cmyc

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

APTO-253 (LOR-253) inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through the induction of the KLF4 tumor suppressor.

CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC50 values of 1.07 nM for CBP/HTRF and 5.96 nM for Myc.

KSI-3716 is a c-Myc inhibitor used as a bladder chemotherapy agent. It blocks the formation of the c-MYC/MAX complex with the target gene promoter and induces cell cycle arrest and apoptosis. It can be used for bladder cancer research.

MYCi361 (NUCC-0196361) is an inhibitor of MYC (binding to MYC with Kd of 3.2 μM).

MYCi975 (NUCC-0200975) is an orally active MYC inhibitor.

MYCMI-6 (NSC-354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions,reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

KJ Pyr 9 is an MYC inhibitor (Kd: 6.5 nM in vitro assay).

sAJM589 is a Myc inhibitor that dose-dependently disrupts Myc-Max heterodimers, thereby decreasing Myc protein levels. Myc is a multifunctional nuclear phosphoprotein that plays a key role in cell cycle progression, apoptosis, and cellular transformation. sAJM589 inhibits the cellular proliferation of a variety of Myc-dependent cancer cell lines and the adherent, non-dependent growth of Raji cells’ Growth.

SYHA1815, an orally active RET inhibitor (IC50=0.9 nmol/L), demonstrates antitumor activity. It exhibits greater selectivity for RET over KDR (IC50=15.9 nmol/L). SYHA1815 operates by downregulating c-Myc, arresting the G1 cell cycle, and inhibiting RET-driven cell proliferation.

10058-F4 (c-Myc Inhibitor) is a cell-permeable thiazolidinone that specifically inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression; induces cell-cycle arrest and apoptosis.

10074-G5 is an inhibitor of c-Myc-Max dimerization.

IRES-C11 is a specific inhibitor of translation that targets the internal ribosome entry site (IRES) of the c-MYC gene. It functions by blocking the interaction between heterogeneous nuclear ribonucleoprotein A1, a trans-acting factor required for c-MYC IRES activity, and its corresponding IRES. Notably, IRES-C11 does not inhibit the IRES activity of BAG-1, XIAP, and p53.

ML327 is a MYC blocker. ML327 can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).

Mycro 3 is potent and selective for c-Myc in whole cell assays.

VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX. VPC-70063 exhibits Myc-Max transcriptional activity inhibition of 106% with an IC50 of 8.9 μM and Myc-Max/UBE2C downstream pathway inhibition of 94%. VPC-70063 can be used for studies about anticancer.

WBC100 (14-D-Valine-TPL) is a potent, selective, orally active c-Myc glue degrader targeting the ubiquitin E3 ligase CHIP-mediated 26S proteasome pathway, primarily used in research for c-Myc overexpressing tumors [1].

MYC-RIBOTAC, a ribonuclease-targeting chimera (RIBOTAC) specific to the MYC internal ribosome entry site (IRES), comprises an MYC mRNA-binding element tethered to a small molecule that recruits and activates RNase L1. This interaction promotes the degradation of MYC mRNA, subsequently reducing MYC protein levels and inducing apoptosis, thereby presenting potential applications in anticancer research [1].

MDEG-541 is a potent MYC-MAX degrader that exhibits antiproliferative activity by downregulating the expression of GSPT1, MYC, GSPT2, and PLK1 proteins [1].

c-Myc inhibitor 11 (Compound 67e), a c-MYC inhibitor (p EC 50: 6.4), demonstrates high clearance, moderate volume of distribution, and a short half-life in rat pharmacokinetic assays, making it suitable for cancer research [1].

Compound 67h, also known as c-Myc inhibitor 12, is a potent inhibitor of c-Myc, exhibiting a pEC50 value of 6.4 [1].

m-Se3 is a potent, selective inhibitor of c-MYC transcription with demonstrated capability to inhibit tumor growth and exhibit anti-cancer activity [1].

CCI 007 is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485

BTYNB (MDK6620) is an inhibitor of the oncofetal mRNA-binding protein IMP1 (IC50 = 5 μM for IMP1 binding to c-Myc mRNA). MDK6620 downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). It disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association