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Search Results for " at 101 "

53

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。
T5170	KHS101 hydrochloride 盐酸KHS101	FGFR; Microtubule Associated	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	KHS101 hydrochloride 能够选择性的诱导神经元分化表型，能够与转化酸性含螺旋蛋白发生相互作用。
T6761	Ossirene AS101	IL Receptor; Caspase; Interleukin	Apoptosis; Immunology/Inflammation; Proteases/Proteasome
	Ossirene (AS101) 是一种免疫调节抑制剂，是一种新型 IL-1beta 转化酶抑制剂，可用于自身免疫性疾病和某些恶性肿瘤。它通过抑制IL-10消除 STAT3 的磷酸化，有效抑制Caspase-1。
T21919	UCF 101	Apoptosis	Apoptosis
	UCF 101 是竞争性的促凋亡蛋白酶Omi/HtrA2选择性抑制剂。它对 MI/R 损伤具有明显的心脏保护作用，还具有一定的神经保护作用。它在 543 nm 处具有天然的红色荧光，可用于监视其进入哺乳动物细胞的能力。
T5403	ULK-101	Autophagy	Autophagy
	ULK-101 是一种选择性 ULK1抑制剂，可抑制自噬，对 ULK1和 ULK2 的 IC50值分别为 8.3 nM 和 30 nM。
T14081	Enmetazobactam AAI101	Antibacterial	Microbiology/Virology
	Enmetazobactam (AAI101) 是一种广谱β-lactamase 抑制剂，有抗耐药革兰氏阴性细菌。
T3476	JI-101 CGI-1842,JI 101	VEGFR; PDGFR; Ephrin Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	JI-101 (CGI-1842) 是一种有口服活性的多靶点激酶抑制剂，能够抑制VEGFR2，PDGFRβ和EphB4，具有抗癌作用。
T14989	CMPD101	ROCK; GRK; PKC	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells
	CMPD101 是膜透性的 GRK2/3高选择性小分子抑制剂，IC50分别为 18 nM 和 5.4 nM。它针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM，可研究心衰疾病。
T4968	KHS 101	Microtubule Associated	Cytoskeletal Signaling
	KHS 101 是一种新型转化酸性卷曲螺旋蛋白 3 (TACC3) 的抑制剂。它是神经元分化的选择性诱导剂。
T4138	UCPH-101 UCPH 101	transporter	Metabolism
	UCPH-101 是一种兴奋性氨基酸转运子亚型 1 (EAAT1) 的抑制剂(IC50:0.66 μM)。
T5347	CXD101 CXD-101	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	CXD101 是一种选择性和具有口服活性的 I 类HDAC 抑制剂，有抗肿瘤活性，对HDAC1、HDAC2和HDAC3的IC50分别为 63、570 和 550 nM。
T19062	Sulforhodamine 101 磺基罗丹明101,磺基罗丹明 101,SR101	Others	Others
	Sulforhodamine 101 (SR101) 是一种两性罗丹明红色荧光染料 (excitation/emission: 586/605 nm)，常用于神经元形态的研究，并作为星形胶质细胞的细胞类型选择性荧光标记物，在体内和切片制备中都有应用。
T2451	GlyH-101 GlyH 101	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	GlyH-101 是一种可渗透入细胞的 CFTR 阻断剂，Ki 为1.4 uM。
T13247	UK-101 UK101,UK 101	Proteasome	Proteases/Proteasome; Ubiquitination
	UK-101 是一种强效且具有选择性的免疫蛋白酶体 LMP2 的抑制剂，对 β1i (LMP2) 、 β1c (LMP2) 和 β5 (LMP2) 具有抑制作用，IC50 为 104nM 、15 μM 和 1 μM 。UK-101 对 β1i 的亲和力比β1c 和 β5 亚基分布高的 144 倍和 10 倍。UK-101 可诱导细胞凋亡且可用于研究前列腺癌的相关疾病。
T8651	CAL-101 (S)-2-(1-(9H-Purin-6-ylamino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one,GS-1101,Idelalisib	PI3K	PI3K/Akt/mTOR signaling
	CAL-101 (Idelalisib) 是 p110δ 的选择性抑制剂（IC50：2.5 nM；在无细胞试验中）；显示对 p110δ 的选择性比 p110α/β/γ 高 40 到 300 倍，对 p110δ 的选择性比 C2β、hVPS34、DNA-PK 和 mTOR 高 400 到 4000 倍。
TP2105L	UFP-101 acetate UFP-101 acetate(849024-68-6 free base)	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	UFP-101 acetate 是一种特异性和竞争性 NOP 受体拮抗剂 (pKi = 10.24)，其特异性是 δ、μ 和 κ 阿片受体的 3000 倍以上。
