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18

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7389	G15	Estrogen Receptor/ERR	Endocrinology/Hormones
	G15 是一种高亲和力的、选择性的 G 蛋白偶联雌激素受体(GPER/GPR30)拮抗剂(Ki:20 nM)。
T11769	KRAS G12C inhibitor 15	Ras	GPCR/G Protein; MAPK
	KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor .
T74607	KRAS G12D inhibitor 15
	KRAS G12D inhibitor 15 是一种有效的 KRAS G12D 抑制剂。KRAS G12D inhibitor 15 具有研究各种疾病或病症的潜力，例如癌症或癌症转移。
T3546	STO-609 STO 609	CaMK; AMPK; Autophagy	Autophagy; Chromatin/Epigenetic; Neuroscience; PI3K/Akt/mTOR signaling
	STO-609 是一种特异性和细胞渗透性的 Ca2+/钙调蛋白依赖性蛋白激酶激酶抑制剂，用于重组 CaM-KKα 和 CaM-KKβ，Ki 值分别为 80 和 15 ng/mL。它抑制 Hela 细胞溶解物中的 AMP 活化蛋白激酶激酶活性，IC50值约为 0.02 g/ml。
T36944	Ara-G	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物，可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP)，从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。
T37816	SB 243213
	SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1]. SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows...
T73264	L2H2-6OTD
	L2H2-6OTD, 为含有一至四个G-四联体结合环的端粒抑制素类似物，显示出对端粒酶 (telomerase) 的抑制活性，其IC50值达到15 nM。
T39165	Treprostinil palmitil Treprostinil palmitil,INS-1009
	Treprostinil Palmitil (TP), a prodrug of the DP1 and EP2 agonist Treprostinil (UT-15), exhibits EC50 values of 0.6 and 6.2 nM, respectively. It is a pure prodrug without any inherent binding affinity for G-protein coupled receptors, including prostanoid receptors.
T36968	ARN-21934	Topoisomerase	DNA Damage/DNA Repair
	ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。
T38365	CAY10597
	The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the...
T37794	Rec 15/2615 (hydrochloride)
	Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50...
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
T36215	17R(18S)-EpETE
	17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases ...
T36132	3β-OH-7-Oxocholenic Acid
	3β-OH-7-Oxocholenic acid is a bile acid.1 It is also a metabolite of 7β-hydroxy cholesterol in rats. Conjugated forms of 3β-OH-7-oxocholenic acid have been found in the urine of patients with Neimann-Pick disease type C.2,3 \|1. Norii, T., Yamaga, N., and Yamasaki, K. Metabolism of 7β-hydroxycholesterol-4-14C in rat. Steroids 15(3), 303-326 (1970).\|2. Alvelius, G., Hjalmarson, O., Griffiths, W.J., et al. Identification of unusual 7-oxygenated bile acid sulfates in a patient with Niemann-Pick dise...
T37297	Ru360
	Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce...
T37761	Fura-FF (potassium salt)
	Fura-FF is a difluorinated derivative of the calcium indicator fura-2. Unlike, fura-2, fura-FF has negligible magnesium sensitivity, thus reducing interference from this cation.[1] Fura-FF also has a higher calcium dissociation constant than fura-2 (Kd(calcium) = 6 and 0.14 μM, respectively).[1],[2]However, the spectral properties of fura-FF and fura-2 are similar with fura-FF displaying excitation/emission spectra of 365/514 nm in the absence of calcium, with a shift to 339/507 nm in the presen...
T36717	RWJ-56110 dihydrochloride
	RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap...
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...

化合物

Cat.No: T7389

Target: Estrogen Receptor/ERR

KRAS G12C inhibitor 15

Cat.No: T11769

Target: Ras

KRAS G12D inhibitor 15

Cat.No: T74607

Cat.No: T3546

Synonym: STO 609

Target: CaMK, AMPK, Autophagy

Cat.No: T36944

Target: Nucleoside Antimetabolite/Analog

Cat.No: T37816

Cat.No: T73264

Treprostinil palmitil

Cat.No: T39165

Synonym: Treprostinil palmitil,INS-1009

Cat.No: T36968

Target: Topoisomerase

Cat.No: T38365

Rec 15/2615 (hydrochloride)

Cat.No: T37794

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat.No: T36215

3β-OH-7-Oxocholenic Acid

Cat.No: T36132

Cat.No: T37297

Fura-FF (potassium salt)

Cat.No: T37761

RWJ-56110 dihydrochloride

Cat.No: T36717

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Cat. No.	Product Name	Target	Signaling Pathways
T3929	Kaurenoic acid Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid	Others	Others
	Kaurenoic acid (kaurenoate) 是一种二萜，来源于 Sphagneticola trilobata 中，可以抑制细胞因子的产生和激活 NO–cyclic GMP–PKG–ATP- 敏感型钾通道信号通路，并抑制炎症疼痛。
TMA0692	Diosbulbin G 山药	Others	Others
	Diosbulbin G是一种天然产物，属于薯蓣科薯蓣属，其产品编号为 TMA0692，CAS号为 67567-15-1。Diosbulbin G可用作对照参考。
T83660	3(Z),6(Z),9(Z),12(Z),15(Z)-Octadecapentaenoic Acid C18:5 n-3,C18:5(3Z,6Z,9Z,12Z,15Z),all-cis-3,6,9,12,15-Octadecapentaenoic Acid
	3(Z),6(Z),9(Z),12(Z),15(Z)-Octadecapentaenoic acid 是一种在 G. kowalevskii 中发现的微藻 PUFA，常作为微藻和甲藻的化学分类生物标志物使用。
T37272	9(S),12(S),13(S)-TriHOME
	9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME...
T36000	3-Hydroxyterphenyllin
	3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methi...

天然产物

Cat.No: T3929

Synonym: Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid

Target: Others

Cat.No: TMA0692

Synonym: 山药

Target: Others

3(Z),6(Z),9(Z),12(Z),15(Z)-Octadecapentaenoic Acid

Cat.No: T83660

Synonym: C18:5 n-3,C18:5(3Z,6Z,9Z,12Z,15Z),all-cis-3,6,9,12,15-Octadecapentaenoic Acid

9(S),12(S),13(S)-TriHOME

Cat.No: T37272

3-Hydroxyterphenyllin

Cat.No: T36000

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