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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T22338 |
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
GDC046 |
Others; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells |
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046) 是一种具有口服活性的选择性TYK2抑制剂,对 TYK2、JAK1、JAK2 和 JAK3 的Ki 分别为 4.8、0.7、0.7 和 0.4 nM。 | |||
T21694 |
(R)-Lisofylline
(R)-Lisophylline |
STAT | JAK/STAT signaling; Stem Cells |
(R)-Lisofylline ((R)-Lisophylline) 是溶血磷脂酸酰基转移酶的抑制剂 (IC50 = 0.6 µM)。 (R)-Lisofylline 可中断 IL-12 信号介导的 STAT4 激活,可用于治疗 1 型糖尿病和自身免疫性疾病的研究。 | |||
T3533 |
Apilimod mesylate
阿吡莫德甲磺酸盐,STA 5326 mesylate |
IL Receptor; PI3K; Interleukin | Immunology/Inflammation; PI3K/Akt/mTOR signaling |
Apilimod mesylate (STA 5326 mesylate) 是一种 IL-12/IL-23 的有效抑制剂,抑制人和猴的 PBMC 细胞中的 IL-12的IC50值为 1 nM 和 2 nM。Apilimod 是高效的、选择性的PIKfyve 抑制剂。 | |||
T9913 |
Ustekinumab
|
Interleukin | Immunology/Inflammation |
Ustekinumab 是一种人源化靶向抗IL-12/IL-23的单克隆 IgG1κ 抗体。 | |||
T2018 |
Apilimod
阿匹莫德,阿吡莫德,STA 5326 |
IL Receptor; PI3K; Interleukin | Immunology/Inflammation; PI3K/Akt/mTOR signaling |
Apilimod (STA 5326) 是一种有效的、高度选择性的PIKfyve 抑制剂,是一种 IL-12/IL-23 的有效抑制剂,抑制人和猴的 PBMC 细胞中的 IL-12,IC50值为 1 nM 和 2 nM。 | |||
T28958 |
TG6-129
TG6 129 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
TG6-129 是有效的EP2受体选择性拮抗剂,可降低 butaprost 诱导的 P388D1 巨噬细胞中炎症因子的表达。 | |||
T14687 |
Deucravacitinib
BMS-986165 |
Tyrosine Kinases; JAK; IFNAR; Interleukin | Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Deucravacitinib (BMS-986165) 是一种高选择性、口服生物可利用的变构 TYK2 抑制剂,用于治疗自身免疫性疾病。它通过稳定调节 JH2 结构域来阻断受体介导的 Tyk2 激活,可抑制IL-12/23和 I 型IFN 途径。它选择性结合 TYK2 假激酶 (JH2) 结构域,IC50为1.0 nM。 | |||
T7649 |
Tyrphostin A1
AG9,(4-甲氧基苄烯)丙二腈,Tyrphostin 1 |
EGFR; Interleukin | Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Tyrphostin A1 (Tyrphostin 1) 对巨噬细胞培养中CD40L 刺激的IL-12产生和抗原诱导的Th1细胞生成具有抑制作用。 | |||
T2061 |
APY0201
|
PI3K; Interleukin | Immunology/Inflammation; PI3K/Akt/mTOR signaling |
APY0201 是PIKfyve 抑制剂,能够抑制 PtdIns3P 转化为PtdIns(3,5)P2 (IC50:5.2 nM),还能够抑制IL-12/IL-23产生。 | |||
T38294 |
4-Deoxypyridoxine hydrochloride
|
S1P Receptor | GPCR/G Protein |
4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解,与 S1P 一样,减少化学诱导的胰岛素瘤细胞系的细胞凋亡。 | |||
T76935 | Briakinumab | ||
Briakinumab (ABT-874) 是一种全人抗 IL-12/23p40单克隆抗体。Briakinumab 靶向并中和 IL-12和 IL-23。Briakinumab 可用于类风湿性关节炎、炎症性肠病和多发性硬化症的研究。 | |||
T26280 |
TL4-12
TL4 12 |
||
TL4-12 is a MAP4K2 (GCK) inhibitor that inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation in vitro. | |||
T70394 | Deucravacitinib HCl | ||
Deucravacitinib HCl is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM), and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional resp... | |||
T78175 |
JAK-IN-25
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK-IN-25(化合物19)是一种高效的JAK抑制剂,对TYK2、JAK1、JAK2和JAK3的IC50值分别为6 nM、21 nM、8 nM、1051 nM。该化合物还能抑制人全血中IL-12(HEB IL-12),IC50为28 nM,显示其在癌症研究中的潜在应用价值。 | |||
TP1978 |
11R-VIVIT
NFAT inhibitor, Cell Permeable |
||
NFAT inhibitor. Inhibits LPS or LPS plus IFN-γ-induced IL-12 p40, IL-12 p70, IL-23 and TNF secretion from bone marrow-derived macrophages (BMDMs). Also attenuates NO production and Nos2 mRNA expression in LPS-stimulated BMDMs. Improves symptoms in a mouse | |||
T40123 | BMS-986251 | ||
BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis. | |||
T74971 |
