39
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9575 |
MRTX9768
|
Histone Methyltransferase | Chromatin/Epigenetic |
MRTX-9768 是一种有效的、选择性的、具有口服活性的 PRMT5-MTA 复合体抑制剂,可选择性靶向 MTAP/CDKN2A 缺失的肿瘤。 | |||
T13044 |
Mevociclib
SY-1365 |
CDK | Cell Cycle/Checkpoint |
Mevociclib (SY-1365) 是一种高效选择性 CDK7抑制剂,Ki 值为 17.4 nM。它具有抗血液肿瘤和侵袭性实体肿瘤作用,有抗增殖和凋亡活性。 | |||
T60152 |
AZ5576
|
CDK | Cell Cycle/Checkpoint |
AZ5576 是一种有效且高选择性的 CDK9抑制剂。AZ5576 可用于血液恶性肿瘤研究。 | |||
T1890 |
Pracinostat
SB939 |
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Pracinostat (SB939) 是一种组蛋白去乙酰化酶抑制剂,对 HDACs 的IC50值为 40-140 nM,可用于研究癌症。 | |||
T13058 |
T025
|
CDK | Cell Cycle/Checkpoint |
T025 是一种泛 CLK 抑制剂,对 CLK1-4 的 Kd 分别为 4.8、0.096、6.5、0.61 和 0.074 nM。 T025 在血液学和实体癌细胞系中表现出抗增殖活性,IC50 为 30-300 nM。 T025 可用于 MYC 驱动疾病的研究。 | |||
TQ0236 |
Tirabrutinib
ONO-4059,GS-4059,Velexbru |
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
Tirabrutinib (GS-4059) (ONO-4059) 是一种口服有效的高选择性 Bruton’s Tyrosine Kinase (BTK) 抑制剂 (能透过血脑屏障),其 IC50 值为 6.8 nM。Tirabrutinib 不可逆共价结合 BTK 并抑制异常 B 细胞受体信号传导。Tirabrutinib 可用于自身免疫性疾病和血液学恶性肿瘤的研究。 | |||
T38951 |
Isatuximab
SAR-650984,hu38SB19,Isatuximab-irfc |
Apoptosis; CD38 | Apoptosis; Immunology/Inflammation |
Isatuximab 是一种在血液系统恶性细胞中靶向跨膜受体和胞外酶 CD38 的单克隆抗体,是在多发性骨髓瘤中高度表达的蛋白。Isatuximab 具有抗肿瘤活性、抗体依赖性细胞介导的细胞毒性、补体依赖性细胞毒性、抗体依赖性细胞吞噬作用,可在无交联情况下直接诱导细胞凋亡 (apoptosis)。Isatuximab 对 CD38 胞外酶活性有抑制作用,这与许多细胞功能有关。 | |||
T19661 |
8-Chloroadenosine
NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷 |
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
8-Chloroadenosine (NSC-354258) 是一种 5' AMP 激活的蛋白激酶激动剂,可能用于治疗慢性淋巴细胞白血病。 它的活性与 mTOR 通路的抑制有关。它是一种核苷类似物。在体内代谢为 8-氯-ATP。在转录过程中掺入 RNA 并抑制 RNA 合成。在 MM.1S、RPMI-8226 和 U266 癌细胞系中表现出细胞毒性;在 A549 和 H1299 细胞中诱导 G2/M 细胞周期停滞和有丝分裂灾难。它已被证明可消耗 ATP 并抑制血液恶性肿瘤以及肺癌和乳腺癌细胞系中的肿瘤生长。 | |||
T11603 |
Ibrutinib-MPEA
|
Others | Others |
Ibrutinib-MPEA is ibrutinib derivative. Ibrutinib is a covalent and irreversible BTK inhibitor that has been used to treat hematological malignancies. | |||
T61337 |
PTG-0861
|
||
PTG-0861 is a highly specific inhibitor of histone deacetylase 6 (HDAC6), demonstrating an impressive IC50 value of 5.92 nm. This compound effectively triggers apoptosis and holds potential for research pertaining to acute myeloid leukemia, multiple myeloma, and other hematological cancers [1]. | |||
T21329 |
Gemcitabine monophosphate disodium salt
Gemcitabine monophosphate disodium salt monohydrate,Gemcitabine monophosphate disodium,GemMP |
||
R306465 is a novel HDAC inhibitor with broad-spectrum antitumor activity against solid (IC50: 30 to 300 nM) and hematological malignancies. R306465 was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro. | |||
