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94

抑制剂 & 化合物

2

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Cat. No.	Product Name	Target	Signaling Pathways
T7080	CCT245737 SRA737	Chk	Cell Cycle/Checkpoint
	CCT245737 (SRA737) 是一种具有口服活性的选择性 Chk1 抑制剂，IC50值为 1.3 nM。
T6093	AZD-7762 AZD7762	Chk	Cell Cycle/Checkpoint
	AZD-7762 是一种有效的 ATP 竞争性的细胞周期检测点激酶抑制剂，抑制 Chk1的 IC50为 5 nM。
T5697	BMS-1166	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	BMS-1166 是 PD-1/PD-L1免疫检查点抑制剂。它促使 PD-L1 形成 PD-L1 同源二聚体，进而阻断其与 PD-1 的相互作用，其 IC50为 1.4 nM。它阻断了 PD-1/PD-L1 免疫检查点对 T 细胞活化的抑制作用。
T21331	SAR-020106	Chk	Cell Cycle/Checkpoint
	SAR-020106 是一种强效、ATP 竞争性和选择性 CHK1 抑制剂，IC50为 13.3 nM。它对 CHK2 具有良好的选择性，可通过选择抗癌药物增强抗肿瘤活性。
T10565	BMS-1001 hydrochloride	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	BMS-1001 hydrochloride 是一种人 PD-L1/PD-1免疫检查点的抑制剂，具有口服活性且细胞毒性低。
T2517	SCH900776 MK 8776,MK-8776	Chk; CDK	Cell Cycle/Checkpoint
	SCH900776 (MK-8776) 是一种靶向细胞周期检查点激酶 1(Chk1) 的抑制剂，IC50值为 3 nM。它比对 CDK2 和 Chk2 的选择性分别高 50 和 500 倍，具有潜在的放射增敏和化学增敏活性。
T6084	Rabusertib LY2603618,IC-83	Chk; PDK; Autophagy	Autophagy; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling
	Rabusertib (IC-83) 是一种有效的选择性的Chk1抑制剂，IC50为 7 nM。它有潜在的化学增强活性，用于各种癌症和肿瘤治疗的试验。
T2033	BML-277 C 3742,Chk2 Inhibitor II,BML 277	Apoptosis; Chk	Apoptosis; Cell Cycle/Checkpoint
	BML-277 (C 3742) 是一种选择性的检测点激酶 2 抑制剂，IC50为 15 nM。
T6350	CHIR-124 CHIR124,CHIR 124	Apoptosis; GSK-3; FLT; Chk; PDGFR; Src	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	CHIR-124 是一种选择性 Chk1抑制剂，IC50值为 0.3 nM，可有效抑制 PDGFR 和 FLT3，IC50值分别为 6.6 nM 和 5.8 nM。
T7300	GDC-0575 ARRY-575,RG7741	Chk	Cell Cycle/Checkpoint
	GDC-0575 (ARRY-575) 是一种高选择性，有口服活性的小分子Chk1抑制剂，IC50值为1.2 nM。
T4327	Prexasertib dihydrochloride LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368	Apoptosis; Chk; S6 Kinase	Apoptosis; Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling
	Prexasertib dihydrochloride (LY2606368) 是一种选择性的，ATP 竞争性的细胞周期检测点激酶 1 抑制剂，Ki 为 0.9 nM，IC50为 <1 nM。它抑制 CHK2(IC50=8 nM) 和 RSK1 (IC50=9 nM)。它引起双链 DNA 断裂和复制突变，导致细胞凋亡，有抗肿瘤活性。
T4310	Prexasertib 5-[[5-[2-(3-氨基丙氧基)-6-甲氧基苯基]-1H-吡唑-3-基]氨基]-2-吡嗪甲腈,LY2606368	Apoptosis; Chk	Apoptosis; Cell Cycle/Checkpoint
	Prexasertib (LY2606368) 是一种具有潜在抗肿瘤活性的检查点激酶 1 抑制剂。它可引起双链 DNA 断裂和复制突变，导致细胞凋亡。
T6028	PF 477736 PF 00477736,PF-477736,PF-736,PF-00477736,PF477736	c-Fms; VEGFR; FGFR; FLT; c-RET; Chk; CDK; Src; Aurora Kinase	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
	PF 477736 (PF-736,PF-00477736) 是一种特异性、有效且具有 ATP 竞争性的 Chk1 抑制剂，Ki 值为0.49 nM。它也是Chk2抑制剂，Ki 值为 47 nM。它还抑制VEGFR2、Fms、Yes、Aurora-A、FGFR3、Flt3和Ret。
T2077	Adavosertib AZD1775,MK-1775,Adavosertib (MK-1775)	Wee1	Cell Cycle/Checkpoint
	Adavosertib (MK-1775) 是一种Wee1抑制剂，IC50值为 5.2 nM。它阻碍了 G2 DNA 损伤检查点。
