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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T11520	GW806742X	MLK; VEGFR	Angiogenesis; MAPK; Tyrosine Kinase/Adaptors
	GW806742X 是ATP 模拟物，是MLKL 抑制剂，可结合 MLKL 假激酶结构域，Kd 值为 9.3μM。它对VEGFR2的IC50为 2 nM，延缓 MLKL 膜移位并抑制坏死。
T6057	URMC-099	ROCK; MLK; VEGFR; SGK; DNA Alkylation; Trk receptor; c-Met/HGFR; LRRK2; MEK; IGF-1R; Syk; Bcr-Abl; CDK; Src; Aurora Kinase; Autophagy	Angiogenesis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors
	URMC-099 是一种具有优异的血脑屏障穿透性的，可口服的混合谱系激酶 3 抑制剂，IC50为14 nM。
T6904	Necrosulfonamide (E)-Necrosulfonamide	MLK	MAPK
	Necrosulfonamide ((E)-Necrosulfonamide) 是一种坏死性凋亡抑制剂，通过选择性靶向(MLKL)，可阻止 MLKL-RIP1-RIP3 坏死小体复合体与其下游效应子相互作用。MLKL 是诱导坏死过程中 RIP3 的重要底物。
T9399	Menin-MLL inhibitor 20	Epigenetic Reader Domain; Histone Methyltransferase	Chromatin/Epigenetic
	Menin-MLL inhibitor 20 是一种不可逆的menin-MLL 相互作用抑制剂，具有抗肿瘤活性。
T1725	Y-27632 dihydrochloride 反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐,Y-27632 2HCl	ROCK; Apoptosis	Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	Y-27632 dihydrochloride (Y-27632 2HCl) 是一种 ROCK-I 和 ROCK-II 抑制剂，具有口服有效性、ATP 竞争性。Y-27632 dihydrochloride 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。
T3082	SGC0946	Histone Methyltransferase	Chromatin/Epigenetic
	SGC0946是一种组蛋白甲基转移酶DOT1L 高选择性抑制剂，IC50值为0.3nM，可选择性地杀死混合谱系白血病细胞。
T77245	Mannan	Endogenous Metabolite	Metabolism
	Mannan 是从藻类、蘑菇、酵母和高等植物中分离出的，可作为免疫调节剂。Mannan 抑制肝脏巨噬细胞（M1谱系）的促炎活性对许多肝脏病变（例如坏死或脂肪变性）具有保护作用。
T11925	M‑89	Epigenetic Reader Domain; Histone Methyltransferase	Chromatin/Epigenetic
	M-89 可抑制 Menin-MLL 蛋白之间的相互作用，有研究混合谱系白血病的潜力。它是一种强特异性 menin 抑制剂，结合到 menin 的Kd 值为 1.4 nM。
T6825	Eltrombopag Olamine Promacta Olamine,Revolade,艾曲泊帕乙醇胺盐,Eltrombopag diethanolamine salt,SB497115,艾曲波帕乙醇胺盐,SB-497115GR	Thrombin	Proteases/Proteasome
	Eltrombopag Olamine (Eltrombopag diethanolamine salt) 是 Eltrombopag 的口服活性乙醇胺盐，是一种血小板生成素(TPO)受体激动剂，用于血小板减少的某些病症研究。
T8768	MM-102 TFA HMTase Inhibitor IX TFA	Histone Methyltransferase	Chromatin/Epigenetic
	MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5/MLL 相互作用抑制剂，在 WDR5 结合检测中，IC50为 2.4 nM，Ki 小于 1 nM。
T36944	Ara-G	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物，可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP)，从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。
T24471	MIV-6
	MIV-6 is an inhibitor of the menin-mixed lineage leukemia interaction.
T12002	Menin-MLL inhibitor 4	Others	Others
	Menin-MLL inhibitor 4 has antitumor activity.Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction .
T12091L	MM-589 TFA	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T17010	TC13172	Others	Others
	TC13172 is an inhibitor of mixed lineage kinase domain-like protein (EC50: 2 nM for HT-29 cells).
T26887	BOP
	BOP is anantagonist of alpha4beta1/alpha9beta1 integrins. BOP rapidly mobilizes long-term multi-lineage reconstituting hematopoietic stem cells (HSC).
T34604	Selenodicysteine
