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68

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22223	3PO	Glucokinase; Autophagy	Autophagy; Metabolism
	3PO 是一种 PFKFB3 的小分子抑制剂，IC50值为22.9 μM。它抑制几种人类恶性造血和腺癌细胞系的增殖，IC50在1.4到24 μM 之间。它抑制葡萄糖摄取，并降低 Fru-2,6-BP、乳酸、ATP、NAD+ 和 NADH 的细胞内浓度。
T2121	SW033291	Dehydrogenase	Metabolism
	SW033291 是有效的15-PGDH 抑制剂，与15-PGDH 亲和力高，Ki 为 0.1 nM。它增加骨髓和其他组织中前列腺素 PGE2 的水平。它还可促进组织再生。
T11438	GNE-1858	Others; MAPK	MAPK; Others
	GNE-1858 是高效的 ATP 竞争性造血祖细胞激酶-1抑制剂，能够抑制野生型(IC50:1.9 nM)、活性模拟突变株 HPK1-TSEE (IC50:1.9 nM)、 HPK1-SA (IC50:4.5 nM)的活性。
T69730	F092 inhibitor
	F092 inhibitor, also called Prostaglandin D synthase (hematopoietic-type) inhibitor F092, is an inhibitor of hematopoietic-type prostaglandin D synthase (H-PGDS).
T3590	NSC23005	CDK	Cell Cycle/Checkpoint
	NSC23005 是一种 p18INK 抑制剂，可有效促进造血干细胞 (HSC) 扩增 (ED50: 5.21 nM)。
T1776L	Plerixafor octahydrochloride 盐酸普乐沙福,JM3100 octahydrochloride,Plerixafor 8HCl (AMD3100 8HCl),Plerixafor 8HCl,SID791 octahydrochloride,AMD 3100 octahydrochloride,JM 3100 8HCl	Virus Protease; HIV Protease; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Plerixafor octahydrochloride (JM3100 octahydrochloride) 是一种选择性的CXCR4拮抗剂，IC50为 44 nM。Plerixafor 是一种具有造血干细胞动员活性的双环霉素。
T8883	Pizuglanstat	Others; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Others
	Pizuglanstat 是一种前列腺素 D 合酶抑制剂，对人造血前列腺素 D 合酶的IC50为 76 nM，可用于肌再生性疾病研究。
T7948	HPGDS inhibitor 2 GSK-2894631A	PGE Synthase	Immunology/Inflammation
	HPGDS inhibitor 2 (GSK-2894631A) 是高效的造血前列腺素 D 合成酶(H-PGDS)选择性抑制剂(IC50:9.9 nM)。
T24580	P18IN003 P18IN 003,P18IN-003	CDK	Cell Cycle/Checkpoint
	P18IN003 是一种具有选择性和有效性的 p18(INK4C) 抑制剂，可抑制 p18 蛋白的活性可用于研究造血干细胞的体外扩增。
T16699	PYZD-4409	Others; E1/E2/E3 Enzyme	Others; Ubiquitination
	PYZD-4409 是一种特异性 UBA1 抑制剂，IC50 为 20 μM。 PYZD-4409 在恶性细胞中诱导细胞死亡，并且对恶性细胞的细胞毒性优于对正常造血细胞的细胞毒性。
T3589	NSC23005 Sodium	CDK	Cell Cycle/Checkpoint
	NSC23005 sodium 是新型 p18 抑制剂 (ED50=5.21 nM)，在小鼠和人类模型中促进造血干细胞扩增。
T21785	AG957	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Tyrphostin AG957 是一种酪氨酸激酶抑制剂，具有抗BCR/ABL 酪氨酸激酶活性。它能够抑制p210bcr/abl 酶活性 (IC50:2.9 μM)。
T1804	HPGDS inhibitor 1 HPGDS-inhibitor-1	PGE Synthase	Immunology/Inflammation
