Chromatin/Epigenetics

2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR), a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.

Ethyl3,4-dihydroxybenzoate(Ethylprotocatechuate)是一种抗氧化剂，是一种在花生种子的种皮中发现的脯氨酰羟化酶(prolyl-hydroxylase)抑制剂。Ethyl3,4-dihydroxybenzoate通过激活NO合酶(NOsynthase)并产生线粒体ROS来保护心肌。Ethyl3,4-dihydroxybenzoate可诱导ESCC细胞自噬(autophagy)和凋亡(apoptosis)。Ethyl3,4-dihydroxybenzoate是胶原蛋白合成抑制剂，具有骨骼保护作用。

(E/Z)-AG490((E/Z)-TyrphostinAG490)是(E)-AG490和(Z)-AG490的消旋体。(E)-AG490是一种酪氨酸激酶抑制剂，可抑制EGFR，Stat-3和JAK2/3。

Naphthol AS-E 是有效的，具有细胞渗透性的 KIX-KID 相互作用的抑制剂。Naphthol AS-E 直接结合 CBP 的 KIX 域 (Kd: 8.6 µM)，阻断 KIX 域和 KID 域的相互作用 (IC50: 2.26 µM)。Naphthol AS-E 可用于癌症研究。

Verucopeptin 是一种有效的 HIF-1 (IC50=0.22 µM) 抑制剂，可以降低 HIF-1 靶基因的表达和 HIF-1α 的蛋白水平。通过直接靶向 v-ATPase ATP6V1G 亚基 (但不靶向 ATP1V1B2 或 ATP6V1D)，Verucopeptin 强烈抑制 v-ATPase 活性。Verucopeptin 对耐药性癌细胞表现出抗肿瘤活性，常用作癌症相关研究。

Triciferol 是一种具有 VDR 激动剂和 HDAC 拮抗剂联合作用的多配体。Triciferol 直接与 VDR结合 (IC50=87 nM)，在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化，并增强组蛋白乙酰化。抗增殖和细胞毒性活性。

1,4-DPCA ethyl ester 是 1,4-DPCA 的乙酯形式，可以抑制 FIH。

A PKCβ Inhibitor

WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.

Senaparib (IMP4297) 是强效的、选择性的、口服有效的 PARP1/2 抑制剂。Senaparib (IMP4297) 在动物模型中表现强效的抗肿瘤活性。

Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.

Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.

Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.

(2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) 是一种有效的选择性的 JAK3 抑制剂 (IC50=144.8 nM)。详细信息请参考专利US20150158864A1，example 68。

653-47 hydrochloride 是一种增强剂，能显著增强 666-15 的 cAMP 反应元件结合蛋白 (CREB) 抑制活性。653-47 hydrochloride 也是一种很弱的抑制剂，其 IC50 为 26.3 μM。

Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.

N-Descyclopropanecarbaldehyde Olaparib 是含有 DOTA 的奥拉帕尼的类似物。Descyclopropanecarbaldehyde Olaparib 是一种 CRBN 配体，可用于合成新型靶向 EGFR 和 PARP 的双靶点 PROTAC，DP-C-4。N-Descyclopropanecarbaldehyde Olaparib 可以用 F-18 或荧光团进行放射性标记用于正电子发射断层扫描 (PET) 或几种类型的肿瘤的光学成像。

PROTAC EED degrader-1 是靶向 EED 的 PROTAC 分子，pKD 为 9.02。PROTAC EED degrader-1 是靶向 EED 亚基的多梳抑制复合物 2 (PRC2) 抑制剂 (pIC50=8.17)。

An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction

dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.

A TYK2 inhibitor

G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.

PF-9363是一种强效、选择性、口服生物利用度高的KAT6A/B抑制剂，对KAT6A和KAT6B的K i 值分别为0.27nM和2.4nM。

NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter.