JAK/STAT Signaling

STAT3-IN-3 是一种有效和选择性的 STAT3 抑制剂。

Tyk2-IN-7 (Compound 48) 是 TYK2 JH2 抑制剂，与 TYK2 JH2 结构域结合，IC50 和 Ki.app 分别为 0.00053 μM 和 0.00007 μM。Tyk2-IN-7 (Compound 48) 是常规 TYK2 正构抑制剂的高选择性替代，抑制 TYK2/JAK1/JAK2 激酶结构域。Tyk2-IN-7 (Compound 48) 抑制小鼠 IL-12 诱导的 IFNγ 药效学模型中以及抑制在 IL-23 和 IL-12 依赖性小鼠结肠炎模型中的功效。

Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).

A multi-kinase inhibitor

A potent inhibitor of JAK3

Beta-hydroxyisovalerylshikonin 是一种从Lithospermium radix 中分离出的天然产物，是一种有效的 PTK 抑制剂， 对 EGFR 和 v-Src 受体作用的 IC50 分别为 0.7 μM 和 1 μM。Beta-hydroxyisovalerylshikonin 对多种肿瘤细胞系均有抑制作用，能高效诱导 NCI-H522 和 DMS114 细胞的死亡。

A liminoid degradant with diverse biological activities

Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.

Tyrphostin AG30 (AG30), a potent and selective EGFR tyrosine kinase inhibitor, selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.

Cyasterone，一种天然的 EGFR 抑制剂，主要分离自 Ajuga decumbens Thunb (Labiatae)。Cyasterone 通过诱导细胞凋亡 (apoptosis) 和细胞周期阻滞表现出抗增殖作用。 Cyasterone 可作为抗人类肿瘤的临床治疗性药物。

Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.

Golotimod hydrochloride (SCV 07 hydrochloride) 一种具有抗菌活性的免疫调节肽，可显着提高抗结核治疗的功效，刺激胸腺和脾细胞增殖，并改善巨噬细胞功能。Golotimod hydrochloride (SCV 07 hydrochloride) 抑制 STAT3 信号传导并调节接受放疗或放疗与顺铂联合用药的动物模型中口腔粘膜炎的持续时间和严重程度。Golotimod hydrochloride (SCV 07 hydrochloride) 是复发性生殖器单纯疱疹病毒 2 型 (HSV-2) 的潜在治疗药物。

BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFRdel19 T790M C797S as biomarker potency and anti-proliferation potency in BaF3 cells, respectively.

AS2863619是一种口服小分子环依赖性激酶（CDK）8和19抑制剂，IC 50 值分别为0.6099nM和4.277nM。

A dual inhibitor of Cdk8 and Cdk19

Tetramethylcurcumin (FLLL31), a small-molecule signal transducer and activator of transcription 3 (STAT3) inhibitor derived from curcumin, binds selectively to Janus kinase 2 and the STAT3 Src homology-2 domain, which serve crucial roles in STAT3 dimerization and signal transduction.

Reticuline 分离自 Litsea cubeba，通过 JAK2/STAT3 和 NF-κB 信号通路显示抗炎作用。Reticuline 还可抑制 TNF-α 和 IL-6 的 mRNA 表达，并降低 JAK2 和 STAT3 的磷酸化水平。

A dual inhibitor of CK2 and ERK8

An isoprenoid antibiotic and antiviral

An inhibitor of EGFR

An antineoplastic and piscicidal rotenoid

An anticancer phytoalexin

Delphinidin (chloride) 是一种常见的花青素单体形式之一，可以从浆果和红酒中分离得到。

L-Sulforaphene是一种天然的异硫氰酸酯，具有抗炎、抗癌和抗氧化作用。