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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
36 Results for "
myeloid malignancies
" in MedChemExpress (MCE) Product Catalog:
Products (36)
36 Results for "myeloid malignancies" in MCE Product Catalog:
12
12 Cited Publications
Research Areas:
BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.
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9 Cited Publications
SD-36 is a potent STAT3 PROTAC degrader with a Kd of 44.4 nM and a Ki of 11 nM. SD-36 recruits the cereblon/culin 4A E3 ligase complex to mediate ubiquitination and proteasomal degradation of STAT3, inducing G1 phase cell cycle arrest and apoptosis. SD-36 is useful for research on acute myeloid leukemia, anaplastic large cell lymphoma, and hematopoietic and lymphoid malignancies .
1
1 Cited Publications
AZ5576 is a potent and highly selective CDK9 inhibitor (IC50: <5 nM). AZ5576 inhibits the phosphorylation of RNA polymerase II at Ser2, thereby inhibiting transcriptional elongation. AZ5576 can be used for hematological Malignancy research .
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1 Cited Publications
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(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual-targeting PROTAC molecule. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine not only targets the ubiquitination and degradation of Smad3, but also elevates the protein level of HIF-α, thereby exerting multi-pathway anti-fibrotic and renoprotective effects. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can be used in a wide range of tumor studies including cancers with KRAS inhibitor resistance, covering pancreatic ductal adenocarcinoma, acute myeloid leukemia, and various soft tissue sarcomas (such as fibrosarcoma, liposarcoma, chondrosarcoma, etc.). (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can also be applied to research related to various solid tumors and hematological malignancies, involving multiple cancer types such as colon cancer, breast cancer, ovarian cancer, non-small cell lung cancer, glioblastoma, and melanoma .
Synonyms: DSP-5336
Target:
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Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC50=1.4 nM, Kd=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .
Cat. No.: HY-172416
CAS No.: 2939850-17-4
Synonyms: ZE63-0302
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Balomenib (ZE63-0302) is an orally bioavailable menin-KMT2A interaction inhibitor. Balomenib disrupts menin-KMT2A binding, reverses aberrant HOX gene expression. Balomenib inhibits Meis1 mRNA expression in KMT2A-rearranged acute myeloid leukemia cells. Balomenib can be used for the research of leukemia .
Cat. No.: HY-16496
CAS No.: 26599-17-7
Synonyms: OSI-7836
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Thiarabine (OSI-7836) is an orally active cytotoxic antitumor agent that acts as a deoxycytidine kinase substrate and a DNA chain terminator. Thiarabine is metabolized to form its major active metabolite T-araCTP, which potently inhibits DNA synthesis and exhibits a long retention time in tumor cells. Thiarabine is widely applicable to research related to leukemia, lymphoma, hematologic malignancies, acute myeloid leukemia, and advanced solid malignancies .
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APG-2449 is an orally active inhibitor for BCL-2 and multikinase (ALK/FAK/ROS1) with potent antitumor activities. APG-2449 reduces cell viability and enhances apoptosis in acute myeloid leukemia cells in vitro. APG-2449 decreases activation of FAK and its downstream effectors. APG-2449 can be studied in research for mesothelioma tumor, non-small cell lung cancer, ovarian cancer, hematologic and solid malignancies .
Cat. No.: HY-168878
CAS No.: 3050819-22-9
EP652 is a METTL3 inhibitor and antitumor agent with IC50 values of 2 nM, <10 nM, and 37 nM in SPA, intracellular, and ATPlite assays, respectively. EP652 exhibits high selectivity against 40 other methyltransferases and FTO, and possesses favorable pharmacokinetic parameters. EP652 reduces intracellular N 6-methyladenosine (m 6A) levels in mRNA. EP652 inhibits tumor growth and progression of both hematologic malignancies and solid tumors. EP652 can be used for the research of acute myeloid leukemia, ovarian cancer, non-small cell lung cancer, and hypopharyngeal squamous cell carcinoma .
Cat. No.: HY-W018324
CAS No.: 1123-95-1
Synonyms: 5hmC
Target:
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PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC50 = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies .
Cat. No.: HY-168615
CAS No.: 2991818-13-2
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MGD-28 is an orally effective cereblon-dependent molecular glue degrader that potently degrades CK1α, IKZF1, IKZF2, and IKZF3, with respective DC50 values of 7.8, 3.8, 56.3, and 7.1 nM. MGD-28 also induces the degradation of multiple novel substrate proteins including ZFP91, DTWD1, ZNFX1, MBD1, and MBD3 via a CRBN/Cullin- and proteasome-dependent mechanism. MGD-28 induces cell apoptosis. MGD-28 is used in the research of multiple myeloma, acute myeloid leukemia, diffuse large B-cell lymphoma, and related malignancies .
Cat. No.: HY-168983
CAS No.: 2952589-57-8
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Lonitoclax is a B-cell lymphoma 2 (Bcl-2) inhibitor. Lonitoclax has comparable anti-tumor efficacy to Venetoclax (HY-15531) in both B cell and myeloid malignancy models. Lonitoclax is promising for research of relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas .
Cat. No.: HY-176476
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BRD4/FKBP12 ligand 2 is a heterobifunctional BRD4 and FKBP12 (Kd of 1.0 nM) ligand. BRD4/FKBP12 ligand 2 has positive cooperativity in BRD4 binding when pre-bound to FKBP12, and FKBP12-dependent cytotoxicity in cancer cells via the CellTrap effect. BRD4/FKBP12 ligand 2 can be used for the research of hematopoietic malignancy, multiple myeloma, prostate carcinoma, acute myeloid leukemia .
Cat. No.: HY-16379A
CAS No.: 1228923-43-0
Synonyms: SB1518 hydrochloride
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
Cat. No.: HY-168614
CAS No.: 2991817-99-1
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MGD-4 is an orally active cereblon-dependent molecular glue degrader with a phthalazinone scaffold. MGD-4 degrades the Ikaros family proteins IKZF1, IKZF2 and IKZF3 in a dose-dependent manner, with DC50 values of 67.2 nM, 918.2 nM and 95.8 nM, respectively. MGD-4 exhibits weak degradation activity against CK1α. MGD-4 inhibits the viability of multiple myeloma (MM) and acute myeloid leukemia (AML) cells and induces cell apoptosis. MGD-4 is used for the research of multiple myeloma, acute myeloid leukemia, diffuse large B-cell lymphoma and related hematological malignancies .
Cat. No.: HY-158618
CAS No.: 958226-81-8
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Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia .
Cat. No.: HY-P991656
CAS No.: 2125546-89-4
Cat. No.: HY-176701
CAS No.: 3025838-18-7
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PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
