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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
T5354	IRAK4-IN-7 CA-4948	IRAK	Immunology/Inflammation; NF-κB
	IRAK4-IN-7 (CA-4948) 是白介素 1 受体相关激酶 4 (IRAK4) 的选择性抑制剂，口服有活性。它可用于研究癌症以及炎症疾病。
T0916	Butamben Butyl 4-aminobenzoate,4-氨基苯甲酸丁酯	Potassium Channel; Calcium Channel; Sodium Channel	Membrane transporter/Ion channel; Metabolism
	Butamben (Butyl 4-aminobenzoate) 是一种长效局部麻醉剂，用于治疗慢性疼痛。
T4284	Levamlodipine besylate 左旋氨氯地平,(S)-Amlodipine Besylate (103129-82-4(free base))	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Levamlodipine besylate ((S)-Amlodipine Besylate(103129-82-4(free base))) 是一种二氢吡啶钙通道阻滞剂，具有舒张血管的作用，可用于高血压和心绞痛的研究。
T7334	NP118809 39-1B4,1-【4-(二苯甲基)-1-哌嗪基】-3,3-二苯基-1-丙酮	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	NP118809 (39-1B4) 是 N 型钙通道阻滞剂，IC50值为 0.11 μM。它较弱地抑制 L 型钙通道，IC50值为 12.2 μM。
T7550	Barnidipine YM-09730-5(Free base),(4S)-2,6-二甲基-4-(间硝基苯基)-1,4-二氢吡啶-3,5-二羧酸 (3S)-1-苄基-3-吡咯烷基-甲基酯,Mepirodipine	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Barnidipine (YM-09730-5(Free base)) 是一种二氢吡啶类钙通道阻滞剂，对 CaA 受体具有选择性作用。它是一种抗高血压药物，通过减少其血管扩张作用继发的外周血管阻力起作用。
T1606	Fasudil HA-1077,AT877,法舒地尔	ROCK; Serine/threonin kinase; Calcium Channel; PKA; PKC; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors
	Fasudil (HA-1077) 是一种非特异性 RhoA/ROCK 抑制剂，也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用，ROCK1 的 Ki 值为 0.33 μM，ROCK2 和 PKA、PKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。
T3060	Fasudil hydrochloride Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877	ROCK; Serine/threonin kinase; Calcium Channel; HIV Protease; PKA; PKC; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors
	Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA/ROCK 抑制剂，也抑制蛋白激酶，对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。
T8590	4-(benzyloxy)benzene-1-sulfonamide	Others	Others
	4-(benzyloxy)benzene-1-sulfonamide 是人重组 CA-7 的抑制剂。
T35251	YK-5-252 YK 5 252,YK5-252,YK-5252
	YK-5-252 is a dual action combretastatin A-4 (CA-4) prodrug which releases CA-4 through a disulfide bond cleavage mechanism and contains a near-infrared (NIR) fluorophore.
T63276	hCAXII-IN-4
	hCAXII-IN-4 是选择性的、有效的 CA XII 抑制剂，对人CA XII 的Ki 值为 6.4 nM。
T16387	Ombrabulin AVE8062,AC7700	Microtubule Associated	Cytoskeletal Signaling
	Ombrabulin is a derivative of CA-4 phosphate. It is known to show antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.
T16386	Ombrabulin hydrochloride AVE8062 (hydrochloride),AC7700 (hydrochloride)	Microtubule Associated	Cytoskeletal Signaling
	Ombrabulin hydrochloride 是一种合成的、具有选择性的 CA-4 磷酸酯或 Ombrabulin 的衍生物，能破坏内皮细胞的微管蛋白细胞骨架，具有抗血管作用。Ombrabulin 是是一种微管蛋白聚合抑制剂，是 combretastatin a -4化合物类的一员，是一种水溶性的微管蛋白解聚肿瘤血管破坏化合物。
T31573	DPX-3778
	DPX-3778 is the triethanolamine salt of 3-(p-chlorophenyl)-6-methoxy-s-triazine-2,4(1H,3H) dione, at concentrations of 0.124-2.48 μM enhanced ca. 4-5-fold the proliferation of tobacco (Nicotiana tabacum L. cv. Wisconsin 38) callus cultured in the presence
T79195	Cav 3.2 inhibitor 4	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Cav 3.2 inhibitor 4 (compound 21) 是高效的选择性 T 型钙通道 (Cav3.2) 抑制剂，具有外周限制性，其 IC50 值为 0.6 μM，适用于心房颤动研究。
T35713	N-desethyl Brinzolamide (oxalate)
	N-desethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1It inhibits CAII and CAIV activities (IC50s = 1.28 and 128 nM, respectively). 1.Kim, C.-Y., Whittington, D.A., Chang, J.S., et al.Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IVJ. Med. Chem.45(4)888-893(2002)
T76021	Myelin Basic Protein TFA
	Myelin Basic Protein (MHP4-14) TFA 是一种合成肽，包含髓鞘碱性蛋白的残基4-14，是一种非常有选择性的 PKC 底物 (Km=7 μM)。Myelin Basic Protein TFA 不被环腺苷酸依赖性蛋白激酶、酪蛋白激酶 I 和 II、Ca2+/钙调素依赖性蛋白激酶 II 或磷酸化酶激酶磷酸化，可常规用于测定粗组织提取物中低背景的蛋白激酶 C。
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...
T41016	Vercirnon sodium GSK-1605786 sodium,CCX282-Bsodium,维塞诺钠盐,Traficet-ENsodium
	Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9 . Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC 50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC 50 s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC 50 values of 2.8 and 2.6 nM, respectivel...