	Selenodicysteine is the 21st proteinogenic amino acid. Selenocysteine exists naturally in all three domains of life, but not in every lineage.
T78151	Bleximenib oxalate Menin-MLL inhibitor 24 oxalate	Epigenetic Reader Domain	Chromatin/Epigenetic
	Bleximenib (Menin-MLL inhibitor 24) oxalate 是一种用于癌症研究的menin-mixed-lineage leukemia 1（menin-MLL）抑制剂。
T12091	MM-589	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T39102	MLK-IN-1
	MLK-IN-1 (US20140256733A1, compound 68) is a highly potent and selective inhibitor of mixed lineage kinase 3 (MLK-3). It exhibits excellent brain penetration and specifically targets MLK-3.
T71620	iBAP-II
	iBAP-II represses neuroendocrine lineage-specific ASCL1/MYCL/E2F signaling in SCLC cell lines, and dramatically inhibits SCLC cell viability and tumor growth in vivo.
T79899	Cbl-b-IN-12	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-12 (Example 10)为casitas B系淋巴瘤（CBL-B）抑制剂，IC50值<100 nM。
T79731	MLKL-IN-6	Necroptosis	Apoptosis
	MLKL-IN-6（compound P28）是一种针对Mixed Lineage Kinase domain-like（MLKL）的混合谱系激酶抑制剂，具有抗纤维化的潜力。它能够抑制MLKL的磷酸化和寡聚化，从而抑制细胞坏死、免疫细胞死亡，并减少粘附因子的表达。MLKL-IN-6展现出低细胞毒性，并可抑制肝星状细胞的激活，从而降低肝纤维化标志物的水平。
T79896	Cbl-b-IN-9	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-9（Compound 300）为针对casitas B系淋巴瘤（Cbl-b）及c-Cbl的抑制剂，其IC50值分别为5.6 nM与4.7 nM。
T70677	PLS-123
	PLS-123 is a novel covalent irreversible Btk inhibitor with potential anti-proliferative activity. PLS-123 exhibited more potent anti-proliferative effects than ibrutinib in multiple cellular and in vivo preclinical models of B-cell lineage malignancy, including 14 kinds of cell lines, patients’ primary tumor cells and mouse xenograft model.
T79895	Cbl-b-IN-8	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-8 (Compound 293)，一种casitas B系淋巴瘤（Cbl-b）及c-Cbl的抑制剂，其IC50值分别为5.5 nM和7.8 nM。
T79894	Cbl-b-IN-7	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-7 (Compound 248)作为针对casitas B系淋巴瘤(Cbl-b)和c-Cbl的抑制剂，其IC50值分别为6.7 nM与5.2 nM。
T79897	Cbl-b-IN-10	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-10（Compound 463）为针对casitas B系淋巴瘤（Cbl-b）和c-Cbl的抑制剂，其IC50值分别为6.0 nM和3.5 nM。
T70593	GW-841819X
	GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X displayed activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia. Bromodomain and extra-terminal (BET) proteins belong to a class of proteins collectively called epigenetic readers". BET bromodomains have emerged as promising drug targets for treatment of cancers
T78904	Anticancer agent 110	Apoptosis	Apoptosis
	Anticanceragent 110 是抗癌化合物，表现出体外抗肿瘤活性和对抗白血病的卓越效力。该化合物在 K-562 慢性粒细胞白血病细胞系中展示了显著的纳摩尔级别细胞毒性，并能引发 DNA 损伤和细胞凋亡(apoptosis)。
T79893	Cbl-b-IN-6	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-6 (Compound 246)，作为casitas B系淋巴瘤（Cbl-b）和c-Cbl的抑制剂，其IC50值分别为5.8 nM和4.4 nM。
T79898	Cbl-b-IN-11	E1/E2/E3 Enzyme	Ubiquitination
	Cbl-b-IN-11 (Compound 466)作为casitas B系淋巴瘤 (Cbl-b) 及c-Cbl的抑制剂，显示出对Cbl-b和c-Cbl的高度选择性，其IC50值分别为6.4 nM 和6.1 nM。
T76052	ELA-32(human) TFA
	ELA-32(human) TFA is a potent, high affinityapelin receptoragonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