T9252	LY2880070	Chk	Cell Cycle/Checkpoint
	LY2880070 是一种用于癌症治疗的新型检查点激酶 1 (CHK1) 抑制剂。
T10791	CHK1-IN-3	Chk	Cell Cycle/Checkpoint
	CHK1-IN-3 是一种检测点激酶 (CHK1) 抑制剂，IC50 值为 0.4 nM。
T6931	PD0166285 PD-166285	Apoptosis; Wee1; Chk	Apoptosis; Cell Cycle/Checkpoint
	PD0166285是 P-gp 的底物，是一种有效的 Wee1 和 Chk1 抑制剂弱抑制。
T10792L	CHK1-IN-4 hydrochloride CHK1-IN-4 hydrochloride（2120398-41-4 Free base）	Chk	Cell Cycle/Checkpoint
	CHK1-IN-4 hydrochloride 是有效的checkpoint kinase 1 (chk1) 抑制剂，对肿瘤细胞中 chk1 磷酸化具有有效的抑制作用。CHK1-IN-4 hydrochloride 显示出抗肿瘤活性。
T10406	Tuvusertib M1774,ATR inhibitor 1	Apoptosis; ATM/ATR; Others; Chk	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling
	Tuvusertib (M1774) 是一种可口服的共济失调毛细血管扩张和 Rad3相关(ATR)激酶抑制剂(Ki< 1 µΜ)，具有选择性和潜在的抗肿瘤活性。Tuvusertib 选择性抑制 ATR 活性，阻断丝氨酸/苏氨酸蛋白激酶检查点激酶1 (CHK1)的下游磷酸化，从而抑制 DNA 损伤检查点激活，破坏 DNA 损伤修复，诱导肿瘤细胞凋亡。
T3700	SCH900776 (S-isomer) MK-8776 S-isomer,SCH900776 S-isomer	Chk; CDK	Cell Cycle/Checkpoint
	SCH900776 S-isomer (MK-8776 S-isomer) 是SCH900776的S 型同分异构体。
T14765	BOS-172722	Kinesin	Cytoskeletal Signaling
	BOS-172722 是一种单极纺锤体 1 (MPS1) 检查点抑制剂，对MPS1 (1 mM ATP) 和P-MPS1 的IC50值分别为 11 nM 和 63 nM。它可研究多种乳腺癌。
T35362	NSC622608	Others	Others
	NSC622608 是 V 域 Ig 抑制 T 细胞活化 (VISTA) 的小分子配体，VISTA 是影响 T 细胞攻击肿瘤能力的免疫检查点。
T16446	PD 407824 PD-407824	Wee1; Chk	Cell Cycle/Checkpoint
	PD 407824 是一种化学 BMP 增敏剂，能促进细胞对亚阈值量 BMP4 的敏感性提高。PD 407824 是一种高效的检查点激酶 Chk1 和 WEE1 抑制剂（IC50 分别为 47 和 97 nM）。
T9906	Ipilimumab	Others	Others
	Ipilimumab 是全人类单克隆抗体 IgG1κ，能够抗 CTLA-4。其中CTLA-4是一种由活化的 T 细胞产生的免疫抑制分子。
T9907	Nivolumab	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	Nivolumab 是PD-1抗体类抑制剂，可用于研究晚期（转移性）非小细胞肺癌。
T77471	Tinurilimab BAY 1834942
	Tinurilimab (Bay 1834942) 是一种单克隆抗体，靶向并抑制 CEACAM6，CEACAM6 属于免疫检查点调节剂。 Tinurilimab 可用于效应 T 细胞对抗肿瘤的研究。
T2440	IC261 SU-5607	Apoptosis; Casein Kinase; CDK	Apoptosis; Cell Cycle/Checkpoint; Metabolism; Stem Cells
	IC261 (SU-5607) 是一种选择性的，ATP 竞争性的CK1抑制剂，可触发有丝分裂检查点控制。对Ckiδ、Ckiε、 Ckiα1 和Cdk5的IC50值分别为 1 μM、1 μM 、16 μM 和4.5mM。
T6543	Indoximod NLG-8189,Indoximod (NLG-8189）,1-Methyl-D-tryptophan,吲哚莫德	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Indoximod (Indoximod (NLG-8189)) 是一种具有口服具有活力的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。它在调节 mTOR 中充当 Trp 模拟物。它是一种可用于癌症研究的免疫代谢佐剂。
T76750	Cemiplimab REGN-2810,SAR-439684	Others	Others
	Cemiplimab (Anti-Human PD-1) 是一种针对程序性细胞死亡受体 1 （PD-1）的人单克隆抗体，也是一种检查点抑制剂，可阻断 PD-1/PD-L1 介导的 T 细胞抑制，可用于转移性癌症和鳞状细胞皮肤癌研究。
T76691	Monalizumab	IFNAR; Chk	Cell Cycle/Checkpoint; Immunology/Inflammation
	Monalizumab 是一种新型靶向自然杀伤细胞群 2A (NKG2A) 的免疫检查点抑制剂。Monalizumab 是一种人源化抗 NKG2A 的单克隆抗体，可促使 IFN-γ 产生，从而激活自然杀伤细胞功能。Monalizumab 具有抗肿瘤活性，可用于研究颈部鳞状细胞癌 (HNSCC)。
T77761	BMS-502	Others	Others