T26690	AVN-101	5-HT Receptor; Adrenergic Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	AVN-101 是一种非常有效的 5-HT7 受体拮抗剂 (Ki = 153 pM)。 AVN-101 还对组胺 H1 (Ki = 0.58 nM) 和肾上腺素能 α2A、α2B 和 α2C (Ki = 0.41-3.6 nM) 受体表现出相当高的亲和力。 AVN-101在中枢神经系统疾病动物模型中显示出良好的口服生物利用度和促进脑血屏障通透性、低毒性和合理的疗效。
T13362	XY101	ROR	Metabolism
	XY101 是一种有效选择性的、代谢稳定的口服 RORγ 反向激动剂，IC50 为 30 nM，Kd 为 380 nM。
T8550	NDMC101	Others; NF-κB; Proteasome	NF-κB; Others; Proteases/Proteasome; Ubiquitination
	NDMC101 是有效的破骨细胞形成抑制剂，通过下调 NFATc1 调控基因表达抑制破骨细胞分化。它与 DPP4底物相似，通过抑制DPP4抑制早期 T 细胞激活。它能够用于骨疾病的研究，如类风湿关节炎、滑膜炎等。
T3108	CUDC-101 CUDC 101,CUDC101	EGFR; HER; HDAC	Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	CUDC-101 是一种高效的EGFR、HDAC 和HER2抑制剂，对应的IC50值分别为 2.4、4.4 和 15.7 nM。
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。
T39347	RG-101
	RG-101 is a hepatocyte-targeted N-acetylgalactosamine conjugated oligonucleotide that functions as an antagonist for miR-122, an essential host factor in the replication of the hepatitis C virus (HCV).
T68187	NIP-101
	NIP-101 is a potent calcium antagonist.
T81294	Retrocyclin-101 RC-101
	Retrocyclin-101 是一款具有抗菌和抗病毒特性的肽类化合物。
T72056	KYN-101
	KYN-101是一种高效、选择性的芳香烃受体(AHR)合成拮抗剂,在人HepG2 DRE 荧光素酶报告基因检测中IC50为22 nM,在小鼠Hepa1 Cyp-luc 检测中IC50为23 nM。KYN-101逆转IDO/TDO 介导的肿瘤进展,提高PD-1阻断B16 IDO 荷瘤小鼠和表达内源性高水平IDO 的CT26结直肠癌模型的疗效。
T70902	AQ-101
	AQ-101 is a inhibitor of MDM2, which induces MDM2 protein degradation through a self-ubiquitination and proteasome-mediated mechanism.
T68796	Thr101
	Thr101, also known as NOX Inhibitor VII, is a dose-dependent inhibitor of HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9. Thr101 is also a NOX inhibitor.
T70144	ORP-101
	ORP-101 is a new chemical entity designed with intent to create a large stable molecule and to confer partial μ agonist and full κ-antagonist receptor pharmacology.
T63269	Antibacterial agent 101
	Antibacterial agent 101 表现出抗细菌和抗真菌作用(MIC=4-32 μg/mL)。
T70509	INU-101
	INU-101 is an 11β-HSD1 inhibitor. In KKAy mice, ob/ob mice, and ZDF rats, oral administration of INU-101 led to enhanced insulin sensitivity and the lowering of the fasting level of glucose in the blood. INU-101 therefore shows promise as a potential treatment for type 2 diabetes and metabolic syndrome.
T70845	FOBISIN101
	FOBISIN101 is a novel inhibitor of all 14-3-3 isoforms in 14-3-3 PPIs.
T75895	UFP-101 TFA
	UFP-101 TFA 是一种强效、选择性和竞争性的 NOP 受体拮抗剂，pKi 为 10.24。UFP-101 TFA 对 δ、μ 和 κ 类阿片受体的选择性大于 3000 倍。UFP-101 TFA 具有抗抑郁药样作用。
T83685	UFP101 TFA
	UFP101是一种合成肽类物质，作为nociceptin受体的拮抗剂（Ki为0.06 nM，测试于表达人类受体的CHO细胞中）。它对nociceptin受体的选择性高于κ-opioid受体（Ki为204 nM，测试于表达大鼠受体的CHO细胞中）。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS（EC50为1.86 nM）。通过脑室内给药，UFP101（10 nmol/每只动物）能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中，UFP101（0.003、0.03及0.3 mg/kg）能提高生存率。
T83095	Anticancer agent 101
	Anticanceragent 101，一种丁卡因衍生物，展现出抗癌活性。
T78871	PLM-101