	HPGDS inhibitor 1 是口服具有活性的HPGDS 选择性抑制剂，在酶和细胞分析中的IC50值分别为 0.6 nM 和 32 nM，但对 L-PGDS、mPGES、COX-1、COX-2 、5-LOX 无抑制作用。
T60081	BV02 2-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1,3-dioxoisoindoline-5-carboxylic acid	Others	Others
	BV02 是 14-3-3 蛋白-蛋白相互作用的抑制剂，可用于治疗慢性粒细胞白血病的研究。 BV02 破坏表达 IM 抗性 T315I 突变和 IM 敏感的野生型 Bcr-Abl 的造血细胞。
T8836	CY5-SE triethylamine salt Fluorolink Cy5 triethanolamine salt,Cy5-SE (triethylamine salt)	Others	Others
	CY5-SE triethylamine salt (Fluorolink Cy5 triethanolamine salt) 是一种用于标记肽, 蛋白质, 寡核苷酸的氨基基团的反应染料 (Ex=649 nm; Em=670 nm)。
T11053	DJ001	Phosphatase	Metabolism
	DJ001 是一种高度特异性，选择性和非竞争性的蛋白酪氨酸磷酸酶-σ (PTPσ) 抑制剂，IC50 为 1.43 μM。DJ001 对其他磷酸酶无抑制活性，对蛋白质磷酸酶 5 仅有中等抑制活性。DJ001 促进造血干细胞再生。
T9017	HPK1-IN-2 Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2,HPK1-IN-2	Others; FLT; Src	Angiogenesis; Others; Tyrosine Kinase/Adaptors
	HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) 是一种有效且具有口服活性的造血祖细胞激酶-1 抑制剂(HPK1；IC50<0.05 µM)。它还抑制 Lck (0.05 µM<IC50<0.5 µM) 和 Flt3 (IC50<0.05 µM) 激酶活性，具有抗肿瘤活性。
T76870	Narsoplimab OMS 721	SARS-CoV	Microbiology/Virology
	Narsoplimab (OMS 721) 是一种选择性全人免疫球蛋白γ 4 (IgG4) 单克隆抗体，是一种甘露聚糖结合凝集素相关的丝氨酸蛋白酶-2（MASP-2）抑制剂，可结合 MASP-2 并阻止凝集素通路激活，对凝集素通路有抑制作用。Narsoplimab 可用于研究成人造血干细胞移植相关疾病。
T22070	DBIBB	LPA Receptor	GPCR/G Protein
	DBIBB 是一种特异性溶血磷脂酸 (LPA2) 的 2 型 G 蛋白偶联受体的非脂质激动剂，是一种能够治疗高强度γ 射线对造血和胃肠系统引起的急性放射综合征的潜在活性分子，是一种作未有机合成和药物研究中的中间体。 DBIBB 可用于制备各种化合物，可减轻胃肠道辐射综合征，增加肠隐窝存活率和肠细胞增殖，并减少细胞凋亡。
T21493	Cyclosporin H	Others	Others
	Cyclosporin H 是一种 FPR-1(甲酰肽受体 1) 的选择性强效抑制剂。它缺乏 Cyclosporin A 具有的免疫抑制活性。它是一种病毒转导增强剂，可使人脐带血来源的造血干细胞和祖细胞中慢病毒转导增强 10 倍。它与雷帕霉素或前列腺素 E2 联合使用时表现出累加效应。
T24870	TFC-007 TFC007
	TFC-007 is an inhibitor of hematopoietic prostaglandin D synthase.
T39709	HPK1-IN-19 HPK1-IN-19
	HPK1-IN-19 is an inhibitor of hematopoietic progenitor kinase 1 (HPK1).
T40188	HPK1-IN-20 HPK1-IN-20
	HPK1-IN-19 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1).
TP2339	Goralatide
	Goralatide, isolated from fetal calf bone marrow, exerts a high inhibitory activity on the proliferation of hematopoietic pluripotent stem cells.
T29166	XIE18-6 XIE186
	XIE18-6, a novel INK4C inhibitor, specifically blocks the bioactivity of p18 protein and promotes human and murine hematopoietic stem cell ex vivo expansion.
