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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
19 Results for "
MYC-driven
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "MYC-driven" in MCE Product Catalog:
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20 Publications Verification
Research Areas:
CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer .
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20 Publications Verification
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DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .
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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 .
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Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
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MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis .
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1 Cited Publications
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(1S,2S,3R)-DT-061 is an enantiomer of DT-061 (HY-112929). DT-061 is an orally active activator of protein phosphatase 2A (PP2A). (1S,2S,3R)-DT-061 can be used as a negative control in the research of KRAS-mutant and MYC-driven lung cancer tumorigenesis .
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MRT-2359 is an orally active and selective GSPT1 molecular glue degrader, with a DC50 of 5 nM. MRT-2359 induces CRBN/GSPT1 ternary complex formation to drive CRBN- and degron-dependent proteasomal GSPT1 degradation, with selectivity for wild-type GSPT1 over the GSPT1G575N mutant. MRT-2359 disrupts protein translation, induces ribosome stalling, downregulates MYC family proteins and their transcriptional output, reduces proliferation, and induces apoptosis in cancer cells. MRT-2359 can be used for the research of non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), neuroendocrine lung cancer, high grade neuroendocrine cancers, diffuse large B-cell lymphoma, prostate cancer, and MYC-driven solid tumors .
Cat. No.: HY-148837
CAS No.: 2883535-99-5
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PROTACs c-Myc CD276/B7-H3 IAP Casein Kinase Eukaryotic Release Factor (eRF) Oxidative Phosphorylation Apoptosis
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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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LL-K8-22 is a dual degrader of CDK8 and cyclin C HyT, with DC50 values of 2.52 μM and 2.64 μM, respectively. LL-K8-22 inhibits phosphorylation of STAT1 Ser 727, phosphorylation of the C-terminal domain Ser 2/5 of RNA polymerase II, and phosphorylation of Rb. LL-K8-22 represses E2F- and MYC-driven transcriptional programs and exhibits antiproliferative effects. LL-K8-22 synchronously induces proteasome-dependent selective degradation of CDK8 and cyclin C without degrading CDK19, other CDK family members, or other cyclins. LL-K8-22 can be used in the research of triple-negative breast cancer and colon cancer .
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JHU395 is an orally active prodrug of 6-diazo-5-oxo-l-norleucine (HY-108357) and an antagonist of Glutamine amidotransferase. JHU395 blocks de novo purine synthesis, inhibits glutamine utilization, and induces Apoptosis. JHU395 exhibits antitumor activity. JHU395 can be used in research related to malignant peripheral nerve sheath tumors and MYC-driven medulloblastomas .
Cat. No.: HY-156747
CAS No.: 2803879-60-7
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GSPT1 degrader-2 is an orally active GSPT1 molecular glue degrader that promotes the degradation of intracellular GSPT1 protein, with DC50 values of 3 nM and 22 nM in NCI-H1155 and ABC-1 cells with high N-Myc expression, respectively. GSPT1 degrader-2 can be used in the research of N-Myc-driven cancers, such as lung cancer .
Cat. No.: HY-174255
CAS No.: 3062125-47-4
WDR5-MYC-IN-2 is an inhibitor of WDR5-MYC protein-protein interaction (PPI) with IC50 of 0.59 μM. WDR5-MYC-IN-2 can be studied in research for MYC-driven cancer and development of other effective WDR5-MYC PPI inhibitors .
Cat. No.: HY-169921
c-Myc inhibitor 15 (Compound A5) is a selective c-Myc inhibitor that exerts anticancer effects by disrupting the interaction between c-Myc and Max, leading to the degradation of c-Myc protein and the induction of apoptosis. Its IC50 values are 4.08 μM and 7.86 μM in A549 and NCI-H1299 lung cancer cell lines, respectively, demonstrating strong cytotoxic activity. In a syngeneic tumor model, c-Myc inhibitor 15 exhibited outstanding antitumor efficacy, achieving a tumor growth inhibition rate of 76.4% and significantly reducing c-Myc protein expression levels. c-Myc inhibitor 15 holds promise for research related to c-Myc-driven lung cancers .
Cat. No.: HY-181473
CAS No.: 3102226-11-6
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Antiproliferative agent-75, Pyrrole (HY-Y0807) derivative, is an antiproliferative agent with an IC50 value of 0.06 μM against Myc-driven human B-cells. Antiproliferative agent-75 can be used for the development of pyrrole-based Myc inhibitor .
Cat. No.: HY-187521
CAS No.: 102537-38-2
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MYCMI-7 hydrobromide is a potent and selective MYC/MYCN inhibitor, with a Kd of 4 μM for MYC and an IC50 of 10 μM for topoisomerase IIα (Topoisomerase IIα). MYCMI-7 hydrobromide binds directly to MYC, selectively inhibits the interactions of MYC:MAX and MYCN:MAX, reduces MYC-driven transcription levels, induces MYC/MYCN protein degradation, and blocks the binding of MYC to chromatin, thereby inducing tumor cell growth arrest, apoptosis and reducing cell viability, while only inducing G1 phase growth arrest in normal cells. MYCMI-7 hydrobromide can be used in research related to MYC-driven acute myeloid leukemia and breast cancer, MYCN-amplified neuroblastoma, glioblastoma, Burkitt's lymphoma, melanoma, colon cancer, osteosarcoma, cervical cancer and histiocytic lymphoma .
Cat. No.: HY-181541
HIT211504993 is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.070 μM. HIT211504993 suppresses cancer cell proliferation, cause G1 phase cell cycle arrest and induces apoptosis. HIT211504993 inhibits Myc-driven tumorigenesis via nucleocytoplasmic acetylation, p53 modulation, and Wnt/β-catenin signaling modulation. HIT211504993 inhibits tumor growth in a colon cancer xenograft mouse model. HIT211504993 can be used for the research of colon cancer .
Cat. No.: HY-115569
CAS No.: 1966107-70-9
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DC-34 is a selective stabilizer of MYC G-quadruplexes (G4s), with measured Kd values of 9.4 μM (FIA), 1.4 μM (SPR), and 16.5 μM (NMR) across different assays. DC-34 downregulates MYC levels in cancer cells in a G4-dependent manner, reduces cell viability, and induces G0-G1 cell cycle arrest and p16-marked senescence in MYC-driven multiple myeloma cells. DC-34 can serve as a probe for G4-dependent gene regulation studies and is applicable to research on multiple myeloma .
Cat. No.: HY-183070
CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia .
Cat. No.: HY-101488R
CAS No.: 1010100-07-8
CC-885 (Standard) is the analytical standard of CC-885 (HY-101488). This product is intended for research and analytical applications. CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer .
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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