	PLM-101是一种口服抗癌剂，针对FLT3和RET具有选择性抑制作用，有效抑制急性髓系白血病（AML）细胞。通过抑制RET，PLM-101促使FLT3的自噬降解，并且通过抑制PI3K和Ras/ERK信号通路来发挥其抗白血病的活性。在小鼠MV4-11侧翼异种移植模型中，PLM-101以口服剂量3及10 mg/kg显示出抗肿瘤效果，并且在同种异种移植小鼠模型中，剂量为40 mg/kg（口服）亦展现出明显的抗肿瘤功效。
T67948	OY-101
	OY-101为口服生效的特异性P-glycoprotein(P-gp)抑制剂。该化合物可增强耐药性肿瘤的敏感性，并有效逆转多药耐药现象。相较于Tetrandrine，OY-101在水溶性、细胞毒性以及逆转活性方面均表现出改进。
T69358	S101
	S101 is an inhibitor of proliferating T-cells, rescuing mice from superantigen-induced shock.
T81490	PHI-101
	PHI-101是口服FLT3抑制剂，在克服多耐药突变方面表现出高效。该化合物对FLT3的ITD或TKD单突变体表现出显著抑制作用，同时也能抑制包括双重（ITD/D835Y或ITD/F691L）和三重（ITD/D835Y/F691L）耐药突变。PHI-101在治疗复发或难治性急性髓系白血病（AML）的研究中显示出应用潜力。
T69732	LEI 101 hydrochloride
	LEI 101 hydrochloride is potent and selective CB2 partial agonist.
T64692	AMY-101 acetate
	Complement component C3 plays a particularly versatile role in this process by keeping the cascade alert, acting as a point of convergence of activation pathways, fueling the amplification of the complement response, exerting direct effector functions, and helping to coordinate downstream immune responses[3]. In C3-/- mice alcohol-induced liver steatosis is absent or strongly reduced after chronic or acute alcohol exposure. This suggests that the complement system and its component C3 contribute...
T36273	VH 101 phenol-alkylC4-amine VH 101 phenol-alkylC4-amine
	Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC4 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.
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.
T79249	Antitumor agent-101	Histone Methyltransferase	Chromatin/Epigenetic
	Antitumor agent-101是一种针对赖氨酸甲基转移酶G9a/GLP的选择性共价抑制剂，其对G9a的IC50为8.5 nM，对GLP为5.5 nM。在PANC-1异种移植模型中，Antitumor agent-101展现了其抗肿瘤活性。
T36274	VH 101 phenol-alkylC6-amine VH 101 phenol-alkylC6-amine
	Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC6 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.
T71231	VMY-1-101
	VMY-1-101 is a synthesized fluorescent CDK inhibitor. VMY-1-101 demonstrates potent CDK inhibitory activity, enhanced induction of G2/M arrest and modest apoptosis as compared to purvalanol B.
T71593	AVN-101 free base
	AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a multi-target drug candidate for the treatment of CNS disorders.
T68934	VT101 free base
	VT101 is a TEAD Auto-palmitoylation inhibitor that Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT101 inhibited the firefly luciferase reporter dose-dependently and had no 204 effect on the Renilla luciferase reporter.
T68973	EVT-101 free base
	EVT-101, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist.
T80521	Caveolin-1 (82-101) amide (human, mouse, rat) Caveolin-1 scaffolding domain peptide	c-Met/HGFR	Tyrosine Kinase/Adaptors
	Caveolin-1 (82-101) amide (human, mouse, rat) (Caveolin-1 scaffolding domain peptide) 是抑制酪氨酸激酶的肽，可逆转多器官衰老相关的有害变化。
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。

