kd-16

Haloperidol decanoate (KD 16) 是一种典型的抗精神病药物，用作精神分裂症和情绪障碍的维持治疗，配制成用于肌肉注射的酯。

CM-579 是首创的、可逆的，G9a 和 DNA 甲基转移酶 (DNMT) 的双抑制剂，其 IC50 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。

CM-579 trihydrochloride is a first-in-class reversible and dual inhibitor of G9a and DNMT (IC50s: 16 nM, 32 nM) with potent in vitro cellular activity in a wide range of cancer cells.

LV-320 是一种有效且非竞争性的ATG4B 抑制剂，其IC50值为 24.5 μM，Kd 值为 16 μM。 LV-320 抑制ATG4B 的酶促活性，阻断细胞自噬，并且稳定无毒，在体内具有活性。

NMS-P515 is an effective, orally active, and stereospecific PARP-1 inhibitor (Kd: 16 nM and an IC50: 27 nM (in Hela cells)). It has anti-tumor activity.

GPX4-IN-16 ((R)-9i) 是一种有效的GPX4抑制剂，其KD值为20.4 nM，表现出细胞毒性与抗癌活性。

High affinity XIAP antagonist (Kd = 16 nM for the BIR3 domain of XIAP). Exhibits cytotoxicity in a wide range of cancer cell lines in vitro (EC50 = 13 nM in MDA-MB-231 cells). Also displays antitumor activity in a mouse breast cancer xenograft model. Enhances TRAIL-induced apoptosis in chronic lymphocytic leukemia (CLL) cells. Oost et al (2004) Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J.Med.Chem. 47 4417 PMID:15317454 |Loeder et al (2009) A novel paradigm to trigger apoptosis in chronic lymphocytic leukemia. Cancer Res. 69 8977 PMID:19920200

CCT241736 是一种口服生物可利用的双重 FLT3 Aurora 激酶抑制剂，还抑制临床相关的 FLT3 耐药突变体，包括 FLT3-ITD 和 FLT3。它是 CCT137690 的高级类似物，是治疗人类恶性肿瘤的临床前开发候选物。

GID4 Ligand 3 (compound 16) 是GID4的结合物，体外Kd 值为 110 μM，IC50值为 148.5 μM。GID4 Ligand 3 可用于 cereblon(CRBN) 和Von Hippel-Lindau(VHL)的相关研究。

SARS-CoV-2-IN-16 (Compound 12) 是SARS-CoV-2核衣壳蛋白的有效抑制剂，具有强效的抗病毒活性(EC50 = 3.69 μM)。SARS-CoV-2-IN-16 以7.82 μM 的低Kd 值与 NPro 结合，这表明 SARS-CoV-2-IN-16 是一种有效的 NPro 配体。

SARS-CoV-2-IN-17 (Compound 16) is a highly effective inhibitor of SARS-CoV-2 nucleocapsid protein (NPro). It demonstrates potent anti-viral activity, with an EC50 value of 2.18 μM. Furthermore, SARS-CoV-2-IN-17 binds to NPro with a low Kd value of 7.82 μM, highlighting its potency as a NPro ligand [1].

SNX2112 (PF 04928473) 是一种具有口服活性的 Hsp90 抑制剂，Kd 为 16 nM。

CM-579 trihydrochloride 是首创的、可逆的，G9a 和 DNA 甲基转移酶(DNMT)的双抑制剂，其 IC50值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。

Pegdinetanib (BMS-844203; CT-322) 是一种选择性 VEGFR-2(VEGFR) 抑制剂，对人和鼠 VEGFR-2 的 Kd 分别为 11 nM 和 250 nM，IC50分别为 16 nM 和 240 nM。Pegdinetanib 不与 VEGFR-1或 VEGFR-3结合。Pegdinetanib 具有抗肿瘤活性。

Thanatin acetate 是一种具有抗菌活性的阳离子肽，抑制细菌和真菌的生长，通过靶向 LptC-LptA 相互作用和降低 LptA 稳定性来损害脂多糖转运复合物组装。

AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= >10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg kg.

[Nle20] H4 peptide (16−23) 是一种多肽,对组蛋白甲基转移酶SETD8展示出高度的抑制效力 (Kd=0.14 μM).该多肽通过竞争性结合SETD8的底物结合位点,有效阻断了SETD8对组蛋白 H4 的甲基化.因其显著的生物活性,[Nle20] H4 peptide (16−23) 可被视为抗癌治疗的潜在先导化合物.

Galanin (1-16), mouse, porcine, rat is a potent agonist of the hippocampal galanin receptor with a Kd of 3 nM, and it exhibits high biological activity on locus coeruleus neurons.

Galanin (1-16), mouse, porcine, rat 是一种有效的甘丙肽受体激动剂，Kd 为 3 nM。

CNI103 是一种高效且代谢稳定的钙调磷酸酶细胞通透性肽 (cell-permeable peptide) 抑制剂。它能选择性地阻断钙调神经磷酸酶和 NFATc3 之间的相互作用 (KD=16 nM)，从而抑制体外和体内的 NFATc3 激活。CNI103 可用于研究急性呼吸窘迫综合征 (ARDS) 和其他炎症性疾病。