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7

抑制剂 & 化合物

1

天然产物

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Cat. No. Product Name Target Signaling Pathways
T6396 (R)-(-)-Gossypol acetic acid

(-)-Gossypol acetic acid,AT-101 (acetic acid),(R)-Gossypol acetic acid,AT101醋酸,AT101,AT101 acetate

BCL; Autophagy Apoptosis; Autophagy
(R)-(-)-Gossypol acetic acid (AT101 acetate) 是天然产物 Gossypol 的左旋异构体,与 Bcl-2、Bcl-xL 和 Mcl-1 结合,Ki 为 0.32 μM、0.48 μM 和 0.18 μM。
T26686 AV-101

L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine

NMDAR Neuroscience
AV-101 (4-Cl-KYN) 是 NMDA 受体甘氨酸位点的前药拮抗剂,具有抗抑郁活性,可减少 MPTP 猴子中左旋多巴诱导的运动障碍。
T36935 PKUMDL-LC-101-D04

GPX4-Activator-1d4,PKUMDL-LC-101-D04

GPX oxidation-reduction
PKUMDL-LC-101-D04是一种高效的谷胱甘肽过氧化物酶4(GPX4)的异位激活剂,是一种铁死亡的调节剂。 当在无细胞试验中使用浓度为20 μM 时,GPX4活性增加到对照水平的150%;在野生型而非Gpx4-/-小鼠胚胎成纤维细胞(MEF)提取物中使用浓度为61 μM 时,GPX4活性增加到对照水平的150%。PKUMDL-LC-101-D04(200 μM)能减少胆固醇过氧化氢诱导的MEF 死亡。
T3631 PF-8380

PDE Metabolism
PF8380 是有效的autotaxin 抑制剂,在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。
T26048 RB 101

RB101,RB-101

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.
T71290 EVT-101 HCl

EVT-101 is a GluN2B antagonist, binding at the same GluN1/GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions.
T70049 Ro 04-5595 free base

Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol/L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and...

化合物

(R)-(-)-Gossypol acetic acid
Cat.No: T6396
Synonym: (-)-Gossypol acetic acid,AT-101 (acetic acid),(R)-Gossypol acetic acid,AT101醋酸,AT101,AT101 acetate
Target: BCL, Autophagy
AV-101
Cat.No: T26686
Synonym: L-4-Cl-KYN,L-4-chlorokynurenine,4-Cl-KYN,4ClKYN,4-Chlorokynurenine,(S)-4-Chlorokynurenine
Target: NMDAR
PKUMDL-LC-101-D04
Cat.No: T36935
Synonym: GPX4-Activator-1d4,PKUMDL-LC-101-D04
Target: GPX
PF-8380
Cat.No: T3631
Synonym:
Target: PDE
RB 101
Cat.No: T26048
Synonym: RB101,RB-101
Target:
EVT-101 HCl
Cat.No: T71290
Synonym:
Target:
Ro 04-5595 free base
Cat.No: T70049
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2730 Gossypol (acetic acid)

(±)-Gossypol-acetic acid,Pogosin,AT101,醋酸棉酚,乙酸棉子酚,Gossypol acetic acid

BCL Apoptosis
Gossypol acetic acid (AT101) 是一种从棉籽中分离出来的多酚天然产物,分别与 Bcl-xL 蛋白和 Bcl-2蛋白结合,Ki 值分别为 0.5-0.6 μM 和 0.2-0.3 mM。

天然产物

Gossypol (acetic acid)
Cat.No: T2730
Synonym: (±)-Gossypol-acetic acid,Pogosin,AT101,醋酸棉酚,乙酸棉子酚,Gossypol acetic acid
Target: BCL
TargetMol Loading
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