hl-2

HL2-m5 是 sonic hedgehog patched (Shh PTCH1) 相互作用的抑制剂，其对 Shh 的 Kd 为 170 nM。HL2-m5 能有效抑制 Hedgehog 信号通路的激活和 Gli 控制基因的转录，IC50 为 230 nM。

HL271, a derivative of metformin, is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment.

HL22 是骆驼蓬碱的衍生物。它对 HCT116、MGC803 和 MCF7 三种癌细胞系表现出显著的抑制作用，并能够抑制 MGC803 细胞的迁移和单克隆形成。HL22 的抗癌机制涉及多种代谢通路，适用于肿瘤研究。

HL23是一种HDAC抑制剂，对抗HCC具有活性。通过增强TXNIP启动子乙酰化，此化合物上调TXNIP表达，进而介导钾通道活性并触发TXNIP依赖性钾剥夺，抑制HCC的进展和转移。HL23与Sorafenib联合应用时显示出协同作用，并且其效力超过Sorafenib与Vorinostat的联用。

CHL2310 是 CYP46A1 的一种抑制剂，IC50 为 0.11 nM，Kd 为 0.37 nM，并且能够穿透血脑屏障。CHL2310 经放射性 18F 标记后，可作为 PET 成像剂使用。

Flavopiridol hydrochloride (MDL 107826A) 是一种CDK 的广谱抑制剂，与 ATP 竞争性地抑制 CDK1，CDK2 和 CDK4 的活性，IC50值分别为 30, 170, 100 nM。

ABT-737 是 BH3 模拟物，是一种 Bcl-2、Bcl-xL 和 Bcl-w 的抑制剂 (EC50=30.3 nM 78.7 nM 197.8 nM)。ABT-737 具有抗肿瘤活性和抗衰老活性。

Valproic Acid (2-Propylpentanoic Acid) 是一种 HDAC 抑制剂，可抑制 HDAC1 活性，诱导 HDAC2 降解，具有口服活性。Valproic Acid 可以用于癫痫和躁郁症的研究。

GP 1a 是cannabinoid receptor 2（CB2）的强效激动剂（EC50=7.1),是在cAMP、GTPγS 和β-arrestin 招募试验中显示的。GP 1a 对CB2受体的选择性约为CB1受体的30倍，且在体外增加HL-60细胞的P-ERK1 2表达。GP 1a 对皮肤伤口愈合有益。GP 1a 可抑制炎症和纤维生成，同时促进上皮的重新形成。

Cyclophosphamide 是一种烷化剂，具有抗肿瘤及免疫抑制活性，用于治疗多种癌症。

Alisertib (MLN 8237) 是一种 Aurora A 激酶抑制剂 (IC50=1.2 nM)，具有口服活性和选择性。Alisertib 具有抗肿瘤活性，可以诱导细胞凋亡和自噬，诱导细胞周期阻滞。

Clofilium tosylate 是一种钾通道阻滞剂，可诱导人早幼粒细胞白血病细胞凋亡，具有抗心律失常作用。

Tamarixetin (4'-O-Methyl Quercetin) 是一种槲皮素的天然类黄酮衍生物，具有抗氧化、抗炎作用，能够防止心肌肥厚。

Erianin 能抑制吲哚胺-2,3-双加氧酶诱导的肿瘤血管生成，可用作退烧药和止疼剂。

O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism in isolated neonatal and fetal rabbit hepatocytesPediatr. Res.15(11)1406-1410(1981) 2.Morgan, A.G.M., Babu, D., Michail, K., et al.An evaluation of myeloperoxidase-mediated bio-activation of NSAIDs in promyelocytic leukemia (HL-60) cells for potential cytotoxic selectivityToxicol. Lett.28048-56(2017) 3.Torisu, K., Kobayashi, K., Iwahashi, M., et al.Discovery of new chemical leads for prostaglandin D2 receptor antagonistsBioorg. Med. Chem. Lett.14(17)4557-4562(2004)

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 μM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day. 1.Wang, G., Zhao, Y., Liu, Y., et al.Discovery of a novel dual-target inhibitor of ERK1 and ERK5 that induces regulated cell death to overcome compensatory mechanism in specific tumor typesJ. Med. Chem.63(8)3976-3995(2020)

Myelopeptide-2 分离于猪骨髓细胞培养上清，能够恢复 HL-60 白血病细胞或麻疹病毒条件抑制下人 T 淋巴细胞的丝裂原反应活性、白细胞介素-2 (IL-2) 合成水平和白细胞介素-2受体 (IL-2R) 表达水平。Myelopeptide-2 参与免疫稳态调节，在抗肿瘤和抗病毒研究中具有广阔的应用前景。

Dihydrochelerythrine (12,13-Dihydrochelerythrine) 是一种从榕树叶片分离出的天然化合物，具有抗真菌活性，有潜力治疗多丝蚴引起的严重感染。

WKYMVM-NH2 是一种六肽，通过激活 FPRL1 和 FPRL2 受体来活化中性粒细胞和髓系细胞。在 HL-60-FPRL1 和 HL-60-FPRL2 细胞中的 EC50 分别为 2 nM 和 80 nM。它在稳定表达 FPRL2 的 HL-60 细胞中诱导趋化性，最佳迁移效果出现在 10-50 nM 的剂量范围内。此外，WKYMVM-NH2 可诱导中性粒细胞产生超氧化物，其 EC50 为 75 nM。该化合物适用于炎症相关疾病的研究。

(2S)-2'-Methoxykurarinone 是一种分离自苦参根中的化合物，具有抗炎、解热、抗糖尿病和抗肿瘤活性。它对人髓系白血病 HL-60 细胞具有细胞毒活性。它能够下调 RANKL 信号，抑制破骨细胞形成和骨吸收。

Stachybotrysin B is a fungal metabolite originally isolated from S. chartarum and has antiviral and anticancer activities.1,2 It has antiviral activity against HIV in SupT1 cells (IC50 = 19.2 μM).1 Stachybotrysin B is cytotoxic to K562, HeLa, and HL-60 cells (IC50s = 21.72, 39.63, and 18.5 μM, respectively).2 |1. Zhao, J., Feng, J., Tan, Z., et al. Stachybotrysins A-G, phenylspirodrimane derivatives from the fungus Stachybotrys chartarum. J. Nat. Prod. 80(6), 1819-1826 (2017).|2. Ma, X.-h., Zheng, W.-m., Sun, K.-h., et al. Two new phenylspirodrimanes from the deep-sea derived fungus Stachybotrys sp. MCCC 3A00409. Nat. Prod. Res. 33(3), 386-392 (2018).

7-Oxo-beta-sitosterol (7-Ketositosterol) 是一种从芒草 (x giganteus) 果实中分离得到的植物甾醇， 具有抗癌抗肿瘤活性，抑制 HL-60 急性髓性白血病 （AML） 细胞增殖，通过下调 S1P 、 p-44 42 ERK1 2 和 p-NF-κB p65 蛋白水平刺激神经酰胺积累和凋亡，可用于研究乳腺癌。

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)

1,4,5,6-Tetrahydroxy-7-prenylxanthone exhibits anti-cancer activity, demonstrating moderate cytotoxicity against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines, with GI50 values of 2.