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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
81 Results for "
hematological cancer cells
" in MedChemExpress (MCE) Product Catalog:
Products (81)
81 Results for "hematological cancer cells" in MCE Product Catalog:
72
72 Publications Verification
Research Areas:
CX-5461 is a selective, orally active RNA polymerase I inhibitor. CX-5461 disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors .
72
72 Publications Verification
Cat. No.: HY-13323A
Purity: 99.41%
Research Areas:
CX-5461 dihydrochloride is a selective, orally active RNA polymerase I inhibitor. CX-5461 dihydrochloride disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 dihydrochloride upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 dihydrochloride induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 dihydrochloride can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors .
56
56 Cited Publications
Synonyms: INK-128; MLN0128; TAK-228
Target:
mTOR Apoptosis Akt ERK CDK Ribosomal S6 Kinase (RSK) Collagen HIF/HIF Prolyl-Hydroxylase Wnt
Research Areas:
Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies .
52
Research Areas:
Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC50 of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors .
48
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
16
Target:
Research Areas:
Indisulam (E 7070) is a carbonic anhydrase inhibitor and RBM39 molecular glue degrader, with Ki values of 31, 15, and 24 nM against human carbonic anhydrase I, II, and IX, respectively, and a Ki value of 65 nM against bovine carbonic anhydrase IV. Indisulam promotes the recruitment of RBM39 to the CUL4-DCAF15 E3 ubiquitin ligase complex, triggering polyubiquitination and proteasomal degradation of RBM39. Indisulam induces aberrant pre-mRNA splicing, G1 cell cycle arrest, and cell death in cancer cells. As an anticancer agent, Indisulam drives tumor regression and growth inhibition in xenograft models. Indisulam can be used in research related to solid tumors, hematologic and lymphoid malignancies, colorectal cancer, and non-small cell lung cancer .
10
10 Cited Publications
Research Areas:
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.) .
10
10 Cited Publications
Research Areas:
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.) .
4
4 Cited Publications
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
2
2 Cited Publications
Target:
Research Areas:
FHT-1015 is a selective SMARCA4 (IC50 = 4 nM) and SMARCA2 (IC50 = 5 nM) (also known as BRG1 and BRM) inhibitor. FH-1015 is an allosteric inhibitor that causes conformation change in the BRG1/BRM protein upon interaction with an allosteric site, inhibiting ATPase activity. FH-1015 interferes with tumor cell growth and migration. FH-1015 can be studied in research for uveal melanoma and hematologic cancer .
1
1 Cited Publications
DB2115 tetrahydrochloride is a highly selective PU.1 inhibitor that suppresses the binding of PU.1 to DNA (IC50: 2.3 nM). DB2115 tetrahydrochloride can inhibit tumor cell proliferation and induce apoptosis. DB2115 tetrahydrochloride can be used in the research of tumors such as leukemia .
1
1 Cited Publications
Target:
Research Areas:
NUC-7738, an aryloxy phosphoramidate of 3′-Deoxyadenosine, is a 5′-aryloxy phosphoramidate prodrug of 3′-Deoxyadenosine (3′-dA). NUC-7738 has potent cytotoxic activity against a panel of hematological cancer cell lines. NUC-7738 can be used in research of cancer .
1
1 Cited Publications
Research Areas:
(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 .
1
1 Cited Publications
MS-L6 is a OXPHOS inhibitor and antimalarial agent. MS-L6 inhibits NADH oxidation and electron transport. MS-L6 induces OXPHOS uncoupling, dissipates mitochondrial membrane potential, increases non-ATP-coupled oxygen consumption, and reduces ATP synthesis. MS-L6 triggers the production of ROS. MS-L6 exhibits anti-amoebic activity. MS-L6 exerts antitumor activity in mouse lymphoma xenograft models. MS-L6 can be used in research related to B-cell lymphoma, T-cell lymphoma, and non-Hodgkin B-cell lymphoma .
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Research Areas:
ABBV-467 is a selective MCL-1 inhibitor (Ki: <0.01 nM). ABBV-467 induces apoptosis. ABBV-467 induces cancer cell death and inhibits tumor growth in models of hematological malignancies, such as multiple myeloma .
Target:
Research Areas:
AcBut-N-Ac-γ-Calicheamicin is an ADC cytotoxic payload that induces cell cycle arrest and apoptosis by causing DNA double-strand breaks. AcBut-N-Ac-γ-Calicheamicin is primarily used in the synthesis of antibody-drug conjugates (ADC) and holds promise for research in the field of cancer, including acute lymphoblastic leukemia (ALL) and other hematological malignancies .
Cat. No.: HY-176083
CAS No.: 2093449-12-6
ASTX295 is an orally active and selective MDM2 antagonist with an IC50 of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer .
Cat. No.: HY-16366
CAS No.: 865783-99-9
Synonyms: ON 014185
Research Areas:
Briciclib (ON 014185) is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib can be used for the study of hematological system tumors and solid tumors .
Research Areas:
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-148837
CAS No.: 2883535-99-5
Target:
PROTACs c-Myc CD276/B7-H3 IAP Casein Kinase Eukaryotic Release Factor (eRF) Oxidative Phosphorylation Apoptosis
Research Areas:
GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC50 of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers .
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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
