smac

Xevinapant (Debio-1143) 是一种有效的 Smac 模拟物和 IAP 的拮抗剂，能够抑制 XIAP，cIAP1 和 cIAP2 蛋白，Ki 值分别为 66.4，1.9 和 5.1 nM。

Xevinapant hydrochloride (AT-406 HCl) 是口服生物可利用的 Smac 模拟物，也是细胞凋亡蛋白抑制剂的拮抗剂。它在无细胞功能测定中有效拮抗 XIAP BIR3 蛋白，诱导细胞 cIAP1 蛋白的快速降解，并抑制各种人类癌细胞系中的癌细胞生长。它在诱导异种移植肿瘤细胞凋亡方面非常有效。

XIAP Tracer mF-Smac是一种荧光标记肽，在TR-FRET检测中与铽标记的BIR域抗体共用作为受体染料。该化合物在BIR3 (XIAP)的Kd值为4.7 nM，而在XIAP偏振测定中的Kd值为17.9 nM。

Smac-based peptide为具有生物活性的肽，源自SMAC与BIR3结构域的结合。

Xylosmacin is a biochemical.

Jasmacyclen is a compound in which has an aroma.

Glasmacinal 是一种大环内酯类化合物，具有显著的抗炎活性。

KY-05009 是 ATP 竞争性的、有效的 TNIK 抑制剂，Ki 为 100 nM。KY-05009抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制TNIK 的蛋白表达和Wnt 靶基因的转录活性，并诱导癌细胞凋亡，显示抗癌活性。

Laropiprant (MK-0524) 是 DP receptor 的选择性拮抗剂，Ki 为 0.57 nM，对 TP 受体的 Ki 为 2.95 nM。

Polysaccharide of Atractylodes macrocephala 是一种天然产物，可用作天然产物对照品，用于生命科学相关领域的研究，其产品编号为 TN8889。

(9S)-Macrocidin B 的除草活性不如macrocidin A。

parathyroid hormone (7-34) [Homo sapiens] [Macaca fascicularis] is a peptide with the sequence H2N-LMHNLGKHLNSMERVEWLRKKLQDVHNF-OH, MW= 3474.03. Parathyroid hormone (PTH) is secreted by the chief cells of the parathyroid glands as a polypeptide containing

Birinapant (TL32711) 是一种二价 Smac 模拟物，是 XIAP 和 cIAP1的强效拮抗剂，Kd 值分别为 45 nM 和小于 1 nM。它靶向与 TRAF2 相关的 cIAP，并消除 TNF 诱导的 NF-κB 活化。

SM-164 是细胞渗透性 Smac 类似物，与含有 BIR2 和 BIR3 结构域的 XIAP 蛋白结合，IC50值为 1.39 nM，它用作XIAP 的强效拮抗剂。

LCL161 是一种 SMAC 模拟物，一种 IAP 拮抗剂，具有口服活性，抑制 HEK293 细胞中 XIAP (IC50=35 nM)，也抑制 MDA-MB-231 细胞中 cIAP1 (IC50=0.4 nM)。LCL161 具有潜在抗肿瘤活性。

SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.

LBW242 is a 3-mer and Smac mimetic and is an effective and orally active proapoptotic IAP inhibitor. LBW242 has activity against multiple myeloma and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells. LBW242 displays effec

SM-433 是 Smac 模拟物，是凋亡抑制蛋白(IAPs)的抑制剂。SM-433 对 XIAP BIR3 蛋白具有较强的亲和力 (IC50<1 μM)。

SBP-0636457 (SB1-0636457) is a SMAC mimetic and an inhibitor of inhibitor of apoptosis (IAP) proteins. It specifically binds to the BIR-domains of IAP proteins with a Ki value of 0.27 μM. SBP-0636457 holds potential for research in the fields of solid tumors and hematologic cancers.

RI-962是一种有效和选择性的的RIPK1抑制剂，通过抑制RIPK1、RIPK3和MLKL磷酸化，剂量依赖性地保护细胞免受TNFα、Smac模拟物和Z-VAD-FMK诱导的坏死性凋亡，EC50=10.0 nM~17.8 nM，在两种炎症模型中提高小鼠的生存率。

CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and Bcl-x(L). CGP74514A treatment (5 microM; 18 hr) resulted in increased p21(CIP1) expression, p27(KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34(CDC2). It also induced early (i.e., within 2 hr) inhibition of CDK1 activity and dephosphorylation of pRb, followed by pRb degradation, but did not block pRb phosphorylation at CDK2- and CDK4- specific sites. These findings indicate that the selective CDK1 inhibitor, CGP74514A , induces complex changes in cell cycle......

SM-433 hydrochlorid 是一种 Smac 模拟物，是一种凋亡抑制蛋白(IAPs)抑制剂。SM-433 hydrochlorid 能够强力结合 XIAP BIR3 蛋白 (IC50<1 μM)。

SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains(IC50 value of 1.39 nM) and functions as an extremely potent antagonist of XIAP.

Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice. Hennessy et al (2013) Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582). J.Med.Chem. 56 9897 PMID:24320998