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19

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T11279 FGFR1/DDR2 inhibitor 1

Discoidin Domain Receptor (DDR); FGFR; Others Angiogenesis; Others; Tyrosine Kinase/Adaptors
FGFR1/DDR2 inhibitor 1 是一种具有口服活性的成纤维细胞生长因子受体 1 和盘状蛋白域受体 2 的抑制剂,能够抑制 FGFR1 (IC50:31.1 nM) 和 DDR2 (IC50:3.2 nM),具有抗肿瘤作用。
T11847L Liarozole

R75251 dihydrochloride,利阿唑

P450; Retinoid Receptor Metabolism
Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物,是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA),具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM),导致组织维甲酸水平增加。
T7417 Avatrombopag

YM477,AKR-501,1-[3-氯-5-[[[4-(4-氯-2-噻吩基)-5-(4-环己基-1-哌嗪基)-2-噻唑基]氨基]羰基]-2-吡啶基]-4-哌啶羧酸,E5501

Thrombin; Thrombopoietin Receptor Immunology/Inflammation; Proteases/Proteasome
Avatrombopag (YM477) 是一种新型口服血小板生成素 (TPO) 受体激动剂,可激活 TPO 受体并增加巨核细胞增殖/分化和血小板生成。
T80378 Tilapia piscidin 3

Tilapia piscidin 3 是具抗菌谱广的肽类化合物,有效对抗多种革兰氏阳性菌与阴性菌,其对 V. vulnificus 204、V. alginolyticus、S. agalactiae 819、E. faecalis BCRC 10066、S. agalactiae BCRC 10787 的最小抑菌浓度 (MIC) 分别为 2.44、2.44、9.78、19.55、0.61 μg/mL。同時,Tilapia piscidin 3 对鱼红细胞显示出溶血性。
TP1521 Piscidin-1 (22-42) (TFA)

Piscidin-1 (22-42) (TFA) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides).
T80286 TP4 (Nile tilapia piscidin)

Necroptosis Apoptosis
TP4(Nile tilapia piscidin)是一种piscidin样的抗菌肽,其口服活性被证实。此化合物对多种革兰氏阳性及阴性菌株均有效(MIC: 0.03-10 μg/mL),并展现了溶血性。TP4还能增强免疫响应、提升抗氧化能力和改善肠道健康,助于防御细菌感染。除此之外,TP4显示抗肿瘤效果,并可通过激发癌细胞线粒体功能障碍导致坏死(necrosis)。
TP1475 Piscidin-1 (22-42)

Piscidin-1 (22-42) is a highly potent, multi-functional Antimicrobial Peptide (AMP) produced by Orange-spotted grouper (Epinephelus coioides).
T30152 Ascididemin

Leptoclinidinone,CRL 8274,NSC-675670,NSC 675670,NSC675670

Ascididemin can be regarded as a fused phenanthroline with quinoline.
T11151 Ecteinascidin-Analog-1

Others Others
Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities. Ecteinascidin-Analog-1 is a useful intermediate for chemical sythesis of Ecteinascidin analogues.
T124820 Piscidic acid

Piscidic acid 是一种有用的有机化合物,可用于生命科学领域的相关研究,其产品编号为 T124820。
T60248 4-Aminobenzamidine dihydrochloride

p-Aminobenzamidine dihydrochloride

Serine Protease Proteases/Proteasome
4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) 是一种强胰蛋白酶 (trypsin)抑制剂,也是一种相对较弱的尿激酶型纤溶酶原激活剂 (uPA) 抑制剂 (Ki=82 μM)。4-Aminobenzamidine 可抑制 SCID 小鼠体内前列腺肿瘤的生长。
T78305 Briquilimab

JSP-191

Briquilimab (JSP-191) 是针对 CD117 (c-Kit) 的无毒人源化单克隆抗体,用于消耗造血干细胞 (HSC)。它被应用于重度联合免疫缺陷 (SCID) 治疗中,以清空宿主骨髓生态位,为供体造血干细胞移植及免疫重建创造条件。
T36674 DMU-212

Apoptosis; ERK Apoptosis; MAPK
DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物,表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T68346 KRN383

KRN383 also inhibited the proliferation of the ITD-positive cell lines with IC(50) values of < or =2.9 nM. A single oral administration of 80 mg/kg of KRN383 eradicated ITD-positive xenograft tumors in nude mice and prolonged the survival of SCID mice carrying ITD-positive AML cells. The effectiveness of a single oral dose of KRN383 suggests that it has the potential to be used in a wide variety of clinical regimens, including multicycle and combination therapies.
T78805 AD4

Others Others
AD4是一种青蒿素衍生的PROTACs,具有针对PCLAF的高效降解能力,在RS4;11细胞中的IC50仅为0.6 nM。通过激活p21/Rb轴,AD4展现出明显的抗肿瘤活性。此外,AD4在NOD/SCID小鼠移植的RS4;11模型中显著延长了生存时间,证实了其体内疗效。
T71252 PC-046

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with di...
T69822 Ritlecitinib tosylate

Ritlecitinib, also known as PF-06651600, is a potent and selective JAK3 inhibitor. PF-06651600 is a potent and low clearance compound with demonstrated in vivo efficacy. The favorable efficacy and safety profile of this JAK3-specific inhibitor PF-06651600 led to its evaluation in several human clinical studies. JAK3 was among the first of the JAKs targeted for therapeutic intervention due to the strong validation provided by human SCID patients displaying JAK3 deficiencies.
T69821 AMP423

AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226/S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T/C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.
T35675 SW203668 (trifluoroacetate salt)

SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production...