T26887	BOP
	BOP is anantagonist of alpha4beta1/alpha9beta1 integrins. BOP rapidly mobilizes long-term multi-lineage reconstituting hematopoietic stem cells (HSC).
T27591	II-B08 II-B 08,FAP1 Inhibitor,II-B-08,LMWPTP Inhibitor,Lyp Inhibitor III,CD45 Inhibitor V
	II-B08 is a cell-permeable SHP2 inhibitor (IC50 = 5.5 µM). II-B08 blocks growth factor stimulated ERK1/2 activation and hematopoietic progenitor proliferation.
T10046	16,16-Dimethyl prostaglandin E2 16,16-dimethyl PGE2	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	16,16-Dimethyl prostaglandin E2 is an orally active vertebrate Hematopoietic stem cells homeostasis critical regulator. It can act through EP2/EP4 and has an interaction with the Wnt pathway.
T37603	Osteogenic Growth Peptide (10-14)
	YGFGG, C-terminal pentapeptide fragment of the osteogenic growth peptide (OGP), (H-8640), showed the full spectrum of OGP-like bioactivities. It has attracted considerable interest as bone anabolic agent and hematopoietic stimulator.
T72052	HPK1-IN-34
	HPK1-IN-34是一种造血祖细胞激酶1(HPK1)抑制剂，IC50<100nM。
T72036	HPK1-IN-36	Others	Others
	HPK1-IN-36（compound 2）作为一种HPK1抑制剂，表现出高效性，其IC50为0.5 nM。
T33267	Me6TREN 4HCl Me6TREN Tetrahydrochloride,Me6-TREN Tetrahydrochloride,Me6 4HCl,Me 6 4HCl,Me-6 4HCl
	Me6TREN 4HCl is a potent and efficacious mobilizing agent of hematopoietic stem and progenitor cells (HSPCs) that can act by activating MMP-9 expression and disrupting the SDF-1α/CXCR4 axis, exhibiting more significant mobilizing effects than G-CSF or AMD
T77993	Goralatide acetate
	Goralatide为一种内源性四肽，作为造血生理调节剂。该化合物能够抑制原始造血细胞的增殖。
T62859	MEIS-IN-1
	MEIS-IN-1 是一种有效的诱导小鼠和人类造血干细胞扩增的 MEIS 抑制剂。
T63046	HPK1-IN-15
	HPK1-IN-15 是一种选择性的、有效的 HPK1 抑制剂。其中从造血祖细胞克隆的造血祖细胞激酶1 (HPK1) 属于 MAP4Ks 家族。HPK1-IN-15 能够用于与 HPK1 活性相关的疾病或病症 (如癌症) 的研究、预防或改善。
T62547	HPK1-IN-17
	HPK1-IN-17 是一种选择性的、有效的 HPK1 抑制剂。造血祖细胞激酶1 (HPK1) 是 MAP4Ks 的家族成员，从造血祖细胞克隆。HPK1-IN-17 能够用于研究、预防或改善与 HPK1 活性相关的疾病或病症（如癌症）。
TP2141L	Balixafortide POL6326	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. Balixafortide blocks β-arresti
T15503	HQL-79	Others	Others
