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Cat. No. Product Name CAS No. Information
PC-60543

CBL0137

1197996-80-7

CBL0137 (Curaxin CBL0137) is a histone chaperone FACT (facilitates chromatin transcription) and MYC signal inhibitor that markedly reduced tumor initiation and progression in vivo; simultaneously activates p53 and inhibits NF-κB without causing detectable genotoxicity, causes phosphorylation of p53 Ser(392) by CK2 and inhibition of NF-κB-dependent transcription in neuroblastoma cells; eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.

Brain Cancer

Phase 1 Clinical

PC-60241

sAJM-589

2089-82-9

sAJM-589 is a novel, potent small molecule Myc inhibitor that disrupts the Myc-Max leucine-zipper heterodimer with IC50 of 1.8 uM; preferentially inhibits transcription of MYC target genes in P493-6 cell; suppresses cellular proliferation in diverse MYC-dependent cancer cell lines, including P493-6, Ramos, HL-60 and KG1a (IC50=0.8-2 uM); reduces Myc protein levels in these cells, possibly by promoting ubiquitination and degradation of Myc protein.

PC-35731

MYC inhibitor DC-34

1966107-70-9 MYC inhibitor DC-34 is a potent small molecule that selectively inhibits MYC at the transcriptional level only when a G-quadruplex (G4) is present in the promoter, binds to MYC G4 with Kd of 9.4 uM; does not transcriptionally downregulate several other G4-dependent genes to the same extent; binds independently to the MYC G4 3'and 5' ends, demonstrates cytotoxicity in L363 MM cells with IC50 of 3.5 uM.
PC-35303

MYCMI-6

681282-09-7 MYCMI-6 (NSC354961) is a selective, high affinity inhibitor of MYC-MAX interaction, blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with Kd of 1.6 uM in SPR assay; specifcally targets MYC:MAX interaction without interfering with other MYC activities, selectively suppresses MYC-driven tumor cell growth with high efficacy, efficiently inhibits anchorage-independent growth of MYCN-amplifed neuroblastoma cells with GI50 values of <0.4, 5 and 0.75 μM, respectively; reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects
PC-35076

APTO-253 hydrochloride

1422731-37-0 APTO-253 is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels; APTO-253 is converted intracellularly from a monomer to a ferrous complex [Fe(253)3]; selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells without producing myelosuppression in various animal species and humans, induces DNA Damage in AML cells.

Blood Cancer

Phase 1 Clinical

PC-35075

APTO-253

1422826-80-9 APTO-253 is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels; APTO-253 is converted intracellularly from a monomer to a ferrous complex [Fe(253)3]; selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells without producing myelosuppression in various animal species and humans, induces DNA Damage in AML cells.

Blood Cancer

Phase 1 Clinical

PC-43158

10058-F4

403811-55-2 10058-F4 is a specific c-Myc inhibitor that disrupts the association between the c-Myc and Max, inhibits HL60 cell growth with IC50 of 51 uM; arrests AML cells at G0/G1 phase, downregulates c-Myc expression and upregulates CDK inhibitors p21 and p27; induces apoptosis through activation of mitochondrial pathway shown by downregulation of Bcl-2, upregulation of Bax, release of cytoplasmic cytochrome C, and cleavage of caspase 3, 7, and 9; also induces myeloid differentiation.

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