oxygen Species (ROS) Cancer
    PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis .
    PI3Kα-IN-6
  • HY-161769

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
    HL435
  • HY-P10622

    Apoptosis Reactive Oxygen Species (ROS) Metabolic Disease Cancer
    SHLP-3 is a mitochondrial derived peptide encoded by the 16S ribosomal RNA (MT-RNR2) gene. SHLP-3 increases cell viability and reduces apoptosis in insulinoma NIT-1β cells and human prostate cancer 22Rv1 cells. SHLP-3 increases mitochondrial function and exerts cytoprotective effects by increasing mitochondrial oxygen consumption rate (OCR), cellular ATP and reducing the ability to produce ROS. SHLP-3 can be used in the study of diabetes and cancer .
    SHLP-3
  • HY-133044

    PROTAC Linkers Cancer
    Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Boc-Pip-alkyne-Ph-COOH

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