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Hec1

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By Targets:	Apoptosis (6) Caspase (1) Estrogen Receptor/ERR (1) Keap1-Nrf2 (1) NEKs (7)
By Research Areas:	Cancer (10) Endocrinology (1) Metabolic Disease (1)
Click Chemistry:	Azide (1)

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Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

*Nek2/Hec1-IN-2*	NEKs	Cancer
Nek2/Hec1-IN-2 (Compound 14) is an inhibitor of *Nek2/Hec1. Nek2/Hec1*-IN-2 inhibits cancer cell proliferation with IC₅₀ >25 μM ^[1].

INH1 IBT13131	NEKs Apoptosis	Cancer
INH1 specifically disrupts the Hec1/Nek2 interaction via direct *Hec1* binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo ^[1].

INH6	NEKs Apoptosis	Cancer
INH6 is a potent *Nek2/Hec1* inhibitor; inhibits the growth of HeLa cells with an IC₅₀ of 2.4 μM.

INH154 1 Publications Verification	NEKs	Cancer
INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC₅₀s of 200 nM and 120 nM for INH in Hela and MB468 cells.

TAI-1	NEKs Apoptosis	Cancer
TAI-1, an orally active anticancer agent, is a highly potent first-in-class *Hec1* inhibitor, with a GI₅₀ of 13.48 nM in K562 cells ^[1].

T-1101 tosylate 1 Publications Verification TAI-95 tosylate	NEKs Apoptosis	Cancer
T-1101 tosylate (TAI-95 tosylate) is the tosylate salt form of T-1101 (HY-120356). T-1101 tosylate is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 tosylate blocks the interaction between *Hec1* and NEK2, exhibits cytotoxicity in human liver cancer cells with GI₅₀ of 15-70 nM. T-1101 tosylate induces apoptosis in Huh-7. T-1101 tosylate exhibits antitumor efficacy in mouse models ^[1].

T-1101 TAI-95	Apoptosis NEKs	Cancer
T-1101 (TAI-95) is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 blocks the interaction between *Hec1* and NEK2, exhibits cytotoxicity in human liver cancer cells with GI₅₀ of 15-70 nM. T-1101 induces apoptosis in Huh-7. T-1101 exhibits antitumor efficacy in mouse models ^[1].

(R)-DPN	Estrogen Receptor/ERR	Endocrinology
(R)-DPN (compound 3) is a selective ERβ ligand with EC₅₀s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC₅₀s of 286, 205 nM, respectively ^[1].

*Nek2/Hec1-IN-1* Nec2/Hec1 inhibitor	Others	Cancer
N-[4-(2,4-Dimethylphenyl)-2-thiazolyl]-4-pyridinecarboxamide is a derivative of INH1 with anticancer activity. It is cytotoxic to MDA-MB-231, MDA-MB-488, HeLa, and K562 cells (IC₅₀s=1.1, 3.4, 1.6, and 1.2 μM, respectively).

SM1044	Caspase Apoptosis	Cancer
SM1044 is a dihydroartemisinin (DHA) dimer. SM1044 activates caspase, induces apooptosis in RL95-2 and KLE cells. SM1044 inhibits proliferations of cancer cells RL95-2, KLE, HEC-50, HEC-1-A, HEC-1-B, AN3CA, with IC₅₀ < 3.6 μM . SM1044 inhbits tumor growth in RL95-2 xenograft mouse model ^[1].

α-Terthienylmethanol	Others	Others
α-Terthienylmethanol is a terthiophene isolated from the n-hexane fraction of E. prostrata. α-Terthienylmethanol has potent cytotoxic activity against human endometrial cancer cells (Hec1A and Ishikawa) (IC₅₀ < 1 μM). α-Terthienylmethanol increases the intracellular level of ROS and decreases that of GSH ^[1].

Keap1-Nrf2-IN-21	Keap1-Nrf2	Metabolic Disease Cancer
Keap1-Nrf2-IN-21 (compound 4d) is a glucose metabolism inhibitor with antitumor activity. Keap1-Nrf2-IN-21 inhibits glycolytic activity of cancer cells by targeting the glycolytic pathway, especially by affecting the *Keap1-Nrf2* signaling pathway, thereby inhibiting tumor growth. Keap1-Nrf2-IN-21 exhibits cytotoxicity against the HEC1A cell line (IC₅₀=2.60 μM) ^[1].

Cat. No.	Compare	Product Name	Application	Reactivity

	HEC1 Antibody (YA3339) Hec; HsHec1; hsNDC80; Kinetochore protein Hec1; Kinetochore-associated protein 2; KNTC2; ndc80; TID3	WB, IP	Human, Mouse, Rat
	HEC1 Antibody (YA3339) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3339), targeting HEC1, with a predicted molecular weight of 74 kDa (observed band size: 74 kDa). HEC1 Antibody (YA3339) can be used for WB, IP experiment in human, mouse, rat background.

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Cat. No.	Product Name		Classification

Keap1-Nrf2-IN-21		Azide
Keap1-Nrf2-IN-21 (compound 4d) is a glucose metabolism inhibitor with antitumor activity. Keap1-Nrf2-IN-21 inhibits glycolytic activity of cancer cells by targeting the glycolytic pathway, especially by affecting the *Keap1-Nrf2* signaling pathway, thereby inhibiting tumor growth. Keap1-Nrf2-IN-21 exhibits cytotoxicity against the HEC1A cell line (IC₅₀=2.60 μM) ^[1].

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