T37077 |
Syk-IN-4
|
||
Syk-IN-4 is a potent, selective, and orally bioavailable inhibitor of SYK, demonstrating an IC50 of 0.31 nM. It targets SYK, which has been identified as a potential therapeutic target for autoimmunity and hematological cancers[1]. | |||
T76929 | Betifisolimab | ||
Betifisolimab (MSB-2311) 是一种针对PD-L1免疫抑制配体的人源化单克隆抗体。该化合物展现出针对晚期实体瘤和血液恶性肿瘤研究的潜力。 | |||
T63955 |
MU1656
|
||
MU1656 是一种有效和选择性的组蛋白甲基转移酶 DOT1L 抑制剂,IC50值为 2 nM。MU1656 可用于血液系统恶性肿瘤的研究。 | |||
T79839 |
Bocodepsin
OKI-179 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Bocodepsin (OKI-179) 是一种口服活性且选择性的HDAC抑制剂,展现出抗肿瘤效果。该化合物适用于抑制实体瘤及血液系统恶性肿瘤。 | |||
T61370 |
DNA-PK-IN-6
|
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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]. | |||
T83219 | ABBV-467 | ||
ABBV-467为选择性MCL-1抑制剂(Ki:<0.01 nM),能够诱导细胞凋亡(apoptosis),在血液恶性肿瘤(例如多发性骨髓瘤)模型中有效诱导癌细胞死亡并阻断肿瘤生长。 | |||
T77183 | Ripertamab | ||
Ripertamab (SCT400),一种重组人鼠嵌合抗CD20 IgG1κ单抗,主要用于研究血液系统恶性肿瘤,如非霍奇金淋巴瘤(NHL)。 | |||
T78516 |
NUC-7738
|
Others | Others |
NUC-7738为3'-脱氧腺苷(3'-dA)的5'-芳氧基氨基磷酸酯前药,其对一组血液癌细胞系表现出有效细胞毒活性,可用于癌症研究。 | |||
T14493 |
Balapiravir
R1626,Ro 4588161 |
Others | Others |
Balapiravir (R1626, Ro 4588161) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479). IC50 Value: Target: HCV Balapiravir was discontinued for safety reasons in 28-36% of patients (m | |||
T79810 |
Porcn-IN-2
|
||
Porcn-IN-2(Example 107)是Wnt信号通路的一种高效抑制剂,具有0.05 nM的IC50。该化合物适用于癌症、肉瘤、黑色素瘤、皮肤癌、血液肿瘤、淋巴瘤以及白血病等多种恶性肿瘤的研究。 | |||
T79840 |
Bocodepsin hydrochloride
OKI-179 hydrochloride |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Bocodepsin hydrochloride (OKI-179) 是一种口服活性的选择性HDAC抑制剂,具抗肿瘤特性,适用于治疗实体瘤和血液系统恶性肿瘤。 | |||
T69766 | Gusacitinib HCl | ||
Gusacitinib, also known as ASN-002 and EN-3351, is a potent dual inhibitor of SYK/JAK kinases. ASN002 showed strong antitumor activity in both hematological and solid tumor xenograft models. ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways as measured in pLAT and pSTAT assays, respectively. When profiled in a panel of 178 cell lines, ASN002 showed strong anti-proliferative activity in many lymphoid/leukemia cell lines, including SU-DHL-6, SU-DHL-4, OCI-LY10, H929 and... | |||
T79443 |
Syk-IN-8
|
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
Syk-IN-8(compound 19q)是一款Syk抑制剂,有效抗血液肿瘤细胞增殖。该化合物能够阻断PLCγ2的磷酸化过程,常用于血癌的科学研究。 | |||
T79798 |
PHD-IN-2
|
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
PHD-IN-2(Compound 91)是一种高效的PHD拮抗剂,具有IC50值小于5 nM,能在HEP3B细胞中诱导促红细胞生成素的合成,EC50值小于2.5 μM。此化合物主要用于心血管、代谢、血液、肺部、肾脏、肝脏疾病、伤口愈合以及癌症等研究领域。 | |||
T78277 |
ATG-031
|
||
