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hematological+tumor

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17

阻害剤およびアゴニスト

2

阻害性抗体

製品番号 製品名 Target 研究分野 構造式
  • HY-162858
    BRD-810

    		Bcl-2 Family Caspase Apoptosis Cancer
    BRD-810 is a potent and selective MCL1 inhibitor with a Kd of 0.3 nM. BRD-810 can specifically block the BH3 binding groove of MCL1, while having little effect on other anti-apoptotic proteins (such as Bcl-2, Bcl-xL). BRD-810 effectively destroys the MCL1-BAK complex (IC50 = 1.2 nM) in cancer cells, rapidly activates Caspase and induces cell apoptosis. BRD-810 can be used in the research of various cancers such as hematological tumors and solid tumors .
    BRD-810
  • HY-101870
    Uzansertib

    INCB053914

    		 Pim Cancer
    Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
    Uzansertib
  • HY-101870B
    Uzansertib phosphate

    INCB053914 phosphate

    		 Pim Cancer
    Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
    Uzansertib phosphate
  • HY-136910
    USP7-797

    USP7-IN-7

    		 Deubiquitinase MDM-2/p53 Cancer
    USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
    USP7-797
  • HY-153803
    GBD-9

    		PROTACs Molecular Glues Btk Cancer
    GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
    GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
    GBD-9
  • HY-177768
    HDAC-IN-96

    		HDAC Apoptosis Cancer
    HDAC-IN-96 (Compound 3f) is a selective HDAC1/2 inhibitor with IC50 values of 457.1 and 433.7 nM. HDAC-IN-96 has strong inhibitory activity against multiple hematological tumor cells (RS4;11, K562, RPMI-8226, U266), with IC50 values ranging from 2.11 to 5.35 μM. HDAC-IN-96 can induce cancer cells apoptosis and S phase arrest. HDAC-IN-96 can be used for the research of cancer, such as acute lymphoblastic leukemia .
    HDAC-IN-96
  • HY-157215
    HDAC-IN-66

    		HDAC Cancer
    HDAC-IN-66 (compound 2F) is a selective HDAC inhibitor and Pomalidomide (HY-10984) derivative that potently inhibits hematological tumor cells .
    HDAC-IN-66
  • HY-146358
    Anticancer agent 49

    		Microtubule/Tubulin Cancer
    Anticancer agent 49 (compound 69) is a broad spectrum anticancer agent. Anticancer agent 49 inhibits tubulin polymerization. Anticancer agent 49 shows antiproliferative activity. Anticancer agent 49 has the potential for the research of solid and hematological tumors .
    Anticancer agent 49
  • HY-146357
    Anticancer agent 48

    		Microtubule/Tubulin Cancer
    Anticancer agent 48 (compound 48) is a broad spectrum anticancer agent. Anticancer agent 48 inhibits tubulin polymerization. Anticancer agent 48 shows antiproliferative activity. Anticancer agent 48 shows antitumor activity in vivo. Anticancer agent 48 has the potential for the research of solid and hematological tumors .
    Anticancer agent 48
  • HY-144038
    DNA-PK-IN-5

    		DNA-PK Cancer
    DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2) .
    DNA-PK-IN-5
  • HY-144039
    DNA-PK-IN-6

    		DNA-PK Cancer
    DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6) .
    DNA-PK-IN-6
  • HY-161694
    DNMT1-IN-3

    		DNA Methyltransferase Cancer
    DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
    DNMT1-IN-3
  • HY-P992395
    JNJ-64164711

    JNJ-711

    		 TNF Receptor NF-κB Cancer
    JNJ-64164711 (JNJ-711) is a bifunctional antibody that simultaneously targets human GITR/TNFRSF18 and FcγRIIIa. JNJ-64164711 binds to the GITR domain to activate the NF-κB signaling pathway, while binding to FcγRIIIa to support antibody-dependent cellular cytotoxicity (ADCC). JNJ-64164711 can specifically eliminate GITR-positive hematological tumor cells, activated T cells and intratumoral regulatory T cells through the ADCC mechanism, thereby significantly enhancing the body's anti-tumor immune response. JNJ-64164711 can be used in research related to non-small cell lung cancer, colorectal cancer, prostate cancer, renal cell carcinoma and hematological tumors .
    JNJ-64164711
  • HY-P992405
    MEDI-3185

    		CXCR Cancer
    MEDI-3185 is a potent CXCR4 antagonist. MEDI-3185 binds CXCR4 via CDR3H and ECL2 β-strand/β-strand interaction, blocks SDF-1 access and displaces SDF-1. MEDI-3185 can be used for the research of hematologic tumors, ovarian tumors .
    MEDI-3185
  • HY-101870BR
    Uzansertib phosphate (Standard)

    INCB053914 phosphate (Standard)

    		 Reference Standards Pim Cancer
    Uzansertib phosphate (Standard) is the analytical standard of Uzansertib phosphate (HY-101870B). This product is intended for research and analytical applications. Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
    Uzansertib phosphate (Standard)
  • HY-180836
    DIX-01

    		Molecular Glues IKZF Family Apoptosis Cancer
    DIX-01 is a molecular gel degrader that can simultaneously induce the degradation of IKZF1/3 and GSPT1 mediated by CRBN. Its DC50 values are: IKZF1 (19.80 nM), IKZF3 (45.31 nM), and GSPT1 (120.1 nM). DIX-01 exhibits nanomolar-level potent anti-proliferative activity in various cancer cell lines. DIX-01 induces apoptosis in MV4-11 cells and significantly inhibits the growth of leukemia cells in zebrafish. DIX-01 can be used for the study of malignant hematological tumors .
    DIX-01
  • HY-181996
    BTK-IN-47

    		Btk Caspase Apoptosis PARP Cancer
    BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies .
    BTK-IN-47

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