eg5

Eg5 Inhibitor V, trans-24, is a specific and potent Eg5 inhibitor with an IC50 value of 0.65 μM, suitable for use in cancer research.

Eg5-IN-1 is a potent inhibitor of the kinesin family of motor proteins (Eg5) with an IC50 value of 1.97 µM for Eg5.Eg5-IN-1 can be used in cancer research.

Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity.

AZD-4877 is a potent spindle kinesin (Eg5) inhibitor with an IC50 value of 2 nM. AZD-4877 is an alternative configuration of Ispinesib that inhibits mitosis, induces the formation of a unipolar spindle phenotype, and mediates apoptosis. AZD-4877 has antitumor activity and inhibits circulating peripheral blood mononuclear cells (PBMC).

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.

Dimethylenastron, an Eg5 inhibitor, arrests cells with monopolar spindles to which all chromosomes attach in a syntelic manner.

Monastrol ((±)-Monastrol) is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5.

ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

Eg5-IN-3 (5) is an Eg5 inhibitor targeting a novel allosteric site (α4/α6/L11). It disrupts tubulin assembly, leading to abnormal and irregular formations, which subsequently causes typical mitotic arrest, akin to the effects of Monastrol.

Eg5-IN-2 (Compound Scaffold B (4)), with an IC50 of less than 0.5 nM, acts as an effective Eg5 inhibitor. This compound is suitable for use as an ADC payload in the synthesis of ADCs [1].

Hydroxy-PEG6-Boc, a PEG-based PROTAC linker, is utilized in PROTAC synthesis [1].

N-Boc-PEG5-bromide is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) and serves as a PROTAC linker based on PEG and Alkyl/ether.

Acid-C1-PEG5-Boc, a PEG-based PROTAC linker, is utilized in PROTAC synthesis.

Cbz-NH-PEG5-CH2COOH is a PEG-based PROTAC linker used in PROTAC synthesis.

Mal-PEG5-Boc (Mal-PEG5-COOtBu) is a PEG-based PROTAC linker. Mal-PEG5-Boc can be used in the synthesis of PROTACs.

Propargyl-PEG5-Ms (Propargyl-PEG6-Ms) is a PEG-based PROTAC linker. Propargyl-PEG5-Ms can be used in the synthesis of PROTACs.

Acid-PEG5-C2-Boc, a PEG-based linker for PROTACs, facilitates the connection of two essential ligands necessary for PROTAC molecule formation, enabling selective protein degradation via the ubiquitin-proteasome system within cells.

Acid-PEG5-mono-methyl ester, a PEG-based PROTAC linker, enables the synthesis of PROTACs[1].

Acid-PEG5-TEMPO is a PEG-based linker for PROTACs, joining two essential ligands crucial for PROTAC molecule formation, and facilitates selective protein degradation using the ubiquitin-proteasome system within cells.

Ald-CH2-PEG5-azide is a non-cleavable linker comprising a five-unit PEG chain, frequently used in the synthesis of antibody-drug conjugates (ADCs)[1].

Ald-CH2-PEG5-Boc is a PEG- and alkyl/ether-based PROTAC linker suitable for synthesizing PROTACs [1].

Amino-PEG5-amine, a PEG-based linker containing 5 units, is utilized in PROTAC synthesis.

Amino-PEG5-Boc is a PEG-based linker for PROTACs, crucial for joining two essential ligands and enabling selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

Amino-PEG5-C2-acid is a non-cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].