	BMS-502 是一种二酰基甘油激酶 (DGK) α 和 ζ 的强效双重抑制剂，诱导人和小鼠T细胞的免疫反应，阻断 T 细胞中细胞内检查点信号传导。BMS-502 以剂量依赖的方式刺激免疫反应，可用于研究与免疫相关的疾病。
T15576	Indibulin 2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Indibulin (D 24851) 是一种口服有效的微管蛋白合成抑制剂，具有抗有丝分裂和抗肿瘤活性，且神经毒性小。它降低了肌间神经张力，产生异常的纺锤体，激活有丝分裂检查点蛋白 Mad2 和 BubR1，并诱导有丝分裂停滞和细胞凋亡。
T27407	GDC0575 monohydrochloride ARRY-575,GDC-0575,GDC 0575,ARRY575,GDC0575	Chk	Cell Cycle/Checkpoint
	GDC0575 monohydrochloride (ARRY575) 是一种有效的、选择性的细胞周期检查点激酶 1(Chk1) 抑制剂，IC50 为 1.2 nM。GDC0575 monohydrochloride (ARRY575) 特异性结合并抑制 Chk1；这可能导致肿瘤细胞在 S 期和 G2/M 期绕过 Chk1 依赖性细胞周期停滞，从而允许细胞在进入有丝分裂之前进行 DNA 修复。
T6093L	AZD7762 HCl AZD7762 Hydrochloride
	AZD7762 HCl is a checkpoint kinase inhibitor, driving checkpoint abrogation and enhancing DNA-targeted treatment.
T24768	SC-203885 SC 203885,SC203885
	SC-203885 is a checkpoint kinase 2 inhibitor.
T23447	TCS 2312	Others	Others
	checkpoint kinase 1 (chk1) inhibitor
T68895	CBP-93872
	CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy.
T23865	CCT-271850 MPS1-IN-77,MPS1IN77,CCT271850,CCT 271850,MPS1 IN 77
	CCT-271850 is an inhibitor of the spindle checkpoint function of Monospindle 1.
T10790	CHK1-IN-2	Chk	Cell Cycle/Checkpoint
	CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).
T70553	CCT245737(S)
	CCT245737(S) is a highly selective oral checkpoint kinase 1 (CHK1) inhibitor.
T17223	VER-00158411	Chk	Cell Cycle/Checkpoint
	VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).
T69163	BML277 Acid
	BML277 Acid is a metabolite of BML277 which is a selective checkpoint kinase 2 inhibitor.
T70286	BMS-37
	BMS-37 is a novel inhibitor of PD-1/PD-L1 immune checkpoint.
T14904	CCT244747	Chk	Cell Cycle/Checkpoint
	CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).
T69091	CBP501
	CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle.
T10792	CHK1-IN-4	Chk	Cell Cycle/Checkpoint
	CHK1-IN-4 is a potent inhibitor of checkpoint kinase 1 (chk1) and potently inhibits chk1 phosphorylation in the tumor cells with anti-tumor activity.
T10272	AHR antagonist 5	Others	Others
	AHR antagonist 5 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist(example 39; IC50 < 0.5 μΜ). It significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
T16848	SB-218078	Chk; PKC	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling
	SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 inhibitor that inhibits Chk1 phosphorylation of cdc25C (IC50: 15 nM).
T71032	Melafolone
	Melafolone is a natural dual inhibitor of cox-2 and egfr, improving program death 1 (pd-1) checkpoint blockade therapy through normalizing tumor vasculature and pd-l1 downregulation
TP1076	AUNP-12 NP-12
	AUNP-12, a new immune checkpoint modulator, is an inhibitor of the PD-1 pathway.

