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27

抑制剂 & 化合物

9

天然产物

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Cat. No. Product Name Target Signaling Pathways
T5821 BC-1215

Others; Ligand for E3 Ligase Others; PROTAC
BC-1215 是一种 F-box protein 3 抑制剂。它能够稳定 TRAF1-TRAF6 来抑制 Fbxo3-TRAF 激活途径。它与 ApaG 相互作用,阻碍来自人 PBMC 广谱 TH1 细胞因子的分泌。
T5622 BAY-218

AHR antagonist 1

AhR; Aryl Hydrocarbon Receptor Immunology/Inflammation; Metabolism
BAY-218 (AHR antagonist 1) 是一种芳基烃受体(AHR)拮抗剂,在人细胞系中的IC50值为 39.9 nM。
T8531 m-3M3FBS

2,4,6-三甲基-N-[3-(三氟甲基)苯基]苯磺酰胺

Apoptosis; Phospholipase Apoptosis; Metabolism
m-3M3FBS 是一种有效的磷脂酶C 激活剂,刺激人中性粒细胞产生超氧物,上调细胞内钙离子浓度,刺激多种细胞产生磷酸肌醇。它诱导单核细胞白血病细胞凋亡。
T63055 RIPK1-IN-9

RIP kinase Apoptosis; NF-κB
RIPK1-IN-9是是一种强效且具有选择性的 RIPK1抑制剂,是一种二氢萘酮化合物。RIPK1-IN-9对 U937细胞和 L929细胞具有抑制作用,IC50分别为2 nM 和1.3 nM。
T77697 BML-278

BML278,BML 278

Sirtuin; Histone Methyltransferase Chromatin/Epigenetic; DNA Damage/DNA Repair
BML-278 是一种 SIRT1 激活剂 ,EC150 值为 1 μM。BML-278 增加父本和母本原核中的 H3K9 甲基化并抑制 H3K9 乙酰化,可用于改善早期胚胎发育。BML-278 促使原代人间充质细胞的细胞周期停止在 G1/S 期,可用于延缓衰老。BML-278 减少 U937 细胞中的微管蛋白乙酰化,增加小鼠 C2C12 成肌细胞的线粒体密度。
T78156 MC4033

Apoptosis Apoptosis
MC4033是一种选择性的,可逆的KAT8赖氨酸乙酰转移酶抑制剂,IC50为12.1μM,具有抗癌活性,并能诱导凋亡(apoptosisautophagy)。
T4057 Hoechst 33258 trihydrochloride

Hoechst 33258,Pibenzimol,Bisbenzimide,H 33258 trihydrochloride,bisBenzimide H 33258 trihydrochloride,HOE 33258

Parasite Microbiology/Virology
Hoechst 33258 trihydrochloride (Bisbenzimide) 是一种能够用于 DNA 染色的荧光染料。
T63854 Cathepsin C-IN-3

Cathepsin C-IN-3 是组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 61.79 nM),也能抑制 THP-1 细胞 (IC50: 101.5 nM) 和 U937 细胞 (IC50: 86.5 nM)。
T26775 Bepafant

WEB-2170,WEB2170,STY 2108,STY-2108,WEB 2170

Bepafant is a platelet activating factor (PAF) antagonist. Bepafant may produce significant anti-inflammatory effects. Bepafant triggered apoptosis in NB4, KG1, and NB4-MR4 cells where PTEN was expressed, but not in THP1 and U937 cells where PTEN was abse
T10050 1alpha-Hydroxy VD4

1α-Hydroxy vitamin D4

Others Others
1alpha-Hydroxy VD4 can effectively induce the differentiation of monoblastic leukaemia U937, P39/TSU, and P31/FUJ cells.
T62499 RIPK1-IN-14

RIPK1-IN-14 (Compound 41) 是一种 RIPK1 的有效抑制剂 (IC50: 92 nM)。RIPK1-IN-14 在 U937 细胞的坏死性凋亡模型中具有明显的抗坏死性凋亡效果。
T62659 Cathepsin C-IN-4

Cathepsin C-IN-4 是一种组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 65.6 nM)。Cathepsin C-IN-4 对 THP-1 (IC50: 203.4 nM)和 U937 (IC50: 177.6 nM) 细胞具有抑制作用。
T36322 C8 D-threo Ceramide (d18:1/8:0)

C8 D-threo Ceramide (d18:1/8:0)

C8 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 17 μM) and induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 ceramide . C8 D-threo Ceramide is a substrate for E. coli diacylglycerol kinase. It activates ceramide-activated protein kinase (CAPK) in U937 cells. C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein r...
T36319 C6 L-erythro Ceramide (d18:1/6:0)

C6 L-erythro Ceramide (d18:1/6:0)

C6 L-erythro Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is metabolized by ceramide glucosyltransferase to form C6 L-erythro glucosylceramide. C6 L-erythro Ceramide is cytotoxic to U937 cells (IC50 = 18 μM).
T37907 DL 175

Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.
T36324 C8 L-threo Ceramide (d18:1/8:0)

C8 L-threo Ceramide (d18:1/8:0)

C8 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 10 μM) and, like C8 D-threo ceramide , induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 L-erythro ceramide . C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein release, with a 50% release dose (RD50) value of ~30 μg/ml.
T36943 Aminopeptidase N Inhibitor

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.
T36320 C6 L-threo Ceramide (d18:1/6:0)

C6 L-threo Ceramide (d18:1/6:0)

C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 L-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 L-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 L-threo Ceramide enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM.
T35929 O-Demethyl Apremilast

O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral admi...
T68667 Oxanosine

Oxanosine is an analog of guanosine that has been found in S. capreolus and has diverse biological activities, including antibacterial, antiviral, and anticancer properties. It is active against a variety of bacteria, including S. flexneri, P. mirabilis, and E. coli (MICs = 6.25, 12.5, 25 µg/ml, respectively, on peptone, but not nutrient, agar). Oxanosine inhibits replication of the HIV-1 strain IIIb in infected CEM and U937, but not H9, cells (EC50s = 7, 27, and >500 µg/ml, respectively). It al...
T37565 C6 D-threo Ceramide (d18:1/6:0)

C6 D-threo Ceramide (d18:1/6:0)

C6 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 D-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 D-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 D-threo Ceramide promotes survival of isolated rat spinal neurons when used at concentrations up to 2.5 μM but induces cell death at concentrations greater...
T60439 CAY10789

CAY10789 (化合物 6) 是有效的CysLT1R 拮抗剂 ,IC50值为2.80 μM。CAY10789 也是一种GPBAR1激动剂 ,EC50为3 μM。CAY10789 显著降低 U937 细胞对 HAEC 的粘附并降低 TNF-α 的表达。CAY10789 表现出有前途的代谢稳定性和出色的药代动力学。 CAY10789 可用于结肠炎、代谢综合征和其他 GPBAR1/CysLT1R 相关疾病的研究。
T35536 Tpl2 Kinase Inhibitor (hydrochloride)

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5...
T37684 CAY10412

CAY10412

Anandamide (arachidonoyl ethanolamide; AEA) is an endogenous lipid with cannabinergic activity; along with 2-arachidonoyl glycerol, it forms part of the endocannabinoid system. AEA undergoes reuptake into neurons by a facilitated process. Controversy exists as to whether there is a specific AEA transporter, or instead the uptake process is simply driven by hydrolysis of AEA by intracellular fatty acyl amide hydrolase (FAAH). CAY10412 is an analog of AEA that has no intrinsic binding affinity for...
T69200 CGP74514A

CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and...
T35775 HT-2 Toxin-13C22

HT-2 Toxin-13C22

HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human...
T35406 α-MSH TFA

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube fo...

化合物

BC-1215
Cat.No: T5821
Synonym:
Target: Others, Ligand for E3 Ligase
BAY-218
Cat.No: T5622
Synonym: AHR antagonist 1
Target: AhR, Aryl Hydrocarbon Receptor
m-3M3FBS
Cat.No: T8531
Synonym: 2,4,6-三甲基-N-[3-(三氟甲基)苯基]苯磺酰胺
Target: Apoptosis, Phospholipase
RIPK1-IN-9
Cat.No: T63055
Synonym:
Target: RIP kinase
BML-278
Cat.No: T77697
Synonym: BML278,BML 278
Target: Sirtuin, Histone Methyltransferase
MC4033
Cat.No: T78156
Synonym:
Target: Apoptosis
Hoechst 33258 trihydrochloride
Cat.No: T4057
Synonym: Hoechst 33258,Pibenzimol,Bisbenzimide,H 33258 trihydrochloride,bisBenzimide H 33258 trihydrochloride,HOE 33258
Target: Parasite
Cathepsin C-IN-3
Cat.No: T63854
Synonym:
Target:
Bepafant
Cat.No: T26775
Synonym: WEB-2170,WEB2170,STY 2108,STY-2108,WEB 2170
Target:
1alpha-Hydroxy VD4
Cat.No: T10050
Synonym: 1α-Hydroxy vitamin D4
Target: Others
RIPK1-IN-14
Cat.No: T62499
Synonym:
Target:
Cathepsin C-IN-4
Cat.No: T62659
Synonym:
Target:
C8 D-threo Ceramide (d18:1/8:0)
Cat.No: T36322
Synonym: C8 D-threo Ceramide (d18:1/8:0)
Target:
C6 L-erythro Ceramide (d18:1/6:0)
Cat.No: T36319
Synonym: C6 L-erythro Ceramide (d18:1/6:0)
Target:
DL 175
Cat.No: T37907
Synonym:
Target:
C8 L-threo Ceramide (d18:1/8:0)
Cat.No: T36324
Synonym: C8 L-threo Ceramide (d18:1/8:0)
Target:
Aminopeptidase N Inhibitor
Cat.No: T36943
Synonym:
Target:
C6 L-threo Ceramide (d18:1/6:0)
Cat.No: T36320
Synonym: C6 L-threo Ceramide (d18:1/6:0)
Target:
O-Demethyl Apremilast
Cat.No: T35929
Synonym:
Target:
Oxanosine
Cat.No: T68667
Synonym:
Target:
C6 D-threo Ceramide (d18:1/6:0)
Cat.No: T37565
Synonym: C6 D-threo Ceramide (d18:1/6:0)
Target:
CAY10789
Cat.No: T60439
Synonym:
Target:
Tpl2 Kinase Inhibitor (hydrochloride)
Cat.No: T35536
Synonym:
Target:
CAY10412
Cat.No: T37684
Synonym: CAY10412
Target:
CGP74514A
Cat.No: T69200
Synonym:
Target:
HT-2 Toxin-13C22
Cat.No: T35775
Synonym: HT-2 Toxin-13C22
Target:
α-MSH TFA
Cat.No: T35406
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2S1040 Jolkinolide B

