b-02

RAD51 Inhibitor B02 (B02) 是一种人 RAD51的抑制剂，IC50值为27.4 μM。

EAPB-0202，EAPB0203的去甲基化代谢产物，表现出相比参考用药fotemustine和imiquimod，对A375具有显著的体外活性。

OSUAB-0284 是一种细菌拓扑异构酶 (bacterial topoisomerase) 抑制剂，具有显著的抗葡萄球菌活性，特别是对耐甲氧西林金黄色葡萄球菌 (MRSA) 的作用明显。通过抑制细菌拓扑异构酶，OSUAB-0284 展现出其抗菌特性。该化合物可用于研究由 MRSA 等耐药菌引起的感染。

GFB-024 是靶向 CB1 的人源化抗体，可用于研究肥胖。

RCB-02-4-8，一种可电离的阳离子脂质，主要用于构建脂质纳米颗粒(LNPs)以传递mRNA，能有效提升小鼠肺部的转染效率。

EMB-02 是一种双特异性抗体，作用于PD-1和LAG-3。EMB-02 能够抑制由PD-1和LAG-3引起的T细胞活化和增殖的下调，展现出显著的抗癌活性。

Baricitinib (INCB028050) 是一种 JAK1 和 JAK2 抑制剂 (IC50=5.9/5.7 nM)，具有选择性和口服活性。Baricitinib 具有潜在的抗炎、免疫调节和抗肿瘤活性。

Epacadostat (INCB 024360) 是一种口服、高效且具有选择性的 IDO1 抑制剂，IC50值为71.8 nM。

CCB02 是选择性的 CPAP-tubulin 相互作用抑制剂。CCB02能够与 tubulin 结合，竞争 β-tubulin 的 CPAP 结合位点，IC50 值为 689 nM，显示出高效的抗肿瘤活性。CCB02 对其他的蛋白没有抑制作用，包括中心体、细胞周期相关蛋白，对 Aurora A，Plk1，Plk2，CDK2 和 CHK1 的磷酸化状态也无作用。

Gimsilumab (MORAb-022) 是一种靶向粒细胞巨噬细胞集落刺激因子的人源化单克隆抗体，可用于研究 COVID-19 引起的炎症和低氧血症。

ART-CHEM-BB B025267 是 utrophin 生成的上调剂，EC50 为 1.8 μM，可用于治疗 Duchenne 肌营养不良症的研究。

B022 是一种具有选择性和高效性的 NF-κB 诱导激酶（NIK）抑制剂（Ki：4.2 nM），是治疗肝脏炎症和损伤的化学探针。B022 可避免肝脏免受氧化应激和毒素引起的炎症和损伤。

KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[1].

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader, known as a molecular glue. It facilitates the degradation of nuclear FKBP12 by covalently modifying DCAF16, an E3 ligase. Moreover, KB02-SLF enhances the longevity of protein degradation in biological systems. The compound SLF acts as a linker, binding to the ubiquitin E3 ligase ligand KB02, resulting in the formation of KB02-SLF[1].

FCOB02 是一种针对单胺氧化酶 B (MAO-B) 的配体。FCOB02 可以被标记为 [18F]FCOB02，这是一种类4-甲基香豆素的靶向探针。[18F]FCOB02 对 MAO-B 显示出高亲和力，其 IC50 值为 10.68 nM。[18F]FCOB02 可用于特异性地对 MAO-B 进行成像及体内定量分析。

(2S)-SB02024 (SB02877) 是 SB02024 的 S-对映体，并作为 Vps34 抑制剂。

BIIB021 (CNF2024) 是一种可口服的合成 HSP90 抑制剂，Ki 值和EC50值分别为 1.7 nM 和 38 nM。

Baricitinib phosphate (INCB028050) 是一种选择性的，可口服的 JAK1 JAK2抑制剂，IC50值分别为 5.9 和 5.7 nM。

AB023a is an antibiotic with antifungal properties.

AB023b is an antibiotic with antifungal properties.

Dynamin-related GTPase DRP1 partial inhibitor (IC50 = 1.2 μM). Selective for DRP1 over other dynamin-related GTPases, OPA1 and DYN1. Increases mitochondrial DNA levels in mfn1- knockout MEFs deficient in mitochondrial fusion. Mallat et al (2018) Discovery and characterization of selective small molecule inhibitors of the mammalian mitochondrial division dynamin, DRP1. Biochem.Biophys.Res.Commun. 499 556 PMID:29601815

KB02-COOH is a synthetic fragment derived from ubiquitin E3 ligase ligand KB02, which possesses potential utility in the synthesis of PROTAC compounds. Notably, KB02-COOH can be employed in the generation of PROTAC constructs like KB02-JQ1 and KB02-SLF.

B026 是选择性的、口服具有活力的 p300 CBP 组蛋白乙酰转移酶 (p300 CBP HAT) 抑制剂，能够作用于 p300 (IC50: 1.8 nM) 和 CBP (IC50: 9.5 nM)。B026 对雄激素受体阳性 (AR+) 前列腺癌细胞表现出抗癌效果。

BIIB028 is a small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2 Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to other molecules involved in cell cycle regulation and immune responses.