化合物

Cat.No: T7080

Synonym: SRA737

Target: Chk

Cat.No: T6093

Synonym: AZD7762

Target: Chk

Cat.No: T5697

Target: PD-1/PD-L1

Cat.No: T21331

Target: Chk

BMS-1001 hydrochloride

Cat.No: T10565

Target: PD-1/PD-L1

Cat.No: T2517

Synonym: MK 8776,MK-8776

Target: Chk, CDK

Cat.No: T6084

Synonym: LY2603618,IC-83

Target: Chk, PDK, Autophagy

Cat.No: T2033

Synonym: C 3742,Chk2 Inhibitor II,BML 277

Target: Apoptosis, Chk

Cat.No: T6350

Synonym: CHIR124,CHIR 124

Target: Apoptosis, GSK-3, FLT, Chk, PDGFR, Src

Cat.No: T7300

Synonym: ARRY-575,RG7741

Target: Chk

Prexasertib dihydrochloride

Cat.No: T4327

Synonym: LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368

Target: Apoptosis, Chk, S6 Kinase

Cat.No: T4310

Synonym: 5-[[5-[2-(3-氨基丙氧基)-6-甲氧基苯基]-1H-吡唑-3-基]氨基]-2-吡嗪甲腈,LY2606368

Target: Apoptosis, Chk

Cat.No: T6028

Synonym: PF 00477736,PF-477736,PF-736,PF-00477736,PF477736

Target: c-Fms, VEGFR, FGFR, FLT, c-RET, Chk, CDK, Src, Aurora Kinase

Cat.No: T2077

Synonym: AZD1775,MK-1775,Adavosertib (MK-1775)

Target: Wee1

Cat.No: T9252

Target: Chk

Cat.No: T10791

Target: Chk

Cat.No: T6931

Synonym: PD-166285

Target: Apoptosis, Wee1, Chk

CHK1-IN-4 hydrochloride

Cat.No: T10792L

Synonym: CHK1-IN-4 hydrochloride（2120398-41-4 Free base）

Target: Chk

Cat.No: T10406

Synonym: M1774,ATR inhibitor 1

Target: Apoptosis, ATM/ATR, Others, Chk

SCH900776 (S-isomer)

Cat.No: T3700

Synonym: MK-8776 S-isomer,SCH900776 S-isomer

Target: Chk, CDK

Cat.No: T14765

Target: Kinesin

Cat.No: T35362

Target: Others

Cat.No: T16446

Synonym: PD-407824

Target: Wee1, Chk

Cat.No: T9906

Target: Others

Cat.No: T9907

Target: PD-1/PD-L1

Cat.No: T77471

Synonym: BAY 1834942

Cat.No: T2440

Synonym: SU-5607

Target: Apoptosis, Casein Kinase, CDK

Cat.No: T6543

Synonym: NLG-8189,Indoximod (NLG-8189）,1-Methyl-D-tryptophan,吲哚莫德

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T76750

Synonym: REGN-2810,SAR-439684

Target: Others

Cat.No: T76691

Target: IFNAR, Chk

Cat.No: T77761

Target: Others

Cat.No: T15576

Synonym: 2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851

Target: Apoptosis, Microtubule Associated

GDC0575 monohydrochloride

Cat.No: T27407

Synonym: ARRY-575,GDC-0575,GDC 0575,ARRY575,GDC0575

Target: Chk

Cat.No: T6093L

Synonym: AZD7762 Hydrochloride

Cat.No: T24768

Synonym: SC 203885,SC203885

Cat.No: T23447

Target: Others

Cat.No: T68895

Cat.No: T23865

Synonym: MPS1-IN-77,MPS1IN77,CCT271850,CCT 271850,MPS1 IN 77

Cat.No: T10790

Target: Chk

Cat.No: T70553

Cat.No: T17223

Target: Chk

Cat.No: T69163

Cat.No: T70286

Cat.No: T14904

Target: Chk

Cat.No: T69091

Cat.No: T10792

Target: Chk

AHR antagonist 5

Cat.No: T10272

Target: Others

Cat.No: T16848

Target: Chk, PKC

Cat.No: T71032

Cat.No: TP1076

Synonym: NP-12

Cat. No.	Product Name	Target	Signaling Pathways
TN3724	Cryptomoscatone D2	p53	Apoptosis
	Cryptomoscatone D2 is a highly efficacious inhibitor of the G(2) checkpoint, and G(2) checkpoint inhibitors can force cells arrested in G(2) phase by DNA damage to enter mitosis.
TN3721	Cryptofolione	Antifection	Microbiology/Virology
	Z-Cryptofolione and Cryptomoscatone D2 as highly efficacious inhibitors of the G(2) checkpoint, G(2) checkpoint inhibitors can force cells arrested in G(2) phase by DNA damage to enter mitosis. Cryptofolione shows moderate cytotoxicity in both macrophages and T. cruzi amastigotes, it also displays a mild inhibitory effect on the promastigote form of Leishmania spp.

天然产物

Cryptomoscatone D2

Cat.No: TN3724

Target: p53

Cat.No: TN3721

Target: Antifection

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