ERK; IL Receptor; BCL; p38 MAPK; TNF; NF-κB; Akt; Caspase; PI3K; JAK; JNK; STAT; mTOR Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
Jolkinolide B 是一种从 Euphorbia fischeriana Steud 的根中分离出来的具有生物活性的二萜。 Jolkinolide B 诱导癌细胞凋亡。 Jolkinolide B 可用于预防和治疗骨溶解的研究。
TN2054 Periplocymarin

Calcium Channel Membrane transporter/Ion channel; Metabolism
Periplocymarin 是一种强心苷,从 Periploca sepium 和 Periploca graeca 中分离得到,具有抗癌潜力。
T5S1923 Schisandrin C

五味子丙素,Schizandrin-C,Wuweizisu-C

Apoptosis; Others; Virus Protease Apoptosis; Microbiology/Virology; Others
Schisandrin C (Wuweizisu-C) 是从五味子中分离得到的一种植物化学木脂素。它具有抗癌、抗炎和抗氧化等多种生物活性,可研究癌症、阿尔茨海默病、肝病。
T3229 Cytochalasin D

ATPase; p38 MAPK; Calcium Channel; Akt; PI3K Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling
Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
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。
TN1211 2-Hydroxy-3-methylanthraquinone

ERK; p38 MAPK; Caspase Apoptosis; MAPK; Proteases/Proteasome
2-Hydroxy-3-methylanthraquinone enhances apoptosis of U937 cells,in part,through activation of p-p38MAPK and downregulation of p-ERK1/2; triggers caspase-3 activation mediated apoptotic induction.
TN6198 Mahanine

Mahanine has effects on the activation of the apoptotic pathway in human leukemia U937 cells, causes the mitochondrial membranes to lose their permeability, resulting in caspase-3 activation and apoptosis. Mahanine can reverse an epigenetically silenced g
T14317 ar-Turmerone

(+)-ar-Turmerone

Others Others
ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.
T72152 Eicosapentaenoic Acid sodium

二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium

Eicosapentaenoic Acid (EPA) sodium 为口服活性 ω-3 长链多不饱和脂肪酸 (ω-3 LC-PUFAs)。其通过DNA去甲基化,促进肿瘤抑制基因CCAAT/增强子结合蛋白δ (C/EBPδ)的重新表达,并通过H-RAS内含子1 CpG岛的去甲基化,激活U937白血病细胞中RAS/ERK/C/EBPβ途径。此外,该化合物能够促进血管平滑肌细胞松弛和血管舒张。

天然产物

Jolkinolide B
Cat.No: T2S1040
Synonym:
Target: ERK, IL Receptor, BCL, p38 MAPK, TNF, NF-κB, Akt, Caspase, PI3K, JAK, JNK, STAT, mTOR
Periplocymarin
Cat.No: TN2054
Synonym:
Target: Calcium Channel
Schisandrin C
Cat.No: T5S1923
Synonym: 五味子丙素,Schizandrin-C,Wuweizisu-C
Target: Apoptosis, Others, Virus Protease
Cytochalasin D
Cat.No: T3229
Synonym:
Target: ATPase, p38 MAPK, Calcium Channel, Akt, PI3K
Crebanine
Cat.No: T2S2215
Synonym:
Target: Apoptosis, Others, Akt
2-Hydroxy-3-methylanthraquinone
Cat.No: TN1211
Synonym:
Target: ERK, p38 MAPK, Caspase
Mahanine
Cat.No: TN6198
Synonym:
Target:
ar-Turmerone
Cat.No: T14317
Synonym: (+)-ar-Turmerone
Target: Others
Eicosapentaenoic Acid sodium
Cat.No: T72152
Synonym: 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium
Target:
TargetMol Loading
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