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20

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0987	Gimeracil 吉美嘧啶,吉莫斯特,Gimestat	Autophagy	Autophagy
	Gimeracil (Gimestat) 是一种竞争性可逆的 DPYD(二氢嘧啶脱氢酶，DPD) 有效抑制剂，是口服氟嘧啶衍生物 S-1 的成分，能够抑制 DNA DSB 的修复。
T77764	DC-Y13-27	Others	Others
	DC-Y13-27 是一种 DC-Y13 的衍生物，是一种有效的 YTHDF2 抑制剂 (KD: 37.9 μM)。DC-Y13-27 具有抗肿瘤活性，可增强放疗和免疫疗法对肿瘤的响应。
T2265	Bimiralisib 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine,PQR309,PI3K-IN-2	Others; PI3K; S6 Kinase; mTOR	MAPK; Others; PI3K/Akt/mTOR signaling
	Bimiralisib (PI3K-IN-2) 是一种有效的，可渗透脑的 mTOR/PI3K 抑制剂，是一种 mTORC1和 mTORC2抑制剂。它能够抑制 PI3Kα,PI3Kδ,PI3Kβ,PI3Kγ和 mTOR，IC50分别为 33 nM，451 nM，661 nM，708 nM 和 89 nM。
T2610L	BMS-599626 2HCL(714971-09-2 Free base) BMS 599626 dihydrochloride,BMS-599626 2HCL(714971-09-2 Free base),AC480 2HCl	HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	BMS-599626 2HCL (AC480 2HCl) 是BMS-599626 衍生物。BMS-599626 是一种可口服且具有选择性的 HER1 和 HER2 双重抑制剂， IC50 分别为 20 和 30 nM。BMS-599626 抑制肿瘤细胞增殖，并有可能增加肿瘤对放疗的反应。
T31977	GLYN NSC 137875,NSC137875,Glycidyl nitrate,NSC-137875
	GLYN, a nitric oxide donor, acts by enhancing the therapeutic efficacy of chemotherapy and radiotherapy.
T70134	L-778123 Dihydrochloride
	L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed.
T3182L	L-778123 free base L-778,123,L 778123,L-778123,L778123,L 778,123
	L-778123 is an inhibitor of FPTase and GGPTase-I. The combination of L-778123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer.
T27052	CMP3a CMP-3a,CMP 3a
	CMP3a is a NEK2 kinase inhibitor. CMP3a efficiently attenuated GBM growth in a mouse model and exhibited a synergistic effect with radiotherapy. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase E
T21119	Cevimeline AF-102B,西维美林,FKS 508,SNI 2011,HSDB 7286
	Cevimeline, a parasympathomimetic and muscarinic agonist, affects M1 and M3 receptors. Cevimeline has been shown to treat dry mouth and Sj gren's syndrome. It is also used to reduce Xerostomia symptoms and increase salivary flow in head and neck cancer survivors after radiotherapy.
T21310	Nimustine Nimustine Hydrochloride,Nidran,pimustine hydrochloride,ACNU 50,Nimustine HCl,ACNU
	NIMUSTINE, an antineoplastic agent especially effective against malignant brain tumors, has been used in combination with other antineoplastic agents or with radiotherapy for the treatment of various neoplasms.
T68663	GPI-15427
	GPI-15427 is a potent PARP-1 inhibitor capable of crossing the blood-brain barrier, which can significantly increased the antitumor activity of the methylating agent TMZ against malignant melanoma, glioblastoma multiforme, or lymphoma growing at the CNS site. GPI-15427 acts as a potent inhibitor of the enzyme, being capable of inhibiting the activity of purified PARP-1 at nanomolar concentrations. GPI-15427 induced significant sensitization to radiotherapy, representing a promising new treatment...
T14035	3M-011	TLR	Immunology/Inflammation
	3M-011, a potent dual toll-like receptor TLR7/8 agonist and cytokine inducer, serves as a powerful adjuvant to radiotherapy, eliciting significant local and systemic immune responses. Additionally, it effectively inhibits H3N2 influenza viral replication in the nasal cavity and exhibits strong antitumor activity[1][2][3].
T69922	EPZ020411 HCl
	EPZ020411 is a potent and selective PRMT6 inhibitor tool compound. EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. EPZ020411 suppresses RCC1 arginine methylation and improves the cytotoxic activity of radiotherapy against GSC brain tumor xenografts.
T81424	Polysaccharidase Tremella polysaccharide
	Polysaccharidase (Tremella polysaccharide) 是一种提升免疫功能的真菌多糖。该化合物展现出治疗化疗和放疗导致的白细胞减少症的研究潜力。
T2589	Dolasetron Mesylate hydrate Dalasetron Mesylate Hydrate,多拉司琼甲磺酸盐一水合物	5-HT Receptor	GPCR/G Protein; Neuroscience
	Dolasetron Mesylate hydrate (Dalasetron Mesylate Hydrate) 是一种选择性血清素受体拮抗剂，可竞争性阻断血清素对 5HT3 受体的作用，从而抑制化疗和放疗引起的恶心和呕吐。
T61370	DNA-PK-IN-6
	DNA-PK-IN-6, a robust DNA-PK inhibitor, effectively hampers the activity of DNA-PKcs, thereby significantly impairing the DNA repair mechanism in tumors and instigating apoptosis in cells. Additionally, DNA-PK-IN-6 amplifies the responsiveness of tumor tissues to radiotherapy, overcomes the challenge of drug resistance, and augments its inhibitory impact on a diverse range of solid and hematological tumors[1].
T62191	DNA-PK-IN-5
	DNA-PK-IN-5 是一种 DNA-PK 的有效抑制剂。DNA-PK-IN-5 能够抑制 DNA-PKcs 活性，明显降低肿瘤 DNA 修复，并诱导细胞凋亡。DNA-PK-IN-5 能够提高肿瘤组织对放疗的敏感性，克服耐药问题，提高对多种实体瘤和血液肿瘤的抑制效果。
T61751	DNA-PK-IN-3
	DNA-PK-IN-3 is a highly potent inhibitor of DNA-PK. This compound exerts a synergistic effect when combined with radiotherapy and chemotherapy, resulting in enhanced therapeutic outcomes and significant inhibition of tumor growth. Furthermore, DNA-PK-IN-3 demonstrates remarkable efficacy in reducing damage to normal cells, effectively minimizing adverse side effects. Due to these compelling properties, DNA-PK-IN-3 holds great potential for cancer research applications[1].
T33699	NLCQ-1 HCl NLCQ1,NLCQ-1, NLCQ 1,NSC 709257
	NLCQ-1 is a novel weak DNA-intercalative bioreductive compound. NLCQ-1 exhibited a C50 of 44 microM. NLCQ-1 demonstrated significant hypoxic selectivity in several rodent (V79, EMT6, SCCVII) or human (A549, OVCAR-3) tumor cell lines. Its potency as a hypo
T60953	BSc5367
	BSc5367 是Nek1激酶结构域的有效抑制剂，IC50值为 11.5 nM。Nek1 是一种NIMA 相关的蛋白激酶，在细胞周期调节、DNA 修复和微管调节中起着关键作用。Nek1 功能障碍在肌萎缩侧索硬化症 (ALS)、多囊肾病 (PKD) 和几种类型的放疗耐药性癌症中发挥关键作用。BSc5367 为更好的理解上述疾病提供了有用工具。

