RNA-Protein Translation Inhibitors

The DNA that makes up an organism’s genome contains genes that hold the nucleic acid codes for protein synthesis, resulting in the production of unique proteins that perform numerous and specific functions.
Protein synthesis involves two steps: transcription and translation. Transcription creates a complementary RNA copy of a DNA sequence and translation is the subsequent process where RNA is used to synthesize the actual protein from amino acids. Inhibition of this translation step has the effect of blocking protein production and ultimately its function.
Sigma-Aldrich offers several small molecules that inhibit protein translation, making these compounds useful research tools to better understand the role proteins play in certain disease states.

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C0621 CI−994 ≥98% (HPLC), powder CI-994 is the acetylated derivative form of the original compound Dinaline (PD 104 208). It is an oral cytostatic drug with impressive differential activity against leukemic cells & normal stem-cells. It is used for combination therapy for selected tumors including non-small cell lung, pancreatic, breast, and colorectal cancers. It acts as a histone deacetylase inhibitor. CI-994 blocks cells in the G1-S phase of the cell cycle. The 16 kDa phosphoprotein is confined to the nuclear compartment. Loss of the 16-kDa nuclear phosphoprotein appears to be a direct effect of CI-994 treatment and that the inhibition of this phosphoprotein may play a critical role in the mechanism of action of CI-994.
C3394 Cordycepin from Cordyceps militaris Cordycepin is an adenosine analogue that is readily converted to cordycepin 5′-triphosphate; can be used for 3′-end labeling of RNA.
C7698 Cycloheximide from microbial, ≥94% (TLC) Cycloheximide (CHX) is an antibiotic produced by S. griseus. Its main biological activity is translation inhibition in eukaryotes resulting in cell growth arrest and cell death. CHX is widely used for selection of CHX-resistant strains of yeast and fungi, controlled inhibition of protein synthesis for detection of short-lived proteins and super-induction of protein expression, and apoptosis induction or facilitation of apoptosis induction by death receptors.
C4859 Cycloheximide solution Ready-Made Solution, microbial, 100 mg/mL in DMSO, 0.2 μm filtered Cycloheximide (CHX) is an antibiotic produced by S. griseus. Its main biological activity is translation inhibition in eukaryotes resulting in cell growth arrest and cell death. CHX is widely used for selection of CHX-resistant strains of yeast and fungi, controlled inhibition of protein synthesis for detection of short-lived proteins and super-induction of protein expression, and apoptosis induction or facilitation of apoptosis induction by death receptors.
D5569 DCHC ≥98% (HPLC), solid DCHC is a SIRT1 activator. It increases peroxisome proliferator-activated receptor gamma co-activator 1α (PGC1α) expression, resulting in mitochondrial biogenesis. DCHC activates SIRT1 at low micromolar concentrations (5–10 μM) and increases SIRT1 activity at 100 μM. It is different from 5,7,4′-T in that it induces the activation of recombinant SIRT1, but does not increase SIRT1 expression.
D0564 Diphtheria Toxin from Corynebacterium diphtheriae lyophilized powder Inhibits protein synthesis by catalyzing ADP-ribosylation of eukaryotic aminoacyltransferase II.
D2189 [Glu52]-Diphtheria toxin from Corynebacterium diphtheriae lyophilized powder  
SML0197 4E1RCat ≥97% (HPLC) 4E1RCat ilnhibits the eIF4F translation initiation complex by binding to IF4E b and inhibiting the interaction between IF4E:eIF4G (IC50 = 3.2 μM). In in vitro translation experiments using MDA-MB-231 cells, 4E1RCat dose dependently inhibited cap-dependent translation, led to a decrease in polysome and 80S ribosomal subunits and reduced levels of the eIF4F-dependant proteins Mcl-1 and c-Myc.
E2375 Emetine dihydrochloride hydrate  
F0756 Fusidic acid Suppresses nitric oxide lysis of pancreatic islet cells. Inhibits protein synthesis in prokaryotes by inhibiting the ribosome-dependent activity of G factor and translocation of peptidyl-tRNA.
F0881 Fusidic acid sodium salt ≥98% (TLC) Suppresses nitric oxide lysis of pancreatic islet cells. Inhibits protein synthesis in prokaryotes by inhibiting the ribosome-dependent activity of G factor and translocation of peptidyl-tRNA.
G1397 Gentamicin solution 50 mg/mL in deionized water, liquid, sterile-filtered, BioReagent, suitable for cell culture Mode of Action: Gentamicin inhibits protein synthesis by binding to the 30S subunit of the ribosome.