ATG-031是一款人源化抗CD24单克隆抗体,能有效激活巨噬细胞介导的吞噬作用,阻断多种癌症细胞表面的“不要吃我”信号,诱导癌细胞清除。此抗体适用于血液恶性肿瘤和实体瘤研究。 | |||
T72527 |
Umbralisib sulfate
TGR-1202 sulfate ; RP-5264 sulfate,TGR-1202 sulfate,RP-5264 sulfate |
||
Umbralisib (TGR-1202) sulfate 是一种口服有效、选择性的 PI3Kδ和 酪蛋白激酶-1-ε (CK1ε) 双抑制剂,其 EC50分别为 22.2 nM 和 6.0 μM。 Umbralisib sulfate 显示出对慢性淋巴细胞白血病 (CLL) T 细胞独特的免疫调节作用。Umbralisib sulfate 可用于血液系统恶性肿瘤的研究。 | |||
T78708 |
JAK/HDAC-IN-2
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK/HDAC-IN-2 是一款高效的 JAK/HDAC 双靶点抑制剂,能在纳摩尔浓度范围内有效抑制 HDAC3/6 与 JAK1/2。此化合物不仅促进细胞凋亡,还能抑制组蛋白去乙酰化和 STAT3 磷酸化,对血液肿瘤和实体肿瘤细胞展现出了显著的抗增殖效果。 | |||
T76770 | Camidanlumab | ||
Camidanlumab (HuMax-TAC) 作为一种CD25单克隆抗体,专门针对细胞表面CD25抗原,该抗原在多种血液肿瘤中过度表达,而在正常组织的表达则有限。因其特定目标,Camidanlumab被广泛应用于合成抗体活性分子偶联物(ADCs),旨在针对包括淋巴瘤和白血病在内的多种疾病进行研究。 | |||
T69589 |
PX-316
|
||
PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg/kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor activity against early human MCF-7 breast cancer and HT-29 colon cancer xenografts in mice. PX-316 formulated in 20% hydroxypropyl-beta-cyclodextrin for intravenous administration is well tolerated in mice and rats with no hemolysis and no hematological toxicity. Thus, PX-316 is the... | |||
T71227 | LGB-321 HCl | ||
LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor). LGB321 is unique relative to previously described PIM inhibitors, in that it is active in PIM2 dependent cell lines. , a kinase that has proven difficult to inhibit in the cellular context. Consistent with its activity on all three PIM kinases, LGB321 inhibits proliferation of a number of cell lines derived from diverse hematological malignancies, including MM, AML, CML and B-Cel... | |||
T72465 |
Umbralisib tosylate
RP5264 tosylate,TGR-1202 tosylate ; RP5264 tosylate,TGR-1202 tosylate |
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Umbralisib (TGR-1202) tosylate是一种口服有效、具有选择性的PI3Kδ和酪蛋白激酶-1-ε (CK1ε) 双重抑制剂,EC50值分别为22.2 nM和6.0 μM。该化合物针对慢性淋巴细胞白血病 (CLL) 中的T细胞显示出独特的免疫调节作用,适用于血液系统恶性肿瘤的研究。 | |||
T34707 |
SST-02
SST 02,SST02 |
||
SST-02 is a potent cationic lipid for siRNA-Lipid Nanoparticles. SST-02 possesses a simple chemical structure and is synthesized just in one step. SST-02 showed an ID50 of 0.02 mg/kg in the factor VII (FVII) model. Rats administered with 3 mg/kg of SST-02 | |||
T80528 |
Ssm spooky toxin
SsTx Toxin |
Potassium Channel | Membrane transporter/Ion channel |
Ssm Spooky Toxin是从Scolopendra mutilans中分离出的化合物,其特点是有效抑制KCNQ(电压门控钾通道家族7)通道,表现出对血液和呼吸系统的致命毒性。Ssm Spooky Toxin对Kv7.4、Kv1.3和Shal通道的IC50值分别为2.8 μM、5.26 μM和0.1-0.3 M,且能够通过针对T细胞中的KV1.3通道抑制细胞因子的产生,在蜈蚣的循环系统中起着关键作用。 | |||
T69963 |
Birabresib dihydrate
|
||