化合物

Cat.No: T5354

Synonym: CA-4948

Target: IRAK

Cat.No: T0916

Synonym: Butyl 4-aminobenzoate,4-氨基苯甲酸丁酯

Target: Potassium Channel, Calcium Channel, Sodium Channel

Levamlodipine besylate

Cat.No: T4284

Synonym: 左旋氨氯地平,(S)-Amlodipine Besylate (103129-82-4(free base))

Target: Calcium Channel

Cat.No: T7334

Synonym: 39-1B4,1-【4-(二苯甲基)-1-哌嗪基】-3,3-二苯基-1-丙酮

Target: Calcium Channel

Cat.No: T7550

Synonym: YM-09730-5(Free base),(4S)-2,6-二甲基-4-(间硝基苯基)-1,4-二氢吡啶-3,5-二羧酸 (3S)-1-苄基-3-吡咯烷基-甲基酯,Mepirodipine

Target: Calcium Channel

Cat.No: T1606

Synonym: HA-1077,AT877,法舒地尔

Target: ROCK, Serine/threonin kinase, Calcium Channel, PKA, PKC, Autophagy

Fasudil hydrochloride

Cat.No: T3060

Synonym: Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877

Target: ROCK, Serine/threonin kinase, Calcium Channel, HIV Protease, PKA, PKC, Autophagy

4-(benzyloxy)benzene-1-sulfonamide

Cat.No: T8590

Target: Others

Cat.No: T35251

Synonym: YK 5 252,YK5-252,YK-5252

Cat.No: T63276

Cat.No: T16387

Synonym: AVE8062,AC7700

Target: Microtubule Associated

Ombrabulin hydrochloride

Cat.No: T16386

Synonym: AVE8062 (hydrochloride),AC7700 (hydrochloride)

Target: Microtubule Associated

Cat.No: T31573

Cav 3.2 inhibitor 4

Cat.No: T79195

Target: Calcium Channel

N-desethyl Brinzolamide (oxalate)

Cat.No: T35713

Myelin Basic Protein TFA

Cat.No: T76021

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Vercirnon sodium

Cat.No: T41016

Synonym: GSK-1605786 sodium,CCX282-Bsodium,维塞诺钠盐,Traficet-ENsodium

Cat. No.	Product Name	Target	Signaling Pathways
T6212	Combretastatin A4 CA4,康普瑞汀,Z)-3,4,5,4',-四甲氧基-3'-羟基二苯乙烯,CRC 87-09	Microtubule Associated	Cytoskeletal Signaling
	Combretastatin A4 (CA4) 是一种微管靶向剂，可结合 β-tubulin，Kd 值为 0.4 μM。
T2782	Catharanthine (+)-3, 4-Didehydrocoronaridine,长春质碱,(+)-3,4-Didehydrocoronaridine	Calcium Channel; AChR	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Catharanthine ((+)-3,4-Didehydrocoronaridine) 是长春花中的一种生物碱，可抑制电压门控 L 型钙离子通道，具有抗肿瘤和降血压活性。
T2S2215	Crebanine	Apoptosis; Others; Akt	Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
	Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
T4S2326	Cornuside 7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside	ERK; p38 MAPK; NF-κB; JNK	MAPK; NF-κB
	Cornuside (Comuside) 是从山茱萸的果实中分离出的环烯醚萜苷，可用于炎症疾病的研究和促进血液循环。它通过下调 MAPK 和 NF-κB 信号通路抑制肥大细胞介导的过敏反应，用于炎性过敏性疾病中的潜能。
T82692	Comosone II
	Comosone II (化合物4)，一种从姜黄(Curcuma zedoaria)分离的化合物，展现中度抗增殖活性。对于Ca Ski癌细胞，其IC50值为76 μg/mL，显示其对癌细胞生长的抑制作用。

天然产物

Combretastatin A4

Cat.No: T6212

Synonym: CA4,康普瑞汀,Z)-3,4,5,4',-四甲氧基-3'-羟基二苯乙烯,CRC 87-09

Target: Microtubule Associated

Cat.No: T2782

Synonym: (+)-3, 4-Didehydrocoronaridine,长春质碱,(+)-3,4-Didehydrocoronaridine

Target: Calcium Channel, AChR

Cat.No: T2S2215

Target: Apoptosis, Others, Akt

Cat.No: T4S2326

Synonym: 7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside

Target: ERK, p38 MAPK, NF-κB, JNK

Cat.No: T82692

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