	HQL-79 is a selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor. It inhibits the synthesis of PGD2 and acts as an anti-allergic agent (Kd: 0.8 μM and IC50: 6 μM). It also shows no obvious effect on COX-1, COX-2, m-P
T13627	CP-10	CDK	Cell Cycle/Checkpoint
	CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.
T60973	HPK1-IN-24
	HPK1-IN-24 (example 51) 可用于癌症领域研究，它是造血祖细胞激酶 1 (HPK1)的抑制剂 (Ki = 100 nM)。
T78852	HPK1-IN-39
	HPK1-IN-39（Compound 10n）为一选择性HPK1抑制剂，IC50值为29 nM。该化合物能抑制SLP76磷酸化，可用于癌症免疫治疗研究。
T61449	HPK1-IN-18
	HPK1-IN-18 is a highly effective and specific HPK1 inhibitor. HPK1, a MAP kinase kinase kinase kinases (MAP4K) member, was initially isolated from hematopoietic progenitor cells. This compound, known as HPK1-IN-18, is valuable for investigating, preventing, or managing diseases or conditions linked to HPK1 activity, such as cancer[1].
T61733	HPK1-IN-25
	HPK1-IN-25 (示例 94) 为一种造血祖细胞激酶1 (HPK1) 抑制剂，具有129 nM的IC50值，展现出在癌症研究中的潜力。
T63661	HF51116
	HF51116 是 XCR4 的有效拮抗剂。HF51116 能够显著拮抗 SDF-1α 诱导的细胞迁移、钙动员和 CXCR4 内化，并利用 CXCR4 抑制 HIV-1 感染。HF51116 对HIV-1感染、造血干细胞动员和癌症转移表现出研究潜力。
T76748	Foralumab
	Foralumab（NI-0401）为口服有效的人源化单克隆抗体，针对CD3进行靶向。其能够调控NSG小鼠体内，由人类造血干细胞重建的人类细胞的免疫反应。
T36545	Prostaglandin D2 methyl ester Prostaglandin D2 methyl ester
	Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2.
T75752	N-Acetyl-Ser-Asp-Lys-Pro acetate
	N-Acetyl-Ser-Asp-Lys-Pro (Ac-SDKP) acetate 是血管紧张素转换酶 (ACE) N 端活性位点的特异性底物。N-Acetyl-Ser-Asp-Lys-Pro acetate 是多能干细胞增殖的天然抑制剂。N-Acetyl-Ser-Asp-Lys-Pro acetate 具有抗炎和抗纤维化特性。
T61250	HPGDS inhibitor 3
	HPGDS inhibitor 3 is a powerful oral compound that selectively inhibits the hematopoietic prostaglandin D synthase (H-PGDS). With an IC50 value of 9.4 nM and EC50 of 42 nM, it demonstrates high potency in peripherally restricting H-PGDS. Moreover, HPGDS inhibitor 3 exhibits excellent selectivity with no associated central nervous system toxicity. This compound also possesses favorable pharmacokinetic properties in mouse, rat, and dog models. Additionally, HPGDS inhibitor 3 displays noteworthy an...
T63659	HPK1-IN-10
	HPK1-IN-10 是 HPK1 的有效抑制剂。HPK1 是一种丝氨酸/苏氨酸蛋白激酶，由造血祖细胞克隆得到，是哺乳动物Ste-20相关蛋白激酶MAP4K 家族成员之一。HPK1-IN-10 对HPK1 相关疾病具有研究潜力。
T36296	BIO5192 hydrate
	BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days...