Diamino lipid DAL4
|
||
Diamino lipid DAL4 是一种新型脂质纳米颗粒 (LNPs),可包裹编码 IL-12、IL-27 和 GM-CSF 等细胞因子的 mRNA。Diamino lipid DAL4 能够传递细胞因子 mRNA 给肿瘤细胞,发挥抗肿瘤效力。 | |||
T83866 | LCC-12 formate | ||
LCC-12是一种铜(II)螯合剂,为二甲双胍的衍生物。作为单体,它能结合铜(II)并在20 µM的浓度下减少氢过氧化物依赖的NADH向NAD+的氧化。在10 µM的浓度下,LCC-12降低一次性人类细胞因子激活的单核衍生的巨噬细胞(MDMs)中IL-1β、IL-2、IL-6、IL-8和TNF-α的细胞因子水平,以及JAK2、STAT2和IL-1受体相关激酶4(IRAK4)的水平。此外,同样浓度的LCC-12减少了细胞因子激活的MDMs中CD80+和CD86+的数量。每日0.3 mg/kg的剂量可提高LPS或盲肠结扎穿孔模型小鼠的存活率。 | |||
T73034 |
NLRP3-IN-12
|
||
NLRP3-IN-12 是一种特异性的 NLRP3炎症小体抑制剂。NLRP3-IN-12 通过靶向 NLRP3蛋白抑制 IL-1β 的释放,IC50值为 0.45 μM。NLRP3-IN-12 可用于研究炎症性肠病。 | |||
T62451 |
TYK2-IN-12
|
||
TYK2-IN-12 (compound 30) 是一种选择性的、口服具有活力的 TYK2 (酪氨酸激酶 2) 抑制剂 (Ki: 0.51 nM)。TYK2-IN-12 对 IL-12 诱导的人和小鼠全血中 IFNγ 具有抑制作用,他们的 IC50 值分别为 2.7 和 7.0 μM。TYK2-IN-12 能够用于研究银屑病。 | |||
T76602 |
(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat)
|
||
(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) 作为一种CRF拮抗剂,能有效阻断IL-1a诱发的黄体生成素 (LH) 抑制作用。 | |||
TP1978L1 |
11R-VIVIT TFA (592517-80-1 Free base)
|
||
11R-VIVIT TFA (592517-80-1 Free base) 是一种 NFAT 抑制剂。 11R-VIVIT TFA 抑制 LPS 或 LPS 加 IFN-γ 诱导的骨髓源性巨噬细胞 (BMDM) 分泌 IL-12 p40、IL-12 p70、IL-23 和 TNF。 11R-VIVIT TFA 减弱 LPS 刺激的 BMDM 中 NO 的产生和 Nos2 mRNA 的表达。 11R-VIVIT TFA 改善结肠炎小鼠模型的症状。 11R-VIVIT TFA 表现出免疫抑制作用并提高小鼠移植物的存活率。 11R-VIVIT TFA 具有细胞渗透性。 | |||
T62803 | STAT3-IN-12 | ||
STAT3-IN-12 是一种 STAT3 的有效信号抑制剂,对 IL-6 诱导的 JAK/STAT3 信号通路的激活具有抑制作用。STAT3-IN-12 对癌细胞生长、迁移具有抑制作用,可阻滞细胞周期并诱导细胞凋亡。STAT3-IN-12 能够用于癌症的相关研究(如肝细胞癌 (HCC) 、食管癌)。 | |||
T78762 | SIKs-IN-1 | ||
SIKs-IN-1(compound 8h)为一种嘧啶-5-羧酰胺衍生物,并充当盐诱导激酶(SIKs)的抑制剂。该化合物通过抑制SIK活性,上调IL-10抗炎细胞因子,下调IL-12促炎细胞因子,调控M1/M2巨噬细胞的极化,并在DSS诱导的结肠炎模型中展现出明显的抗炎效果。 | |||
T81331 |
QL-1200186
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
QL-1200186为具备口服活性与选择性的TYK2抑制剂。经口服后,该药剂量依赖性抑制因interleukin-12刺激所诱导的interferon-γ产生,并在银屑病模型小鼠中显著改善皮肤病变状况。 | |||
T78508 |
Delmitide acetate
RDP-58 acetate |
IFNAR | Immunology/Inflammation |
Delmitide acetate (RDP58) 是一种 d-异构体十肽,具有抗炎活性和口服活性。该化合物能够抑制 TNF-α、IFN-γ 以及白细胞介素 (IL)-12 的生成,同时提高血红素加氧酶 1 的活性,可用于针对溃疡性结肠炎的研究。 | |||
T22172 |
YS-121
|
||
YS121 是微粒体前列腺素 E2 合酶-1 (mPGES-1;IC50=3.4 μM) 和 5-脂氧合酶 (5-LOX;IC50=6.5 μM) 的双重抑制剂。在 IL-1β 刺激的 A549 细胞中,YS121以剂量依赖性地方式减少 PGE2 的产生,EC50为 12 μM。 | |||
T37564 |
C4 Ceramide (d18:1/4:0)
C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0) |
||
C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7/Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing... | |||
T36998 |
7β,27-dihydroxy Cholesterol
7β,27-DHC,7β,27-dihydroxy Cholesterol |
||
7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated hum... | |||
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. | |||
T68485 | Apilimod HCl | ||
Apilimod dimesylate is a potent and selective PIKfyve inhibitor. It exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Apilimod dimesylate inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. It reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. It also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma ... | |||
T68321 |
AS1940477
|
||
AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent c... | |||
T64280 | ODN 2216 | ||
ODN 2216 是一种 TLR9 (toll-like receptor 9) 配体或激动剂,能够诱导产生大量的 IFN-α 和 IFN-β。ODN 2216 可以利用 pDC (浆细胞样 DC) 诱导 IFN-α,以及利用 DC (树突状细胞) 产生IL-12 (p40)。ODN 2216 能够间接的、在 IFN-α/β 介导下刺激外周血单核细胞 (PBMC) 产生 IFN-γ。ODN 2216 可以激活 NK 细胞,诱导 IFN-γ 产生 TCR 触发的 CD4+T 细胞。 | |||