Antimicrobial spectrum: Includes Gram-negative and Gram-positive bacteria, including strains resistant to tetracycline, chloramphenicol, kanamycin and colistin, particularly strains of Pseudomonas, Proteus, Staphylococcus and Streptococcus.
G3632 Gentamicin sulfate salt potency: ≥590 μg Gentamicin base per mg Mode of action: Gentamicin causes codon misreading by binding to the 30S ribosomal subunit, blocking the translocation of peptidyl-tRNA from the acceptor site to the donor site.1,2 The bactericidal effect of gentamicin on Pseudomonas aeruginosa is exerted by the binding of gentamicin to the outer membrane, where it displaces natural cations, destabilizes the membrane, and forms holes in the cell surface.3

Antimicrobial spectrum: Includes Gram-negative and Gram-positive bacteria, including strains resistant to tetracycline, chloramphenicol, kanamycin and colistin, particularly strains of Pseudomonas, Proteus, Staphylococcus and Streptococcus.
SML1091 Homoharringtonine ≥98% (HPLC) New Homoharringtonine (Omacetaxine mepesuccinate) is a translation elongation inhibitor, a cytotoxic alkaloid originally isolated from the evergreen tree, Cephalotaxus hainanensis. Homoharringtonine binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. Homoharringtonine blocks progression of leukemic cells from G1 phase into S phase and from G2 phase into M phase. Homoharringtonine (Omacetaxine mepesuccinate) was approved in October 2012 (Synribo) for the treatment of adult patients with Chronic Myelogenous Leukemia (CML) with resistance and/or intolerance to two or more tyrosine kinase inhibitors.
H3274 Hygromycin B from Streptomyces hygroscopicus powder, BioReagent, suitable for cell culture, suitable for insect cell culture Mode of Action: The product acts by inhibiting protein synthesis by inducing the misreading of the m-RNA template in the prokaryote, with the potency to inhibit translation.

Antimicrobial Spectrum: Hygromycin B acts against bacteria, fungi and higher eukaryotic cells.
I4659 ICRF-193 apoptosis inducer, arabinosidase substrate ICRF-193 induces a G2 checkpoint that is associated with an ATR-dependent inhibition of polo-like kinase 1 (plk1) activity and a decrease in cyclin B1 phosphorylation.1 Induces apoptosis in several cell lines including K562 and Molt-4 cells.2,,,1 ICRF-193 is a topoisomerase II inhibitor, more potent against topoisomerase II-β than topoisomerase II-α3, and may in addition cause DNA strand breaks.4
I9785 Imidazolo-oxindole PKR inhibitor C16 ≥98% (HPLC) Imidazolo-oxindole PKR inhibitor C16 is a selective inhibitor of RNA-dependent protein kinases (PKR, Eif2ak2). C16 is a first reported, potent and selective PKR inhibitor. Its inhibition effect on PKR is ATP-binding site directed. C16 specifically inhibits the apoptotic PKR/eIF2a signaling pathway without stimulating the proliferative mTOR/p70S6K signaling mechanism.
I0161 IWR-1 ≥98% (HPLC) The Wnt/b-catenin (‘canonical’) pathway maintains transcriptional programs that enable stem cells to remain multipotent. Hyperactivation of the Wnt/b-catenin pathway leads to disease stage. IWR-3 act as inhibitors of Wnt response. It appear that IWR compounds induce stabilization of Axin proteins via a direct interaction, which is a part of the b-catenin destruction complex (consists of Apc, Axin, Ck1 and Gsk3b).
K4000 Kanamycin sulfate from Streptomyces kanamyceticus Animal Component-free Mode of Action: The product acts by binding to the 70S ribosomal subunit, inhibiting translocation and eliciting miscoding.

Mode of Resistance:Aminoglycoside-modifying enzymes (including acetyltransferase, phosphotransferase, nucleotidyltransferase) can alter this antibiotic, preventing its interaction with ribosomes.

Antimicrobial spectrum: Kanamycin sulfate is effective against gram-negative and gram-postiive bacteria, and mycoplasma.
K1507 Kirromycin from Streptomyces collinus ≥90% (HPLC) Binding of kirromycin to EF-Tu prevents EF-TuGDP from being ejected from the ribosome, which immobilizes the ribsome, as well as all of the following ribosomes on the mRNA2.
L5139 Lycorine hydrochloride ≥98% (TLC), powder A selective inhibitor of peptidyl transferase center (PTC). In HL-60 (leukemia) cells, lycorine arrests the cell cycle at G2/M and induces apoptosis by a caspase-mediated pathway.1
K4394 PKF118-310 ≥98% (HPLC), powder PKF118-310 is an antagonist of the Tcf4/b-catenin signaling. The compound disrupts the Tcf4/b-catenin complex and inhibits expression of Tcf4 responsive genes. PKF118-310 inhibits expression of survivin and induces apoptosis in HCC, colon tumor and lymphocytic leukemia cell lines.
P0052 PNU-74654 ≥98% (HPLC), solid PNU-74654 inhibits the Wnt-β catenin pathway by blocking the interaction between β-catenin and TCF (T cell factor). PNU-74654 is also an anti-tumor agent. Aberrant activation of the Wnt/β-catenin pathway (canonical pathway) is implicated in driving development/progression of different tumors, such as colon cancer, through interaction between β-catenin and T cell factor (TCF), which regulates the expression of target genes in cell proliferation and differentiation. Inhibition of this pathway activity in cancer cell lines efficiently blocks their growth. PNU-74654 inhibits this pathway by blocking the interaction between β-catenin and TCF.
SML0807 PreQ1 dihydrochloride ≥98% (HPLC) PreQ1 (pre-queuosine1) is an intermediate of the queuosine pathway. Also, PreQ1 binds with high affinity to the aptamer of PreQ1 riboswitch, which attenuates protein expression.
P9620 Puromycin dihydrochloride Ready Made Solution, from Streptomyces alboniger, 10 mg/mL in H2O, 0.2 μm filtered Mode of Action: Puromycin inhibits protein synthesis by causing premature chain termination acting as an analog of the 3′-terminal end of the aminoacyl-tRNA. Puromycin also acts as a reversible inhibitor of dipeptidyl-peptidase II (serine peptidase) and cytosol alanyl aminopeptidase.