化合物

Cat.No: T22223

Target: Glucokinase, Autophagy

Cat.No: T2121

Target: Dehydrogenase

Cat.No: T11438

Target: Others, MAPK

Cat.No: T69730

Cat.No: T3590

Target: CDK

Plerixafor octahydrochloride

Cat.No: T1776L

Synonym: 盐酸普乐沙福,JM3100 octahydrochloride,Plerixafor 8HCl (AMD3100 8HCl),Plerixafor 8HCl,SID791 octahydrochloride,AMD 3100 octahydrochloride,JM 3100 8HCl

Target: Virus Protease, HIV Protease, CXCR

Cat.No: T8883

Target: Others, Prostaglandin Receptor

HPGDS inhibitor 2

Cat.No: T7948

Synonym: GSK-2894631A

Target: PGE Synthase

Cat.No: T24580

Synonym: P18IN 003,P18IN-003

Target: CDK

Cat.No: T16699

Target: Others, E1/E2/E3 Enzyme

NSC23005 Sodium

Cat.No: T3589

Target: CDK

Cat.No: T21785

Target: Bcr-Abl

HPGDS inhibitor 1

Cat.No: T1804

Synonym: HPGDS-inhibitor-1

Target: PGE Synthase

Cat.No: T60081

Synonym: 2-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1,3-dioxoisoindoline-5-carboxylic acid

Target: Others

CY5-SE triethylamine salt

Cat.No: T8836

Synonym: Fluorolink Cy5 triethanolamine salt,Cy5-SE (triethylamine salt)

Target: Others

Cat.No: T11053

Target: Phosphatase

Cat.No: T9017

Synonym: Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2,HPK1-IN-2

Target: Others, FLT, Src

Cat.No: T76870

Synonym: OMS 721

Target: SARS-CoV

Cat.No: T22070

Target: LPA Receptor

Cat.No: T21493

Target: Others

Cat.No: T24870

Synonym: TFC007

Cat.No: T39709

Synonym: HPK1-IN-19

Cat.No: T40188

Synonym: HPK1-IN-20

Cat.No: TP2339

Cat.No: T29166

Synonym: XIE186

Cat.No: T26887

Cat.No: T27591

Synonym: II-B 08,FAP1 Inhibitor,II-B-08,LMWPTP Inhibitor,Lyp Inhibitor III,CD45 Inhibitor V

16,16-Dimethyl prostaglandin E2

Cat.No: T10046

Synonym: 16,16-dimethyl PGE2

Target: Prostaglandin Receptor

Osteogenic Growth Peptide (10-14)

Cat.No: T37603

Cat.No: T72052

Cat.No: T72036

Target: Others

Cat.No: T33267

Synonym: Me6TREN Tetrahydrochloride,Me6-TREN Tetrahydrochloride,Me6 4HCl,Me 6 4HCl,Me-6 4HCl

Goralatide acetate

Cat.No: T77993

Cat.No: T62859

Cat.No: T63046

Cat.No: T62547

Cat.No: TP2141L

Synonym: POL6326

Target: CXCR

Cat.No: T15503

Target: Others

Cat.No: T13627

Target: CDK

Cat.No: T60973

Cat.No: T78852

Cat.No: T61449

Cat.No: T61733

Cat.No: T63661

Cat.No: T76748

Prostaglandin D2 methyl ester

Cat.No: T36545

Synonym: Prostaglandin D2 methyl ester

N-Acetyl-Ser-Asp-Lys-Pro acetate

Cat.No: T75752

HPGDS inhibitor 3

Cat.No: T61250

Cat.No: T63659

BIO5192 hydrate

Cat.No: T36296

Cat. No.	Product Name	Target	Signaling Pathways
TN2883	3',4'-Dimethoxyflavone	Others; PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair; Others
	3',4'-Dimethoxyflavone 是类黄酮化合物的参考标准，类黄酮化合物具有多种药用活性。
T31836	Folate sodium Folic acid, monosodium salt,Folvite sodium
	Folate sodium, as a member of the vitamin B family, can stimulate the hematopoietic system. Folic acid can be used in the treatment and prevention of folate deficiencies and megaloblastic anemia.
TN5094	Tangshenoside I	Glucokinase	Metabolism
	Tangshenoside I might be a potential bioactive marker related to the hematopoietic and immunologic functions of Codonopsis Radix, which could be recommended as the index compound. It has α-glucosidase inhibition activity.

天然产物

3',4'-Dimethoxyflavone

Cat.No: TN2883

Target: Others, PARP

Cat.No: T31836

Synonym: Folic acid, monosodium salt,Folvite sodium

Tangshenoside I

Cat.No: TN5094

Target: Glucokinase

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