T28630	RX-37 RX37
	RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell
T69624	TC-5115
	TC-5115 is a potent inhibitor of MLL methyltransferase with IC50 value of 16 nM. TC-5115 may lead to the development of a new therapy for the treatment of human MLL leukemia. The mixed-lineage leukemia (MLL) protein, also known as MLL1, is a lysine methyltransferase specifically responsible for methylation of histone 3 lysine 4. MLL has been pursued as an attractive therapeutic target for the treatment of acute leukemia carrying the MLL fusion gene or MLL leukemia.
T69014	Sekikaic Acid
	Sekikaic acid is a phenolic lichen metabolite that has been found in H. obscurata and has diverse biological activities. It scavenges superoxide and DPPH radicals in cell-free assays when used at a concentration of 0.5 µM. Sekikaic acid is active against the rg recombinant strain of respiratory syncytial virus (RSV; IC50 = 5.69 µg/ml). It inhibits the protein-protein interaction between mixed lineage leukemia 1 (MLL1) and the GACKIX domain of CREB-binding protein (CBP; IC50 = 34 µM).
T69629	M‑89 MLL inhibitor
	M‑89 is a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein−Protein Interaction (Kd = 1.4 nM; IC50 = 25nM). M-89 binds to menin with a Kd value of 1.4 nM and effectively engages cellular menin protein at low nanomolar concentrations. M-89 inhibits cell growth in the MV4;11 and MOLM-13 leukemia cell lines carrying MLL fusion with IC50 values of 25 and 55 nM, respectively, and demonstrates >100-fold selectivity over the HL-60 leukemia cell line lacking MLL fusion.
T82763	CD33 splicing modulator 1 hydrochloride
	"CD33splicing modulator 1 (Compound 1) hydrochloride 是一种调节CD33/Siglec 3活性的化合物。CD33/Siglec 3 为髓系细胞表面受体，涉及小胶质细胞功能。该化合物通过提升细胞mRNA池中外显子2的剪接变异，展现在神经退行性疾病研究中的应用潜力，包括阿尔茨海默病。"
T74681	NecroIr2
	NecroIr2 是一种铱 (III) 复合物，是顺铂 (Cisplatin) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr2 选择性积累在线粒体中，导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr2 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL)，调节CDK4表达。
T82598	DDO-2213
	DDO-2213是一口服有效的WDR5-MLL1抑制剂，具有29 nM的IC50和72.9 nM的Kd值针对WDR5蛋白。该化合物对MLL组蛋白甲基转移酶活性及MLL易位细胞增殖具有选择性抑制作用，可用于研究MLL融合型白血病。
T74680	NecroIr1
	NecroIr1 是一种铱 (III) 复合物，是顺铂 (Cisplatin) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr1 选择性积累在线粒体中，导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr1 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL)，调节CDK4表达。
TP2097	ELA-32(human) ELA-32 (human)
	Potent, high affinity apelin receptor agonist (IC50 = 0.27 nM; Kd = 0.51 nM). Exhibits no binding GPR15 and GPR25. Activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. Also potentiates the T
T64072	Cbl-b-IN-2
	Cbl-b-IN-2 是一种口服具有活力的生物化合物，能够抑制泛素蛋白酶体通路中的 E3 酶Casitas b 系淋巴瘤原癌基因-b (Cbl-b)，可以用于调节免疫系统和易受免疫系统调节疾病的研究。Cbl-b-IN-2 也能够单独或与一种或多种免疫检查点抑制剂，抗肿瘤剂和放射剂联合应用于癌症的研究。
T36574	GW841819X GW841819X
	GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70...

