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17

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T28352	PDE9-IN-(S)-C33 (S)-C33	PDE	Metabolism
	PDE9-IN-(S)-C33 ((S)-C33) 是一种有效的选择性 PDE9 抑制剂 (IC50 = 11 nM)。 PDE9-IN-(S)-C33 可用于中枢神经系统疾病和糖尿病的相关研究。
T14364	AZ-Dyrk1B-33 3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) 是高选择性的Dyrk1B 激酶抑制剂，其IC50=7 nM。
T81585	Oxyntomodulin (human, mouse, rat) Proglucagon (33-69)
	Oxyntomodulin (human, mouse, rat) (Proglucagon (33-69)) 是由胰高血糖素前体产生，融合了完整胰高血糖素序列和C端八肽，含37个氨基酸。
TP2134	c-JUN peptide
	Peptide comprising residues 33 - 57 of the JNK binding (δ) domain of human c-Jun. Disrupts JNK/c-Jun interaction leading to inhibition of serum-induced c-Jun phosphorylation, up-regulation of p21cip/waf and modulation of inflammatory gene expression. Spec
T37206	CCK (27-33) (non-sulfated)
	CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in m...
T83741	S7 TFA Leu-Ser-Leu-Iso-Thr-Arg-Leu-OH
	S7是一种IL-6受体的肽类拮抗剂，能够浓度依赖性地抑制IL-6与IL-6受体的结合。在C-33 A宫颈癌细胞和RPMI-8226 B细胞淋巴细胞中，S7 (50 µM) 能抑制IL-6诱导的VEGF水平增加。在每两天给药一次，剂量为50 mg/kg的条件下，S7能减少IL-6过表达的C-33 A宫颈癌小鼠异种移植模型中的肿瘤体积。当S7与半胱氨酸结合，并连接到包裹多柔比星的脂质纳米粒子(LNPs)表面时，能增强LNPs对胶质瘤的靶向性，并在U251胶质母细胞瘤小鼠异种移植模型中提高生存率。
T83757	RG33 TFA
	RG33是一种33个氨基酸的合成肽，与apolipoprotein A1 (ApoA1)的C-末端域中两个Y类螺旋的209-219和220-241氨基酸相对应。它能溶解含有1,2-dimyristoyl-sn-glycero-3-PC (DMPC)的多层囊泡(MLVs)，形成重组HDL。与脂质结合的RG33在J774巨噬细胞中诱导胆固醇外流。RG33 (12 mg/kg)可降低胰岛素抵抗性小鼠的血糖水平。
T83485	[Thr28, Nle31]-Cholecystokinin (25-33), sulfated
	[Thr28, Nle31]-Cholecystokinin (25-33) 是一种具备CCK8所有生物活性的胆囊收缩素 (CCK) 类似物，表现出食欲抑制功效。它在胃肠道系统和中枢神经系统中担任激素和神经递质角色。此肽通过 Thr28 和 Nle31 的特殊替代，展现出在酸性条件下的高稳定性，并能抵抗空气氧化（防止蛋氨酸受损）。其主要构象特征为以Thr4为核心的γ转角和Gly5分隔的C末端螺旋片段。
T37052	Tetranactin
	Tetranactin is a macrotetrolide and a monovalent cation ionophore that has been found in S. aureus and has antibacterial, insecticidal, and mitogenic activities. It exhibits an equilibrium permeability ratio 1,000-fold greater for lithium than sodium or cesium ions accross bilayer membranes at low voltages. Tetranactin inhibits the growth of Gram-positive bacteria and C. miyabeanus and R. solani fungi when used at concentrations less than 0.9 μg/ml. Tetranactin (0.5-1.5 μg per insect) dose-depen...
T83911	CYY292
	CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂（IC50分别为5.35、4.6、28、28和78 nM）。该化合物对这些激酶的选择性高于FGFR4（IC50 > 1,000 nM），但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体（IGF-1R；IC50分别为67、33、36和75 nM），以及EGFR、布鲁顿酪氨酸激酶（BTK）、细胞周期依赖性激酶4（Cdk4）/cyclin D3和MET（IC50分别为128、198、214和396 nM）。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖（IC50分别为0.84、0.76、1.36和0.72 µM）。在0.3和0.5 µM的浓度下，它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292（30 mg/kg）在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。
T35686	3-Acetyl Betulinaldehyde
	3-Acetyl betulinaldehyde is a triterpene and derivative of the cholesterol biosynthesis inhibitor betulin that has been found inA. japonica.1It is an intermediate in the synthesis of 3-acetylbetulinic acid, as well as various lupine and germanicane triterpenes and saponins with anticancer activity.2 1.Tung, N.H., Kwon, H.-J., Kim, J.-H., et al.An anti-influenza component of the bark of Alnus japonicaArch. Pharm. Res.33(3)363-367(2010) 2.Thibeault, D., Gauthier, C., Legault, J., et al.Synthesis a...
T35742	IKD-8344
	IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties.1,2,3 It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg/ml) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.2,3 It is active against T. spiralis in vit...
T37963	Methylchloroisothiazolinone/Methylisothiazolinone Mixture
	Methylchloroisothiazolinone/methylisothiazolinone mixture (MCIT/MIT) is a mixture of isothiazolinone-derived biocides.1,2It is effective against Gram-positive and Gram-negative bacteria with MIC values of 0.0002, 0.0002, 0.00005, and 0.00005% (w/w) forS. aureus,P. aeruginosa,A. niger, andC. albicans, respectively.2MCIT/MIT can elicit contact sensitization.3Formulations containing MCIT/MIT have been used for controlling microbial growth in industrial and household products. 1.Frenzel, E., Schmidt...
T37536	Carbazomycin A
	Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg/ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg/ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg/ml, respectively).2 1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermenta...
T14072	A-443654	ERK; VEGFR; GSK-3; FLT; Casein Kinase; MAPK; Akt; PKA; Chk; CDK; Src; PKC; S6 Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	A-443654 是 pan-Akt 抑制剂，对Akt1，Akt2，和Akt3具有同等效力的抑制作用，Ki=均为 160 pM。
T36521	Alaproclate (hydrochloride)
	Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentratio...
T10311	Amphotericin X1 两性霉素 X1	Others	Others
	Amphotericin X1 is a derivative of Amphotericin B with good antifungal activity. Amphotericin X1 inhibits Candida albicans 33/079, Cryptococcus neoformans 451, C.parapsilosis 937A, Aspergillus niger 57A and A.fumigatus (MICs: 1 μg/mL, 1 μg/mL, 8 μg/mL, 2

