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88

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9491	Pyraclostrobin	Antibacterial; Antifungal	Microbiology/Virology
	Pyraclostrobin 是一种球果苷杀菌剂，可诱导 3T3-L1 细胞内甘油三酯的积累，还可抑制真菌和哺乳动物细胞的线粒体复合物 III 。
T13173	TMPA	Others; AMPK	Chromatin/Epigenetic; Others; PI3K/Akt/mTOR signaling
	TMPA 是一种核受体 Nur77 和 LKB1 相互作用的拮抗剂。
T61054	Type II topoisomerase inhibitor 1
	Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂，IC50值为 1.7 nM，并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性，IC50值为 0.98 μM。
T72289	Type II TRK inhibitor 1	Trk receptor	Tyrosine Kinase/Adaptors
	Type II TRK inhibitor 1 是有效抑制多种TRK融合蛋白及野生型的TRK抑制剂。对携有CD74-TRKAG667C及ETV6-TRKCG696C融合蛋白的Ba/F3细胞表现出抗增殖活性，其IC50值分别为6 nM与1.7 nM。
T12493	PK68	Others; RIP kinase	Apoptosis; NF-κB; Others
	PK68 是 II 型受体相互作用激酶 1 (RIPK1, IC50 = 90 nM) 的有效特异性抑制剂。 PK68可用于治疗炎症性疾病和癌症转移的研究。
T9924	Obinutuzumab 奥滨尤妥珠单抗,Obinutuzumab/afutuzumab	Others	Others
	Obinutuzumab (Obinutuzumab/afutuzumab)/afutuzumab 是一种新型糖工程化 II 型 CD20单克隆抗体，用于研究非霍奇金淋巴瘤。
T9098	DMG-PEG 2000 DMG-PEG2000	Others	Others
	DMG-PEG 2000 (DMG-PEG2000) 可用于脂质纳米颗粒制备，用于口服质粒 DNA 的体内传递途径，提高纳米颗粒的黏液渗透性和传递效率。它也可用于 siRNA 转染的脂质体的制备，能够提高转染效率。
T20029	Buformin hydrochloride NSC528218,NSC-528218,盐酸丁双胍,NSC 528218	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	Buformin hydrochloride (NSC-528218) 是一种有效的 AMPK 激活剂，是一种双胍类的口服抗糖尿病药物。Buformin 延缓胃肠道对葡萄糖的吸收，增加胰岛素敏感性和葡萄糖对细胞的吸收，并抑制肝脏对葡萄糖的合成。Buformin 也具有抗癌活性，可用于各种癌症研究。
T1615	Irbesartan 厄贝沙坦,SR-47436,BMS-186295	Apoptosis; RAAS	Apoptosis; Endocrinology/Hormones
	Irbesartan (SR-47436) 是一种 1 型血管紧张素 II 受体拮抗剂，IC50为1.3 nM。
T1800	GW788388 GW 788388	ALK; TGF-beta/Smad	Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
	GW788388 是一种 ALK5抑制剂(IC50:18 nM)。它也抑制 TGF-β II 型受体和激活素 II 型受体的活性，但对 BMP II 型受体无影响。
TQ0061	CHZ868	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	CHZ868 是II型 JAK 抑制剂，具有潜在的抗肿瘤活性，可逆转 I 型 JAK 抑制剂的持续存在，可用于研究白血病。
T24612	Pentachloropseudilin PClP
	Pentachloropseudilin is a selective inhibitor of Myosin-1. In target cells, It acts by suppressing transforming growth factor-β activity by accelerating cell-surface type II TGF-β receptor turnover.
T15603	ITX5061 ITX-5061	HCV Protease; p38 MAPK	MAPK; Microbiology/Virology; Proteases/Proteasome
	ITX5061 是 p38 MAPK 的 II 型抑制剂和清道夫受体 B1（SRB1）拮抗剂，可用于研究丙型肝炎病毒感染。
T2123	LY2109761	Autophagy; TGF-beta/Smad	Autophagy; Stem Cells
	LY2109761 是一种新型选择性 TGF-β 受体 I/II 型 (TβRI/II) 双重抑制剂，Ki 分别为 38 nM 和 300 nM。
T4268	CHMFL-BMX-078	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	CHMFL-BMX-078 是一种高效的、选择性的 II 型不可逆 BMX 激酶抑制剂，其 IC50=11 nM。
T0158	Mitoxantrone dihydrochloride 米托蒽醌二盐酸盐,盐酸米托蒽醌,Mitoxantrone 2HCl,Mitoxantrone hydrochloride,NSC-301739,mitozantrone dihydrochloride	Topoisomerase; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair
	Mitoxantrone dihydrochloride (NSC-301739) 是一种拓扑异构酶 II 的抑制剂；也可抑制蛋白激酶C (PKC)，IC50值为8.5 μM。
T27643	Izonsteride LY-320236,LY320236,UNII-A5E8C36F34	Reductase	Endocrinology/Hormones; Metabolism
	Izonsteride (LY320236) 是一种选择性强效 5α 还原酶抑制剂，对酶的 I 型和 II 型同工酶具有双重作用。Izonsteride 可用于治疗肿瘤和泌尿生殖系统疾病，可用于研究前列腺癌。
T16333	NKY80 Adenylyl cyclase type V Inhibitor	Adenylyl cyclase	Neuroscience
	NKY80 调节心脏和肺组织中的腺苷酸环化酶催化活性。 NKY80 是腺苷酸环化酶 V 型亚型的非竞争性抑制剂（IC50 值：V、III 和 II 型分别为 8.3 µM、132 µM 和 1.7 mM）。
T10800	CHMFL-ABL-121	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	CHMFL-ABL-121 是一种 II 型 ABL 激酶高效抑制剂，抑制纯化的非活性 ABL wt 和 T315I 激酶蛋白的 IC50 值分别为 2 nM 和 0.2 nM。
T63544	RIPK3-IN-1
	RIPK3-IN-1 是一种 II 型 RIPK3DFG-out 位点抑制剂 (IC50: 9.1 nM)，能够抑制 RIPK1 (IC50: 5.5 μM) 和 RIPK2 (IC50>10 μM)。RIPK3-IN-1 是一种 c-Met 激酶抑制剂 (IC50: 1.1 μM)。
T2153	1-NM-PP1 PP1 Analog II,1 nM-PP1	Serine/threonin kinase; CDK; Src	Angiogenesis; Cell Cycle/Checkpoint; Metabolism; Tyrosine Kinase/Adaptors
	1-NM-PP1 (PP1 Analog II) 是一种有效的Src 家族激酶抑制剂，是一种细胞渗透性 PP1 类似物，对 v-Src-as1 与 c-Fyn-as1 的IC50值分别为 4.3 nM、3.2 nM。
T6866	AUZ 454 K03861	CDK	Cell Cycle/Checkpoint
	AUZ 454 (K03861) 是一种 II 型 CDK2 抑制剂，Kd 值是 8.2 nM。它对 CDK2(WT)、CDK2(C118L)、CDK2(A144C) 和 CDK2(C118L/A144C) 的 Kd 分别为 50 nM、18.6 nM、15.4 nM 和 9.7 nM。
T60085	MM3122 GTPL11533,MM-3122,Ac-GQFR-kbt	SARS-CoV	Microbiology/Virology
	MM3122 (MM-3122) 是一种选择性的 II 型跨膜丝氨酸蛋白酶 (TMPRSS2) 抑制剂，IC50为 0.34 nM。MM3122 可以有效阻断 TMPRSS2，从而抑制 SARS-CoV-2 和 MERS-CoV 进入人类细胞。
T12730	RIPK1-IN-4	RIP kinase	Apoptosis; NF-κB
	RIPK1-IN-4 是有效的 II 型激酶受体相互作用蛋白1 (RIP1) 激酶抑制剂，并且与 DL1-out 无活性形式的 RIP1 结合。RIPK1-IN-4抑制 RIP1 和 ADP-Glo 激酶，IC50 分别是 16 nM 和 10 nM。
T78169	Enpp-1-IN-16	PDE	Metabolism
	Enpp-1-IN-16 是一种靶向 ENPP1 的抑制剂，具有潜在的抗癌症活性。Enpp-1-IN-16 可用于研究胰岛素抵抗与II型糖尿病和软骨钙化病和骨关节炎类由 ENPP1介导的各类疾病。
T38683	SCD1 inhibitor-3 SCD1-IN-3,SCD1 inhibitor-3,SCD1 inhibitor 17a	Dehydrogenase	Metabolism
	SCD1 inhibitor-3 (ML-270) 是一种高效、口服的化合物，可以抑制SCD1，且安全性极高。 SCD1 inhibitor-3 显示出在代谢疾病(包括肥胖、二型糖尿病和血脂异常，以及痤疮和癌症等各种皮肤病)方面的巨大研究潜力。
T10799	CHMFL-ABL-039	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	CHMFL-ABL-039 是一种具有高效选择性的 Ⅱ 型野生型 ABL 激酶和耐药 V299L 突变型 BCR-ABL 激酶的抑制剂，IC50 分别为 7.9 nM、27.9 nM。CHMFL-ABL-039 可用于慢性粒细胞白血病 (CML) 的研究。
TP2158	TRV-120027 TFA TRV-120027 TFA (1234510-46-3 free base)	RAAS; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂，可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂，可与 ß-arrestins 结合，同时阻断 G 蛋白信号传导。它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌，并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。
T30534	BMS-639432
	BMS-639432 is a potent sodium-glucose cotransporter type II (SGLT2) inhibitor.
T68967	AFG206
	AFG206 is the novel first-generation type II" FLT3 inhibitor."
T12114	MSC1094308	p97	Ubiquitination
	MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase.
T27848	LP10 LP-10,LP 10
	LP10 is a reverse type I inhibitor of Mycobacterium tuberculosis CYP125A1 and a Potent type II inhibitor of Trypanosoma cruzi CYP51.
T28299	PAT-078 PAT078,PAT 078
	PAT-078 is an inhibitor of type II autotaxin.
T11391L	Gepotidacin GSK2140944	Others	Others
	Gepotidacin is a novel triazaacenaphthylene inhibitor of bacterial type II topoisomerase.
T28301	PAT-494 PAT 494,PAT494
	PAT-494 is an inhibitor of type II Autotaxin.
T69702	AFG210
	AFG210 is a novel first-generation “type II” FLT3 inhibitor.
T27598	Imigliptin Dihydrochloride Imigliptin
	Imigliptin Dihydrochloride, a selective dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type II diabetes.
T71354	AMG-222 tosylate
	AMG-222 tosylate is a DPP-IV inhibitor in clinical development for type II diabetes.
T24098	GP17 GP-17,GP 17
	GP17 is a type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α.
T24099	GP29 GP-29,GP 29
	GP29 is a Type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α.
T12396	PDGFRα kinase inhibitor 1	PDGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	PDGFRα kinase inhibitor 1 is a highly selective inhibitor of type II PDGFRα kinase (PDGFRα and PDGFRβ with IC50s of 132 nM and 6115 nM , respectively).
T13406L	Zabofloxacin hydrochloride DW-224a	Raf	MAPK
	Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.
T10647	c-Fms-IN-8	CSF-1R	Tyrosine Kinase/Adaptors
	c-Fms-IN-8 is a colony-stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor (IC50: 9.1 nM). It is compound 4a in the reference.
T13406	Zabofloxacin DW-224a Free base	Others	Others
	Zabofloxacin is a potent and seletive bacterial type II and IV topoisomerases inhibitor, and has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.
T68558	BML-288
	BML-288 is a phosphodiesterase Type II (PDE2) inhibitor that demonstrates no inhibition of 5-lipoxygenase (5-LO) or cyclooxygenase (COX-1).
T11559	HG-12-6	Others	Others
	HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 (IC50: 165 nM). HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation.
T61192	CBR-6672
	CBR-6672, a type II NADH dehydrogenase inhibitor, demonstrates potent antimycobacterial activity against mycobacterium tuberculosis (Mtb) with a minimum inhibitory concentration (MIC) of 0.14 μM [1].
T13125	TD-0212	Others	Others
	TD-0212 is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP).
T13125L	TD-0212 TFA	Others	Others
	TD-0212 TFA is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP).
T10801	CHMFL-ABL/KIT-155 CHMFL-ABL-KIT-155	c-Kit	Tyrosine Kinase/Adaptors
	CHMFL-ABL/KIT-155 is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s: 46 nM/75 nM). It arrests cell cycle progression and induces apoptosis.