化合物

FGFR1/DDR2 inhibitor 1
Cat.No: T11279
Synonym:
Target: Discoidin Domain Receptor (DDR), FGFR, Others
Liarozole
Cat.No: T11847L
Synonym: R75251 dihydrochloride,利阿唑
Target: P450, Retinoid Receptor
Avatrombopag
Cat.No: T7417
Synonym: YM477,AKR-501,1-[3-氯-5-[[[4-(4-氯-2-噻吩基)-5-(4-环己基-1-哌嗪基)-2-噻唑基]氨基]羰基]-2-吡啶基]-4-哌啶羧酸,E5501
Target: Thrombin, Thrombopoietin Receptor
Tilapia piscidin 3
Cat.No: T80378
Synonym:
Target:
Piscidin-1 (22-42) (TFA)
Cat.No: TP1521
Synonym:
Target:
TP4 (Nile tilapia piscidin)
Cat.No: T80286
Synonym:
Target: Necroptosis
Piscidin-1 (22-42)
Cat.No: TP1475
Synonym:
Target:
Ascididemin
Cat.No: T30152
Synonym: Leptoclinidinone,CRL 8274,NSC-675670,NSC 675670,NSC675670
Target:
Ecteinascidin-Analog-1
Cat.No: T11151
Synonym:
Target: Others
Piscidic acid
Cat.No: T124820
Synonym:
Target:
4-Aminobenzamidine dihydrochloride
Cat.No: T60248
Synonym: p-Aminobenzamidine dihydrochloride
Target: Serine Protease
Briquilimab
Cat.No: T78305
Synonym: JSP-191
Target:
DMU-212
Cat.No: T36674
Synonym:
Target: Apoptosis, ERK
KRN383
Cat.No: T68346
Synonym:
Target:
AD4
Cat.No: T78805
Synonym:
Target: Others
PC-046
Cat.No: T71252
Synonym:
Target:
Ritlecitinib tosylate
Cat.No: T69822
Synonym:
Target:
AMP423
Cat.No: T69821
Synonym:
Target:
SW203668 (trifluoroacetate salt)
Cat.No: T35675
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3932 Viscidulin I

Others Others
Viscidulin I 存在于黄芩中,是一种天然产物。
TN2302 Viscidulin III

Ganhuangenin

Glucosidase Metabolism
Viscidulin III (Ganhuangenin) 存在于黄芩中,可作为α-葡萄糖苷酶抑制剂。
TN4801 Piscidinol A

Others Others
Piscidinol A is toxic against the 4T1 and HEp2 cancer cell lines, the IC50 of 8.0 ± 0.03 and 8.4 ± 0.01 uM, respectively. It can inhibit NO production in mouse peritoneal macrophages with inhibitory ratios ranging from 39.8±7.7 to 68.2±4.5%.
TN5239 Viscidulin III tetraacetate

Others Others
Viscidulin III tetraacetate 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 TN5239,CAS号为 96684-81-0。
TN5238 Viscidulin II

IL Receptor; TNF Apoptosis; Immunology/Inflammation
Viscidulin II can be potential therapeutic agents against P. acnes-induced skin inflammation, it can significantly suppress P. acnes-induced IL-8 and IL-1β production in THP-1 cells, concomitant intradermal injection of viscidulin II with P. acnes can effectively attenuate P. acnes-induced ear swelling, and decrease the production of IL-6 and tumor necrosis factor-α in ear homogenates.
T11150 Ecteinascidin 770

Ecteinascidine 770,Et-770

Others Others
Ecteinascidin 770 (ET-770) inhibits U373MG cells and is a 1,2,3, 4-tetrahydroisoquinoline alkaloid with strong anticancer activity.IC50 is 4.83 nM.

天然产物

Viscidulin I
Cat.No: T3932
Synonym:
Target: Others
Viscidulin III
Cat.No: TN2302
Synonym: Ganhuangenin
Target: Glucosidase
Piscidinol A
Cat.No: TN4801
Synonym:
Target: Others
Viscidulin III tetraacetate
Cat.No: TN5239
Synonym:
Target: Others
Viscidulin II
Cat.No: TN5238
Synonym:
Target: IL Receptor, TNF
Ecteinascidin 770
Cat.No: T11150
Synonym: Ecteinascidine 770,Et-770
Target: Others
TargetMol Loading
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