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阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1452 Ispinesib (SB-715992) <1 mg/mL 103 mg/mL 103 mg/mL
S2182 SB743921 HCl 22 mg/mL 111 mg/mL 111 mg/mL
S7090 GSK923295 <1 mg/mL 100 mg/mL 100 mg/mL
S7355 ARQ 621 <1 mg/mL 100 mg/mL 100 mg/mL
S0279 Dimethylenastron <1 mg/mL 60 mg/mL 1.5 mg/mL
S6953 GW406108X <1 mg/mL 80 mg/mL ''<1 mg/mL
S8439 Monastrol <1 mg/mL 58 mg/mL '58 mg/mL
S5522 H-Cys(Trt)-OH -1 mg/mL 5 mg/mL '-1 mg/mL
S5933 K 858 <1 mg/mL 55 mg/mL 4 mg/mL
S6796 BTB-1 <1 mg/mL 60 mg/mL 2 mg/mL

Kinesin製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1452

Ispinesib (SB-715992)

Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death. Phase 2.

S2182

SB743921 HCl

SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2.

S7090

GSK923295

GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. GSK923295 induces post-mitotic apoptosis. Phase 1.

S7355

ARQ 621

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

S0279

Dimethylenastron

Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.

S6953

GW406108X

GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK.

S8439

Monastrol

Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.

S5522

H-Cys(Trt)-OH

H-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM.

S5933

K 858

K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily.

S6796

BTB-1

BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1452

Ispinesib (SB-715992)

Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death. Phase 2.

S2182

SB743921 HCl

SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2.

S7090

GSK923295

GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. GSK923295 induces post-mitotic apoptosis. Phase 1.

S7355

ARQ 621

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

S0279

Dimethylenastron

Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.

S6953

GW406108X

GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK.

S8439

Monastrol

Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.

S5522

H-Cys(Trt)-OH

H-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM.

S5933

K 858

K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily.

S6796

BTB-1

BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM.

Tags: KSP inhibition | Kinesin inhibition | Kinesin assay | Kinesin phosphorylation | Kinesin cancer | KSP inhibitors cancer | KSP inhibitor clinical trial | Kinesin inhibitors list | Kinesin inhibitor review