Birabresib dihydrate was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibitor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and dif... | |||
T80919 |
Tumour-associated MUC1 epitope
|
||
Tumour-associated MUC1 epitope是一种具有标志性的生物活性肽。作为高度糖基化的I型跨膜糖蛋白MUC1的一部分,该肽通过特定的胞外结构域展现,该结构域包含20个氨基酸组成的可变数量串联重复序列(VNTR)。在多种人类腺癌及血液恶性肿瘤(如多发性骨髓瘤和B细胞淋巴瘤)中细胞表面表达过量,因此,MUC1是许多免疫治疗策略的关键靶点。 | |||
T37323 |
Succinyl-Coenzyme A sodium salt
Succinyl-CoA sodium salt,Succinyl-Coenzyme A (sodium salt),Succinyl-CoA |
Endogenous Metabolite | Metabolism |
Succinyl-Coenzyme A sodium salt(Succinyl-CoA sodium salt) 参与柠檬酸循环,在柠檬酸循环中转化为琥珀酸。Succinyl-Coenzyme A (sodium salt) 在生物体内参与多种代谢反应,在体内有着举足轻重的作用 Succinyl-Coenzyme A sodium salt 参与血红素的合成,可用于研究由营养性维生素 B12 缺乏症 (致使 Succinyl-Coenzyme A 合成缺乏) 所引起的代谢疾病、神经疾病和血液学异常导致的疾病。 | |||
T65387 | Paromomycin, sulfate (1:1) | ||
Paromomycin (Sulfate Salt) is an aminoglycoside that is active against Gram-negative and many Gram-positive bacteria as well as some protozoa and cestodes. Paromomycin in combination with sodium stibogluconate has proven to be effective in African and Indian VL (visceral leishmaniasis) and improves survival in African VL[3]. PS (Paromomycin Sulfate) is effective for elimination of B. coli without hematological side effects[4]. The activity of phosphoglucose isomerase was slightly inhibited by 10... | |||
T64692 |
AMY-101 acetate
|
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Complement component C3 plays a particularly versatile role in this process by keeping the cascade alert, acting as a point of convergence of activation pathways, fueling the amplification of the complement response, exerting direct effector functions, and helping to coordinate downstream immune responses[3]. In C3-/- mice alcohol-induced liver steatosis is absent or strongly reduced after chronic or acute alcohol exposure. This suggests that the complement system and its component C3 contribute... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0783 |
Mianserin hydrochloride
Mianserin HCl,Org GB 94,盐酸米安色林,ORG GB-94 HCl |
Dopamine Receptor; 5-HT Receptor; Opioid Receptor; Adrenergic Receptor; Histamine Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Mianserin hydrochloride (Org GB 94) 是一种有抗抑郁活性的 H1 受体反向激动剂。 | |||
T15111 |
Diacetoxyscirpenol
|
Others | Others |
Diacetoxyscirpenol, a trichothecene mycotoxin, is a secondary metabolite product of fungi. Diacetoxyscirpenol consumption induces hematological disorders in humans and animals. | |||
T35000 |
Uproleselan sodium
GMI 1271,GMI1271,GMI-1271 |
||
Uproleselan sodium (GGI-1271) is a small molecule E-selector antagonist originally targeted at AML as an adjuvant to standard chemotherapy for hematological malignancies. |