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hematologic toxicity

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17

Inhibitors & Agonists

1

Inhibitory Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101467
    Trilaciclib
    1 Publications Verification

    G1T28

    		 CDK Cancer
    Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
    Trilaciclib
  • HY-136241
    OT-82
    1 Publications Verification

    		 NAMPT Caspase Cancer
    OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and?induces cell death in a NAD + dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies .
    OT-82
  • HY-128586
    TAS4464
    Maximum Cited Publications
    9 Publications Verification

    		 Apoptosis Carbonic Anhydrase NEDD8-activating Enzyme Cancer
    TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
    TAS4464
  • HY-101467A
    Trilaciclib hydrochloride
    1 Publications Verification

    G1T28 hydrochloride

    		 CDK Cancer
    Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
    Trilaciclib hydrochloride
  • HY-138684
    MRTX9768

    		Histone Methyltransferase Cancer
    MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor .
    MRTX9768
  • HY-128586A
    TAS4464 hydrochloride
    Maximum Cited Publications
    9 Publications Verification

    		 NEDD8-activating Enzyme Carbonic Anhydrase Apoptosis Cancer
    TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
    TAS4464 hydrochloride
  • HY-114414
    HDACs/mTOR Inhibitor 1
    1 Publications Verification

    		 HDAC mTOR Apoptosis Cancer
    HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
    HDACs/mTOR Inhibitor 1
  • HY-120574
    TH1338

    		ADC Payload Topoisomerase Cancer
    TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
    TH1338
  • HY-176868
    Rodin-C

    		HDAC Neurological Disease
    Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18   and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research .
    Rodin-C
  • HY-153953
    Bcl-2-IN-11

    		Bcl-2 Family Cancer
    Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2 family proteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia .
    Bcl-2-IN-11
  • HY-178028
    PRMT5-IN-53

    		Histone Methyltransferase Cancer
    PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
    PRMT5-IN-53
  • HY-175261
    DHI1

    		CDK Wee1 Checkpoint Kinase (Chk) Cancer
    DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies .
    DHI1
  • HY-138684A
    MRTX9768 hydrochloride

    		Histone Methyltransferase Cancer
    MRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor .
    MRTX9768 hydrochloride
  • HY-101467R
    Trilaciclib (Standard)

    G1T28 (Standard)

    		 CDK Reference Standards Cancer
    Trilaciclib (Standard) is the analytical standard of Trilaciclib (HY-101467). This product is intended for research and analytical applications. Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
    Trilaciclib (Standard)
  • HY-181086
    FLT3/HDAC-IN-3

    		FLT3 HDAC Apoptosis Reactive Oxygen Species (ROS) Cancer
    FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3 D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies .
    FLT3/HDAC-IN-3
  • HY-185561
    Misitatug blivedotin

    RC88

    		 Mesothelin Cancer
    Misitatug blivedotin (RC88) is an antibody-drug conjugate (ADC) targeting mesothelin (MSLN). Misitatug blivedotin binds to mesothelin and exhibits dose‐dependent antitumor activity. Misitatug blivedotin can be used for the research of ovarian cancer, non-squamous non-small-cell lung carcinoma, cervical cancer .
    Misitatug blivedotin
  • HY-P992339
    cT84.66

    		Radionuclide-Drug Conjugates (RDCs) Cancer
    cT84.66 is a highly efficient tumor-targeting agent against carcinoembryonic antigen (CEA). cT84.66 engages in bivalent binding with CEA via variable region antigen-binding sites, enabling precise targeting of CEA-producing tumor cells for delivery of therapeutic radiation. cT84.66 exhibits high tumor uptake rate, rapid clearance rate, and excellent tumor-to-blood ratio. With dual functions as an imaging agent and an antibody-directed radiotherapy agent, cT84.66 is widely used in studies of colorectal cancer and metastatic CEA-positive malignancies .
    cT84.66

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