化合物

Cat.No: T9491

Target: Antibacterial, Antifungal

Cat.No: T13173

Target: Others, AMPK

Type II topoisomerase inhibitor 1

Cat.No: T61054

Type II TRK inhibitor 1

Cat.No: T72289

Target: Trk receptor

Cat.No: T12493

Target: Others, RIP kinase

Cat.No: T9924

Synonym: 奥滨尤妥珠单抗,Obinutuzumab/afutuzumab

Target: Others

Cat.No: T9098

Synonym: DMG-PEG2000

Target: Others

Buformin hydrochloride

Cat.No: T20029

Synonym: NSC528218,NSC-528218,盐酸丁双胍,NSC 528218

Target: AMPK

Cat.No: T1615

Synonym: 厄贝沙坦,SR-47436,BMS-186295

Target: Apoptosis, RAAS

Cat.No: T1800

Synonym: GW 788388

Target: ALK, TGF-beta/Smad

Cat.No: TQ0061

Target: JAK

Pentachloropseudilin

Cat.No: T24612

Synonym: PClP

Cat.No: T15603

Synonym: ITX-5061

Target: HCV Protease, p38 MAPK

Cat.No: T2123

Target: Autophagy, TGF-beta/Smad

Cat.No: T4268

Target: BTK

Mitoxantrone dihydrochloride

Cat.No: T0158

Synonym: 米托蒽醌二盐酸盐,盐酸米托蒽醌,Mitoxantrone 2HCl,Mitoxantrone hydrochloride,NSC-301739,mitozantrone dihydrochloride

Target: Topoisomerase, PKC

Cat.No: T27643

Synonym: LY-320236,LY320236,UNII-A5E8C36F34

Target: Reductase

Cat.No: T16333

Synonym: Adenylyl cyclase type V Inhibitor

Target: Adenylyl cyclase

Cat.No: T10800

Target: Bcr-Abl

Cat.No: T63544

Cat.No: T2153

Synonym: PP1 Analog II,1 nM-PP1

Target: Serine/threonin kinase, CDK, Src

Cat.No: T6866

Synonym: K03861

Target: CDK

Cat.No: T60085

Synonym: GTPL11533,MM-3122,Ac-GQFR-kbt

Target: SARS-CoV

Cat.No: T12730

Target: RIP kinase

Cat.No: T78169

Target: PDE

SCD1 inhibitor-3

Cat.No: T38683

Synonym: SCD1-IN-3,SCD1 inhibitor-3,SCD1 inhibitor 17a

Target: Dehydrogenase

Cat.No: T10799

Target: Bcr-Abl

Cat.No: TP2158

Synonym: TRV-120027 TFA (1234510-46-3 free base)

Target: RAAS, Arrestin

Cat.No: T30534

Cat.No: T68967

Cat.No: T12114

Target: p97

Cat.No: T27848

Synonym: LP-10,LP 10

Cat.No: T28299

Synonym: PAT078,PAT 078

Cat.No: T11391L

Synonym: GSK2140944

Target: Others

Cat.No: T28301

Synonym: PAT 494,PAT494

Cat.No: T69702

Imigliptin Dihydrochloride

Cat.No: T27598

Synonym: Imigliptin

AMG-222 tosylate

Cat.No: T71354

Cat.No: T24098

Synonym: GP-17,GP 17

Cat.No: T24099

Synonym: GP-29,GP 29

PDGFRα kinase inhibitor 1

Cat.No: T12396

Target: PDGFR

Zabofloxacin hydrochloride

Cat.No: T13406L

Synonym: DW-224a

Target: Raf

Cat.No: T10647

Target: CSF-1R

Cat.No: T13406

Synonym: DW-224a Free base

Target: Others

Cat.No: T68558

Cat.No: T11559

Target: Others

Cat.No: T61192

Cat.No: T13125

Target: Others

Cat.No: T13125L

Target: Others

CHMFL-ABL/KIT-155

Cat.No: T10801

Synonym: CHMFL-ABL-KIT-155

Target: c-Kit

Cat. No.	Product Name	Target	Signaling Pathways
T3417	Amentoflavone Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin	Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal	Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
	Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物，有抗炎、抗氧化和神经保护等作用。
T3S1612	kuwanon G 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G	Phosphatase; Antibacterial; Bombesin Receptor; AChR; AChE; Glucosidase	GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
	Kuwanon G (Moracenin B) 是一种从桑树中得到的黄酮类蛙皮素受体拮抗剂，具有杀菌作用。
T60692	Masoprocol
	Masoprocol (meso-Nordihydroguaiaretic acid) 是口服有效的脂氧合酶 (lipoxygenase) 抑制剂。Masoprocol 具有出抗高血糖活性，可用于 II 型糖尿病的研究。 Masoprocol 可降低体内肝甘油三酯和葡萄糖浓度。

天然产物

Cat.No: T3417

Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal

Cat.No: T3S1612

Synonym: 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G

Target: Phosphatase, Antibacterial, Bombesin Receptor, AChR, AChE, Glucosidase

Cat.No: T60692

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