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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T3560 Desmethylanethol trithione

ADT-OH

VEGFR; Akt Angiogenesis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
Desmethylanethol trithione (ADT-OH) 是合成硫化氢的供体。它利用上调 FADD 诱导细胞凋亡,并对体内黑色素瘤的形成具有一定的抑制作用,可用于研究癌症疾病。
T76124 Acyl coenzyme A synthetase

Acyl coenzyme A synthetase (ACS),一种生化研究中常用的酶,主要通过两步硫酯化反应激活脂肪酸与辅酶A结合,形成酰基辅酶A。该过程为脂质代谢中的多种合成与分解代谢途径,以及参与TCA循环中的有氧呼吸提供了关键中间物。
T36782 TAK1-IN-2

TAK1-IN-2

TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562.
T36946 PW0464

PW0464

PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1]. PW0464 (compound 24) is found to elicit complete G protein bias, showing no activity for D1R-mediated β-arrestin recruitment[1].PW0464 (compound 24), the non-catechol agonist, forms bonds with S1985.42 and S2025.46 via its fluorine atom[2]. [1]. Pingyuan Wang, et al. Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Recept...
T35488 (S)-PI3Kα-IN-4

(S)-PI3Kα-IN-4

(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitor...
T38106 JC-171

JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ...
T35817 Photoswitchable PAD Inhibitor (technical grade)

Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK29...
T36504 STY-BODIPY

STY-BODIPY,Styrene-BODIPY

STY-BODIPY is a styrene-conjugated fluorogenic probe for radical-trapping antioxidant (RTA) activity.1 Co-autoxidation of the STY-BODIPY signal carrier and a hydrocarbon co-substrate can be quantified by monitoring the loss of absorbance at 571 nm. STY-BODIPY has been used to measure the activity of RTAs, as well as the kinetics and stoichiometry of RTA reactions in cell-free assays.1,2,3References1. Haidasz, E.A., Van Kessel, A.T.M., and Pratt, D.A. A continuous visible light spectrophotometric...
T35638 SR 1903

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of th...
T35527 PI3Kα-IN-4

PI3Kα-IN-4

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t...

化合物

Desmethylanethol trithione
Cat.No: T3560
Synonym: ADT-OH
Target: VEGFR, Akt
Acyl coenzyme A synthetase
Cat.No: T76124
Synonym:
Target:
TAK1-IN-2
Cat.No: T36782
Synonym: TAK1-IN-2
Target:
PW0464
Cat.No: T36946
Synonym: PW0464
Target:
(S)-PI3Kα-IN-4
Cat.No: T35488
Synonym: (S)-PI3Kα-IN-4
Target:
JC-171
Cat.No: T38106
Synonym:
Target:
Photoswitchable PAD Inhibitor (technical grade)
Cat.No: T35817
Synonym:
Target:
STY-BODIPY
Cat.No: T36504
Synonym: STY-BODIPY,Styrene-BODIPY
Target:
SR 1903
Cat.No: T35638
Synonym:
Target:
PI3Kα-IN-4
Cat.No: T35527
Synonym: PI3Kα-IN-4
Target:
Cat. No. Product Name Target Signaling Pathways
T36950 Rubrofusarin triglucoside

Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM[1]. [1]. Pradeep Paudel, et al. Rubrofusarin as a Dual Protein Tyrosine Phosphate 1B and Human Monoamine Oxidase-A Inhibitor: An in Vitro and in Silico Study. ACS Omega. 2019 Jul 3;4(7):11621-11630.

天然产物

Rubrofusarin triglucoside
Cat.No: T36950
Synonym:
Target:
TargetMol Loading
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