Mode of Resistance: Puromycin acetyltransferase is an effective resistance gene.

Antimicrobial Spectrum: This product is active against gram-positive microorganisms, less active against acid-fast bacilli and more weakly active against gram-negative microorganisms. Puromycin can prevent growth of bacteria, protozoa, algae and mammalian cells and acts quickly, killing 99% of cells within 2 days.
P7255 Puromycin dihydrochloride from Streptomyces alboniger ≥98% (HPLC), powder Mode of Action: Puromycin inhibits protein synthesis by causing premature chain termination acting as an analog of the 3′-terminal end of the aminoacyl-tRNA.

Mode of Resistance: Puromycin acetyltransferase is an effective resistance gene.

Antimicrobial Spectrum: This product is active against gram-positive microorganisms, less active against acid-fast bacilli and more weakly active against gram-negative microorganisms. Puromycin can prevent growth of bacteria, protozoa, algae and mammalian cells and acts quickly, killing 99% of cells within 2 days.
P8833 Puromycin dihydrochloride from Streptomyces alboniger powder, BioReagent, suitable for cell culture Mode of Action: Puromycin inhibits protein synthesis by causing premature chain termination acting as an analog of the 3′-terminal end of the aminoacyl-tRNA.

Mode of Resistance: Puromycin acetyltransferase is an effective resistance gene.

Antimicrobial Spectrum: This product is active against gram-positive microorganisms, less active against acid-fast bacilli and more weakly active against gram-negative microorganisms. Puromycin can prevent growth of bacteria, protozoa, algae and mammalian cells and acts quickly, killing 99% of cells within 2 days.
S4451 Sal003 ≥98% (HPLC) Sal003 inhibits the late long-term potentiation (L-LTP) and long-term memory formation in mammalian hippocampal slices. The effect of Sal003 on L-LTP is mediated by the transcription factor, ATF4.2,3
Sal003 is a potent and cell-permeable eIF-2a phosphatase inhibitor.
SML0951 Salubrinal ≥98% (HPLC) Salubrinal is a selective Inhibitor of eIF2α (eukaryotic translation initiation factor 2 α-subunit) dephosphorylation, inhibiting global protein translation. Salubrinal is a specific inhibitor of ER Stress induced apoptosis.
S9896 Saporin from Saponaria officinalis seeds lyophilized powder A ribosome inactivating protein.
S0692 Spectinomycin Ready Made Solution, 100 mg/mL in DMSO/H2O, 1:1, 0.2 μm filtered Mode of Action: Spectinomycin acts by inhibiting protein synthesis and elongation by binding to the bacterial 30S ribosomal subunit and interfering with peptidyl tRNA translocation.

Mode of Resistance: A mutation in rpsE, the gene for ribosomal protein S5, prevents the binding of spectinomycin. Resistance is also conferred by the aminoglycoside-3′-adenyltransferase gene (aadA).

Antimicrobial spectrum: Spectinomycin acts against gram-negative and gram-positive bacteria.
S4014 Spectinomycin dihydrochloride pentahydrate powder, BioReagent, suitable for cell culture Mode of Action: Spectinomycin acts by inhibiting protein synthesis and elongation by binding to the bacterial 30S ribosomal subunit and interfering with peptidyl tRNA translocation.

Mode of Resistance: A mutation in rpsE, the gene for ribosomal protein S5, prevents the binding of spectinomycin. Resistance is also conferred by the aminoglycoside-3′-adenyltransferase gene (aadA).

Antimicrobial spectrum: Spectinomycin acts against gram-negative and gram-positive bacteria.


S6501 Streptomycin sulfate salt powder Mode of Action: Streptomycin acts by inhibiting prokaryote protein synthesis by binding to the S12 protein of the 30S ribosomal subunit, thus preventing the transition from imitation complex to chain-elongating ribosome. This causes miscoding or inhibits initiation.

Mode of Resistance: A mutation in rpsL, a gene for S12 ribosomal protein, prevents binding of streptomycin to the ribosome. An aminoglycoside phosphotransferase also inactivates streptomycin.

Antimicrobial spectrum: Streptomycin acts against gram-negative and gram-positive bacteria.
T8902 Thiostrepton from Streptomyces azureus ≥90% (HPLC) Peptide antibiotic that prevents the binding of elongation factor G (EF-G) and GTP to the 50S ribosomal subunit.