化合物

Cat.No: T0987

Synonym: 吉美嘧啶,吉莫斯特,Gimestat

Target: Autophagy

Cat.No: T77764

Target: Others

Cat.No: T2265

Synonym: 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine,PQR309,PI3K-IN-2

Target: Others, PI3K, S6 Kinase, mTOR

BMS-599626 2HCL(714971-09-2 Free base)

Cat.No: T2610L

Synonym: BMS 599626 dihydrochloride,BMS-599626 2HCL(714971-09-2 Free base),AC480 2HCl

Target: HER

Cat.No: T31977

Synonym: NSC 137875,NSC137875,Glycidyl nitrate,NSC-137875

L-778123 Dihydrochloride

Cat.No: T70134

L-778123 free base

Cat.No: T3182L

Synonym: L-778,123,L 778123,L-778123,L778123,L 778,123

Cat.No: T27052

Synonym: CMP-3a,CMP 3a

Cat.No: T21119

Synonym: AF-102B,西维美林,FKS 508,SNI 2011,HSDB 7286

Cat.No: T21310

Synonym: Nimustine Hydrochloride,Nidran,pimustine hydrochloride,ACNU 50,Nimustine HCl,ACNU

Cat.No: T68663

Cat.No: T14035

Target: TLR

Cat.No: T69922

Polysaccharidase

Cat.No: T81424

Synonym: Tremella polysaccharide

Dolasetron Mesylate hydrate

Cat.No: T2589

Synonym: Dalasetron Mesylate Hydrate,多拉司琼甲磺酸盐一水合物

Target: 5-HT Receptor

Cat.No: T61370

Cat.No: T62191

Cat.No: T61751

Cat.No: T33699

Synonym: NLCQ1,NLCQ-1, NLCQ 1,NSC 709257

Cat.No: T60953

Cat. No.	Product Name	Target	Signaling Pathways
TN2108	Protohypericin	Others	Others
	Protohypericin 是一种从贯叶连翘中提取的天然石脑粉。放射性碘化 Protohypericin 能用于肿瘤坏死靶向放射研究。
T3S2344	β,β-Dimethylacrylshikonin β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin	ERK; HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; MAPK; Metabolism
	β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) 是一种萘醌衍生物，从 Arnebia nobilis 中提取得到。它利用 PI3K 通路诱导 eNOS、VEGF 和 HIF-1α 的表达，促进血管生成，具有抗肿瘤活性。

天然产物

Cat.No: TN2108

Target: Others

β,β-Dimethylacrylshikonin

Cat.No: T3S2344

Synonym: β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin

Target: ERK, HIF/HIF Prolyl-Hydroxylase

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