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... | |||
T35927 |
C2 L-threo Ceramide (d18:1/2:0)
C2 L-threo Ceramide (d18:1/2:0) |
||
C2 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide . C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1... | |||
T23028 |
MRT67307 HCl (1190378-57-4 free base)
MRT67307 HCl |
Others | Others |
MRT67307 is an inhibitor for TBK1, IKKε , MARK1-4 and NUAK1 with IC50 value of 19, 160, 27-52 and 230nM , respectively [1]. It is an inhibitor for ULK1and ULK2 with IC50 value of 45 and 38nM, respectively [2]. Also, it is a salt inducible kinase (SIK) inhibitor with IC50 value of 250, 67 and 430nM for SIK1, SIK2 and SIK3, respectively.<br />SIKs prevent the formation of regulatory macrophages and their inhibition induces increasing in some markers of regulatory macrophages, such as IL-10 and oth... | |||
T36629 | Givinostat | ||
Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1... | |||
T35453 |
β-Defensin-4 (human) (trifluoroacetate salt)
|
||
β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and pro... | |||
T68306 |
INCB16562
|
||
INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of ... | |||
T36713 |
Streptochlorin
|
||
Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the productio... | |||
T35451 |
β-Defensin-2 (human) (trifluoroacetate salt)
|
||
β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes whe... | |||
T36648 | Tucatinib hemiethanolate | ||
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3765 |
L-asarinin
細辛素,(-)-Episesamin |
Others | Others |
L-asarinin ((-)-Episesamin) 降低外周血 IL-12 浓度并抑制 CXCR3 和 TLR4 的表达,这意味着 Asarinin 可能在 TLR4 通路中发挥作用,并延长同种异体心脏的存活时间。 | |||
TN1787 |
Isomucronulatol 7-O-glucoside
Isomucronulatol 7-O-beta-glucoside,黄芪紫檀烷苷,3-羟基-9,10-二甲氧基紫檀烷 |
Others | Others |
Isomucronulatol 7-O-glucoside 具有潜在的抗炎活性,在体外对 LPS 刺激产生的 IL-12 p40 表现出微弱的抑制作用。 | |||
T3859 |
Isomucronulatol
7,2'-Dihydroxy-3',4'-dimethoxyisoflavan,7,2'-二羟基-3',4'-二甲氧基异黄烷,异短尖剑豆酚 |
Others | Others |
Isomucronulatol (7,2'-Dihydroxy-3',4'-dimethoxyisoflavan) 是一种黄酮类化合物,分离自 A. membranaceus 根。它在体外对 LPS 刺激产生的 IL-12 p40 有抑制作用,具有潜在的抗炎作用。 | |||
TN1189 |
13-Methylberberine chloride
13-甲基小檗碱,13-Methylberberine |
Others | Others |
13-Methylberberine chloride 是一种黄连素类似物,可增加 IL-12 的产生,并在 LPS 激活的巨噬细胞转录后抑制 iNOS 的表达,具有抗脂肪和抗肿瘤作用。 | |||
TN4190 | Hedycoronen A | IL Receptor; TNF | Apoptosis; Immunology/Inflammation |
Hedycoronen A and hedycoronen B have the potential anti-inflammatory benefits, they are potent inhibitors of LPS-stimulated interleukin-6 (IL-6) and IL-12 p40, with IC(50) ranging from 4.1±0.2 to 9.1±0.3 uM, they also show moderate inhibitory activity on | |||
T16733 |
Resolvin E1
RvE1 |
Others | Others |
Resolvin E1 is an effective endogenous pro-resolving mediator of inflammation. Resolvin E1 has unique counterregulatory actions that inhibit PMN transendothelial migration. Resolvin E1 also acts as an effective inhibitor of leukocyte infiltration, dendrit | |||
TN5474 |
Bonducellin
|
||
Bonducellin has anti-inflammatory activities, it can significantly and dose-dependently inhibit the inflammatory mediators; nitric oxide (NO), and cytokines [tumor necrosis factor (TNF)-alpha and interleukin (IL)-12. Bonducellin shows weak antimalarial ac | |||
T35741 |
Gliovirin
|
||
Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease... |