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シグナル伝達経路

研究分野

  • 阻害剤の選択性比較
  • 溶解度
カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S2215 DAPT (GSI-IX) <1 mg/mL 86 mg/mL 50 mg/mL
S1575 RO4929097 <1 mg/mL 93 mg/mL 16 mg/mL
S1594 Semagacestat (LY450139) <1 mg/mL 72 mg/mL 41 mg/mL
S2660 MK-0752 <1 mg/mL 89 mg/mL 45 mg/mL
S1262 Avagacestat (BMS-708163) <1 mg/mL 104 mg/mL <1 mg/mL
S2711 Dibenzazepine (YO-01027) <1 mg/mL 92 mg/mL <1 mg/mL
S2714 LY411575 <1 mg/mL 95 mg/mL 13 mg/mL
S8018 Nirogacestat (PF-03084014, PF-3084014) <1 mg/mL 97 mg/mL 97 mg/mL
S8280 IMR-1 <1 mg/mL 70 mg/mL <1 mg/mL
S7673 L-685,458 <1 mg/mL 100 mg/mL 6 mg/mL
S7399 FLI-06 <1 mg/mL 88 mg/mL 8 mg/mL
S7169 Crenigacestat (LY3039478) <1 mg/mL 92 mg/mL 71 mg/mL
S7323 CHF 5074 <1 mg/mL 59 mg/mL 9 mg/mL
S8603 NGP 555 <1 mg/mL 40 mg/mL 3 mg/mL

亜型選択性的な製品

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
S2215

DAPT (GSI-IX)

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.

S1575

RO4929097

RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.

S1594

Semagacestat (LY450139)

Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3.

S2660

MK-0752

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.

S1262

Avagacestat (BMS-708163)

Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

S2711

Dibenzazepine (YO-01027)

Dibenzazepine (YO-01027) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.

S2714

LY411575

LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells.

S8018

Nirogacestat (PF-03084014, PF-3084014)

Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Phase 2.

S8280

IMR-1

IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μmol/L.

S7673

L-685,458

L-685,458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.

S7399

FLI-06

FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.

S7169

Crenigacestat (LY3039478)

Crenigacestat (LY3039478) is an oral Notch inhibitor with an IC50 of 0.41 nM.

S7323

CHF 5074

CHF5074 is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.

S8603

NGP 555

NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically.

Tags: Gamma-secretase inhibition | Gamma-secretase inhibitor Notch | Gamma-secretase activity | Gamma-secretase assay | Gamma-secretase cleavage | Gamma-secretase inhibitor in clinical trial | Gamma-secretase inhibitor review
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誠に勝手ながら、弊社では下記の期間を年末年始による休業とさせていただきます。
【休業期間】
2018年12月29日(土)から2019年1月6日(日)
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