化合物

Cat.No: T11520

Target: MLK, VEGFR

Cat.No: T6057

Target: ROCK, MLK, VEGFR, SGK, DNA Alkylation, Trk receptor, c-Met/HGFR, LRRK2, MEK, IGF-1R, Syk, Bcr-Abl, CDK, Src, Aurora Kinase, Autophagy

Necrosulfonamide

Cat.No: T6904

Synonym: (E)-Necrosulfonamide

Target: MLK

Menin-MLL inhibitor 20

Cat.No: T9399

Target: Epigenetic Reader Domain, Histone Methyltransferase

Y-27632 dihydrochloride

Cat.No: T1725

Synonym: 反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐,Y-27632 2HCl

Target: ROCK, Apoptosis

Cat.No: T3082

Target: Histone Methyltransferase

Cat.No: T77245

Target: Endogenous Metabolite

Cat.No: T11925

Target: Epigenetic Reader Domain, Histone Methyltransferase

Eltrombopag Olamine

Cat.No: T6825

Synonym: Promacta Olamine,Revolade,艾曲泊帕乙醇胺盐,Eltrombopag diethanolamine salt,SB497115,艾曲波帕乙醇胺盐,SB-497115GR

Target: Thrombin

Cat.No: T8768

Synonym: HMTase Inhibitor IX TFA

Target: Histone Methyltransferase

Cat.No: T36944

Target: Nucleoside Antimetabolite/Analog

Cat.No: T24471

Menin-MLL inhibitor 4

Cat.No: T12002

Target: Others

Cat.No: T12091L

Target: JAK

Cat.No: T17010

Target: Others

Cat.No: T26887

Selenodicysteine

Cat.No: T34604

Bleximenib oxalate

Cat.No: T78151

Synonym: Menin-MLL inhibitor 24 oxalate

Target: Epigenetic Reader Domain

Cat.No: T12091

Target: JAK

Cat.No: T39102

Cat.No: T71620

Cat.No: T79899

Target: E1/E2/E3 Enzyme

Cat.No: T79731

Target: Necroptosis

Cat.No: T79896

Target: E1/E2/E3 Enzyme

Cat.No: T70677

Cat.No: T79895

Target: E1/E2/E3 Enzyme

Cat.No: T79894

Target: E1/E2/E3 Enzyme

Cat.No: T79897

Target: E1/E2/E3 Enzyme

Cat.No: T70593

Anticancer agent 110

Cat.No: T78904

Target: Apoptosis

Cat.No: T79893

Target: E1/E2/E3 Enzyme

Cat.No: T79898

Target: E1/E2/E3 Enzyme

ELA-32(human) TFA

Cat.No: T76052

Cat.No: T28630

Synonym: RX37

Cat.No: T69624

Cat.No: T69014

M‑89 MLL inhibitor

Cat.No: T69629

CD33 splicing modulator 1 hydrochloride

Cat.No: T82763

Cat.No: T74681

Cat.No: T82598

Cat.No: T74680

Cat.No: TP2097

Synonym: ELA-32 (human)

Cat.No: T64072

Cat.No: T36574

Synonym: GW841819X

Cat. No.	Product Name	Target	Signaling Pathways
T75661	Thymopentin acetate
	Thymopentin acetate为胸腺皮质及髓质上皮细胞主要分泌的生物活性肽，是一有效免疫调节剂，具有极短的血浆半衰期(30秒)，能促进自人类胚胎干细胞生成T细胞群。

天然产物

Thymopentin acetate

Cat.No: T75661

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