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

KHS101 hydrochloride

Cat.No: T5170

Synonym: 盐酸KHS101

Target: FGFR, Microtubule Associated

Cat.No: T6761

Synonym: AS101

Target: IL Receptor, Caspase, Interleukin

Cat.No: T21919

Target: Apoptosis

Cat.No: T5403

Target: Autophagy

Cat.No: T14081

Synonym: AAI101

Target: Antibacterial

Cat.No: T3476

Synonym: CGI-1842,JI 101

Target: VEGFR, PDGFR, Ephrin Receptor

Cat.No: T14989

Target: ROCK, GRK, PKC

Cat.No: T4968

Target: Microtubule Associated

Cat.No: T4138

Synonym: UCPH 101

Target: transporter

Cat.No: T5347

Synonym: CXD-101

Target: HDAC

Sulforhodamine 101

Cat.No: T19062

Synonym: 磺基罗丹明101,磺基罗丹明 101,SR101

Target: Others

Cat.No: T2451

Synonym: GlyH 101

Target: CFTR, Autophagy

Cat.No: T13247

Synonym: UK101,UK 101

Target: Proteasome

Cat.No: T8651

Synonym: (S)-2-(1-(9H-Purin-6-ylamino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one,GS-1101,Idelalisib

Target: PI3K

UFP-101 acetate

Cat.No: TP2105L

Synonym: UFP-101 acetate(849024-68-6 free base)

Target: Opioid Receptor

Cat.No: T26690

Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor

Cat.No: T13362

Target: ROR

Cat.No: T8550

Target: Others, NF-κB, Proteasome

Cat.No: T3108

Synonym: CUDC 101,CUDC101

Target: EGFR, HER, HDAC

PKUMDL-LC-101-D04

Cat.No: T36935

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

Target: GPX

Cat.No: T39347

Cat.No: T68187

Retrocyclin-101

Cat.No: T81294

Synonym: RC-101

Cat.No: T72056

Cat.No: T70902

Cat.No: T68796

Cat.No: T70144

Antibacterial agent 101

Cat.No: T63269

Cat.No: T70509

Cat.No: T70845

Cat.No: T75895

Cat.No: T83685

Anticancer agent 101

Cat.No: T83095

Cat.No: T78871

Cat.No: T67948

Cat.No: T69358

Cat.No: T81490

LEI 101 hydrochloride

Cat.No: T69732

AMY-101 acetate

Cat.No: T64692

VH 101 phenol-alkylC4-amine

Cat.No: T36273

Synonym: VH 101 phenol-alkylC4-amine

Cat.No: T71290

Antitumor agent-101

Cat.No: T79249

Target: Histone Methyltransferase

VH 101 phenol-alkylC6-amine

Cat.No: T36274

Synonym: VH 101 phenol-alkylC6-amine

Cat.No: T71231

AVN-101 free base

Cat.No: T71593

VT101 free base

Cat.No: T68934

EVT-101 free base

Cat.No: T68973

Caveolin-1 (82-101) amide (human, mouse, rat)

Cat.No: T80521

Synonym: Caveolin-1 scaffolding domain peptide

Target: c-Met/HGFR

Cat.No: T26686

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

Target: NMDAR

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

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