化合物

PDE9-IN-(S)-C33

Cat.No: T28352

Synonym: (S)-C33

Target: PDE

Cat.No: T14364

Synonym: 3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine

Target: DYRK

Oxyntomodulin (human, mouse, rat)

Cat.No: T81585

Synonym: Proglucagon (33-69)

Cat.No: TP2134

CCK (27-33) (non-sulfated)

Cat.No: T37206

Cat.No: T83741

Synonym: Leu-Ser-Leu-Iso-Thr-Arg-Leu-OH

Cat.No: T83757

[Thr28, Nle31]-Cholecystokinin (25-33), sulfated

Cat.No: T83485

Cat.No: T37052

Cat.No: T83911

3-Acetyl Betulinaldehyde

Cat.No: T35686

Cat.No: T35742

Methylchloroisothiazolinone/Methylisothiazolinone Mixture

Cat.No: T37963

Cat.No: T37536

Cat.No: T14072

Target: ERK, VEGFR, GSK-3, FLT, Casein Kinase, MAPK, Akt, PKA, Chk, CDK, Src, PKC, S6 Kinase

Alaproclate (hydrochloride)

Cat.No: T36521

Amphotericin X1

Cat.No: T10311

Synonym: 两性霉素 X1

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
TN6354	Trigochinin C
	Trigochinin C 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN6354，CAS号为 1210299-33-4。
T75570	Justicidin C
	Justicidin C 是一种抗病毒木脂素，对水泡性口炎病毒展现了较强的抗病毒活性，同时在兔肺细胞(RL-33)中显示较低的细胞毒性。
TN2782	2''-O-Acetylsprengerinin C	Others	Others
	2''-O-Acetylsprengerinin C 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN2782，CAS号为 1220707-33-4。
T35910	Petromurin C
	Petromurin C is a bis-indolyl benzenoid fungal metabolite originally isolated from the ascostromata of P. muricatus. It is cytotoxic to NS-1 mouse myeloma cells (IC50 = 33 μg/ml) and has activity against T. foetus in vitro (IC50 = 100 μg/ml).
T80950	Tricetin 7-O-glucoside
	Tricetin 7-O-glucoside (compound 33)为一种黄酮类单-O-糖苷。

天然产物

Cat.No: TN6354

Cat.No: T75570

2''-O-Acetylsprengerinin C

Cat.No: TN2782

Target: Others

Cat.No: T35910

Tricetin 7-O-glucoside

Cat.No: T80950

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