Kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule filaments, and are powered by the hydrolysis of ATP (thus kinesins are ATPases). The active movement of kinesins supports several cellular functions including mitosis, meiosis and transport of cellular cargo. Most kinesins walk towards the plus end of a microtubule, entails transporting cargo from the centre of the cell towards the periphery. Kinesins were discovered as microtubule (MT)-based anterograde intracellular transport motors. The founding member of this superfamily, the genomes of mammals encode more than 40 kinesin proteins, organized into at least 14 families named kinesin-1 through kinesin-14.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H9598 |
Sovilnesib |
2410796-79-9 | AMG-650 is an oral, first in class, selective small molecule inhibitor of KIF18A for treatment of advanced solid tumors. |
H8676 |
MPT0B390 |
1338320-90-3 | MPT0B390 is a novel arylsulfonamide inducer, inhibits tumor growth, metastasis and angiogenesis with GI50 of 0.03 ± 0.01 μM±SD. |
H2377 |
SR31527 |
311814-78-5 | SR31527 is a novel allosteric Kinesin-like protein KIFC1 inhibitor that inhibits microtubule-stimulated KIFC1 ATPase activity with IC50 of 6.6 uM, binds directly to KIFC1 with Kd of 25.4 nM; prevents bipolar clustering of extra centrosomes in TNBC cells and significantly reducesTNBC cell colony formation and viability (MDA-MB-231, BT549 and MDA-MB-435s cells IC50=20-30 uM), with less toxicity to normal fibroblasts. |
H2376 |
SB-743921 |
940929-33-9 | SB-743921 is a potent, selective kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, shows no activity against MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E; also shows high affinity for mouse KSP with Ki of 0.12 nM; blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death in cancer cells, demonstrates improved potency over ispinesib in both biochemical and cellular assays; shows a broad spectrum of tumor inhibition in multiple cancer models. |
H2375 |
S-Trityl-L-cysteine |
2799-07-7 | S-Trityl-L-cysteine (NSC 83265) is a potent, cell-permeable, selective inhibitor of mitotic kinesin Eg5, inhibits basal ATPase activity (IC50=1 mM) and microtubule-activated ATPase activity of Eg5 (IC50=140 nM); induces mitotic arrest in HeLa cells with an IC50 of 700 nM, and displays antitumor activity. |
H2374 |
PVZB-1194 |
1141768-04-8 | PVZB-1194 is a bis(hetero)aryl derivative that inhibits kinesin spindle protein (KSP) ATPase witn IC50 of 0.12 uM; inhibits HeLa cell proliferation with IC50 of 5.5 uM; potently inhibits KSP in a microruble dependent manner and induces a monoastral phenotype to arrest mitotic progression, abnormal KSP localization. |
H2373 |
Propofol |
2078-54-8 | A widely used general anesthetic to induce and maintain anesthesia; influences ligand-gated channels, including the GABAA receptor and others; also inhibits conventional kinesin-1 KIF5B and kinesin-2 KIF3AB and KIF3AC, causing a significant reduction in the distances that these processive kinesins can travel without an effect on velocity (EC50 |
H2372 |
PF-2771 |
2070009-55-9 | PF-2771 is a potent, selective CENP-E inhibitor with IC50 of 16.1 nM; does not inhibit the ATPase activities of highly related kinesins (Eg5/KSP, chromokinesin and MCAK, IC50> 1 uM); selectively inhibits proliferation of basal breast cancer cell lines; regresses tumor growth correlated with increased phospho-HH3-Ser10 levels in a breast cancer xenograft tumor model. |
H2371 |
Monastrol |
329689-23-8 | A potent, specific, allosteric and reversible mitotic kinesin Eg5 inhibitor with IC50 of 14 uM (microtubule motility inhibition); does not inhibit microtubule motility driven by conventional kinesin at 200 uM; inhibits both the basal and the microtubule-stimulated ATPase activity of the Eg5 motor domain, does not compete with ATP binding to Eg5; arrests cells in mitosis with monoastral spindles, and (S)-monastrol is a more potent inhibitor of Eg5 activity in vitro and in vivo. |
H2370 |
MK-8267 |
1146209-50-8 | MK-8267 (SCH 2047069) is a potent, orally bioavailable, brain penetrant kinesin spindle protein (KSP) inhibitor with EC50 of 3 nM; inhibits a broader panel of 57 different tumor cell lines with IC50 |
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