KSP

ARRY 520 hydrochloride is a kinesin spindle protein (KSP) inhibitor.ARRY 520 hydrochloride induces cell death by apoptosis and has potent anti-proliferative activity.

PROTACKSP-IN-1 (Compound 21) is a spindle protein (KSP) degrader as a PROTAC, effectively degrading KSP in HCT-116 cells with a DC50 value of 114.8 nM. It inhibits the proliferation of HCT-116 with an IC50 of 10 nM, causes G2 M phase cell cycle arrest, and induces apoptosis in HCT-116. Additionally, PROTACKSP-IN-1 demonstrates antitumor activity in mouse models.

KSP ligand 1 is a protein ligand that targets KSP (Kinesin) and can be used in the synthesis of PROTAC KSP-IN-1 for cancer research.

KSP-IA is a potent, specific, allosteric, and cell-active KSP inhibitor.

Larkspur alkaloid is a bioactive chemical.

KSPWFTTL is an immunodominant epitope derived from the p15E transmembrane protein. It is Kb-restricted and can enhance the susceptibility of a tumor cell line to cytotoxic T lymphocytes targeting anti-AKR/Gross MuLV.

Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties.

SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).

Filanesib (ARRY 520) is a selective inhibitor of kinesin spindle protein (KSP, IC50 = 6 nM) with potent anti-proliferative activity.

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.

(R)-Filanesib is the R-enantiomer of ARRY-520. (R)-Filanesib is a synthetic kinesin spindle protein (KSP) inhibitor (IC50: 6 nM).

MK-0731, a synthetic small molecule with potential antineoplastic activity, selectively inhibits kinesin spindle protein (KSP), leading to the inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase and apoptosis in

Filanesib (ARRY-520) targets the kinesin spindle protein (KSP) with potential antineoplastic activity. ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during

SB-743921, a kinesin spindle protein (KSP) inhibitor, is used potentially for the treatment of non-Hodgkin's lymphoma (NHL).

CW-069 (IC50=75 μM), an allosteric selective inhibitor of microtubule motor protein HSET, exhibits remarkable specificity over KSP.

AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. KSP inhibitor AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly; activation of the spindle assembly checkpoint; induction of cell cycle arrest during the mitotic phase; and cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. Eg5 is essential for the formation of bipolar spindles and the proper segregation of sister chromatids during mitosis.

CK0106023 was specific inhibitor of KSP. In tumor-bearing mice, CK0106023 exhibited antitumor activity comparable to or exceeding that of paclitaxel and caused the formation of monopolar mitotic figures identical to those produced in cultured cells. KSP was most abundant in proliferating human tissues and was absent from cultured postmitotic neurons.

Compound D7, also known as Mal-PEG8-Val-Ala-PAB-SB-743921, is a drug-linker conjugate for antibody-drug conjugates (ADC). It comprises the KSP inhibitor SB-743921 connected through a linker and is utilized in the synthesis of ADCs [1].

NHS-Ala-Ala-Asn-active metabolite serves as a cleavable linker in the synthesis of antibody-drug conjugates (ADCs) targeting kinesin spindle protein (KSP) inhibitors [1].